A procedure to evaluate the quality consistency of generic drugs based on the impurity profile and the similarity analysis methods was presented in this paper. Nifedipine extended-release tablets from six generic fact...A procedure to evaluate the quality consistency of generic drugs based on the impurity profile and the similarity analysis methods was presented in this paper. Nifedipine extended-release tablets from six generic factories of China were used to evaluate the uniformity with the original drug in the study. The procedure includes: choice of chromatographic methods, data collection and conformity test, evaluation of intra-batch similarity of drugs, evaluation of generic drugs with the original drug and weighted similarity evaluation of generic drugs. The data were collected via high-performance liquid chromatography (HPLC), and then calculated by correlation coefficient, cosine, principal component analysis (PCA) and hierarchical clustering analysis (HCA). It is more suitable to use peak areas as the vector when calculating the similarity of impurity profile. After weighting the peak areas of the unspecified impurities in further evaluation of the generic quality, the generic level of different factories was differentiated and the best generic factory was picked out.展开更多
A dissolution test for fesoterodine low dose extended-release tablets using liquid chromatographic(LC) method equipped with a C18 monolithic column was developed and validated. LC system was operated isocratically a...A dissolution test for fesoterodine low dose extended-release tablets using liquid chromatographic(LC) method equipped with a C18 monolithic column was developed and validated. LC system was operated isocratically at controlled temperature(40 1C) using a mobile phase of acetonitrile:methanol:0.03 M ammonium acetate(p H 3.8)(30:15:55, v/v/v), run at a flow rate of 1.5 m L/min and detected at 208 nm. The best dissolution conditions for this formulation were achieved using a USP apparatus 2(paddle) at 100 rpm and 900 m L of phosphate buffer at p H 6.8 as the dissolution medium.Validation parameters such as the specificity, linearity, accuracy, precision, and robustness were evaluated according to international guidelines, giving results within the acceptable range. The kinetic parameters of drug release were also investigated using model-dependent methods and the dissolution profiles were best described by the Higuchi model. The validated dissolution test can be applied for quality control of this formulation.展开更多
Objective:To investigate and analyze the clinical effect of clopidogrel bisulfate tablets combined with aspirin enteric-coated tablets on acute myocardial infarction(AMI)patients.Methods:The study period was from Janu...Objective:To investigate and analyze the clinical effect of clopidogrel bisulfate tablets combined with aspirin enteric-coated tablets on acute myocardial infarction(AMI)patients.Methods:The study period was from January 2020 to December 2023,the sample source was 82 AMI patients admitted to our hospital,grouped into an observation group(n=41)and a control group(n=41)by the numerical table method.The patients in the control group were treated with aspirin enteric-coated tablets,and the patients in the observation group were treated with aspirin enteric-coated tablets combined with clopidogrel bisulfate.The clinical efficacy,coagulation indexes,and the incidence of cardiovascular adverse events between the two groups were compared.Results:The clinical efficacy of the observation group was higher than that of the control group(P<0.05);the platelet aggregation rate(PAR)of the observation group was lower than that of the con-trol group after treatment(P<0.05),and there was no significant difference in the prothrombin time(PT)and activated partial thromboplastin time(APTT)between the two groups(P>0.05).The incidence of cardiovascular adverse events in the observation group was lower than that of the control group(P<0.05).Conclusion:The treatment effect of clopidogrel bisulfate tablets combined with aspirin enteric-coated tablets on AMI patients is remarkable.It reduces the PAR and the incidence of cardiovascular adverse events,so this treatment method should be popularized.展开更多
The objective of this study is to develop chitosaneanionic polymers based extendedrelease tablets and test the feasibility of using this system for the sustained release of highly water-soluble drugs with high drug lo...The objective of this study is to develop chitosaneanionic polymers based extendedrelease tablets and test the feasibility of using this system for the sustained release of highly water-soluble drugs with high drug loading.Here,the combination of sodium valproate(VPS)and valproic acid(VPA)were chosen as the model drugs.Anionic polymers studied include xanthan gum(XG),carrageenan(CG),sodium carboxymethyl cellulose(CMC-Na)and sodium alginate(SA).The tablets were prepared by wet granulation method.In vitro drug release was carried out under simulated gastrointestinal condition.Drug release mechanism was studied.Compared with single polymers,chitosaneanionic polymers based system caused a further slowdown of drug release rate.Among them,CS exanthan gum matrix system exhibited the best extended-release behavior and could extend drug release for up to 24 h.Differential scanning calorimetry(DSC)and Fourier transform infrared spectroscopy(FTIR)studies demonstrated that polyelectrolyte complexes(PECs)were formed on the tablet surface,which played an important role on retarding erosion and swelling of the matrix in the later stage.In conclusion,this study demonstrated that it is possible to develop highly water-soluble drugs loaded extendedrelease tablets using chitosaneanionic polymers based system.展开更多
The purpose of this study was to develop an extended-release(ER) matrix tablet that shows robust dissolution properties able to account for the variability of pH and mechanical stress in the GI tract using a combinati...The purpose of this study was to develop an extended-release(ER) matrix tablet that shows robust dissolution properties able to account for the variability of pH and mechanical stress in the GI tract using a combination of enteric polymer and hydrophilic polymer. Hypromellose acetate succinate(HPMCAS) and hydroxypropylcellulose(HPC) were selected as ER polymers for the ER matrix tablet(HPMCAS/HPC ER matrix tablet). Oxycodone hydrochloride was employed as a model drug. Dissolution properties of the HPMCAS/HPC ER matrix tablets were evaluated and were not affected by the pH of the test medium or paddle rotating speed.In a USP apparatus 3(bio-relevant dissolution method), dissolution profiles of the HPMCAS/HPC ER matrix tablets containing oxycodone hydrochloride were similar to that of the reference product(OxyC ontin). Moreover, in vivo performance after oral administration of the HPMCAS/HPC ER matrix tablets to humans was simulated by GastroP lus based on dissolution profiles from the USP apparatus 3. The plasma concentration-time profile simulated was similar to that of the reference product. These results suggest that the combination of HPMCAS and HPC shows a robust dissolution profile against pH and paddle rotating speed and indicates the appropriate extended-release profile in humans.展开更多
Background:Jinqi Jiangtang tablets(JQJT)have been approved for the treatment of type 2 diabetes mellitus(T2DM)in China for many years.Exploring the effective substances and mechanisms of JQJT is important for its clin...Background:Jinqi Jiangtang tablets(JQJT)have been approved for the treatment of type 2 diabetes mellitus(T2DM)in China for many years.Exploring the effective substances and mechanisms of JQJT is important for its clinical application and further drug research and development.This study aimed to explore the chemical basis and mechanisms of JQJT in the treatment of T2DM.Methods:With network pharmacology,we screened substances in JQJT and their possible targets,then constructed the action network and enriched the biological functions and pathways associated with the active components,and identified the potential targets and mechanisms of JQJT in the treatment of T2DM.Based on the network pharmacology data,we explored the hypoglycemic mechanisms of coptisine in JQJT through western blot and quantitative real-time polymerase chain reaction.Results:Forty-three compounds with good pharmacokinetic properties were identified in JQJT,together with 146 potential biological targets.Among these potential targets,74 were associated with treatment of T2DM.A compound-target network of the 43 compounds against T2DM was constructed.Biological process and signal pathway enrichment analysis of the network highlighted the FoxO signaling pathway.Western blot and quantitative real-time polymerase chain reaction results showed that coptisine,but not epiberberine,significantly inhibited expression of key genes involved in hepatocyte gluconeogenesis by regulating the FoxO1 signaling pathway.Conclusion:Network pharmacology analysis and cell experiments showed that coptisine regulated glucose homeostasis by inhibiting the FoxO1 signaling pathway and hepatic gluconeogenesis,which may be one of the mechanisms of JQJT in the treatment of T2DM.展开更多
