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50%对映体过量的左旋布比卡因（S75-R25）微球的制备、表征及体外评价

Preparation, characterization and in vitro evaluation of 50% enantiomeric excess bupivacaine (S75-R25)-loaded microspheres.

作者信息

Tanaka Pedro Paulo, Estèbe Jean Pierre, Campos Richard, Chevanne François, Le Corre Pascal, Tenório Sérgio Bernardo, Torres Maria Fernanda

机构信息

CET/SBA do Hospital de Clínicas da Universidade Federal do Paraná, Curitiba, PR.

出版信息

Rev Bras Anestesiol. 2008 Jan-Feb;58(1):15-22. doi: 10.1590/s0034-70942008000100003.

DOI:10.1590/s0034-70942008000100003
PMID:19378540
Abstract

BACKGROUND AND OBJECTIVES

Microspheres can be used as a controlled delivery system to prolong the duration of action of local anesthetics. The objective of this study was the preparation, characterization and analysis of the in vitro release of 50% enantiomeric excess bupivacaine (S75-R25)-loaded microspheres.

METHODS

Microspheres were prepared using the copolymer of polylactide-co-glycolic acid by the spray-dryed method.

RESULTS

Characterization of microspheres regarding their size and content were similar to the theoretical values. The in vitro release demonstrated a biphasic pattern.

CONCLUSIONS

Manufacturing of 50% enantiomeric excess bupivacaine-loaded microspheres by the spray-dryed method with results similar to bupivacaine-loaded microspheres can be done.

摘要

背景与目的

微球可作为一种控释系统，用于延长局部麻醉药的作用时间。本研究的目的是制备、表征和分析负载50%对映体过量布比卡因（S75-R25）的微球的体外释放情况。

方法

采用聚乳酸-乙醇酸共聚物通过喷雾干燥法制备微球。

结果

微球的大小和含量表征与理论值相似。体外释放呈现双相模式。

结论

采用喷雾干燥法可制备负载50%对映体过量布比卡因的微球，其结果与负载布比卡因的微球相似。

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