Objective:To explore the effect of sustained-release recombinant human bone morphogenetic protein-2(rhBMP-2) on ectopic osteogenesis in the muscle pouches of rats through preparing rhBMP-2 sustained-release capsules b...Objective:To explore the effect of sustained-release recombinant human bone morphogenetic protein-2(rhBMP-2) on ectopic osteogenesis in the muscle pouches of rats through preparing rhBMP-2 sustained-release capsules by wrapping morphogenesis protein bones-2(BMP-2)using chitosan nanoparticles,and compositing collagen materials.Methods:Twenty four SpragueDawley rats were randomly divided into four groups with six rats in each group,that is Group A(control group),Group B(only treated with collagen),Group C(rhBMP-2+collagen treated group) and Group D(rhBMP-2/cs+collagen treated group).The composite materials for each group were implanted in the bilateral peroneal muscle pouches in rats.The peroneal muscles were only separated without implanting any materials in control group.Rats were sacrificed 2 weeks and 4 weeks post treatment and samples were cut off for general observation,Micro CT scans and histological observation.Results:General observation showed no new bone formation in Groups A and B mice,while new bones were formed in Groups C and D mice.Two weeks after treatment Micro CT scans showed that The bone volume fraction(BVF),trabecular thickness(Tb. Th),bone mineral density(BMD) in Group C mice were all higher than that in Group D(P<0.05). At the fourth week,the BVK,Tb.Th and BMD were significantly higher than that at the second week(P<0.01).Conclusions:The slow-release effect of rhBMP-2/cs sustained-release capsules can significantly promote ectopic osteogenesis.Its bone formation effect is better than that of rhBMP-2 burst-release group.展开更多
Ins paper describes the development and validation of a liquid chromatography mass spectrometric assay for propafenone and its application to a pharmacokinetic study of propafenone administered as a new propafenone hy...Ins paper describes the development and validation of a liquid chromatography mass spectrometric assay for propafenone and its application to a pharmacokinetic study of propafenone administered as a new propafenone hydrochloride sustained-release capsule (SR-test), as an instant-release tablet (IR-reference) and as the market leader sustained-release capsule (Rythmod SR-reference) in male beagle dogs (n= 8). In Study A comparing SR-test with IR-reference in a crossover design T-max and t(1/2) of propafenone for SR-test were significantly higher than those for IR-reference while C-max and AUC were lower demonstrating the sustained release properties of the new formulation. In Study B comparing SR-test with SR-reference the observed C and A TIC of propafenone for SR test (124.5 +/- 140.0 ng/mL and 612.0 +/- 699.2 ng.h/mL, respectively) were higher than for SR-reference (78.52 +/- 72.92 ng/mL and 423.6 +/- 431.6 ng.h/mL, respectively) although the differences were not significant. Overall, the new formulation has as good if not better sustained release characteristics to the market leader formulation. (C) 2015 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier By All rights reserved.展开更多
Emerging research suggests a potential association of progression of Alzheimer's disease(AD)with alterations in synaptic currents and mitochondrial dynamics.However,the specific associations between these patholog...Emerging research suggests a potential association of progression of Alzheimer's disease(AD)with alterations in synaptic currents and mitochondrial dynamics.However,the specific associations between these pathological changes remain unclear.In this study,we utilized Aβ42-induced AD rats and primary neural cells as in vivo and in vitro models.The investigations included behavioural tests,brain magnetic resonance imaging(MRI),liquid chromatography-tandem mass spectrometry(UPLC-MS/MS)analysis,Nissl staining,thioflavin-S staining,enzyme-linked immunosorbent assay,Golgi-Cox staining,transmission electron microscopy(TEM),immunofluorescence staining,proteomics,adenosine triphosphate(ATP)detection,mitochondrial membrane potential(MMP)and reactive oxygen species(ROS)assessment,mitochondrial morphology analysis,electrophysiological studies,Western blotting,and molecular docking.The results revealed changes in synaptic currents,mitophagy,and mitochondrial dynamics in the AD models.Remarkably,intervention with Dengzhan Shengmai(DZSM)capsules emerged as a pivotal element in this investigation.Aβ42-induced synaptic dysfunction was significantly mitigated by DZSM intervention,which notably amplified the frequency and amplitude of synaptic transmission.The cognitive impairment observed in AD rats was ameliorated and accompanied by robust protection against structural damage in key brain regions,including the hippocampal CA3,primary cingular cortex,prelimbic system,and dysgranular insular cortex.DZSM intervention led to increased IDE levels,augmented long-term potential(LTP)amplitude,and enhanced dendritic spine density and length.Moreover,DZSM intervention led to favourable changes in mitochondrial parameters,including ROS expression,MMP and ATP contents,and mitochondrial morphology.In conclusion,our findings delved into the realm of altered synaptic currents,mitophagy,and mitochondrial dynamics in AD,concurrently highlighting the therapeutic potential of DZSM intervention.展开更多
The aroma sustained-release cotton fabric was prepared by finishing rose fragrance nanocapsules directly on cotton.The structure and properties of nanocapsules were demonstrated by transmission electron microscope(TEM...The aroma sustained-release cotton fabric was prepared by finishing rose fragrance nanocapsules directly on cotton.The structure and properties of nanocapsules were demonstrated by transmission electron microscope(TEM),dynamic light scattering(DLS),fourier transform infrared spectrometer(FTIR),X-ray diffraction (XRD),gas chromatography-mass spectrometry(GC-MS)and electronic nose.The results showed that the spherical nanocapsule dispersed evenly and the average diameter kept 51.4 nm.The existence of COO peak(1741 cm? 1)in the FTIR curve of the finished cotton fabric and the decrease of crystallinity demonstrated that rose fragrance nanocapsules have been incorporated into the cotton fabrics.The washing resistance of the cotton fabrics finished by 51.4 nm nanocapsules was much better than that by rose fragrance alone.Besides,the loss of fragrance from the cotton fabrics finished by 51.4 nm nanocapsules was obviously lower than that by 532 nm nanocapsules and rose fragrance.The smaller the nanocapsule size,the better the sustained release property.Electronic nose analysis also displayed that the aroma released from the cotton fabrics finished by nanocapsules after washing has no obvious variety in contrast to that without washing.The cotton fabrics finished by nanocapsules has the excellent sustained release property.展开更多
The millimeter-scale capsules with controllable morphology,ultra-low permeability and excellent mechanical stability were fabricated by millifluidics.Viscosity of inner phase was adjusted to control the morphology and...The millimeter-scale capsules with controllable morphology,ultra-low permeability and excellent mechanical stability were fabricated by millifluidics.Viscosity of inner phase was adjusted to control the morphology and properties of the capsules.In detail,as the concentration of polyvinyl alcohol(PVA)increased from 0 to 8% in the inner phase of the capsules,the diameter of capsules decreased from 3.33 ± 0.01mm to 2.97 ± 0.01 mm,the shell thickness of capsules decreased from 0.183 ± 0.004 mm to 0.155 ± 0.003 mm.While the capsules had round shape and high sphericity.Notably,the capsules with 2% PVA in the inner phase had remarkably decreased water permeability and good morphological stability.Specifically,the end-time of water losing of the capsules was up to 49 days,while the dehydrated capsules maintained spherical appearance,and crushing force of the capsules was up to 13.73 ± 0.79 N,which ensured stability during processing and transportation.This research provides a new strategy for stable encapsulation of small molecules.展开更多
