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β-环糊精包合作用对卡马西平从羟丙基甲基纤维素骨架片中释放的影响。

Influence of beta-cyclodextrin complexation on carbamazepine release from hydroxypropyl methylcellulose matrix tablets.

作者信息

Koester Letícia S, Xavier Clarissa R, Mayorga Paulo, Bassani Valquiria L

机构信息

Programa de Pós-graduação em Ciências Farmacêuticas, Porto Alegre, RS, Brazil.

出版信息

Eur J Pharm Biopharm. 2003 Jan;55(1):85-91. doi: 10.1016/s0939-6411(02)00127-3.

Abstract

The in vitro release profiles of carbamazepine and beta-cyclodextrin either complexed or simply mixed and subsequently incorporated in hydrophilic matrix tablets containing 15 or 30% hydroxypropyl methylcellulose were evaluated. Solubility studies revealed a linear relationship between the increase in carbamazepine solubility and the increase in beta-cyclodextrin concentration. Drying methods (spray-drying and freeze-drying) were used to obtain carbamazepine/beta-cyclodextrin solid complexes in order to prepare tablets. The results demonstrated that matrix tablets containing carbamazepine/beta-cyclodextrin solid complexes displayed faster carbamazepine and beta-cyclodextrin release compared to that containing simple physical mixture. Gelling and matrix formation was impaired in formulation containing 15% hydroxypropyl methylcellulose and spray-dried complex. The comparison of spray-drying and freeze-drying revealed no significant influence of both drying methods on carbamazepine and beta-cyclodextrin dissolution rate when carbamazepine/beta-cyclodextrin complexes were incorporated in 30% hydroxypropyl methylcellulose matrix tablets. The results point to the possibility of modulating carbamazepine release using a hydroxypropyl methylcellulose matrix associated to the drug complexed with beta-cyclodextrin.

摘要

对卡马西平和β-环糊精(分别为络合或简单混合)随后掺入含15%或30%羟丙基甲基纤维素的亲水性基质片中的体外释放曲线进行了评估。溶解度研究表明,卡马西平溶解度的增加与β-环糊精浓度的增加之间存在线性关系。采用干燥方法(喷雾干燥和冷冻干燥)来制备卡马西平/β-环糊精固体络合物以制备片剂。结果表明,与含有简单物理混合物的片剂相比,含有卡马西平/β-环糊精固体络合物的基质片显示出更快的卡马西平和β-环糊精释放。在含有15%羟丙基甲基纤维素和喷雾干燥络合物的制剂中,胶凝和基质形成受到损害。当将卡马西平/β-环糊精络合物掺入30%羟丙基甲基纤维素基质片中时,喷雾干燥和冷冻干燥的比较表明,两种干燥方法对卡马西平和β-环糊精的溶解速率均无显著影响。结果表明,使用与与β-环糊精络合的药物相关的羟丙基甲基纤维素基质来调节卡马西平释放是可能的。

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