pH响应型β- cd -聚乙基丙烯酸-交联聚合物微颗粒增强瑞舒伐他汀钙溶解度体系的研制及体外、体内评价

Q2 Materials Science

Polymer-Plastics Technology and Engineering Pub Date : 2018-08-13 DOI:10.1080/03602559.2017.1373401

R. M. Sarfraz, M. Ahmad, Asif Mahmood, H. Ijaz

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引用次数: 11

摘要

目前开展了提高瑞舒伐他汀钙溶解度的研究工作。制备了一种高度稳定、生物相容性好、无毒的β-环糊精-g-聚甲基丙烯酸接枝聚合物网络。各制剂的包封效率(%)在82.30±0.25 ~ 89.00±0.25之间，凝胶分数在90.34±1.012 ~ 95.25±1.331之间。HM2在pH 6.8时溶胀释药率为85.74%。最合适的模型是一级动力学，释放机制为异常扩散。同样，在pH为6.8时，溶解度也提高了9.59倍。结果表明，水凝胶微颗粒是提高疏水药物溶解度和生物利用度的有效工具。图形抽象

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Development, In Vitro and In Vivo Evaluation of pH Responsive β-CD-Comethacrylic Acid-Crosslinked Polymeric Microparticulate System for Solubility Enhancement of Rosuvastatin Calcium

ABSTRACT Current research work was conducted for enhancing solubility of rosuvastatin calcium. A highly stable, biocompatible, and nontoxic β-cyclodextrin-g-poly(methacrylic acid) graft polymeric network was developed. Formulations proved entrapment efficacy (%) in between 82.30 ± 0.25 and 89.00 ± 0.25 and gel fraction between 90.34 ± 1.012 and 95.25 ± 1.331. Formulation HM2 had shown optimum swelling and drug release, i.e., 85.74% at pH 6.8. The best-fit model was first-order kinetics with anomalous diffusion as release mechanism. Likewise, solubility enhancement, i.e., 9.59-folds was determined at pH 6.8. It was concluded that hydrogel microparticles are the promising tools for improving solubility and bioavailability of hydrophobic drugs. GRAPHICAL ABSTRACT

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来源期刊

Polymer-Plastics Technology and Engineering 工程技术-高分子科学

CiteScore

1.71

自引率

0.00%

发文量

审稿时长

4 months