Docetaxel-loaded sustained-release preparation based on 2-Hydroxyethyl methacrylate(HEMA)and Methyl methacrylate(MMA)cross-linked copolymer(P(HEMA-co-MMA))was prepared to examine the potential use for preventing poste...Docetaxel-loaded sustained-release preparation based on 2-Hydroxyethyl methacrylate(HEMA)and Methyl methacrylate(MMA)cross-linked copolymer(P(HEMA-co-MMA))was prepared to examine the potential use for preventing posterior capsule opacification(PCO).The preparations were prepared by polymerizing the mixture of HEMA,MMA,cross-linking agent(EGDMA),initiator(AIBN)and docetaxel.The influence factors and mechanism of drug release were studied in the experiments.FT-IR,X-RD and SEM methods were used to characterize the polymer(P(HEMA-co-MMA))and docetaxel-loaded sustained-release preparations.Biocompatibility of P(HEMA-co-MMA)and in-vitro effect of docetaxel-loaded sustained-release preparations were also evaluated.The results showed that docetaxel could release sustainedly from these preparations prepared by cross-linking polymerization.And the release rate could be accelerated by increasing the MMA ratio or EGDMA ratio of the polymer.Release mechanism of docetaxel fitted the Higuchi model well.The results of IR and X-RD showed that only a hydrogen bond was formed between docetaxel and P(HEMA-co-MMA).Docetaxel dispersed in P(HEMA-co-MMA)in amorphous form.The elution test showed that P(HEMA-co-MMA)had good biocompatibility and the in-vitro pharmacodynamics study proved that docetaxel could release stably from the preparations and inhibit HLECs’proliferation.The docetaxel-loaded sustained-release preparations proved to be a promising therapy for preventing PCO.These results also lay a theoretical and experimental foundation for the future.展开更多
This study pharmacokinetically examined the lovastatin sustained-release tablet and sustained-release capsule in Beagle dogs. An reversed-phase HPLC method was established for the determination of lovastatin in Beagl...This study pharmacokinetically examined the lovastatin sustained-release tablet and sustained-release capsule in Beagle dogs. An reversed-phase HPLC method was established for the determination of lovastatin in Beagle dog plasma. Pharmacokinetic findings were compared among three preparation(lovastatin sustained-release tablet,T p; sustained-release capsule,T J and conventional capsule). Our results showed that the pharmacokinetic parameters in 6 dogs after single-dose oral administration of three perparations were calculated. T max, C max and MRT revealed significant difference (P<0.05). Relative bioavailability was 111.5±16.9 % (T P) and 110.4%±9.6 % (T J). The pharmacokinetic parameters in the 6 dogs after multiple-dose oral administration of three perparations, T max, C max MRT and DF had significant difference (P<0.05); C av , C min and AUC 0-24 h displayed no significant difference (P>0.05). It is concluded that the lovastatin sustained-release tablet and sustained-release capsule are able to maintain a sustained-release for 24 h.展开更多
BACKGROUND Cold-dampness-type knee osteoarthritis is a common middle-aged and elderly disease,but its pathogenesis is not fully understood,and its clinical treatment has limitations.Glucosamine sulfate capsules are co...BACKGROUND Cold-dampness-type knee osteoarthritis is a common middle-aged and elderly disease,but its pathogenesis is not fully understood,and its clinical treatment has limitations.Glucosamine sulfate capsules are commonly used for treating arthritis,and San Bi Tang is a classic formula of traditional Chinese medicine(TCM)that has the effects of warming yang,dispelling dampness,relaxing muscles,and activating collaterals.This research hypothesized that the combination of modified San Bi Tang and glucosamine sulfate capsules could enhance the clinical efficacy of treating cold-dampness-type knee osteoarthritis through complementary effects.AIM To analyze the clinical efficacy of San Bi Tang combined with glucosamine sulfate capsules when treating cold-dampness-type knee osteoarthritis.METHODS A total of 110 patients with cold-dampness-type knee osteoarthritis were selected as research subjects and randomly divided into a control group and an experimental group of 55 cases each.The control group received only treatment with glucosamine sulfate capsules,while the experimental group received additional treatment with modified San Bi Tang for a duration of 5 wk.The patients’knee joint functions,liver and kidney function indicators,adverse reactions,and vital signs were evaluated and analyzed using SPSS 26.0 software.RESULTS Before treatment,the two groups’genders,ages,and scores were not significantly different,indicating comparability.Both groups’scores improved after treatment,which could indicate pain and knee joint function improvement,but the test group had better scores.The TCM-specific symptoms and the clinical efficacy of the treatment in the test group were higher.Before and after treatment,there were no abnormalities in the patients’liver and kidney function indicators.CONCLUSION The combination of modified San Bi Tang and glucosamine sulfate capsules is superior to treatment with sulfated glucosamine alone and has high safety.展开更多
[Objectives]To establish the HPLC-DAD fingerprint of Xueshuan Xinmaining Capsule(XXC).[Methods]The chromatographic conditions for the analysis of XXC solution were as follows:XSelect HSS T3 column;acetonitrile-0.1%pho...[Objectives]To establish the HPLC-DAD fingerprint of Xueshuan Xinmaining Capsule(XXC).[Methods]The chromatographic conditions for the analysis of XXC solution were as follows:XSelect HSS T3 column;acetonitrile-0.1%phosphoric acid water was used as mo-bile phase,gradient elution;flow rate:1.0 mL/min;column temperature 30℃;The injection volume is 10μL.The quality of XXC samples produced by different manufacturers was evaluated by similarity evaluation and cluster analysis.[Results]In theHPLC-dad fingerprints of 15 batches of XXC,23 common peaks were identified and 9 peaks were identified,and the similarity was greater than 0.95.According to the re-sults of cluster analysis,15 batches of XXC samples could be divided into two categories,S2,S5,S6,S7 and S8 batches belonged to category Ⅰ,and the rest batches belonged to category Ⅱ.[Conclusions]In this study,a representative and universal identification method of Xxc HPLC-DAD fingerprint was established.The method has high precision,stability and repeatability,is simple and reliable,and provides a pow-erful reference for further improving the quality evaluation system of XXC.展开更多
[Objectives]To investigate the clinical effect of Yinhuang Qingfei capsules in the treatment of asymptomatic and mild/common severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)infection.[Methods]A total of 362...[Objectives]To investigate the clinical effect of Yinhuang Qingfei capsules in the treatment of asymptomatic and mild/common severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)infection.[Methods]A total of 362 patients with SARS-CoV-2 infection were divided into the treatment group with 242 patients and control group with 120 patients according to their treatment regimen.The patients in the control group were given standard treatment regimen and those in the treatment group were given Yinhuang Qingfei capsules in addition to the treatment in the control group.The two groups were observed in terms of average length of hospital stay,mean time for nucleic acid clearance,TCM syndrome score,and progression to severe/critical illness,and clinical outcome was compared between the two groups.[Results]There was a significant difference in the overall response rate between the treatment group and the control group[97.52%(236/242)vs 95.00%(114/120),P<0.05].Compared with the control group,the treatment group had significantly shorter length of hospital stay and time for nucleic acid clearance(P<0.05).After 7 days of treatment,both groups had a significant change in TCM syndrome score,and there was a significant difference in TCM syndrome score between the two groups(P<0.05);after 15 days of treatment,both groups had a TCM syndrome score of 0.Progression to severe/critical illness was not observed in either group.[Conclusions]Compared with the standard treatment regimen alone,standard treatment regimen combined with Yinhuang Qingfei capsules can effectively shorten the length of hospital stay and time for nucleic acid clearance and improve TCM symptoms in patients with asymptomatic and mild/common SARS-CoV-2 infection.展开更多
