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用于酮洛芬控释的喷雾干燥PLGA微球的压缩可生物降解基质。

Compressed biodegradable matrices of spray-dried PLGA microspheres for the modified release of ketoprofen.

作者信息

Gavini E, Sanna V, Juliano C, Giunchedi P

机构信息

Dipartimento di Scienze del Farmaco, University of Sassari, Sassari, Italy.

出版信息

J Microencapsul. 2003 Mar-Apr;20(2):193-201.

Abstract

A spray-drying technique was used to prepare poly(lactide-co-glycolide) (PLGA) drug loaded microspheres. Ketoprofen was chosen as a model NSAID drug. The microspheres were characterized in terms of morphology, drug content and release behaviour. The spray-dried particles were subject to a direct compression process for the preparation of biodegradable matrix tablets. The spray-dried powders were found to have good compaction properties. Tablets were also prepared from a mixture of microspheres and microcrystalline cellulose, mannitol and hydroxypropylmethylcellulose or sodium alginate. The release of ketoprofen in phosphate buffer (pH 7.4) was significantly sustained, indicating the suitability of using tabletted spray-dried PLGA microspheres for controlled drug delivery. The results show that spray-dried PLGA particles have promising properties as direct compression and release controlling excipients in matrix tablets for oral administration.

摘要

采用喷雾干燥技术制备了载药聚乳酸-羟基乙酸共聚物(PLGA)微球。选择酮洛芬作为非甾体抗炎药的模型药物。对微球的形态、药物含量和释放行为进行了表征。将喷雾干燥颗粒进行直接压片工艺,以制备可生物降解的基质片剂。发现喷雾干燥粉末具有良好的压缩性能。片剂也由微球与微晶纤维素、甘露醇、羟丙基甲基纤维素或海藻酸钠的混合物制备而成。酮洛芬在磷酸盐缓冲液(pH 7.4)中的释放显著持续,表明压片后的喷雾干燥PLGA微球适用于控释给药。结果表明,喷雾干燥的PLGA颗粒作为口服基质片剂中直接压片和控释辅料具有良好的性能。

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