[Objectives]This study was conducted to optimize the Formulation Process of glucosamine chondroitin sulfate tablets. [Methods] The orthogonal design with three levels was carried out with microcrystalline cellulose, c...[Objectives]This study was conducted to optimize the Formulation Process of glucosamine chondroitin sulfate tablets. [Methods] The orthogonal design with three levels was carried out with microcrystalline cellulose, calcium hydrophosphate and cross-linked polyvinylpyrrolidone as three factors to optimize the preparation process. [Results] When microcrystalline cellulose 200 mg/tablet, calcium hydrophosphate 150 mg/tablet, and cross-linked polyvinylpyrrolidone 80 mg/tablet were added, the angle of repose could meet the requirements of tablet pressing, and the dissolution could reach more than 95% in 30 min. The results of the orthogonal test showed that the dissolution effect of self-made tablets was faster than that of commercial products. [Conclusions] The glucosamine hydrochloride chondroitin sulfate tablets prepared by this prescription have better quality.展开更多
BACKGROUND Depression is a widespread mental health condition that requires effective treatment.In the treatment of depression,traditional Chinese medicine(TCM)offers obvious advantages,fewer adverse reactions,and a l...BACKGROUND Depression is a widespread mental health condition that requires effective treatment.In the treatment of depression,traditional Chinese medicine(TCM)offers obvious advantages,fewer adverse reactions,and a lower recurrence rate.AIM To evaluate the clinical benefits of Guipi decoction combined with escitalopram oxalate tablets for individuals with depression.METHODS In total,80 patients diagnosed as having depression were enrolled in the study and divided into either an experimental group or a control group.All of the patients were orally administered escitalopram oxalate tablets.Additionally,the experimental group received Jiajian Guipi decoction and reduced Governor vessel fumigation over 4 wk.TCM syndrome scores,Hamilton depression rating scale(HAM-D)scores,self-rating depression scale(SDS)scores,and Pittsburgh sleep quality index scores were measured for the two groups and compared before and after the treatment.The two groups were monitored for any adverse reactions.RESULTS After 4 wk of treatment,both groups exhibited a significant reduction in TCM syndrome scores compared with their pre-treatment scores(P<0.05).However,the experimental group exhibited significantly lower TCM syndrome scores than the control group(P<0.05).Similarly,the post-treatment SDS and HAM-D-24 scores were significantly lower in both groups than the pre-treatment scores(P<0.05),with the experimental group exhibiting lower scores than the control group(P<0.05).The total treatment efficiency was significantly better in the experimental group(97.14%)than in the control group(77.78%)(P<0.05).Furthermore,after 4 wk of treatment,the Pittsburgh sleep quality index scores for both groups were significantly lower than those before the treatment(P<0.05),with the experimental group exhibiting lower scores than the control group(P<0.05).The incidence of adverse reactions was significantly lower in the experimental group than in the control group(P<0.05).CONCLUSION The combination of Guipi decoction and escitalopram oxalate tablets was found to be an effective and safe treatment for depression.This combination could reduce TCM syndrome scores,improve depressive symptoms,and enhance sleep quality.展开更多
Background:Naodesheng tablets(NDST)was widely used in clinical treatment as a drug for cardiovascular diseases,but the mechanism for treating atherosclerosis was unknown.On the basis of network pharmacology and bioinf...Background:Naodesheng tablets(NDST)was widely used in clinical treatment as a drug for cardiovascular diseases,but the mechanism for treating atherosclerosis was unknown.On the basis of network pharmacology and bioinformatics,predict the relevant targets and signalling pathways for NDST in the treatment of atherosclerosis.Methods:First,the targets of NDST and the targets for treating atherosclerosis were looked for in different databases.Next,Venny 2.1.0 was used to find the genes that overlapped between NDST and targets for treating atherosclerosis.Subsequently,the herb-active ingredient-target-disease were obtained to explore the hub compound.Furthermore,the Metascape database was used for Gene Ontology and Kyoto Encyclopedia of Genes and Genomes enrichment analysis.And we constructed the“active ingredient-intersection target-pathway”network by Cytoscape software to gain the hub genes and pathways.Finally,molecular docking was used to verify the affinity of hub ingredients and hub genes.Results:In the results,67 active ingredients and 322 targets of NDST were selected in ingredients-targets network.154 overlapping targets of NDST(322)and atherosclerosis(1330)were obtained.Then,the herb-active ingredient-target-disease showed that quercetin,apigenin and luteolin were the hub ingredients to treat atherosclerosis.Further,the hub genes(PTGS2,RXRA,CASP3)and pathways(lipid and atherosclerosis)were accessed in active ingredient-intersection target-pathway.Finally,the results indicated that quercetin,apigenin and luteolin were better binding the PTGS2,RXRA,CASP3,especially PTGS2 and luteolin in molecular docking.Conclusion:In conclusion,quercetin,apigenin and luteolin,as the main ingredients of NDST could play a important role in PTGS2,RXRA,and CASP3 for treating atherosclerosis via the lipid and atherosclerosis(TNF signaling pathway).展开更多
Objective This study aimed to analyze the clinical efficacy of the Jianpi Shengxue tablet for treating renal anemia.Methods A total of 200 patients with renal anemia from December 2020 to December 2022 were enrolled a...Objective This study aimed to analyze the clinical efficacy of the Jianpi Shengxue tablet for treating renal anemia.Methods A total of 200 patients with renal anemia from December 2020 to December 2022 were enrolled and randomly divided into two groups.Patients in the control group were treated with polysaccharide-iron complex,and those in the experimental group were administered Jianpi Shengxue tablet.After 8 weeks of continuous treatment,the therapeutic outcomes regarding anemia were compared between the two groups.Results After treatment,the red blood cell(RBC)count,hematocrit(HCT),reticulocyte percentage(RET),ferritin(SF),serum iron(SI),transferrin saturation(TSAT),and serum albumin(ALB)all increased(P<0.01),and the clinical symptom score and total iron binding capacity decreased(P<0.01)in the experimental group.Moreover,the improvements in RBC,HCT,RET,SF,SI,TAST,ALB,and clinical symptoms(fatigue,anorexia,dull skin complexion,numbness of hands and feet)in the experimental group were significantly greater than those in the control group(P<0.05).The total effective rate for treating renal anemia was significantly higher in the experimental group than in the control group(P<0.01).Conclusion The Jianpi Shengxue tablet demonstrates efficacy in treating renal anemia,leading to significant improvements in the laboratory examination results and clinical symptoms of patients with renal anemia.展开更多