Objective:To analyze the effectiveness of applying ShuGan JieYu Capsules(SGJYC)combined with trazodone in patients with post-stroke depression(PSD)with insomnia.Methods:60 cases of PSD with insomnia patients admitted ...Objective:To analyze the effectiveness of applying ShuGan JieYu Capsules(SGJYC)combined with trazodone in patients with post-stroke depression(PSD)with insomnia.Methods:60 cases of PSD with insomnia patients admitted to the hospital from May 2022 to May 2023 were selected and randomly divided into a reference group(trazodone)and a research group(SGJYC combined with trazodone)of 30 cases each.Statistics were analyzed using the Hamilton Depression Rating Scale(HAM-D),Pittsburgh Sleep Quality Index(PSQI),and Activities of Daily Living(ADL)scale before treatment and 4,8,and 12 weeks after treatment.Results:Before treatment,The results of HAM-D,PSQI,and ADL scale studies in the two groups before treatment were not statistically significant(P>0.05);4,8,and 12 weeks after treatment,the results of HAM-D and PSQI studies in the research group were lower than that of the reference group,and the results of ADL scale studies were higher than that of the reference group.There was a significant difference between the groups(P<0.05).The total adverse reaction rate of the research group was lower than that of the reference group,and there was a significant difference between the groups(P<0.05).Conclusion:The combination of SGJYC and trazodone reduced depression in post-stroke patients,corrected insomnia,improved sleep quality,was safe,and had a low rate of adverse reactions.展开更多
Aim To establish a LC-MS method for determining the concentration of nifedipine in human plasma and to evaluate the pharmacokinetic characteristics of nifedipine sustained-release tablets. Methods A XB-C18 (5 μm, 4....Aim To establish a LC-MS method for determining the concentration of nifedipine in human plasma and to evaluate the pharmacokinetic characteristics of nifedipine sustained-release tablets. Methods A XB-C18 (5 μm, 4.6 mm ×150 mm) column and a mobile phase of methanol: 0.01 mol·L^-1ammonium acetate (60:40, V/V) were used to separate nifedipine, the detections was accuracy under atmosperic pressure electronic spray ionization (AP-ESI) mode and ion mass spectrum (m/z) of 314.9 [M+H]^+ for nifedipine, and 320.8 [M+H]^+ for lorazepam (Internal Standard, IS). Results The linear range of nifedipine was 0.3 - 80 ng·mL^-1 ( r = 0.9997), and the limit of quantitation (LOQ) was 0.3 ng·mL^-1. The nifedipine pharmacokinetic parameters after a single dose of 20 mg nifedipine sustained-release tablets test (T) or reference (R) were as the followings, t1/2 (6.73 ± 2.00) h and (7.04 ± 2.18) h, Tmax (4.28 ± 0.70) h and (4.48 ± 0.70) h, Cmax(39.66 ± 10.58) ng·mL^-1 and (40.19 ± 10.97) ng·mL^-1, AUC0-36 (391.63 ± 108.55) ng·mL^-1·h and (387.57 ± 121.51) ng·mL^-1·h, and AUC0-∞ (408.28 ± 121.16) ng·mL^-1·h and (406.15 ± 133.13) ng·mL^-1·h. The relative bioavailability of nifedipine sustained-release tablets (test) was (103.02 ± 13.93) %. Conclusion LC-MS method for the determination of concentrations of nifedipine in human plasma was sensitive and accurate, and could be used in nifedipine bioavailability and pharmacokinetic studies.展开更多
Aim To improve the dissolution rate and bioavailability of silybin. Methods Sustained-release silybin microspheres were prepared by the spherical crystallization technique with soliddispersing and release-retarding po...Aim To improve the dissolution rate and bioavailability of silybin. Methods Sustained-release silybin microspheres were prepared by the spherical crystallization technique with soliddispersing and release-retarding polymers. A differential scanning calorimeter and an X-ray diffractometer were used to investigate the dispersion state of silybin in the microspheres. The shape, surface morphology, and internal structure of the microspheres were observed using a scanning electron microscope. Characterization of the microspheres, such as average diameter, size distribution and bulk density of the microspheres was investigated. Results The particle size of the microspheres was determined mainly by the agitation speed. The dissolution rate of silybin from microspheres was enhanced by increasing the amount of the dispersing agents, and sustained by the retarding agents. The release rate of microspheres was controlled by adjusting the combination ratio of the dispersing agents to the retarding agents. The resuits of X-ray diffraction and differential scanning calorimetry analysis indicated that silybin was highly dispersed in the microspheres in amorphous state. The release profiles and content did not change after a three-month accelerated stability test at 40 ℃ and 75% relative humidity. Conclusion Sustained-release silybin microspheres with a solid dispersion structure were prepared successfully in one step by a spherical crystallization technique combined with solid dispersion technique. The preparation process is simple, reproducible and inexpensive. The method is efficient for designing sustained-release microspheres with water-insoluble drugs.展开更多
Aim To investigate whether modified-release cefaclor capsules could lead to a more suitable pharmacokinetic profile in the plasma. Methods Cefaclor pellets were prepared by extrusion/spheronization and coated by Eudra...Aim To investigate whether modified-release cefaclor capsules could lead to a more suitable pharmacokinetic profile in the plasma. Methods Cefaclor pellets were prepared by extrusion/spheronization and coated by Eudragit L30D-55 or Eudragit NE30D, then the two sorts of pellets were filled to capsules in a 35:65 ratio to made a modified-release (MR) capsules. The bioavailability of the MR capsules was studied in 24 healthy volunteers after oral administration in a fast state using a commercially available immediate release (IR) capsule as a reference. Results The results showed that the MR formulation had a relatively good bioavailability compared with the commercial capsules, as well as a longer time keeping drug level above MIC than immediate release capsule. The relative bioavailability of the MR capsules was 97.4- 12.1%. Conclusion The data of the present study indicate that time of cefaclor plasma concentration above MIC can be substantially prolonged if cefaclor is administered as a modified- release product.展开更多
The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assay...The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assayed by HPLC method.The changes in serum concentration were conformed to a l-compartment open model.The t_1/2 (Ke)averaged 2.15±0.17 and ll.60 ± l.95 h,and the areas under the drug concentration curves were 5.87 ± 0.67 and 5.55 ± 0.57μgh/ml for enteric-coated and sustained-release tablet of diclofenac sodium,respectively. The mean relative bioavailability of sustained-release tablet was 0.95 to that of enteric-coated tablet.展开更多
BACKGROUND: Sedative and hypnotic drugs could cure insomnia in a dependent manner, and traditional Chinese medicine has some superiority in treating insomnia. OBJECTIVE: To observe the synergistic action of yinao ca...BACKGROUND: Sedative and hypnotic drugs could cure insomnia in a dependent manner, and traditional Chinese medicine has some superiority in treating insomnia. OBJECTIVE: To observe the synergistic action of yinao capsules with pentobarbital sodium in threshold and sub-threshold dosages in hypnosia and sedation. DESIGN: A completely randomized grouping design and control experiment. SETTING: Pharmacological laboratory, College of Pharmacy, Henan College of Traditional Chinese Medicine. MATERIALS: Totally 200 grade II Kunming mice of 18 - 21 g, either male or female, were used. Yinao capsules, main ingredients of which were turtleback glue, thinleaf milkwort root, Chinese magnoliavine fruit, mythic fungus, tangshen, ginseng and grassleaf sweetflag rhizome, were offered by Chinese-American Huayi Pharmacy, Co.,Ltd. (ratified number: 040901); Kangnaoshuai capsules, main ingredients of which were prepared rehmannia root, tuber fleeceflower root, ginseng, membranous milkvetch root, thinleaf milkwort root, Fushen, grassleaf sweetflag rhizome, spine date seed, lecithin, barbary wolfberry fruit, pueraria root, vitamin E, etc., were produced by Shijiazhuang Siyao, Co.,Ltd. (ratified number: 040964); Pentobarbital sodium was produced by China Medicine (Group) Shanghai Chemical Reagent, Co,.Ltd. (Ratified number: 030816). ZZ-6 mice spontaneous activity apparatus was