Double-layered osmotic pump controlled release tablets of actarit: In vitro and in vivo evaluation

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.

Jet formation and penetration performance of a double-layer charge liner with chemically-deposited tungsten as the inner liner

This paper proposes a type of double-layer charge liner fabricated using chemical vapor deposition(CVD)that has tungsten as its inner liner.The feasibility of this design was evaluated through penetration tests.Double-layer charge liners were fabricated by using CVD to deposit tungsten layers on the inner surfaces of pure T2 copper liners.The microstructures of the tungsten layers were analyzed using a scanning electron microscope(SEM).The feasibility analysis was carried out by pulsed X-rays,slug-retrieval test and static penetration tests.The shaped charge jet forming and penetration law of inner tungsten-coated double-layer liner were studied by numerical simulation method.The results showed that the double-layer liners could form well-shaped jets.The errors between the X-ray test results and the numerical results were within 11.07%.A slug-retrieval test was found that the retrieved slug was similar to a numerically simulated slug.Compared with the traditional pure copper shaped charge jet,the penetration depth of the double-layer shaped charge liner increased by 11.4% and>10.8% respectively.In summary,the test results are good,and the numerical simulation is in good agreement with the test,which verified the feasibility of using the CVD method to fabricate double-layer charge liners with a high-density and high-strength refractory metal as the inner liner.

Release test of alliin/alliinase double-layer tablet by HPLC-Allicin determination

A simple, precise and accurate method was developed and validated for the determination of allicin release from alliin/alliinase double-layer tablets. According to Appendix XC Ⅱ of Chinese Pharmacopoeia 2010 edition Volume II, a small glass-method was adopted at the rotational speed of 100 r/min using 100 mL phosphate buffer （pH 6.8） as release medium. The release amount was determined by HPLC with a C18 column （250 mm × 4.6 mm, 5 μm） using the mobile phase consisting of methanol -0.4% carboxylic acid （65：35） at a flow rate of 1 mL/min and UV detection at 242 nm. The current method demonstrates good linearity over the range 4.052- 405.2 μg/mL （r2=0.9999） with an average recovery of 105.5%（RSD= 1.25%）. The accumulative release of alliin/alliinase double-layer tablets had good homogeneity for withinand betweenbatches. The method established is simple, accurate and repeatable for the determination of allicin release from alliin/alliinase double-layer tablets.

Discovery and Significance of the Triassic–Late Paleozoic Double-layered Basement in the Songliao Basin:Based on the Complete Coring Data from ICDP Borehole SK2

The Songliao Basin(SLB)covers an area of approximately 260,000 km2in northeastern Asia and preserves a continuous and complete Cretaceous terrestrial record(Wang et al.,2021).The region is the most important petroliferous sedimentary basin in China because of its continual annual oil and gas equivalent production of tens of millions of tons(ca.220–440 million barrels per year)since 1959.The SLB was previously thought to have developed on Hercynian basement and accumulated continuous sedimentary deposits during the Late Jurassic and Cretaceous(Wan et al.,2013;Wang et al.,2016).

Performance and Application of Double-layered Microcapsule Corrosion Inhibitors

Double-layered microcapsule corrosion inhibitors were developed by sodium monofluorophosphate as the core material,polymethyl methacrylate as the inner wall material,and polyvinyl alcohol as the outer wall material combining the solvent evaporation method and spray drying method.The protection by the outer capsule wall was used to prolong the service life of the corrosion inhibitor.The dispersion,encapsulation,thermal stability of microcapsules,and the degradation rate of capsule wall in concrete pore solution were analyzed by ultra-deep field microscopy,scanning electron microscopy,thermal analyzer,and sodium ion release rate analysis.The microcapsules were incorporated into mortar samples containing steel reinforcement,and the effects of double-layered microcapsule corrosion inhibitors on the performance of the cement matrix and the actual corrosion-inhibiting effect were analyzed.The experimental results show that the double-layered microcapsules have a moderate particle size and uniform distribution,and the capsules were completely wrapped.The microcapsules as a whole have good thermal stability below 230 ℃.The monolayer membrane structure microcapsules completely broke within 1 day in the simulated concrete pore solution,and the double-layer membrane structure prolonged the service life of the microcapsules to 80 days in the simulated concrete pore solution before the core material was completely released.The mortar samples containing steel reinforcement incorporated with the double-layered microcapsule corrosion inhibitors still maintained a higher corrosion potential than the monolayer microcapsule corrosion inhibitors control group at 60 days.The incorporation of double-layered microcapsules into the cement matrix has no significant adverse effect on the setting time and early strength.

