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含卡托普利的基质型透皮治疗系统:制剂优化、体外和离体表征

Matrix type transdermal therapeutic system containing captopril: formulation optimization, in vitro and ex vivo characterization.

作者信息

Kerimoğlu Oya, Keskin Ebru, Dortunç Betül, Anah Sela

机构信息

Faculty of Pharmacy, Department of Pharmaceutical Technology, Marmara University, 34668 Haydarpaşa, Istanbul, Turkey.

出版信息

Acta Pol Pharm. 2013 Mar-Apr;70(2):291-300.

PMID:23614285
Abstract

Transdermal therapeutic systems (TTS) containing captopril were developed by using synthetic and pH independent polymers, Eudragit RL 100 and RS 100. The formulations were characterized in terms of their appearance, thickness, captopril content, in vitro release rate and diffusion profiles. In vitro release studies demonstrated controlled release for each formulation developed. In viro and ex vivo diffusion rate studies were performed through various synthetic membranes with different thickness, pore size and type (hydrophilic and hydrophobic) and through human skin by using Franz diffusion cells. Type of membrane and composition of the formulation affected the diffusion profiles of captopril from the transdermal therapeutic systems. Transdermal therapeutic systems containing captopril were successfully prepared and especially two of the formulations (F15 and F16) are considered to be suitable to administer captopril via skin.

摘要

采用合成且与pH无关的聚合物Eudragit RL 100和RS 100开发了含卡托普利的透皮治疗系统(TTS)。对这些制剂的外观、厚度、卡托普利含量、体外释放速率和扩散曲线进行了表征。体外释放研究表明所开发的每种制剂均具有控释特性。通过各种具有不同厚度、孔径和类型(亲水性和疏水性)的合成膜以及使用Franz扩散池通过人体皮肤进行了体外和离体扩散速率研究。膜的类型和制剂的组成影响了卡托普利从透皮治疗系统的扩散曲线。成功制备了含卡托普利的透皮治疗系统,尤其是其中两种制剂(F15和F16)被认为适合通过皮肤给药卡托普利。

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