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负载于不同分子量聚(D,L-丙交酯-共-乙交酯)的卡马西平的体外性能

In vitro performance of carbamazepine loaded to various molecular weights of poly (D,L-lactide-co-glycolide).

作者信息

Barakat Nahla S, Radwan Mahasen A

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

出版信息

Drug Deliv. 2006 Jan-Feb;13(1):9-18. doi: 10.1080/10717540500308992.

Abstract

The purpose of this study was to develop and assess the in vitro characteristics of carbamazepine-loaded microspheres. A solvent evaporation method was used to incorporate carbamazepine (CBZ) into poly (D,L-lactide-co-glycolide) (PLGA) with different molecular weights. The optimum conditions for CBZ-PLGA microspheres preparation were considered and the in vitro release of CBZ of PLGA microspheres were followed up to 24 hr in USP dissolution medium. The effect of using different ratios of PLGA microspheres, prepared with different molecular weights, for optimizing CBZ release also was investigated. CBZ encapsulation efficiency was 68 to 82% for all prepared formulations. Thermograms of CBZ-PLGA microspheres suggest that CBZ was totally entrapped with the PLGA polymer. The presence of Pluronic F-68 has improved the encapsulation of CBZ, resulted in better and smoother microspheres surfaces and enhanced its release pattern. CBZ release profiles were biphasic patterns; after an initial burst, a constant CBZ release rate was observed up to 24 hr. The release from these PLGA-based spherical matrices was consistent with the diffusion mechanism. CBZ dissolution T(50%) was significantly affected (> 3-fold) by increasing the lactide percent from 33.3 to 66.6% from different microspheres mixtures. The present study provides evidence that the encapsulation of CBZ to PLGA microspheres, either as a single polymer or mixture of two, was a successful attempt to control the release of CBZ.

摘要

本研究的目的是开发并评估载卡马西平微球的体外特性。采用溶剂蒸发法将卡马西平(CBZ)掺入不同分子量的聚(D,L-丙交酯-共-乙交酯)(PLGA)中。考虑了制备CBZ-PLGA微球的最佳条件,并在USP溶出介质中对PLGA微球中CBZ的体外释放进行了长达24小时的跟踪。还研究了使用不同分子量制备的不同比例PLGA微球对优化CBZ释放的影响。所有制备的制剂中CBZ的包封率为68%至82%。CBZ-PLGA微球的热重曲线表明CBZ完全被PLGA聚合物包裹。泊洛沙姆F-68的存在改善了CBZ的包封,使微球表面更好更光滑,并增强了其释放模式。CBZ的释放曲线呈双相模式;在初始突释后,观察到CBZ的释放速率在24小时内保持恒定。这些基于PLGA的球形基质的释放符合扩散机制。通过将不同微球混合物中丙交酯的百分比从33.3%提高到66.6%,CBZ的溶解T(50%)受到显著影响(>3倍)。本研究提供了证据,证明将CBZ包封到PLGA微球中,无论是作为单一聚合物还是两种聚合物的混合物,都是控制CBZ释放的成功尝试。

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