Clinical Effect of Ilaprazole Enteric-Coated Tablets in Patients with Peptic Ulcer

Objective: To discuss the actual effect of ilaprazole enteric-coated tablets in the treatment of peptic ulcer patients. Methods: 200 peptic ulcer patients who received treatment from January to December 2023 were selected as the study sample, and all patients were randomly and evenly divided into the study group (n = 100) and the control group (n = 100), and the serum inflammatory factors and the disappearance time of symptoms were compared. Results: After treatment, the serum inflammatory factors in the observation group were better than those in the control group, and the time of belching and burning sensation in the observation group was shorter than that in the control group, all of which were statistically significant (P Conclusion: Ilaprazole enteric-coated tablets in the treatment of peptic ulcer have a good effect and can effectively improve the symptoms of patients with clinical signs, with reference significance.

Altered Iron-Mediated Metabolic Homeostasis Governs the Efficacy and Toxicity of Tripterygium Glycosides Tablets Against Rheumatoid Arthritis

Rheumatoid arthritis(RA),a globally increasing autoimmune disorder,is associated with increased disability rates due to the disruption of iron metabolism.Tripterygium glycoside tablets(TGTs),a Tripterygium wilfordii Hook.f.(TwHF)-based therapy,exhibit satisfactory clinical efficacy for RA treatment.However,drug-induced liver injury(DILI)remains a critical issue that hinders the clinical application of TGTs,and the molecular mechanisms underlying the efficacy and toxicity of TGTs in RA have not been fully elucidated.To address this problem,we integrated clinical multi-omics data associated with the anti-RA efficacy and DILI of TGTs with the chemical and target profiling of TGTs to perform a systematic network analysis.Subsequently,we identified effective and toxic targets following experimental validation in a collagen-induced arthritis(CIA)mouse model.Significantly different transcriptome–protein–metabolite profiles distinguishing patients with favorable TGTs responses from those with poor outcomes were identified.Intriguingly,the clinical efficacy and DILI of TGTs against RA were associated with metabolic homeostasis between iron and bone and between iron and lipids,respectively.Particularly,the signal transducer and activator of transcription 3(STAT3)–hepcidin(HAMP)/lipocalin 2(LCN2)–tartrate-resis tant acid phosphatase type 5(ACP5)and STAT3–HAMP–acyl-CoA synthetase long-chain family member 4(ACSL4)–lysophosphatidylcholine acyltransferase 3(LPCAT3)axes were identified as key drivers of the efficacy and toxicity of TGTs.TGTs play dual roles in ameliorating CIA-induced pathology and in inducing hepatic dysfunction,disruption of lipid metabolism,and hepatic lipid peroxidation.Notably,TGTs effectively reversed“iron–bone”disruptions in the inflamed joint tissues of CIA mice by inhibiting the STAT3–HAMP/LCN2–ACP5 axis,subsequently leading to“iron–lipid”disturbances in the liver tissues via modulation of the STAT3–HAMP–ACSL4–LPCAT3 axis.Additional bidirectional validation experiments were conducted using MH7A and AML12 cells to confirm the bidirectional regulatory effects of TGTs on key targets.Collectively,our data highlight the association between iron-mediated metabolic homeostasis and the clinical efficacy and toxicity of TGT in RA therapy,offering guidance for the rational clinical use of TwHF-based therapy with dual therapeutic and toxic potential.

Evaluation of the Clinical Efficacy of Chuzhi Shengfa Tablets and Finasteride in the Treatment of Androgenetic Alopecia

Objective:To explore the clinical efficacy and safety of Chuzhi Shengfa tablets combined with finasteride in the treatment of male androgenetic alopecia(AGA).Methods:Sixty male patients with androgenetic alopecia admitted to our Department of Dermatology between January 2022 and January 2024 were randomly divided into two groups,with 30 patients in each group.The control group was treated with finasteride,while the observation group received a combination of Chuzhi Shengfa tablets and finasteride.The clinical efficacy and adverse reactions in both groups were compared.Results:The overall effectiveness rate in the observation group was 93.33%(28/30),significantly higher than the control group’s 73.33%(22/30),with a statistically significant difference(P<0.05).There was no statistically significant difference in the incidence of adverse reactions between the two groups(P>0.05).Conclusion:The combination of Chuzhi Shengfa tablets and finasteride shows good clinical efficacy in treating male androgenetic alopecia.Additionally,Chuzhi Shengfa tablets are convenient to administer and effectively improve efficacy,significantly improving patients’conditions,and demonstrating good clinical application value.

