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制剂和加工因素对齐多夫定可生物降解微胶囊特性的影响。

Effect of formulation and processing factors on the characteristics of biodegradable microcapsules of zidovudine.

作者信息

Mandal T K, Shekleton M, Onyebueke E, Washington L, Penson T

机构信息

College of Pharmacy, Xavier University of Louisiana, New Orleans 70125, USA.

出版信息

J Microencapsul. 1996 Sep-Oct;13(5):545-57. doi: 10.3109/02652049609026040.

Abstract

Biodegradable microcapsules of zidovudine (AZT) were prepared using poly-(lactide/glycolide) by the solvent evaporation technique. The objective of this project was to focus on the effect of several formulation and processing factors on the efficiency of encapsulation, surface morphology, and drug release profiles. When the drug was incorporated as powder or as aqueous suspension containing a high amount of insoluble particles, to the organic phase the surface of the microcapsules was appeared to be wrinkled. The efficiency of encapsulation decreased when AZT powder was dispersed directly into the organic solvent instead of adding as an aqueous solution. When the relative volume of the aqueous phase containing 1% PVA was changed from 25 up to 125% of the volume of the organic phase, the efficiency of encapsulation, surface morphology, and release profiles did not change significantly. The efficiency of encapsulation decreased from 9 to 3.8% when the drug loading was increased from 10 to 50% of the weight of the polymer.

摘要

采用溶剂蒸发技术,以聚(丙交酯/乙交酯)制备了齐多夫定(AZT)的可生物降解微胶囊。本项目的目的是关注几种制剂和加工因素对包封效率、表面形态和药物释放曲线的影响。当药物以粉末形式或含有大量不溶性颗粒的水悬浮液形式加入有机相时,微胶囊表面似乎出现皱纹。当将AZT粉末直接分散到有机溶剂中而不是作为水溶液加入时,包封效率降低。当含有1%聚乙烯醇(PVA)的水相相对体积从有机相体积的25%增加到125%时,包封效率、表面形态和释放曲线没有显著变化。当药物负载量从聚合物重量的10%增加到50%时,包封效率从9%降至3.8%。

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