produced by Chengdu Taimeng Science and Technology, Co.,Ltd. METHODS: The experiment was carried out in the Animal Experimental Center, Henan College of Traditional Chinese Medicine from October to December in 2005. (1) Influence of Yinao capsules on the spontaneous activity of mice: Fifty mice were randomly divided into five groups with 10 mice in each group: Mice in the large, middle and small dosages of Yinao capsules groups were intragastrically infused with Yinao capsules suspension (1.36, 0.68, 0.34 g/kg); Those in the Kangnaoshuai capsules group were infused with Kangnaoshuai suspension (1.12 g/kg); Those in the control group were given physiologic saline of the same volume. The mice were administrated once a day for 7 days continuously, and they were placed into the mice spontaneous activity apparatus after 60 minutes from the last administration, the times of spontaneous activities and the times of arising within 10 minutes were recorded after adaptation for 5 minutes. (2) Synergistic action in hypnosia by Finao capsules with pentobarbital sodium of threshold dosage: Seventy mice were randomly divided into 5 groups as above-mentioned with 14 mice in each group, and they were treated the same as above. They were intraperitoneally injected with 50 mg/kg pentobarbital sodium after 60 minutes from the last administration, then conditions of falling asleep were observed. The disappearance of righting reflex was taken as the index of falling asleep, the latency of falling asleep was the duration from intraperitoneal injection of pentobarbital sodium to fall asleep, the sleeping time was from falling asleep to the disappearance of righting reflex. (3) Synergistic action in hypnosia by Yinao capsules with pentobarbital sodium of sub-threshold dosage: Eighty mice were randomly divided into 5 groups as above-mentioned with 16 mice in each group, and they were treated the same as above. They were intraperitoneally injected with 27 mg/kg pentobarbital sodium after 60 minutes from the last administration. Mice whose righting reflex disappeared for at least 1 minute within 30 minutes were taken as falling asleep, the number of sleeping animals in each group was recorded, and the rate of falling asleep was calculated. MAIN OUTCOME MEASURES: Synergistic action of Yinao capsules with pentobarbital sodium of threshold and sub-threshold dosages in hypnosia and sedation. RESULTS: All the 200 mice were involved in the analysis of results. (1) Influence of Yinao capsules on the spontaneous activity of mice: The times of spontaneous activities within 10 minutes in the large and middle dosage of Yinao capsules groups and Kangnaoshuai capsules group [(138.0±37.0), (156.8±28.3), (133.3±46.1) times] were obviously fewer than those in the control group [(204.3±61.3) times, P 〈 0.05- 0.01]. The arising times within 10 minutes in the middle and small dosages of Yinao capsules groups and Kangnaoshuai capsules group [(30.7 ± 18.3), (26.5± 11.2), (24.2±11.6) times] were obviously fewer than those in the control [(71.7±38.6) times, P 〈 0.01 ]. (2) Synergistic action in hypnosia by Yinao capsules with pentobarbital sodium of threshold dosage: The sleeping latencies in the large and middle dosages of Yinao capsules groups and Kangnaoshuai capsules group [(4.49±1.84), (4.83±1.72), (3.85± 1.94) minutes] were obviously shorter than that in the control group [(6.73 ±2.75) minutes, P 〈 0.05 - 0.01 ]. The sleeping time in the large, middle and small dosages of Yinao capsules groups and Kangnaoshuai capsules group [(89.0± 38.42), (67.21 ±24.07), (66.28±18.94), (84.36±29.81) minutes] were obviously longer than that in the control group [(45.78±20.78) minutes, P 〈 0.05- 0.01]. (3) Synergistic action in hypnosia by Yinao capsules with pentobarbital sodium of sub-threshold dosage: The rates of falling asleep in the large and middle dosages of Yinao capsules groups were higher than that in the control group [56% (9/1 6), 38% (6/1 6), 6% (6/16), P 〈 0.01, 0.05], whereas Kangnaoshuai capsules and small dosage of Yinao capsules had no synergistic action with pentobarbital sodium of sub-threshold dosage (P 〉 0.05). CONCLUSION: Yinao capsules have synergistic action with pentobarbital sodium in hypnosia. Yinao capsules possess obvious sedative and hypnotic effects in a dosage-dependent manner.展开更多
Small bowel strictures can be missed by current diagnostic methods. The Patency capsule is a new non-endoscopic dissolvable capsule which has as an objective of checking the patency of digestive tract, in a non-invasi...Small bowel strictures can be missed by current diagnostic methods. The Patency capsule is a new non-endoscopic dissolvable capsule which has as an objective of checking the patency of digestive tract, in a non-invasive manner. The available clinical trials have demonstrated that the Patency capsule is a good tool for assessment of the functional patency of the small bowel, and it allows identification of those patients who can safely undergo a capsule endoscopy, despite clinical and radiographic evidence of small-bowel obstruction. Some cases of intestinal occlusion have been reported with the Patency capsule, four of them needed surgery. So, a new capsule with two timer plugs (Agile capsule) has been recently developed in order to minimize the risk of occlusion. This new device stars its dissolution process earlier (30 h after ingestion) and its two timer plugs have been designed to begin the disintegration even when the device is blocked in a tight stricture.展开更多
Monodispersed Fe3O4/polypyrrole (PPy) hollow particles were synthesized via controllable in-situ deposition and polymerization techniques using poly(styrene-co-acrylic) (PSA) latex as template. Field-dependent m...Monodispersed Fe3O4/polypyrrole (PPy) hollow particles were synthesized via controllable in-situ deposition and polymerization techniques using poly(styrene-co-acrylic) (PSA) latex as template. Field-dependent magnetization plot illustrates that the capsules are superparamagnetic at 300 K. FTIR spectrum confirms that the myoglobin (Mb) molecule adsorbed on the surface of Fe3O4/PPy hollow particle essentially retains its native structure. Furthermore, direct electrochemistry of Mb can be realized on Fe3O4/PPy capsules modified pyrolytic graphite disk electrode, which indicates that the magnetic conductive polymer capsules can promote the electron transfer of protein.展开更多
The Xingnao Jieyu capsule has been shown to effectively relieve neurologic impairments and les- sen depression. It remains poorly understood whether this capsule can be used to treat post-stroke depression. Thus, in t...The Xingnao Jieyu capsule has been shown to effectively relieve neurologic impairments and les- sen depression. It remains poorly understood whether this capsule can be used to treat post-stroke depression. Thus, in the present study, we established a rat model of post-stroke depression using left middle cerebral artery occlusions in combination of chronic unpredictable stress and solitary housing during development. Experimental rats received intragastric perfusion with 0.82, 0.41, and 0.20 g/kg Xingnao Jieyu capsules separately dissolved in 2 mL distilled water. Fluoxetine served as a positive control. The treatment was conducted over 28 days. Sugar water consumption test, open-field test, real-time fluorescent quantitative PCR and immunohistochemical staining results demonstrated that intragastric perfusion with various doses of Xingnao Jieyu capsules increased sugar water consumption, voluntary behaviors and synaptotagmin mRNA and protein expression in rats with post-stroke depression. These therapeutic effects were similar to those of fluoxetine. These results indicate that Xingnao Jieyu capsules upregulate synaptotagmin expression in hip pocampi of rats with post-stroke depression, and exert antidepressant effects.展开更多