Objective:To study the therapeutic efficacy of patients with ulcerative colitis receiving Bifidobacterium quadruple viable tablets.Methods:49 cases were selected from ulcerative colitis patients who attended the clini...Objective:To study the therapeutic efficacy of patients with ulcerative colitis receiving Bifidobacterium quadruple viable tablets.Methods:49 cases were selected from ulcerative colitis patients who attended the clinic from February 2021 to November 2022,and were randomly grouped into group A for addition of Bifidobacterium quadruple viable tablets treatment,and group B for conventional medication.The efficacy,inflammatory factors,nutritional indexes,and adverse reactions were compared between the groups.Results:The efficacy of UC patients in group A was higher than that in group B(P<0.05);the inflammatory factors in group A were lower than that in group B(P<0.05);nutritional indicators in group A were higher than that in group B(P<0.05);and the adverse reactions of medication in UC patients in group A were lower than that in group B(P<0.05).Conclusion:The treatment of UC patients with the addition of Bifidobacterium quadruple viable tablets can improve the nutritional status of the organism,inhibit the progression of inflammation,and is safe and efficient in treating ulcerative colitis.展开更多
Objective:To analyze the clinical efficacy of megestrol acetate dispersible tablets in the adjuvant treatment of acute leukemia.Methods:80 patients with acute leukemia admitted from December 2021 to December 2022 were...Objective:To analyze the clinical efficacy of megestrol acetate dispersible tablets in the adjuvant treatment of acute leukemia.Methods:80 patients with acute leukemia admitted from December 2021 to December 2022 were randomly divided into two groups.The control group underwent chemotherapy,and the observation group took megestrol acetate dispersible tablets and underwent chemotherapy.The effect of the treatments were evaluated by analyzing the albumin(Alb)and prealbumin(Palb)indicators,and the adverse reactions were observed.Results:There was no significant difference in Alb and Palb indexes between the two groups before treatment(P>0.05).After treatment,Alb and Palb indexes in the observation group were greater than those in the control group(P<0.05).The incidence of adverse reactions in the control group was 20.00%,which was significantly higher than the observation group(5.00%),with P<0.05.Conclusion:The combination of megestrol acetate dispersible tablets and chemotherapy is more effective in treating patients with acute leukemia,and the Alb and Palb indexes can be optimized.Besides,there are fewer adverse reactions,which means that the treatment is relatively safe.展开更多
Objective:To study the therapeutic effect of Lingze tablets combined with traditional Chinese medicine herbal acupoint plasters on chronic prostatitis.Methods:A total of 64 patients with chronic prostatitis who were a...Objective:To study the therapeutic effect of Lingze tablets combined with traditional Chinese medicine herbal acupoint plasters on chronic prostatitis.Methods:A total of 64 patients with chronic prostatitis who were admitted to the Andrology Clinic of Shuyang County Hospital of Traditional Chinese Medicine from March 2021 to March 2023 were randomly divided into a treatment group and a control group,with 32 cases in each group.The control group took Lingze tablets orally,4 tablets/time,3 times/d;the treatment group took the same medication along with traditional Chinese medicine acupoint herbal plasters.The two groups of patients were treated continuously for 6 weeks,and the differences in the relevant indexes of the curative effect were observed.Results:The NIH-Chronic Prostatitis Symptom Index(NIH-CPSI)scores of the two groups significantly reduced after treatment(P<0.05),and the scores of the patients in the treatment group were lower than those in the control group(P<0.05).The treatment received in the treatment group achieved and efficacy of 96.88%,which was significantly higher than that of the group,which was 81.25%(P<0.05).The maximum flow rate(MFR),average flow rate AFR,and urine output of the patients of both groups improved significantly after treatment(P<0.05).However,the experimental group showed better improvements in these indicators(P<0.05).Conclusion:Lingze tablets combined with traditional Chinese medicine acupoint herbal plasters can significantly improve the symptoms and urodynamic function of patients with chronic prostatitis.展开更多
BACKGROUND The specific benefits of Yangxinshi tablet(YXST)in the treating chronic heart failure(CHF)remain uncertain.AIM To systematically evaluate the efficacy and safety of YXST in the treatment of CHF.METHODS Rand...BACKGROUND The specific benefits of Yangxinshi tablet(YXST)in the treating chronic heart failure(CHF)remain uncertain.AIM To systematically evaluate the efficacy and safety of YXST in the treatment of CHF.METHODS Randomized controlled trials(RCTs)investigating YXST for CHF treatment were retrieved from eight public databases up to November 2023.Meta-analyses of the included clinical studies were conducted using Review Manager 5.3.RESULTS Twenty RCTs and 1845 patients were included.The meta-analysis results showed that the YXST combination group,compared to the conventional drug group,significantly increased the clinical efficacy rate by 23%[relative risk(RR)=1.23,95%CI:1.17-1.29],(P<0.00001),left ventricular ejection fraction by 6.69%[mean difference(MD)=6.69,95%CI:4.42-8.95,P<0.00001]and 6-min walk test by 49.82 m(MD=49.82,95%C:38.84-60.80,P<0.00001),and reduced N-terminal pro-Btype natriuretic peptide by 1.03 ng/L[standardized MD(SMD)=-1.03,95%CI:-1.32 to-0.74,P<0.00001],brain natriuretic peptide by 80.95 ng/L(MD=-80.95,95%CI:-143.31 to-18.59,P=0.01),left ventricular end-diastolic diameter by 3.92 mm(MD=-3.92,95%CI:-5.06 to-2.78,P<0.00001),and left ventricular endsystolic diameter by 4.34 mm(MD=-4.34,95%CI:-6.22 to-2.47,P<0.00001).Regarding safety,neither group reported any serious adverse events during treatment(RR=0.54,95%CI:0.15-1.90,P=0.33).In addition,Egger's test results indicated no significant publication bias(P=0.557).CONCLUSION YXST effectively improves clinical symptoms and cardiac function in patients with CHF while maintaining a favorable safety profile,suggesting its potential as a therapeutic strategy for CHF.展开更多
The aim of this study was to design and evaluate extended-release formulations of a model drug,nicorandil,in order to achieve the desired steady-state plasma concentration of drug in vivo.Simulation was employed to es...The aim of this study was to design and evaluate extended-release formulations of a model drug,nicorandil,in order to achieve the desired steady-state plasma concentration of drug in vivo.Simulation was employed to estimate optimum dissolution and absorption rate of nicorandil.The dissolution test was employed using pH 1.2,4.0,6.8 buffer solution,or water,to measure the in vitro release behaviors of nicorandil formulations.A single dose(15 mg)of each formulation was orally administered to four beagle dogs under fasted conditions,and the pharmacokinetic parameters were calculated.The in vitro/in vivo relationship of the extended-release formulation was confirmed using in vitro dissolution profiles and plasma concentrations of drug in beagle dogs.Nicorandil was released completely within 30 min from the immediate-release tablets and released for 24 h from the extended-release tablets.The nicorandil plasma concentration could be modified by adjusting the drug release rate from the extended-release formulation.The release rate of nicorandil was the rate-limiting step in the overall absorption of drug from the extendedrelease formulations.These results highlight the potential of a nicorandil extended-release formulation in the treatment of angina pectoris.展开更多
Objective:To investigate the therapeutic effect of Biling Weitong Granules combined with oryz-aspergillus enzyme and pancreatin tablets on patients with reflux esophagitis with functional dyspepsia.Methods:Sixty patie...Objective:To investigate the therapeutic effect of Biling Weitong Granules combined with oryz-aspergillus enzyme and pancreatin tablets on patients with reflux esophagitis with functional dyspepsia.Methods:Sixty patients diagnosed with reflux esophagitis with functional dyspepsia who were admitted to the Affiliated Hospital of Hebei University between June 2020 and June 2023 were selected and divided into two groups:the control group and the observation group,each consisting of 30 cases.The control group received oryz-aspergillus enzyme and pancreatin tablets only,while the observation group received Biling Weitong Granules in addition to the tablets.The clinical efficacy,Chinese medicine syndrome points,esophageal kinetic indexes,gastrointestinal hormone levels,and therapeutic safety of both groups were evaluated.Results:The total efficiency of the observation group reached 93.33%,significantly higher than the 73.33%of the control group(P<0.05).After treatment,patients in the observation group exhibited significantly lower scores for Chinese medicine symptoms such as early satiety,belching,abdominal distension,abdominal pain,and loss of appetite compared to the control group(P<0.05).Furthermore,the observation group showed significantly higher upper esophageal sphincter pressure,lower esophageal sphincter pressure,and distal esophageal contraction scores compared to the control group(P<0.05).Additionally,levels of gastric motility hormone,vasoactive intestinal peptide,and gastrin were significantly higher in the observation group compared to the control group(P<0.05).Throughout the treatment period,there was no significant difference in the incidence of adverse reactions between the two groups,indicating comparable safety of the two treatment modalities(P>0.05).Conclusion:The combination of Biling Weitong Granules with oryz-aspergillus enzyme and pancreatin tablets demonstrates significant efficacy in the treatment of reflux esophagitis with functional dyspepsia,with a better safety profile.This finding warrants further clinical promotion.展开更多
