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盐酸二甲双胍 - 硬脂酰聚羟甘油酯固体分散体的制备与表征

Preparation and Characterization of Metformin Hydrochloride - Compritol 888 ATO Solid Dispersion.

作者信息

Jagdale Sc, Patil Sa, Kuchekar Bs, Chabukswar Ar

机构信息

Department of Pharmaceutics, MAEER's Maharashtra Institute of Pharmacy, Pune, Maharashtra, India.

出版信息

J Young Pharm. 2011 Jul;3(3):197-204. doi: 10.4103/0975-1483.83758.

DOI:10.4103/0975-1483.83758
PMID:21897658
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3159272/
Abstract

Metformin hydrochloride (MET) sustained-release solid dispersions (SD) were prepared by the solvent evaporation and closed melt method, using compritol 888 ATO as the polymer with five different drug-carrier ratios. Characterization of solid dispersion was carried out by Fourier Transform Infrared (FTIR) spectroscopy, ultraviolet (UV) spectroscopy, Differential scanning calorimetry (DSC), X-ray powder diffraction (XRPD). The FTIR and UV studies suggested that no bond formation had occurred between the polymer and the drug. DSC and XPRD results ruled out any interaction or complex formation between the drug and the polymer. The formulated SD had acceptable physicochemical characters and SD with a 1 : 4 drug : Polymer ratio, which released the drug over an extended period of eight-to-ten hours. The data obtained from the in vitro release studies were fitted with various kinetic models and were found to follow the Korsmeyer-Peppas equation. The prepared SD showed good stability over the studied time period. The solvent evaporation method was found to be more helpful than the closed melt method, giving the sustained release action. The SD with a 1 : 4 ratio of drug to polymer, by the solvent evaporation method, was selected as the most effective candidate for the subsequent development of a well-timed, sustained-release dosage form of the drug.

摘要

采用溶剂蒸发法和封闭熔融法，以Compritol 888 ATO为聚合物，制备了五种不同药物-载体比例的盐酸二甲双胍（MET）缓释固体分散体（SD）。通过傅里叶变换红外（FTIR）光谱、紫外（UV）光谱、差示扫描量热法（DSC）、X射线粉末衍射（XRPD）对固体分散体进行表征。FTIR和UV研究表明，聚合物与药物之间未形成化学键。DSC和XPRD结果排除了药物与聚合物之间的任何相互作用或复合物形成。所制备的SD具有可接受的物理化学性质，药物与聚合物比例为1:4的SD在8至10小时的延长时间内释放药物。体外释放研究获得的数据与各种动力学模型拟合，发现符合Korsmeyer-Peppas方程。所制备的SD在研究时间段内表现出良好的稳定性。发现溶剂蒸发法比封闭熔融法更有助于实现缓释作用。通过溶剂蒸发法制备的药物与聚合物比例为1:4的SD被选为后续开发该药物定时、缓释剂型的最有效候选物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e8/3159272/dd9eb10c7171/JYPharm-3-197-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e8/3159272/0655240ef7d4/JYPharm-3-197-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e8/3159272/e6d4c36158ec/JYPharm-3-197-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e8/3159272/f6bbc28939c6/JYPharm-3-197-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e8/3159272/b24b018e221b/JYPharm-3-197-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e8/3159272/dd9eb10c7171/JYPharm-3-197-g010.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e8/3159272/0655240ef7d4/JYPharm-3-197-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e8/3159272/e6d4c36158ec/JYPharm-3-197-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e8/3159272/f6bbc28939c6/JYPharm-3-197-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e8/3159272/b24b018e221b/JYPharm-3-197-g009.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b6e8/3159272/dd9eb10c7171/JYPharm-3-197-g010.jpg

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