BACKGROUND The major reason for filtering bleb failure or scarring of the bleb site is due to excessive scarring after glaucoma filtration surgery in the clinic.Traditional Chinese medicine has preeminence in the prev...BACKGROUND The major reason for filtering bleb failure or scarring of the bleb site is due to excessive scarring after glaucoma filtration surgery in the clinic.Traditional Chinese medicine has preeminence in the prevention of fibrosis formation through the regulation of systemic circulation and improvement of the properties of the inflammatory cells in the blood.AIM To examine the clinical efficacy of using the Modified Cortex Mori Capsules(MCMC;Chinese name:Jiawei Sangbaipi Capsules)in the success rate of functional filtering blebs after glaucoma filtering surgery in clinical patients.METHODS Sixty resurgery glaucoma patients were randomly divided into two groups:30 patients in surgery with the placebo group and 30 patients in surgery with the MCMC group.Patients took either the placebo or the MCMC 2 wk before and after surgery.Postoperative morphology and function filtering bleb,visual acuity,intraocular pressure,postoperative complications,the success rate of filtration surgery and clinical efficacy were observed.RESULTS Fifty patients completed the study.The percentage of functional filtering blebs in the surgery plus MCMC group was 84%at 6 mo after surgery,which was higher than surgery plus placebo group(64%,P<0.05).The surgical success rate in the MCMC and placebo groups were 79%±8.3%and 57%±10.6%respectively(P<0.05).The visual acuity,intraocular pressure and the postoperative complications in the two groups had no significant differences.CONCLUSION Glaucoma filtering surgery while taking MCMC not only reduced excessive scar formation and increased the success rate of functional filtering blebs but also improved the success of glaucoma filtration operations.展开更多
基金supported by Guangdong Province Science and Technology Foundation,Guangdong,China(No:2011B080701053)
文摘Objective:To explore the effect of sustained-release recombinant human bone morphogenetic protein-2(rhBMP-2) on ectopic osteogenesis in the muscle pouches of rats through preparing rhBMP-2 sustained-release capsules by wrapping morphogenesis protein bones-2(BMP-2)using chitosan nanoparticles,and compositing collagen materials.Methods:Twenty four SpragueDawley rats were randomly divided into four groups with six rats in each group,that is Group A(control group),Group B(only treated with collagen),Group C(rhBMP-2+collagen treated group) and Group D(rhBMP-2/cs+collagen treated group).The composite materials for each group were implanted in the bilateral peroneal muscle pouches in rats.The peroneal muscles were only separated without implanting any materials in control group.Rats were sacrificed 2 weeks and 4 weeks post treatment and samples were cut off for general observation,Micro CT scans and histological observation.Results:General observation showed no new bone formation in Groups A and B mice,while new bones were formed in Groups C and D mice.Two weeks after treatment Micro CT scans showed that The bone volume fraction(BVF),trabecular thickness(Tb. Th),bone mineral density(BMD) in Group C mice were all higher than that in Group D(P<0.05). At the fourth week,the BVK,Tb.Th and BMD were significantly higher than that at the second week(P<0.01).Conclusions:The slow-release effect of rhBMP-2/cs sustained-release capsules can significantly promote ectopic osteogenesis.Its bone formation effect is better than that of rhBMP-2 burst-release group.
文摘Ins paper describes the development and validation of a liquid chromatography mass spectrometric assay for propafenone and its application to a pharmacokinetic study of propafenone administered as a new propafenone hydrochloride sustained-release capsule (SR-test), as an instant-release tablet (IR-reference) and as the market leader sustained-release capsule (Rythmod SR-reference) in male beagle dogs (n= 8). In Study A comparing SR-test with IR-reference in a crossover design T-max and t(1/2) of propafenone for SR-test were significantly higher than those for IR-reference while C-max and AUC were lower demonstrating the sustained release properties of the new formulation. In Study B comparing SR-test with SR-reference the observed C and A TIC of propafenone for SR test (124.5 +/- 140.0 ng/mL and 612.0 +/- 699.2 ng.h/mL, respectively) were higher than for SR-reference (78.52 +/- 72.92 ng/mL and 423.6 +/- 431.6 ng.h/mL, respectively) although the differences were not significant. Overall, the new formulation has as good if not better sustained release characteristics to the market leader formulation. (C) 2015 Chinese Pharmaceutical Association and Institute of Materia Medica, Chinese Academy of Medical Sciences. Production and hosting by Elsevier By All rights reserved.
基金National Natural Science Foundation of China(Grant No.:82374317)State Key Program of National Natural Science of China(Grant Nos.:82130119 and 82130118)+4 种基金Postdoctoral Research Foundation of China(Grant No.:2021M690450)Traditional Chinese Medicine Research Project of Health Commission of Hubei Province(Grant No.:ZY2021M017)Hubei University of Chinese Medicine Funds for Distinguished Young Scholars(Grant No.:2022ZZXJ004)National Natural Science Foundation of China(Grant No.:82174210)Fundamental Research Funds for the Central Public Welfare Research Institutes(Grant No.:ZZ14-FL-005).
文摘Emerging research suggests a potential association of progression of Alzheimer's disease(AD)with alterations in synaptic currents and mitochondrial dynamics.However,the specific associations between these pathological changes remain unclear.In this study,we utilized Aβ42-induced AD rats and primary neural cells as in vivo and in vitro models.The investigations included behavioural tests,brain magnetic resonance imaging(MRI),liquid chromatography-tandem mass spectrometry(UPLC-MS/MS)analysis,Nissl staining,thioflavin-S staining,enzyme-linked immunosorbent assay,Golgi-Cox staining,transmission electron microscopy(TEM),immunofluorescence staining,proteomics,adenosine triphosphate(ATP)detection,mitochondrial membrane potential(MMP)and reactive oxygen species(ROS)assessment,mitochondrial morphology analysis,electrophysiological studies,Western blotting,and molecular docking.The results revealed changes in synaptic currents,mitophagy,and mitochondrial dynamics in the AD models.Remarkably,intervention with Dengzhan Shengmai(DZSM)capsules emerged as a pivotal element in this investigation.Aβ42-induced synaptic dysfunction was significantly mitigated by DZSM intervention,which notably amplified the frequency and amplitude of synaptic transmission.The cognitive impairment observed in AD rats was ameliorated and accompanied by robust protection against structural damage in key brain regions,including the hippocampal CA3,primary cingular cortex,prelimbic system,and dysgranular insular cortex.DZSM intervention led to increased IDE levels,augmented long-term potential(LTP)amplitude,and enhanced dendritic spine density and length.Moreover,DZSM intervention led to favourable changes in mitochondrial parameters,including ROS expression,MMP and ATP contents,and mitochondrial morphology.In conclusion,our findings delved into the realm of altered synaptic currents,mitophagy,and mitochondrial dynamics in AD,concurrently highlighting the therapeutic potential of DZSM intervention.
基金Supported by the State Key Development Program for Basic Research of China(2009CB226104)the National Natural ScienceFoundation of China(20876097,21076125)+1 种基金Shanghai Chenguang Foundation(10CG60)Shanghai Excellent Talents(yyy10071)
文摘The aroma sustained-release cotton fabric was prepared by finishing rose fragrance nanocapsules directly on cotton.The structure and properties of nanocapsules were demonstrated by transmission electron microscope(TEM),dynamic light scattering(DLS),fourier transform infrared spectrometer(FTIR),X-ray diffraction (XRD),gas chromatography-mass spectrometry(GC-MS)and electronic nose.The results showed that the spherical nanocapsule dispersed evenly and the average diameter kept 51.4 nm.The existence of COO peak(1741 cm? 1)in the FTIR curve of the finished cotton fabric and the decrease of crystallinity demonstrated that rose fragrance nanocapsules have been incorporated into the cotton fabrics.The washing resistance of the cotton fabrics finished by 51.4 nm nanocapsules was much better than that by rose fragrance alone.Besides,the loss of fragrance from the cotton fabrics finished by 51.4 nm nanocapsules was obviously lower than that by 532 nm nanocapsules and rose fragrance.The smaller the nanocapsule size,the better the sustained release property.Electronic nose analysis also displayed that the aroma released from the cotton fabrics finished by nanocapsules after washing has no obvious variety in contrast to that without washing.The cotton fabrics finished by nanocapsules has the excellent sustained release property.