AIM:To compare efficacy,patient compliance,acceptability,satisfaction,safety,and adenoma detection rate of sodium phosphate tablets(NaP,CLICOLONTM)to a standard 4 L polyethylene glycol(PEG)solution for bowel cleansing...AIM:To compare efficacy,patient compliance,acceptability,satisfaction,safety,and adenoma detection rate of sodium phosphate tablets(NaP,CLICOLONTM)to a standard 4 L polyethylene glycol(PEG)solution for bowel cleansing for adults undergoing colonoscopy.METHODS:In this multicenter,randomized,prospective,investigator-blind study,the relatively young(19-60years)healthy outpatients without comorbidity were randomly assigned to one of two arms.All colonoscopy were scheduled in the morning.The NaP group was asked to take 4 tablets,5 times the evening before and4 tablets,3 times early on the morning of the colonoscopy.The PEG group was asked to ingest 2 L of solution the evening before and 2 L early in the morning of the procedure.Adequacy of bowel preparation was scored using the Boston bowel preparation scale.RESULTS:No significant differences were observed between the NaP group(n=158)and PEG group(n=162)in bowel cleansing quality(adequate preparation93.0%vs 92.6%,P=0.877),patient compliance(P=0.228),overall adverse events(63.3%vs 69.1%,P=0.269),or adenoma detection rate(34.8%vs 35.2%,P=0.944).Patient acceptability,satisfaction,and patient rating of taste were higher in the NaP group than in the PEG group(P<0.001).CONCLUSION:NaP tablets,compared with PEG solution,produced equivalent colon cleansing,did not cause more side effects,and had better patient acceptability and satisfaction in the relatively young(age<60years)healthy individuals without comorbidity.An oral tablet formulation could make bowel preparation less burdensome,resulting in greater patient participation in screening programs.展开更多
The objective of this study is to evaluate the feasibility of obtaining extended release of tacrolimus by a novel combination of lipid-based solid dispersion and matrix-type extended release tablet techniques. Tacroli...The objective of this study is to evaluate the feasibility of obtaining extended release of tacrolimus by a novel combination of lipid-based solid dispersion and matrix-type extended release tablet techniques. Tacrolimus solid dispersion was prepared using glycerylbehenate(Compritol~?ATO888) and Pluronic F127 as the carrier materials with hot-melt method, which was then blended with hydrogel matrix materials, such as HPMC and lactose, the powders were directly compressed into tablets. In vitro drug release tests were carried out to evaluate the performance of the solid dispersions and the tablets. The dissolution rate of tacrolimus was significantly improved by the lipid-based solid dispersion, and the incorporation of HPC into the solid dispersion obviously improved its stability after storage. Extended release tablets loaded with tacrolimus solid dispersion showed prolonged drug release patterns over 24 h, the release patterns of the tablets can be tailored by the compositions of the matrix materials, including the types and content of HPMCs. A modified processing method that directly mixed the melted solid dispersion with HPMC powders improved the uniformity of the solid dispersion inside the tablet matrix and release profile. The release data of the extended release tablet fitted well to the Korsmeyer–Peppas model with n value of 0.85, which suggested diffusion-and erosion-controlled release mechanism. The combination of lipid-based solid dispersion and HPMC hydrogel matrix may find wide applications in the extended release dosage forms of high potent, water-insoluble drugs.展开更多
The aim of the study was to develop actarit double-layered osmotic pump tablets to overcome the weak points of actarit common tablets, such as short half-life and large plasma concentration fluctuations. Single factor...The aim of the study was to develop actarit double-layered osmotic pump tablets to overcome the weak points of actarit common tablets, such as short half-life and large plasma concentration fluctuations. Single factor experiment and orthogonal test were applied to optimize the formulation;the pharmacokinetic study was performed in beagle dogs adopting actarit common tablets as reference tablets. The optimal formulation was as follows: drug layer: 150 mg actarit, 240 mg PEO-N80, 50 mg NaCl;push layer: 140 mg PEO-WSR303, 20 mg NaCl;coating solution: 30 g cellulose acetate and 6 g PEG 4000 in 1000 ml 94% acetone solution, 60 mg coating weight gain. The pharmacokinetic study showed that T max was prolonged by the contrast of commercial common tablets with constant drug release rate, but the bioavailability was equivalent. And a good in vivo –in vitro correlation of the actarit osmotic pump tablets was also established. The designed actarit osmotic pump tablets can be applied for rheumatoid arthritis, proposing a promising replacement for the marked common products.展开更多
The objective of this study is to investigate the feasibility of using chitosanesodium alginate(CSeSA)based matrix tablets for extended-release of highly water-soluble drugs by changing formulation variables.Using tri...The objective of this study is to investigate the feasibility of using chitosanesodium alginate(CSeSA)based matrix tablets for extended-release of highly water-soluble drugs by changing formulation variables.Using trimetazidine hydrochloride(TH)as a water-soluble model drug,influence of dissolution medium,the amount of CSeSA,the CS:SA ratio,the type of SA,the type and amount of diluents,on in vitro drug release from CSeSA based matrix tablets were studied.Drug release kinetics and release mechanisms were elucidated.In vitro release experiments were conducted in simulated gastric fluid(SGF)followed by simulated intestinal fluid(SIF).Drug release rate decreased with the increase of CSeSA amount.CS:SA ratio had only slight effect on drug release and no influence of SA type on drug release was found.On the other hand,a large amount of water-soluble diluents could modify drug release profiles.It was found that drug release kinetics showed the best fit to Higuchi equation with Fickian diffusion as the main release mechanism.In conclusion,this study demonstrated that it is possible to design extended-release tablets of watersoluble drugs using CSeSA as the matrix by optimizing formulation components,and provide better understanding about drug release from CSeSA matrix tablets.展开更多
文摘A procedure to evaluate the quality consistency of generic drugs based on the impurity profile and the similarity analysis methods was presented in this paper. Nifedipine extended-release tablets from six generic factories of China were used to evaluate the uniformity with the original drug in the study. The procedure includes: choice of chromatographic methods, data collection and conformity test, evaluation of intra-batch similarity of drugs, evaluation of generic drugs with the original drug and weighted similarity evaluation of generic drugs. The data were collected via high-performance liquid chromatography (HPLC), and then calculated by correlation coefficient, cosine, principal component analysis (PCA) and hierarchical clustering analysis (HCA). It is more suitable to use peak areas as the vector when calculating the similarity of impurity profile. After weighting the peak areas of the unspecified impurities in further evaluation of the generic quality, the generic level of different factories was differentiated and the best generic factory was picked out.