Analysis of the Therapeutic Effect of Clopidogrel Bisulfate Tablets + Aspirin Enteric-Coated Tablets on Acute Myocardial Infarction

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.

Effectiveness of Chuzhi Shengfa Tablets Combined with Ketoconazole Shampoo and Chuzhi Shengfa Tablets Combined with 5%Minoxidil Foam in the Treatment of Male Androgenetic Alopecia

Objective:To investigate the clinical efficacy and safety of Chuzhi Shengfa Tablets combined with ketoconazole shampoo and Chuzhi Shengfa Tablets combined with 5%minoxidil foam in the treatment of male androgenetic alopecia.Methods:From July 2022 to July 2023,120 male patients with androgenetic alopecia were selected from our Department of Dermatology and randomly divided into Control Group 1,Control Group 2,Observation Group 1,and Observation Group 2,with 30 patients in each group.Control Group 1 was treated with ketoconazole shampoo,Control Group 2 with 5%minoxidil foam,Observation Group 1 with ketoconazole shampoo combined with Chuzhi Shengfa Tablets,and Observation Group 2 with 5%minoxidil foam combined with Chuzhi Shengfa Tablets.Hair density,hair diameter,scalp oil secretion(using oil secretion scoring),and adverse reactions were compared before and after treatment across the four groups.Results:After treatment,hair density and hair diameter significantly increased in all four groups compared to before treatment,while scalp oil secretion scores significantly decreased(P<0.05).The improvements in Observation Groups 1 and 2 were significantly better than those in Control Groups 1 and 2(P<0.05).No significant differences in the incidence of adverse reactions were observed among the four groups(P>0.05).Conclusion:Chuzhi Shengfa Tablets combined with ketoconazole shampoo and Chuzhi Shengfa Tablets combined with 5%minoxidil foam are both effective and safe for treating male androgenetic alopecia.These combinations can significantly improve hair growth and are worthy of clinical promotion.

Simultaneous Determination of Baicalin, Berberine and Rhein by HPLC in Traditional Chinese Patent Medicine Sanhuang Tablets

Aim To establish a reversed phase liquid chromatographic method forsimultaneous determination of three main medicinal constituents, baicalin, berberine and rhein, inSanhuang tablets. Methods The separation was performed on a Kromasil C_(18) column with TEA-adjusted0.02 mol·L^(-1) H_3PO_4 (pH 6.78)-acetonitrile-methanol (40 : 9 : 7) as mobile phase at aflow-rate of 1.0 mL·min^(-1), with detection at 254 ran. Considering interaction between acidic andalkaline compounds, three standard markers were added respectively and the volume of samplesolution was doubled in recovery experiments. Results Three regression equations revealed excellentlinear relationship between the peak areas and concentrations and the correlation coefficients allsurpassed 0.999 8. The average recovery was 96.1% (RSD = 2.1%) baicalin, 98.5% (RSD = 2.4%) forberberine, and 101.5% (RSD =1.3%) for rhein. Conclusion The method developed can be used to controlthe quality of Sanhuang tablets comprehensively.

Pharmacokinetics of nifedipine sustained-release tablets in healthy Chinese volunteers

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.