文摘The millimeter-scale capsules with controllable morphology,ultra-low permeability and excellent mechanical stability were fabricated by millifluidics.Viscosity of inner phase was adjusted to control the morphology and properties of the capsules.In detail,as the concentration of polyvinyl alcohol(PVA)increased from 0 to 8% in the inner phase of the capsules,the diameter of capsules decreased from 3.33 ± 0.01mm to 2.97 ± 0.01 mm,the shell thickness of capsules decreased from 0.183 ± 0.004 mm to 0.155 ± 0.003 mm.While the capsules had round shape and high sphericity.Notably,the capsules with 2% PVA in the inner phase had remarkably decreased water permeability and good morphological stability.Specifically,the end-time of water losing of the capsules was up to 49 days,while the dehydrated capsules maintained spherical appearance,and crushing force of the capsules was up to 13.73 ± 0.79 N,which ensured stability during processing and transportation.This research provides a new strategy for stable encapsulation of small molecules.
基金(Lab of Drug Metabolism and Pharmacokinetics,Sun Yat-sen University,Guangzhou,China)for the help and technical assistance.
文摘Docetaxel-loaded sustained-release preparation based on 2-Hydroxyethyl methacrylate(HEMA)and Methyl methacrylate(MMA)cross-linked copolymer(P(HEMA-co-MMA))was prepared to examine the potential use for preventing posterior capsule opacification(PCO).The preparations were prepared by polymerizing the mixture of HEMA,MMA,cross-linking agent(EGDMA),initiator(AIBN)and docetaxel.The influence factors and mechanism of drug release were studied in the experiments.FT-IR,X-RD and SEM methods were used to characterize the polymer(P(HEMA-co-MMA))and docetaxel-loaded sustained-release preparations.Biocompatibility of P(HEMA-co-MMA)and in-vitro effect of docetaxel-loaded sustained-release preparations were also evaluated.The results showed that docetaxel could release sustainedly from these preparations prepared by cross-linking polymerization.And the release rate could be accelerated by increasing the MMA ratio or EGDMA ratio of the polymer.Release mechanism of docetaxel fitted the Higuchi model well.The results of IR and X-RD showed that only a hydrogen bond was formed between docetaxel and P(HEMA-co-MMA).Docetaxel dispersed in P(HEMA-co-MMA)in amorphous form.The elution test showed that P(HEMA-co-MMA)had good biocompatibility and the in-vitro pharmacodynamics study proved that docetaxel could release stably from the preparations and inhibit HLECs’proliferation.The docetaxel-loaded sustained-release preparations proved to be a promising therapy for preventing PCO.These results also lay a theoretical and experimental foundation for the future.
文摘This study pharmacokinetically examined the lovastatin sustained-release tablet and sustained-release capsule in Beagle dogs. An reversed-phase HPLC method was established for the determination of lovastatin in Beagle dog plasma. Pharmacokinetic findings were compared among three preparation(lovastatin sustained-release tablet,T p; sustained-release capsule,T J and conventional capsule). Our results showed that the pharmacokinetic parameters in 6 dogs after single-dose oral administration of three perparations were calculated. T max, C max and MRT revealed significant difference (P<0.05). Relative bioavailability was 111.5±16.9 % (T P) and 110.4%±9.6 % (T J). The pharmacokinetic parameters in the 6 dogs after multiple-dose oral administration of three perparations, T max, C max MRT and DF had significant difference (P<0.05); C av , C min and AUC 0-24 h displayed no significant difference (P>0.05). It is concluded that the lovastatin sustained-release tablet and sustained-release capsule are able to maintain a sustained-release for 24 h.
文摘BACKGROUND Cold-dampness-type knee osteoarthritis is a common middle-aged and elderly disease,but its pathogenesis is not fully understood,and its clinical treatment has limitations.Glucosamine sulfate capsules are commonly used for treating arthritis,and San Bi Tang is a classic formula of traditional Chinese medicine(TCM)that has the effects of warming yang,dispelling dampness,relaxing muscles,and activating collaterals.This research hypothesized that the combination of modified San Bi Tang and glucosamine sulfate capsules could enhance the clinical efficacy of treating cold-dampness-type knee osteoarthritis through complementary effects.AIM To analyze the clinical efficacy of San Bi Tang combined with glucosamine sulfate capsules when treating cold-dampness-type knee osteoarthritis.METHODS A total of 110 patients with cold-dampness-type knee osteoarthritis were selected as research subjects and randomly divided into a control group and an experimental group of 55 cases each.The control group received only treatment with glucosamine sulfate capsules,while the experimental group received additional treatment with modified San Bi Tang for a duration of 5 wk.The patients’knee joint functions,liver and kidney function indicators,adverse reactions,and vital signs were evaluated and analyzed using SPSS 26.0 software.RESULTS Before treatment,the two groups’genders,ages,and scores were not significantly different,indicating comparability.Both groups’scores improved after treatment,which could indicate pain and knee joint function improvement,but the test group had better scores.The TCM-specific symptoms and the clinical efficacy of the treatment in the test group were higher.Before and after treatment,there were no abnormalities in the patients’liver and kidney function indicators.CONCLUSION The combination of modified San Bi Tang and glucosamine sulfate capsules is superior to treatment with sulfated glucosamine alone and has high safety.
文摘[Objectives]To establish the HPLC-DAD fingerprint of Xueshuan Xinmaining Capsule(XXC).[Methods]The chromatographic conditions for the analysis of XXC solution were as follows:XSelect HSS T3 column;acetonitrile-0.1%phosphoric acid water was used as mo-bile phase,gradient elution;flow rate:1.0 mL/min;column temperature 30℃;The injection volume is 10μL.The quality of XXC samples produced by different manufacturers was evaluated by similarity evaluation and cluster analysis.[Results]In theHPLC-dad fingerprints of 15 batches of XXC,23 common peaks were identified and 9 peaks were identified,and the similarity was greater than 0.95.According to the re-sults of cluster analysis,15 batches of XXC samples could be divided into two categories,S2,S5,S6,S7 and S8 batches belonged to category Ⅰ,and the rest batches belonged to category Ⅱ.[Conclusions]In this study,a representative and universal identification method of Xxc HPLC-DAD fingerprint was established.The method has high precision,stability and repeatability,is simple and reliable,and provides a pow-erful reference for further improving the quality evaluation system of XXC.
基金Supported by the Science and Medicine Joint Fund Project of Natural Science Foundation of Hunan Province(2022JJ80001).
文摘[Objectives]To investigate the clinical effect of Yinhuang Qingfei capsules in the treatment of asymptomatic and mild/common severe acute respiratory syndrome coronavirus 2(SARS-CoV-2)infection.[Methods]A total of 362 patients with SARS-CoV-2 infection were divided into the treatment group with 242 patients and control group with 120 patients according to their treatment regimen.The patients in the control group were given standard treatment regimen and those in the treatment group were given Yinhuang Qingfei capsules in addition to the treatment in the control group.The two groups were observed in terms of average length of hospital stay,mean time for nucleic acid clearance,TCM syndrome score,and progression to severe/critical illness,and clinical outcome was compared between the two groups.[Results]There was a significant difference in the overall response rate between the treatment group and the control group[97.52%(236/242)vs 95.00%(114/120),P<0.05].Compared with the control group,the treatment group had significantly shorter length of hospital stay and time for nucleic acid clearance(P<0.05).After 7 days of treatment,both groups had a significant change in TCM syndrome score,and there was a significant difference in TCM syndrome score between the two groups(P<0.05);after 15 days of treatment,both groups had a TCM syndrome score of 0.Progression to severe/critical illness was not observed in either group.[Conclusions]Compared with the standard treatment regimen alone,standard treatment regimen combined with Yinhuang Qingfei capsules can effectively shorten the length of hospital stay and time for nucleic acid clearance and improve TCM symptoms in patients with asymptomatic and mild/common SARS-CoV-2 infection.