基金CAPES(Coordenacao de Aperfeicoamento de Pessoal de Nível Superior)FAPERJ(Fundacao de Amparo a Pesquisa do Estado do Rio de Janeiro)for the financial support
文摘A dissolution test for fesoterodine low dose extended-release tablets using liquid chromatographic(LC) method equipped with a C18 monolithic column was developed and validated. LC system was operated isocratically at controlled temperature(40 1C) using a mobile phase of acetonitrile:methanol:0.03 M ammonium acetate(p H 3.8)(30:15:55, v/v/v), run at a flow rate of 1.5 m L/min and detected at 208 nm. The best dissolution conditions for this formulation were achieved using a USP apparatus 2(paddle) at 100 rpm and 900 m L of phosphate buffer at p H 6.8 as the dissolution medium.Validation parameters such as the specificity, linearity, accuracy, precision, and robustness were evaluated according to international guidelines, giving results within the acceptable range. The kinetic parameters of drug release were also investigated using model-dependent methods and the dissolution profiles were best described by the Higuchi model. The validated dissolution test can be applied for quality control of this formulation.
文摘Objective:To investigate and analyze the clinical effect of clopidogrel bisulfate tablets combined with aspirin enteric-coated tablets on acute myocardial infarction(AMI)patients.Methods:The study period was from January 2020 to December 2023,the sample source was 82 AMI patients admitted to our hospital,grouped into an observation group(n=41)and a control group(n=41)by the numerical table method.The patients in the control group were treated with aspirin enteric-coated tablets,and the patients in the observation group were treated with aspirin enteric-coated tablets combined with clopidogrel bisulfate.The clinical efficacy,coagulation indexes,and the incidence of cardiovascular adverse events between the two groups were compared.Results:The clinical efficacy of the observation group was higher than that of the control group(P<0.05);the platelet aggregation rate(PAR)of the observation group was lower than that of the con-trol group after treatment(P<0.05),and there was no significant difference in the prothrombin time(PT)and activated partial thromboplastin time(APTT)between the two groups(P>0.05).The incidence of cardiovascular adverse events in the observation group was lower than that of the control group(P<0.05).Conclusion:The treatment effect of clopidogrel bisulfate tablets combined with aspirin enteric-coated tablets on AMI patients is remarkable.It reduces the PAR and the incidence of cardiovascular adverse events,so this treatment method should be popularized.
文摘The objective of this study is to develop chitosaneanionic polymers based extendedrelease tablets and test the feasibility of using this system for the sustained release of highly water-soluble drugs with high drug loading.Here,the combination of sodium valproate(VPS)and valproic acid(VPA)were chosen as the model drugs.Anionic polymers studied include xanthan gum(XG),carrageenan(CG),sodium carboxymethyl cellulose(CMC-Na)and sodium alginate(SA).The tablets were prepared by wet granulation method.In vitro drug release was carried out under simulated gastrointestinal condition.Drug release mechanism was studied.Compared with single polymers,chitosaneanionic polymers based system caused a further slowdown of drug release rate.Among them,CS exanthan gum matrix system exhibited the best extended-release behavior and could extend drug release for up to 24 h.Differential scanning calorimetry(DSC)and Fourier transform infrared spectroscopy(FTIR)studies demonstrated that polyelectrolyte complexes(PECs)were formed on the tablet surface,which played an important role on retarding erosion and swelling of the matrix in the later stage.In conclusion,this study demonstrated that it is possible to develop highly water-soluble drugs loaded extendedrelease tablets using chitosaneanionic polymers based system.
文摘The purpose of this study was to develop an extended-release(ER) matrix tablet that shows robust dissolution properties able to account for the variability of pH and mechanical stress in the GI tract using a combination of enteric polymer and hydrophilic polymer. Hypromellose acetate succinate(HPMCAS) and hydroxypropylcellulose(HPC) were selected as ER polymers for the ER matrix tablet(HPMCAS/HPC ER matrix tablet). Oxycodone hydrochloride was employed as a model drug. Dissolution properties of the HPMCAS/HPC ER matrix tablets were evaluated and were not affected by the pH of the test medium or paddle rotating speed.In a USP apparatus 3(bio-relevant dissolution method), dissolution profiles of the HPMCAS/HPC ER matrix tablets containing oxycodone hydrochloride were similar to that of the reference product(OxyC ontin). Moreover, in vivo performance after oral administration of the HPMCAS/HPC ER matrix tablets to humans was simulated by GastroP lus based on dissolution profiles from the USP apparatus 3. The plasma concentration-time profile simulated was similar to that of the reference product. These results suggest that the combination of HPMCAS and HPC shows a robust dissolution profile against pH and paddle rotating speed and indicates the appropriate extended-release profile in humans.
基金the Fundamental Research Funds for the Central Universities(grant number:2021-JYB-XJSJJ-003)the Open Project of State Key Laboratory of Bioactive Substance and Function of Natural Medicines(grant number:GTZK202108)+1 种基金Chinese Society of Toxicology(grant number:CST2021CT101)Discipline Construction Project of Peking Union Medical College(grant number:201920200801).