High Resolution Determination of Ondansetron in Human Plasma by HPLC and Pharmacokinetics of Orally Disintegrating Tablets

Ahn To develop a high resolution HPLC method for the determination of ondansetron in human plasma and to study the pharmacokinetics of ondansetron in orally disintegrating tablets. Methods HPLC determination involved liquid-liquid extraction, separation on a CN column and ultraviolet detection at 310 ran with granisetron as an internal standard. Pharmacokinetics and bioequivalence of ondansetron in orally disintegrating tablets by direct compression and conventional 8 mg tablets were evaluated and compared in 20 healthy human male volunteers after a single oral dose in a randomized cross-over study. Results The limit of quantification was 0.25 ng· mL^-1. The recovery was about 85 % or over for ondan setron and about 90% for internal standard. Linearity was good within the concentration range of 0.5 - 50 ng·mL^-1 with r^2 ranging from 0.997 1 to 0.999 9. Intra- and inter-assay coefficients of variation ranged from 1.78% to 2.38% and 3.88% -5.19%, respectively. Accuracies for spiked concentrations of 2.0, 10.0, and 30.0 ng·mL^-1 were 104.7% ±4.4%, 102.2% ± 1.1%, and99.51% ±2.34%, respectively. Pharmacokinetic parameters of AUCo-t, AUCo-∞ , Cmax, Tmax, and T1/2 were 230.2 ± 78.0 ng·h·L^-1 , 265.2± 101.5 ng·h·mL^-1, 35.67 ± 8.94 ng·mL^-l, 1.51 ±0.79 h, and 5.00± 1.41 h for orally disintegrating tablets, respectively. The analysis of variance did not show any significant difference between orally disintegrating tablets and conventional tablets, and 90% confidence intervals fell within the acceptable range for bioequivalence. Conclusion High resolution HPLC method has been set up and applied in pharmacokinetic evaluation of ondansetron in orally disintegrating tablets.

Compound Metformin/Glipizide Bilayer Extended Release Tablets: Development and in Vitro Release

Aim In this study, compound metformin/glipizide bilayer extended release tablets were formulated with hydroxypropyl methylcellulose （HPMC） by wet granulation technique in order to tackle the problems associated with the muhidrug therapy of non-insulin dependent diabetes mellitus. Me^ls High-dose metformin is difficult to formulate into a tablet dosage form due to its poor compressibility and compactibility. In this study, the way to overcome the difficulty was to utilize stearic alcohol to prepare the tablet formulation. The influences of viscosity, amount of HPMC, and weight of fillers were investigated. The optimal formulation had acceptable physicochemical properties and released metformin and glipizide over 10 h. Results The data of metformin obtained from in vitro release fitted Higuchi kinetics best, while the release of glipizide in vitro was found to follow zero kinetics. Conclusion Compound metformin/glipizide bilayer extended release tablets have been successfully developed.

Double-layer model updating for steel-concrete composite beam cable-stayed bridge based on GPS

In order to establish the relationship between the measured dynamic response and the health status of long-span bridges, a double-layer model updating method for steel-concrete composite beam cable-stayed bridges is proposed. Measured frequencies are selected as the first-layer reference data, and the mass of the bridge deck, the grid density, the modulus of concrete and the ballast on the side span are modified by using a manual tuning technique. Measured global positioning system （GPS） data is selected as the second-layer reference data, and the degradation of the integral structure stiffness EI of the whole bridge is taken into account for the second-layer model updating by using the finite element iteration algorithm. The Nanpu Bridge in Shanghai is taken as a case to verify the applicability of the proposed model updating method. After the first-layer model updating, the standard deviation of modal frequencies is smaller than 7%. After the second-layer model updating, the error of the deflection of the mid-span is smaller than 10%. The integral structure stiffness of the whole bridge decreases about 20%. The research results show a good agreement between the calculated response and the measured response.

Study of Sustained Release Phenylpropanolamine Hydrochloride Hydrophilic Matrix Tablets Containing Hydroxypropylmethylcellulose K100M and Carbopol 971P

选用HPMC K100M和卡波普971P为骨架材料，粉末直接压片法制备骨架片，考察释放度，反相高效液相色谱法检测盐酸苯丙醇胺（PPA·HCl）的浓度。释药曲线均符合Higuchi方程（R＞0．98，P＜0．01）。运用正交设计法，以美国市场的PPA·HCl缓释片Acutrim^R为对照，相似因子f2值为指标，筛选获得了最优处方。其工艺重现性合格。研制片在0．1mol·L^-1 HCl,H2O(pH6.5)，磷酸盐缓冲液（PBS）pH5.0,6.8和7.4的介质中，以及在0.1mol·L^-1HCl中释放2h，转移至PBS6．8中释放10h，相对于对照品的f2值为63－74，表明在各介质中两制剂的释药曲线相似。释药影响因素的考察结果表明：在本实验考察的范围内，骨架片在水中的释药速率与HPMC K100M和卡波普971P的用量呈负相关。HPMC K100M和卡波普971P的比例（保持聚合物总用量相同），硬脂酸镁量和骨架片硬度对释药速率无显著性影响。