基金Research Project on Heilongjiang Province Traditional Chinese Medicine No.ZHY2022-057。
文摘Objective:To analyze the effectiveness of applying ShuGan JieYu Capsules(SGJYC)combined with trazodone in patients with post-stroke depression(PSD)with insomnia.Methods:60 cases of PSD with insomnia patients admitted to the hospital from May 2022 to May 2023 were selected and randomly divided into a reference group(trazodone)and a research group(SGJYC combined with trazodone)of 30 cases each.Statistics were analyzed using the Hamilton Depression Rating Scale(HAM-D),Pittsburgh Sleep Quality Index(PSQI),and Activities of Daily Living(ADL)scale before treatment and 4,8,and 12 weeks after treatment.Results:Before treatment,The results of HAM-D,PSQI,and ADL scale studies in the two groups before treatment were not statistically significant(P>0.05);4,8,and 12 weeks after treatment,the results of HAM-D and PSQI studies in the research group were lower than that of the reference group,and the results of ADL scale studies were higher than that of the reference group.There was a significant difference between the groups(P<0.05).The total adverse reaction rate of the research group was lower than that of the reference group,and there was a significant difference between the groups(P<0.05).Conclusion:The combination of SGJYC and trazodone reduced depression in post-stroke patients,corrected insomnia,improved sleep quality,was safe,and had a low rate of adverse reactions.
文摘Aim To establish a LC-MS method for determining the concentration of nifedipine in human plasma and to evaluate the pharmacokinetic characteristics of nifedipine sustained-release tablets. Methods A XB-C18 (5 μm, 4.6 mm ×150 mm) column and a mobile phase of methanol: 0.01 mol·L^-1ammonium acetate (60:40, V/V) were used to separate nifedipine, the detections was accuracy under atmosperic pressure electronic spray ionization (AP-ESI) mode and ion mass spectrum (m/z) of 314.9 [M+H]^+ for nifedipine, and 320.8 [M+H]^+ for lorazepam (Internal Standard, IS). Results The linear range of nifedipine was 0.3 - 80 ng·mL^-1 ( r = 0.9997), and the limit of quantitation (LOQ) was 0.3 ng·mL^-1. The nifedipine pharmacokinetic parameters after a single dose of 20 mg nifedipine sustained-release tablets test (T) or reference (R) were as the followings, t1/2 (6.73 ± 2.00) h and (7.04 ± 2.18) h, Tmax (4.28 ± 0.70) h and (4.48 ± 0.70) h, Cmax(39.66 ± 10.58) ng·mL^-1 and (40.19 ± 10.97) ng·mL^-1, AUC0-36 (391.63 ± 108.55) ng·mL^-1·h and (387.57 ± 121.51) ng·mL^-1·h, and AUC0-∞ (408.28 ± 121.16) ng·mL^-1·h and (406.15 ± 133.13) ng·mL^-1·h. The relative bioavailability of nifedipine sustained-release tablets (test) was (103.02 ± 13.93) %. Conclusion LC-MS method for the determination of concentrations of nifedipine in human plasma was sensitive and accurate, and could be used in nifedipine bioavailability and pharmacokinetic studies.
文摘Aim To improve the dissolution rate and bioavailability of silybin. Methods Sustained-release silybin microspheres were prepared by the spherical crystallization technique with soliddispersing and release-retarding polymers. A differential scanning calorimeter and an X-ray diffractometer were used to investigate the dispersion state of silybin in the microspheres. The shape, surface morphology, and internal structure of the microspheres were observed using a scanning electron microscope. Characterization of the microspheres, such as average diameter, size distribution and bulk density of the microspheres was investigated. Results The particle size of the microspheres was determined mainly by the agitation speed. The dissolution rate of silybin from microspheres was enhanced by increasing the amount of the dispersing agents, and sustained by the retarding agents. The release rate of microspheres was controlled by adjusting the combination ratio of the dispersing agents to the retarding agents. The resuits of X-ray diffraction and differential scanning calorimetry analysis indicated that silybin was highly dispersed in the microspheres in amorphous state. The release profiles and content did not change after a three-month accelerated stability test at 40 ℃ and 75% relative humidity. Conclusion Sustained-release silybin microspheres with a solid dispersion structure were prepared successfully in one step by a spherical crystallization technique combined with solid dispersion technique. The preparation process is simple, reproducible and inexpensive. The method is efficient for designing sustained-release microspheres with water-insoluble drugs.
文摘Aim To investigate whether modified-release cefaclor capsules could lead to a more suitable pharmacokinetic profile in the plasma. Methods Cefaclor pellets were prepared by extrusion/spheronization and coated by Eudragit L30D-55 or Eudragit NE30D, then the two sorts of pellets were filled to capsules in a 35:65 ratio to made a modified-release (MR) capsules. The bioavailability of the MR capsules was studied in 24 healthy volunteers after oral administration in a fast state using a commercially available immediate release (IR) capsule as a reference. Results The results showed that the MR formulation had a relatively good bioavailability compared with the commercial capsules, as well as a longer time keeping drug level above MIC than immediate release capsule. The relative bioavailability of the MR capsules was 97.4- 12.1%. Conclusion The data of the present study indicate that time of cefaclor plasma concentration above MIC can be substantially prolonged if cefaclor is administered as a modified- release product.
文摘The pharmacokinetics of a sustained- release formulation and an enteric- coated tablet of diclofenac sodium were studied on 8 healthy male volunteers in an open,randomized crossover study.Drug level in serum was assayed by HPLC method.The changes in serum concentration were conformed to a l-compartment open model.The t_1/2 (Ke)averaged 2.15±0.17 and ll.60 ± l.95 h,and the areas under the drug concentration curves were 5.87 ± 0.67 and 5.55 ± 0.57μgh/ml for enteric-coated and sustained-release tablet of diclofenac sodium,respectively. The mean relative bioavailability of sustained-release tablet was 0.95 to that of enteric-coated tablet.