文摘Background:Jinqi Jiangtang tablets(JQJT)have been approved for the treatment of type 2 diabetes mellitus(T2DM)in China for many years.Exploring the effective substances and mechanisms of JQJT is important for its clinical application and further drug research and development.This study aimed to explore the chemical basis and mechanisms of JQJT in the treatment of T2DM.Methods:With network pharmacology,we screened substances in JQJT and their possible targets,then constructed the action network and enriched the biological functions and pathways associated with the active components,and identified the potential targets and mechanisms of JQJT in the treatment of T2DM.Based on the network pharmacology data,we explored the hypoglycemic mechanisms of coptisine in JQJT through western blot and quantitative real-time polymerase chain reaction.Results:Forty-three compounds with good pharmacokinetic properties were identified in JQJT,together with 146 potential biological targets.Among these potential targets,74 were associated with treatment of T2DM.A compound-target network of the 43 compounds against T2DM was constructed.Biological process and signal pathway enrichment analysis of the network highlighted the FoxO signaling pathway.Western blot and quantitative real-time polymerase chain reaction results showed that coptisine,but not epiberberine,significantly inhibited expression of key genes involved in hepatocyte gluconeogenesis by regulating the FoxO1 signaling pathway.Conclusion:Network pharmacology analysis and cell experiments showed that coptisine regulated glucose homeostasis by inhibiting the FoxO1 signaling pathway and hepatic gluconeogenesis,which may be one of the mechanisms of JQJT in the treatment of T2DM.
基金Supported by School-level High-level Talent Project (XGY2021A022)Doctoral Research Startup Fund of Department of Science&Technology of Liaoning Province (2021-BS-252)。
文摘[Objectives]This study was conducted to optimize the Formulation Process of glucosamine chondroitin sulfate tablets. [Methods] The orthogonal design with three levels was carried out with microcrystalline cellulose, calcium hydrophosphate and cross-linked polyvinylpyrrolidone as three factors to optimize the preparation process. [Results] When microcrystalline cellulose 200 mg/tablet, calcium hydrophosphate 150 mg/tablet, and cross-linked polyvinylpyrrolidone 80 mg/tablet were added, the angle of repose could meet the requirements of tablet pressing, and the dissolution could reach more than 95% in 30 min. The results of the orthogonal test showed that the dissolution effect of self-made tablets was faster than that of commercial products. [Conclusions] The glucosamine hydrochloride chondroitin sulfate tablets prepared by this prescription have better quality.
基金The study was approved by the Ethics Committee of Beijing Changping Hospital of Traditional and Western Medicine.
文摘BACKGROUND Depression is a widespread mental health condition that requires effective treatment.In the treatment of depression,traditional Chinese medicine(TCM)offers obvious advantages,fewer adverse reactions,and a lower recurrence rate.AIM To evaluate the clinical benefits of Guipi decoction combined with escitalopram oxalate tablets for individuals with depression.METHODS In total,80 patients diagnosed as having depression were enrolled in the study and divided into either an experimental group or a control group.All of the patients were orally administered escitalopram oxalate tablets.Additionally,the experimental group received Jiajian Guipi decoction and reduced Governor vessel fumigation over 4 wk.TCM syndrome scores,Hamilton depression rating scale(HAM-D)scores,self-rating depression scale(SDS)scores,and Pittsburgh sleep quality index scores were measured for the two groups and compared before and after the treatment.The two groups were monitored for any adverse reactions.RESULTS After 4 wk of treatment,both groups exhibited a significant reduction in TCM syndrome scores compared with their pre-treatment scores(P<0.05).However,the experimental group exhibited significantly lower TCM syndrome scores than the control group(P<0.05).Similarly,the post-treatment SDS and HAM-D-24 scores were significantly lower in both groups than the pre-treatment scores(P<0.05),with the experimental group exhibiting lower scores than the control group(P<0.05).The total treatment efficiency was significantly better in the experimental group(97.14%)than in the control group(77.78%)(P<0.05).Furthermore,after 4 wk of treatment,the Pittsburgh sleep quality index scores for both groups were significantly lower than those before the treatment(P<0.05),with the experimental group exhibiting lower scores than the control group(P<0.05).The incidence of adverse reactions was significantly lower in the experimental group than in the control group(P<0.05).CONCLUSION The combination of Guipi decoction and escitalopram oxalate tablets was found to be an effective and safe treatment for depression.This combination could reduce TCM syndrome scores,improve depressive symptoms,and enhance sleep quality.
基金supported by a grant from Key Project of Education Commission of Hubei Province(D20202802).
文摘Background:Naodesheng tablets(NDST)was widely used in clinical treatment as a drug for cardiovascular diseases,but the mechanism for treating atherosclerosis was unknown.On the basis of network pharmacology and bioinformatics,predict the relevant targets and signalling pathways for NDST in the treatment of atherosclerosis.Methods:First,the targets of NDST and the targets for treating atherosclerosis were looked for in different databases.Next,Venny 2.1.0 was used to find the genes that overlapped between NDST and targets for treating atherosclerosis.Subsequently,the herb-active ingredient-target-disease were obtained to explore the hub compound.Furthermore,the Metascape database was used for Gene Ontology and Kyoto Encyclopedia of Genes and Genomes enrichment analysis.And we constructed the“active ingredient-intersection target-pathway”network by Cytoscape software to gain the hub genes and pathways.Finally,molecular docking was used to verify the affinity of hub ingredients and hub genes.Results:In the results,67 active ingredients and 322 targets of NDST were selected in ingredients-targets network.154 overlapping targets of NDST(322)and atherosclerosis(1330)were obtained.Then,the herb-active ingredient-target-disease showed that quercetin,apigenin and luteolin were the hub ingredients to treat atherosclerosis.Further,the hub genes(PTGS2,RXRA,CASP3)and pathways(lipid and atherosclerosis)were accessed in active ingredient-intersection target-pathway.Finally,the results indicated that quercetin,apigenin and luteolin were better binding the PTGS2,RXRA,CASP3,especially PTGS2 and luteolin in molecular docking.Conclusion:In conclusion,quercetin,apigenin and luteolin,as the main ingredients of NDST could play a important role in PTGS2,RXRA,and CASP3 for treating atherosclerosis via the lipid and atherosclerosis(TNF signaling pathway).
基金financially supported by the National Natural Science Foundation of China(No.82170701).
文摘Objective This study aimed to analyze the clinical efficacy of the Jianpi Shengxue tablet for treating renal anemia.Methods A total of 200 patients with renal anemia from December 2020 to December 2022 were enrolled and randomly divided into two groups.Patients in the control group were treated with polysaccharide-iron complex,and those in the experimental group were administered Jianpi Shengxue tablet.After 8 weeks of continuous treatment,the therapeutic outcomes regarding anemia were compared between the two groups.Results After treatment,the red blood cell(RBC)count,hematocrit(HCT),reticulocyte percentage(RET),ferritin(SF),serum iron(SI),transferrin saturation(TSAT),and serum albumin(ALB)all increased(P<0.01),and the clinical symptom score and total iron binding capacity decreased(P<0.01)in the experimental group.Moreover,the improvements in RBC,HCT,RET,SF,SI,TAST,ALB,and clinical symptoms(fatigue,anorexia,dull skin complexion,numbness of hands and feet)in the experimental group were significantly greater than those in the control group(P<0.05).The total effective rate for treating renal anemia was significantly higher in the experimental group than in the control group(P<0.01).Conclusion The Jianpi Shengxue tablet demonstrates efficacy in treating renal anemia,leading to significant improvements in the laboratory examination results and clinical symptoms of patients with renal anemia.
