In vitro characterization of polyorthoester microparticles containing bupivacaine

被引：18

作者：

Deng, JS ^{[1
]}

Li, L ^{[1
]}

Tian, YQ ^{[1
]}

Ginsburg, E ^{[1
]}

Widman, M ^{[1
]}

Myers, A ^{[1
]}

机构：

[1] Abbott Labs, Hosp Prod Div, Adv Drug Delivery, Abbott Pk, IL 60064 USA

来源：

PHARMACEUTICAL DEVELOPMENT AND TECHNOLOGY | 2003年 / 8卷 / 01期

关键词：

spray congealing; injectable microparticles; polyorthoester; bupivacaine; particle size; syringeability; injectability; in vitro drug release; initial burst-drug release; long acting;

D O I：

10.1081/PDT-120017521

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Laboratory-scale spray-congealing equipment was utilized to fabricate injectable microparticles consisting of polyorthoester and bupivacame. Operating conditions for the spray-congealing process were optimized to produce microparticles with the desired shape and particle size to yield acceptable syringeability and injectability. Characterizations were performed to determine the chemico-physical properties of polyorthoester before and after microparticle fabrication. Microparticles with different drug loadings and comparable particle sizes were produced, and their in vitro drug-release profiles were determined. The in vitro drug release of microparticles with a high drug loading was markedly faster than those with a low drug loading. This is partially attributed to a more significant initial burst-drug release of the microparticles with a high drug loading. The microparticles have demonstrated the potential to be used for long-acting postsurgery pain management by local injection.

引用

页码：31 / 38

页数：8

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