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载有氢溴酸加兰他敏的聚（丙交酯-乙交酯）（PLGA）微球的制备及释放曲线

Preparation and Release Profiles of Galantamine Pamoate Loaded Poly (Lactideco-Glycolide) (PLGA) Microspheres.

作者信息

Du Liping, Liu Shankui, Hao Guizhou, Zhang Li, Zhou Miaomiao, Bao Yueqing, Ding Bing, Sun Qinyong, Zhang Guimin

机构信息

Shandong Engineering Research Center of Complex Injectables, Shangdong New Time Pharmaceutical Co., Ltd., Linyi, China.

School of Biological Science and Technology, University of Jinan, Jinan, China.

出版信息

Front Pharmacol. 2021 Mar 8;11:619327. doi: 10.3389/fphar.2020.619327. eCollection 2020.

DOI:10.3389/fphar.2020.619327
PMID:33762929
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7982595/
Abstract

Patient's poor compliance and the high risk of toxic effects limit the clinical use of galantamine hydrobromide. To overcome these drawbacks, the sustained-release galantamine pamoate microspheres (GLT-PM-MS) were successfully developed using an oil/water emulsion solvent evaporation method in this study. Physicochemical properties of GLT-PM-MS were carefully characterized, and the and drug release behaviors were well studied. Results showed that the morphology of optimized microspheres were spherical with smooth surfaces and core-shell interior structure. Mean particle size, drug loading and entrapment efficiency were 75.23 ± 1.79 μm, 28.01 ± 0.81% and 87.12 ± 2.71%, respectively. The developed GLT-PM-MS were found to have a sustained release for about 24 days and the plasma drug concentration remained stable for 17 days in rats. These results indicated that GLT-PM-MS could achieve the sustained drug release purpose and be used in clinical trial.

摘要

患者依从性差以及毒副作用风险高限制了氢溴酸加兰他敏的临床应用。为克服这些缺点，本研究采用油/水乳液溶剂蒸发法成功研制了延胡索酸加兰他敏缓释微球（GLT-PM-MS）。对GLT-PM-MS的理化性质进行了仔细表征，并对其药物释放行为进行了深入研究。结果表明，优化后的微球形态为表面光滑的球形，内部为核壳结构。平均粒径、载药量和包封率分别为75.23±1.79μm、28.01±0.81%和87.12±2.71%。所研制的GLT-PM-MS在大鼠体内可持续释放约24天，血浆药物浓度在17天内保持稳定。这些结果表明，GLT-PM-MS可实现药物缓释目的，可用于临床试验。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/1699b04a73d0/fphar-11-619327-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/5affebae0ccd/fphar-11-619327-g001.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/6ba86d4c7e70/fphar-11-619327-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/47ec63ac6d35/fphar-11-619327-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/90b4cc028cb5/fphar-11-619327-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/beca336253f5/fphar-11-619327-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/1699b04a73d0/fphar-11-619327-g008.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/5affebae0ccd/fphar-11-619327-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/e9e4ad427f74/fphar-11-619327-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/eaca5d5f3352/fphar-11-619327-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/6ba86d4c7e70/fphar-11-619327-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/47ec63ac6d35/fphar-11-619327-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/90b4cc028cb5/fphar-11-619327-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/beca336253f5/fphar-11-619327-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/304c/7982595/1699b04a73d0/fphar-11-619327-g008.jpg

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