文摘Objective:To study the therapeutic efficacy of patients with ulcerative colitis receiving Bifidobacterium quadruple viable tablets.Methods:49 cases were selected from ulcerative colitis patients who attended the clinic from February 2021 to November 2022,and were randomly grouped into group A for addition of Bifidobacterium quadruple viable tablets treatment,and group B for conventional medication.The efficacy,inflammatory factors,nutritional indexes,and adverse reactions were compared between the groups.Results:The efficacy of UC patients in group A was higher than that in group B(P<0.05);the inflammatory factors in group A were lower than that in group B(P<0.05);nutritional indicators in group A were higher than that in group B(P<0.05);and the adverse reactions of medication in UC patients in group A were lower than that in group B(P<0.05).Conclusion:The treatment of UC patients with the addition of Bifidobacterium quadruple viable tablets can improve the nutritional status of the organism,inhibit the progression of inflammation,and is safe and efficient in treating ulcerative colitis.
文摘Objective:To analyze the clinical efficacy of megestrol acetate dispersible tablets in the adjuvant treatment of acute leukemia.Methods:80 patients with acute leukemia admitted from December 2021 to December 2022 were randomly divided into two groups.The control group underwent chemotherapy,and the observation group took megestrol acetate dispersible tablets and underwent chemotherapy.The effect of the treatments were evaluated by analyzing the albumin(Alb)and prealbumin(Palb)indicators,and the adverse reactions were observed.Results:There was no significant difference in Alb and Palb indexes between the two groups before treatment(P>0.05).After treatment,Alb and Palb indexes in the observation group were greater than those in the control group(P<0.05).The incidence of adverse reactions in the control group was 20.00%,which was significantly higher than the observation group(5.00%),with P<0.05.Conclusion:The combination of megestrol acetate dispersible tablets and chemotherapy is more effective in treating patients with acute leukemia,and the Alb and Palb indexes can be optimized.Besides,there are fewer adverse reactions,which means that the treatment is relatively safe.
文摘Objective:To study the therapeutic effect of Lingze tablets combined with traditional Chinese medicine herbal acupoint plasters on chronic prostatitis.Methods:A total of 64 patients with chronic prostatitis who were admitted to the Andrology Clinic of Shuyang County Hospital of Traditional Chinese Medicine from March 2021 to March 2023 were randomly divided into a treatment group and a control group,with 32 cases in each group.The control group took Lingze tablets orally,4 tablets/time,3 times/d;the treatment group took the same medication along with traditional Chinese medicine acupoint herbal plasters.The two groups of patients were treated continuously for 6 weeks,and the differences in the relevant indexes of the curative effect were observed.Results:The NIH-Chronic Prostatitis Symptom Index(NIH-CPSI)scores of the two groups significantly reduced after treatment(P<0.05),and the scores of the patients in the treatment group were lower than those in the control group(P<0.05).The treatment received in the treatment group achieved and efficacy of 96.88%,which was significantly higher than that of the group,which was 81.25%(P<0.05).The maximum flow rate(MFR),average flow rate AFR,and urine output of the patients of both groups improved significantly after treatment(P<0.05).However,the experimental group showed better improvements in these indicators(P<0.05).Conclusion:Lingze tablets combined with traditional Chinese medicine acupoint herbal plasters can significantly improve the symptoms and urodynamic function of patients with chronic prostatitis.
基金Supported by Hunan Provincial Chinese Medicine Research Program Commissioned Key Projects,No.D2023005。
文摘BACKGROUND The specific benefits of Yangxinshi tablet(YXST)in the treating chronic heart failure(CHF)remain uncertain.AIM To systematically evaluate the efficacy and safety of YXST in the treatment of CHF.METHODS Randomized controlled trials(RCTs)investigating YXST for CHF treatment were retrieved from eight public databases up to November 2023.Meta-analyses of the included clinical studies were conducted using Review Manager 5.3.RESULTS Twenty RCTs and 1845 patients were included.The meta-analysis results showed that the YXST combination group,compared to the conventional drug group,significantly increased the clinical efficacy rate by 23%[relative risk(RR)=1.23,95%CI:1.17-1.29],(P<0.00001),left ventricular ejection fraction by 6.69%[mean difference(MD)=6.69,95%CI:4.42-8.95,P<0.00001]and 6-min walk test by 49.82 m(MD=49.82,95%C:38.84-60.80,P<0.00001),and reduced N-terminal pro-Btype natriuretic peptide by 1.03 ng/L[standardized MD(SMD)=-1.03,95%CI:-1.32 to-0.74,P<0.00001],brain natriuretic peptide by 80.95 ng/L(MD=-80.95,95%CI:-143.31 to-18.59,P=0.01),left ventricular end-diastolic diameter by 3.92 mm(MD=-3.92,95%CI:-5.06 to-2.78,P<0.00001),and left ventricular endsystolic diameter by 4.34 mm(MD=-4.34,95%CI:-6.22 to-2.47,P<0.00001).Regarding safety,neither group reported any serious adverse events during treatment(RR=0.54,95%CI:0.15-1.90,P=0.33).In addition,Egger's test results indicated no significant publication bias(P=0.557).CONCLUSION YXST effectively improves clinical symptoms and cardiac function in patients with CHF while maintaining a favorable safety profile,suggesting its potential as a therapeutic strategy for CHF.
基金supported by the Basic Science Research Program through the National Research Foundation of Korea(NRF)funded by the Korean Ministry of Education,Science and Technology(NRF-2012R1A1A1013210)by a grant of the Korean Health Technology R&D Project,Ministry of Health,Welfare&Family Affairs,Republic of Korea(A092018).
文摘The aim of this study was to design and evaluate extended-release formulations of a model drug,nicorandil,in order to achieve the desired steady-state plasma concentration of drug in vivo.Simulation was employed to estimate optimum dissolution and absorption rate of nicorandil.The dissolution test was employed using pH 1.2,4.0,6.8 buffer solution,or water,to measure the in vitro release behaviors of nicorandil formulations.A single dose(15 mg)of each formulation was orally administered to four beagle dogs under fasted conditions,and the pharmacokinetic parameters were calculated.The in vitro/in vivo relationship of the extended-release formulation was confirmed using in vitro dissolution profiles and plasma concentrations of drug in beagle dogs.Nicorandil was released completely within 30 min from the immediate-release tablets and released for 24 h from the extended-release tablets.The nicorandil plasma concentration could be modified by adjusting the drug release rate from the extended-release formulation.The release rate of nicorandil was the rate-limiting step in the overall absorption of drug from the extendedrelease formulations.These results highlight the potential of a nicorandil extended-release formulation in the treatment of angina pectoris.
