二甲双胍控释片的理化及药动学研究:硅片优化处方

Rumman Reza, Niaz Morshed, Md Nazmus Samdani, Amina Alam Kotha, F. Rahman, Md. Selim Reza
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摘要

全世界有近1.2亿人服用二甲双胍治疗2型糖尿病,其血浆半衰期相对较短,绝对生物利用度较低。本研究采用ADMETLab、SwissADME、SmartCYP、LigandScout网络服务器和软件对二甲双胍的理化和药代动力学特性进行了全面分析,以评价其制剂作为控释基质片的有效性。本研究的目的是利用计算模拟工具,利用不同浓度的亲水性羟丙基甲基纤维素(HPMC)级K4M和K100M聚合物,开发一种口服控释(CR)二甲双胍片剂。使用membrane plus软件模拟运行2小时,检测药物的肠膜通透性。使用DDDPlus软件对制备的配方进行硅溶出研究,模拟环境使用USP 2型仪器以100 rpm旋转。模拟运行2小时,使用0.1N HCl相,然后使用6.8 USP磷酸盐缓冲相8小时。结果表明,在固定的聚合物浓度水平下,高黏度K100M的药物释放速度比低黏度K4M慢。此外,还使用GastroPlus软件生成了配方的血浆浓度-时间曲线。达卡大学药学院。科学22(1):29- 42,2023 (6)
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Physicochemical and Pharmacokinetic Studies of Metformin for Development of Controlled Release Matrix Tablet: Formulation Optimization Using in silico Tools
Metformin, taken by nearly 120 million people across the world as a treatment for type 2 diabetes, has a relatively short plasma half-life and low absolute bioavailability. In this study, physicochemical and pharmacokinetics properties of metformin have been thoroughly assayed using ADMETLab, SwissADME, SmartCYP, LigandScout web-servers and software to evaluate the effectiveness of its formulation as controlledrelease matrix tablets. The objective of the present work was to develop a formulation of an oral controlled-release (CR) metformin tablet, using hydrophilic hydroxylpropylmethylcellulose (HPMC) grades K4M and K100M polymers at different concentrations utilizing computational simulatory tools. Intestinal membrane permeability of the drug has been assayed using 2 hours simulation run with MembranePlus Software. Simulated environment generated for in silico dissolution study, using DDDPlus software, of the prepared formulations used USP Apparatus Type 2 rotating at 100 rpm. The simulation run was for 2 hours using 0.1N HCl phase followed by 8 hours with 6.8 USP Phosphate buffer phase. The results showed that drug release from the higher viscosity grade, K100M was slower as compared to the lower viscosity grade K4M at a fixed polymer concentration level. Furthermore, plasma concentration-time curves for the formulations have been generated using GastroPlus software. Dhaka Univ. J. Pharm. Sci. 22(1): 29-42, 2023 (June)
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