基金New Century Excellent Person With Ability Hold by Ministry of Education, No.NCET-04-0657Cultivating Project of Advanced School Innovate Person with Ability Hold by Henan Province, No.2004-23
文摘BACKGROUND: Sedative and hypnotic drugs could cure insomnia in a dependent manner, and traditional Chinese medicine has some superiority in treating insomnia. OBJECTIVE: To observe the synergistic action of yinao capsules with pentobarbital sodium in threshold and sub-threshold dosages in hypnosia and sedation. DESIGN: A completely randomized grouping design and control experiment. SETTING: Pharmacological laboratory, College of Pharmacy, Henan College of Traditional Chinese Medicine. MATERIALS: Totally 200 grade II Kunming mice of 18 - 21 g, either male or female, were used. Yinao capsules, main ingredients of which were turtleback glue, thinleaf milkwort root, Chinese magnoliavine fruit, mythic fungus, tangshen, ginseng and grassleaf sweetflag rhizome, were offered by Chinese-American Huayi Pharmacy, Co.,Ltd. (ratified number: 040901); Kangnaoshuai capsules, main ingredients of which were prepared rehmannia root, tuber fleeceflower root, ginseng, membranous milkvetch root, thinleaf milkwort root, Fushen, grassleaf sweetflag rhizome, spine date seed, lecithin, barbary wolfberry fruit, pueraria root, vitamin E, etc., were produced by Shijiazhuang Siyao, Co.,Ltd. (ratified number: 040964); Pentobarbital sodium was produced by China Medicine (Group) Shanghai Chemical Reagent, Co,.Ltd. (Ratified number: 030816). ZZ-6 mice spontaneous activity apparatus was produced by Chengdu Taimeng Science and Technology, Co.,Ltd. METHODS: The experiment was carried out in the Animal Experimental Center, Henan College of Traditional Chinese Medicine from October to December in 2005. (1) Influence of Yinao capsules on the spontaneous activity of mice: Fifty mice were randomly divided into five groups with 10 mice in each group: Mice in the large, middle and small dosages of Yinao capsules groups were intragastrically infused with Yinao capsules suspension (1.36, 0.68, 0.34 g/kg); Those in the Kangnaoshuai capsules group were infused with Kangnaoshuai suspension (1.12 g/kg); Those in the control group were given physiologic saline of the same volume. The mice were administrated once a day for 7 days continuously, and they were placed into the mice spontaneous activity apparatus after 60 minutes from the last administration, the times of spontaneous activities and the times of arising within 10 minutes were recorded after adaptation for 5 minutes. (2) Synergistic action in hypnosia by Finao capsules with pentobarbital sodium of threshold dosage: Seventy mice were randomly divided into 5 groups as above-mentioned with 14 mice in each group, and they were treated the same as above. They were intraperitoneally injected with 50 mg/kg pentobarbital sodium after 60 minutes from the last administration, then conditions of falling asleep were observed. The disappearance of righting reflex was taken as the index of falling asleep, the latency of falling asleep was the duration from intraperitoneal injection of pentobarbital sodium to fall asleep, the sleeping time was from falling asleep to the disappearance of righting reflex. (3) Synergistic action in hypnosia by Yinao capsules with pentobarbital sodium of sub-threshold dosage: Eighty mice were randomly divided into 5 groups as above-mentioned with 16 mice in each group, and they were treated the same as above. They were intraperitoneally injected with 27 mg/kg pentobarbital sodium after 60 minutes from the last administration. Mice whose righting reflex disappeared for at least 1 minute within 30 minutes were taken as falling asleep, the number of sleeping animals in each group was recorded, and the rate of falling asleep was calculated. MAIN OUTCOME MEASURES: Synergistic action of Yinao capsules with pentobarbital sodium of threshold and sub-threshold dosages in hypnosia and sedation. RESULTS: All the 200 mice were involved in the analysis of results. (1) Influence of Yinao capsules on the spontaneous activity of mice: The times of spontaneous activities within 10 minutes in the large and middle dosage of Yinao capsules groups and Kangnaoshuai capsules group [(138.0±37.0), (156.8±28.3), (133.3±46.1) times] were obviously fewer than those in the control group [(204.3±61.3) times, P 〈 0.05- 0.01]. The arising times within 10 minutes in the middle and small dosages of Yinao capsules groups and Kangnaoshuai capsules group [(30.7 ± 18.3), (26.5± 11.2), (24.2±11.6) times] were obviously fewer than those in the control [(71.7±38.6) times, P 〈 0.01 ]. (2) Synergistic action in hypnosia by Yinao capsules with pentobarbital sodium of threshold dosage: The sleeping latencies in the large and middle dosages of Yinao capsules groups and Kangnaoshuai capsules group [(4.49±1.84), (4.83±1.72), (3.85± 1.94) minutes] were obviously shorter than that in the control group [(6.73 ±2.75) minutes, P 〈 0.05 - 0.01 ]. The sleeping time in the large, middle and small dosages of Yinao capsules groups and Kangnaoshuai capsules group [(89.0± 38.42), (67.21 ±24.07), (66.28±18.94), (84.36±29.81) minutes] were obviously longer than that in the control group [(45.78±20.78) minutes, P 〈 0.05- 0.01]. (3) Synergistic action in hypnosia by Yinao capsules with pentobarbital sodium of sub-threshold dosage: The rates of falling asleep in the large and middle dosages of Yinao capsules groups were higher than that in the control group [56% (9/1 6), 38% (6/1 6), 6% (6/16), P 〈 0.01, 0.05], whereas Kangnaoshuai capsules and small dosage of Yinao capsules had no synergistic action with pentobarbital sodium of sub-threshold dosage (P 〉 0.05). CONCLUSION: Yinao capsules have synergistic action with pentobarbital sodium in hypnosia. Yinao capsules possess obvious sedative and hypnotic effects in a dosage-dependent manner.
文摘Small bowel strictures can be missed by current diagnostic methods. The Patency capsule is a new non-endoscopic dissolvable capsule which has as an objective of checking the patency of digestive tract, in a non-invasive manner. The available clinical trials have demonstrated that the Patency capsule is a good tool for assessment of the functional patency of the small bowel, and it allows identification of those patients who can safely undergo a capsule endoscopy, despite clinical and radiographic evidence of small-bowel obstruction. Some cases of intestinal occlusion have been reported with the Patency capsule, four of them needed surgery. So, a new capsule with two timer plugs (Agile capsule) has been recently developed in order to minimize the risk of occlusion. This new device stars its dissolution process earlier (30 h after ingestion) and its two timer plugs have been designed to begin the disintegration even when the device is blocked in a tight stricture.
基金the National Natural Science Foundation of China (No.10672154)National Science Fund of Ministry of Education of Anhui Province (No.2005KJ135).
文摘Monodispersed Fe3O4/polypyrrole (PPy) hollow particles were synthesized via controllable in-situ deposition and polymerization techniques using poly(styrene-co-acrylic) (PSA) latex as template. Field-dependent magnetization plot illustrates that the capsules are superparamagnetic at 300 K. FTIR spectrum confirms that the myoglobin (Mb) molecule adsorbed on the surface of Fe3O4/PPy hollow particle essentially retains its native structure. Furthermore, direct electrochemistry of Mb can be realized on Fe3O4/PPy capsules modified pyrolytic graphite disk electrode, which indicates that the magnetic conductive polymer capsules can promote the electron transfer of protein.
基金funded by the Key Science and Technology Project of Shaanxi Provincial "13115"Technology Innovation Engineering,No.2010ZDKG-65
文摘The Xingnao Jieyu capsule has been shown to effectively relieve neurologic impairments and les- sen depression. It remains poorly understood whether this capsule can be used to treat post-stroke depression. Thus, in the present study, we established a rat model of post-stroke depression using left middle cerebral artery occlusions in combination of chronic unpredictable stress and solitary housing during development. Experimental rats received intragastric perfusion with 0.82, 0.41, and 0.20 g/kg Xingnao Jieyu capsules separately dissolved in 2 mL distilled water. Fluoxetine served as a positive control. The treatment was conducted over 28 days. Sugar water consumption test, open-field test, real-time fluorescent quantitative PCR and immunohistochemical staining results demonstrated that intragastric perfusion with various doses of Xingnao Jieyu capsules increased sugar water consumption, voluntary behaviors and synaptotagmin mRNA and protein expression in rats with post-stroke depression. These therapeutic effects were similar to those of fluoxetine. These results indicate that Xingnao Jieyu capsules upregulate synaptotagmin expression in hip pocampi of rats with post-stroke depression, and exert antidepressant effects.
文摘BACKGROUND The major reason for filtering bleb failure or scarring of the bleb site is due to excessive scarring after glaucoma filtration surgery in the clinic.Traditional Chinese medicine has preeminence in the prevention of fibrosis formation through the regulation of systemic circulation and improvement of the properties of the inflammatory cells in the blood.AIM To examine the clinical efficacy of using the Modified Cortex Mori Capsules(MCMC;Chinese name:Jiawei Sangbaipi Capsules)in the success rate of functional filtering blebs after glaucoma filtering surgery in clinical patients.METHODS Sixty resurgery glaucoma patients were randomly divided into two groups:30 patients in surgery with the placebo group and 30 patients in surgery with the MCMC group.Patients took either the placebo or the MCMC 2 wk before and after surgery.Postoperative morphology and function filtering bleb,visual acuity,intraocular pressure,postoperative complications,the success rate of filtration surgery and clinical efficacy were observed.RESULTS Fifty patients completed the study.The percentage of functional filtering blebs in the surgery plus MCMC group was 84%at 6 mo after surgery,which was higher than surgery plus placebo group(64%,P<0.05).The surgical success rate in the MCMC and placebo groups were 79%±8.3%and 57%±10.6%respectively(P<0.05).The visual acuity,intraocular pressure and the postoperative complications in the two groups had no significant differences.CONCLUSION Glaucoma filtering surgery while taking MCMC not only reduced excessive scar formation and increased the success rate of functional filtering blebs but also improved the success of glaucoma filtration operations.