文摘Objective:To investigate the therapeutic effect of Biling Weitong Granules combined with oryz-aspergillus enzyme and pancreatin tablets on patients with reflux esophagitis with functional dyspepsia.Methods:Sixty patients diagnosed with reflux esophagitis with functional dyspepsia who were admitted to the Affiliated Hospital of Hebei University between June 2020 and June 2023 were selected and divided into two groups:the control group and the observation group,each consisting of 30 cases.The control group received oryz-aspergillus enzyme and pancreatin tablets only,while the observation group received Biling Weitong Granules in addition to the tablets.The clinical efficacy,Chinese medicine syndrome points,esophageal kinetic indexes,gastrointestinal hormone levels,and therapeutic safety of both groups were evaluated.Results:The total efficiency of the observation group reached 93.33%,significantly higher than the 73.33%of the control group(P<0.05).After treatment,patients in the observation group exhibited significantly lower scores for Chinese medicine symptoms such as early satiety,belching,abdominal distension,abdominal pain,and loss of appetite compared to the control group(P<0.05).Furthermore,the observation group showed significantly higher upper esophageal sphincter pressure,lower esophageal sphincter pressure,and distal esophageal contraction scores compared to the control group(P<0.05).Additionally,levels of gastric motility hormone,vasoactive intestinal peptide,and gastrin were significantly higher in the observation group compared to the control group(P<0.05).Throughout the treatment period,there was no significant difference in the incidence of adverse reactions between the two groups,indicating comparable safety of the two treatment modalities(P>0.05).Conclusion:The combination of Biling Weitong Granules with oryz-aspergillus enzyme and pancreatin tablets demonstrates significant efficacy in the treatment of reflux esophagitis with functional dyspepsia,with a better safety profile.This finding warrants further clinical promotion.
文摘AIM:To compare efficacy,patient compliance,acceptability,satisfaction,safety,and adenoma detection rate of sodium phosphate tablets(NaP,CLICOLONTM)to a standard 4 L polyethylene glycol(PEG)solution for bowel cleansing for adults undergoing colonoscopy.METHODS:In this multicenter,randomized,prospective,investigator-blind study,the relatively young(19-60years)healthy outpatients without comorbidity were randomly assigned to one of two arms.All colonoscopy were scheduled in the morning.The NaP group was asked to take 4 tablets,5 times the evening before and4 tablets,3 times early on the morning of the colonoscopy.The PEG group was asked to ingest 2 L of solution the evening before and 2 L early in the morning of the procedure.Adequacy of bowel preparation was scored using the Boston bowel preparation scale.RESULTS:No significant differences were observed between the NaP group(n=158)and PEG group(n=162)in bowel cleansing quality(adequate preparation93.0%vs 92.6%,P=0.877),patient compliance(P=0.228),overall adverse events(63.3%vs 69.1%,P=0.269),or adenoma detection rate(34.8%vs 35.2%,P=0.944).Patient acceptability,satisfaction,and patient rating of taste were higher in the NaP group than in the PEG group(P<0.001).CONCLUSION:NaP tablets,compared with PEG solution,produced equivalent colon cleansing,did not cause more side effects,and had better patient acceptability and satisfaction in the relatively young(age<60years)healthy individuals without comorbidity.An oral tablet formulation could make bowel preparation less burdensome,resulting in greater patient participation in screening programs.
文摘The objective of this study is to evaluate the feasibility of obtaining extended release of tacrolimus by a novel combination of lipid-based solid dispersion and matrix-type extended release tablet techniques. Tacrolimus solid dispersion was prepared using glycerylbehenate(Compritol~?ATO888) and Pluronic F127 as the carrier materials with hot-melt method, which was then blended with hydrogel matrix materials, such as HPMC and lactose, the powders were directly compressed into tablets. In vitro drug release tests were carried out to evaluate the performance of the solid dispersions and the tablets. The dissolution rate of tacrolimus was significantly improved by the lipid-based solid dispersion, and the incorporation of HPC into the solid dispersion obviously improved its stability after storage. Extended release tablets loaded with tacrolimus solid dispersion showed prolonged drug release patterns over 24 h, the release patterns of the tablets can be tailored by the compositions of the matrix materials, including the types and content of HPMCs. A modified processing method that directly mixed the melted solid dispersion with HPMC powders improved the uniformity of the solid dispersion inside the tablet matrix and release profile. The release data of the extended release tablet fitted well to the Korsmeyer–Peppas model with n value of 0.85, which suggested diffusion-and erosion-controlled release mechanism. The combination of lipid-based solid dispersion and HPMC hydrogel matrix may find wide applications in the extended release dosage forms of high potent, water-insoluble drugs.
文摘The aim of the study was to develop actarit double-layered osmotic pump tablets to overcome the weak points of actarit common tablets, such as short half-life and large plasma concentration fluctuations. Single factor experiment and orthogonal test were applied to optimize the formulation;the pharmacokinetic study was performed in beagle dogs adopting actarit common tablets as reference tablets. The optimal formulation was as follows: drug layer: 150 mg actarit, 240 mg PEO-N80, 50 mg NaCl;push layer: 140 mg PEO-WSR303, 20 mg NaCl;coating solution: 30 g cellulose acetate and 6 g PEG 4000 in 1000 ml 94% acetone solution, 60 mg coating weight gain. The pharmacokinetic study showed that T max was prolonged by the contrast of commercial common tablets with constant drug release rate, but the bioavailability was equivalent. And a good in vivo –in vitro correlation of the actarit osmotic pump tablets was also established. The designed actarit osmotic pump tablets can be applied for rheumatoid arthritis, proposing a promising replacement for the marked common products.
基金supported by Liaoning Institutions excellent talents support plan(No.LR2013047).
文摘The objective of this study is to investigate the feasibility of using chitosanesodium alginate(CSeSA)based matrix tablets for extended-release of highly water-soluble drugs by changing formulation variables.Using trimetazidine hydrochloride(TH)as a water-soluble model drug,influence of dissolution medium,the amount of CSeSA,the CS:SA ratio,the type of SA,the type and amount of diluents,on in vitro drug release from CSeSA based matrix tablets were studied.Drug release kinetics and release mechanisms were elucidated.In vitro release experiments were conducted in simulated gastric fluid(SGF)followed by simulated intestinal fluid(SIF).Drug release rate decreased with the increase of CSeSA amount.CS:SA ratio had only slight effect on drug release and no influence of SA type on drug release was found.On the other hand,a large amount of water-soluble diluents could modify drug release profiles.It was found that drug release kinetics showed the best fit to Higuchi equation with Fickian diffusion as the main release mechanism.In conclusion,this study demonstrated that it is possible to design extended-release tablets of watersoluble drugs using CSeSA as the matrix by optimizing formulation components,and provide better understanding about drug release from CSeSA matrix tablets.