Development and Validation of an HPLC Method for the Determination of Bupropion Hydrochloride in Tablets

A rapid, accurate and sensitive HPLC method for the determination of bupropion hydrochloride in a new tablet formulation is described. Chromatographic separation of bupropion hydrochloride is achieved using a mobile phase consisting of methanol -0.01 mol·L -1 ammonium dihydrogen phosphate (80:20, v/v, pH 4.8) at a flow rate of 1.0 mL·min -1 on a Hypersil BDS C18 column. Absorbance is monitored at 251 nm where bupropion hydrochloride has maximum absorption in the mobile phase. The linear range of determination for bupropion hydrochloride is between 2.12 and 21.2 μg·mL -1. The proposed method was validated with respect to accuracy, precision, limits of detection and quantification and robustness, etc.

Computation of the Fatigue Life of Road Wheel with Double-Layer Rubber Flange

In order to increase the fatigue life (FL) of road wheels (RW), a kind of double layer rubber flange (DLRF) is put forward. It consists of two layers of rubber, where metal wires are laid in the inner layer and the outer layer has no inlaid metal wires. Stress, strain and temperature field of DLRF were calculated with ANSYS finite element analysis (FEA) software, FL of DLRF RW was also computed with fracture mechanics fatigue theory. The results of computation indicate that the heat generated in RW's rubber flange (RF) can be reduced by the use of DLRF, and the FL of RW can be increased without affecting the mechanical intensity of RW.

Pharmacokinetics of Moclobemide Sustained Release Tablets after Multiple Oral Dose Administration in Healthy Volunteers

To investigate the pharmacokinetic characteristics of moclobemide sustainedrelease tablets after multiple oral dose administration in healthy Chinese volunteers. MethodsMoclobemide sustained release tablets were given as a multiple oral dose regimen of 300 mg oncedaily for five consecutive days to 12 healthy volunteers. The concentrations of moclobemide inplasma were determined by reversed-phase high performance liquid chromatography. The partialpharmacokinetic parameters were calculated using 3p97 pharmacokinetic program. Results Theconcentration-time profile fitted an one-compartment model best. The steady-state pharmacokineticparameters of moclobemide sustained release tablets after multiple oral doses were as follows:C_(max) was (1 950 +- 156) μg· L^(-1), T_(max) was (6.00 +-1.55) h, T_(1/2(kel)) was (3.14 +-0.12)h, AUC_(ss 0-24) was (22 836 +- 1 842) μg·h· L^(-1), MRT was (7.68+-0.36) h, CL/F_((s)) was(20.2+-2.1) L·h^(-1), and V/F_((c)) was (91.4+-9.4) L, respectively. No marked adverse events werenoted during this study. Conclusion The formulation has a sustained-release effect and goodtolerance in the healthy volunteers, which provides useful information for clinical practice.

Pharmacokinetics of Controlled Release and Immediate Release Morphine Sulphate Tablets after a Single Dose and Multiple Doses in Chinese Volunteers

The pharmacokinetics of morphine sulphate was studied in 10 Chinese healthy volunteers after a single oral dose. Blood samples were collected before and after administration of controlled release tablets (CRMS, 30 mg) and immediate release tablets (IRMS, 20 mg). The plasma concentration of morphine was determined by GC MS. The pharmacokinetic parameters of controlled release tablets and immediate release tablets were calculated∶ C max was 19.38±3.80 and 21.27±6.21 ng/ml, t max was 2.36 ±0.37 h and 0.56±0.16 h, t 1/2β was 3.53±0.87 and 3.03±0.74 h, AUC was 145.15±17.65 and 93.08±16.65 ng/ml, respectively. The steady state plasma concentration of morphine sulphate in cancer patients after multiple doses was achieved, C max of CRMS and IRMS was 27.43±0.33 ng/ml and 22.68±0.16 ng/ml, C min of CRMS and IRMS was 19.45±1.44 ng/ml and 18.14±0.49 ng/ml, respectively.