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基于拉曼成像技术评估 HPMC 取代物含量及其对市售缓控释片剂释药性能的影响。

A Raman imaging-based technique to assess HPMC substituent contents and their effects on the drug release of commercial extended-release tablets.

机构信息

State Key Laboratory of Natural Medicines, Center for Research Development and Evaluation of Pharmaceutical Excipients and Generic Drugs, and Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, 24 Tong Jia Xiang, Nanjing 210009, China; NMPA Key Laboratory for Quality Research and Evaluation of Chemical Drugs, Institute for Chemical Drug Control, National Institutes for Food and Drug Control, 31 Huatuo Road, Beijing 102629, China.

NMPA Key Laboratory for Quality Research and Evaluation of Chemical Drugs, Institute for Chemical Drug Control, National Institutes for Food and Drug Control, 31 Huatuo Road, Beijing 102629, China.

出版信息

Carbohydr Polym. 2020 Sep 15;244:116460. doi: 10.1016/j.carbpol.2020.116460. Epub 2020 May 28.

Abstract

In this study, we tried to assess the substitute contents of HPMC used in commercial extended-release tablets directly by an innovative Raman imaging-based analysis technique and find their effects on the in vitro performance of these pharmaceuticals. Twenty-seven batches of metformin hydrochloride extended-release tablets from various sources were collected in the Chinese mainland market. While Raman imaging was used to qualitatively analyze the composition of the tablets, the MeO and HPO contents of HPMC were quantitatively assessed by a newly proposed calculation method based on the Raman intensity of corresponding characteristic band. Additionally, the dissolution test was performed to evaluate the relationship between HPMC substitution pattern and in vitro behavior. In sum, our findings indicate that the drug release rate can be downregulated by increasing the MeO content of HPMC, while the high HPO content would largely eliminate the variation of drug release profiles among batches.

摘要

在这项研究中,我们试图通过一种创新的基于拉曼成像的分析技术直接评估商业缓释片中 HPMC 的替代物含量,并研究它们对这些药物体外性能的影响。我们收集了中国大陆市场上来自不同来源的 27 批盐酸二甲双胍缓释片。在使用拉曼成像对片剂的组成进行定性分析的同时,我们还通过一种基于相应特征带的拉曼强度的新提出的计算方法对 HPMC 的 MeO 和 HPO 含量进行了定量评估。此外,我们还进行了溶出度试验以评估 HPMC 替代模式与体外行为之间的关系。总之,我们的研究结果表明,通过增加 HPMC 的 MeO 含量可以降低药物释放速率,而高 HPO 含量则会大大消除不同批次间药物释放曲线的差异。

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