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一种用于硝苯地平控释的挤压型渗透片。

A squeeze-type osmotic tablet for controlled delivery of nifedipine.

作者信息

Park Jung Soo, Shin Jun Hyun, Lee Dong Hun, Kim Moon Suk, Rhee John M, Lee Hai Bang, Khang Gilson

机构信息

BK-21 Polymer BIN Fusion Research Team, Chonbuk National University, 664-14 Dukjin, Jeonju 561-756, South Korea.

出版信息

J Biomater Sci Polym Ed. 2008;19(1):31-45. doi: 10.1163/156856208783227622.

Abstract

Osmotic delivery systems are based on osmotic driving force. Nifedipine tablets, available under the trade names Procardia XL (Pfizer) and Adalat (Bayer), are commercialized drug-delivery systems of an elemental osmotic pump that the push-pull osmotic tablet operates successfully in delivering water-insoluble drugs. For the improvement of the release pattern and the solubility of the drug, we developed a squeeze-type osmotic tablet (SQT) for nifedipine as a model drug. The SQT was composed of one or more ring type of squeeze-push layer (squeeze-disc) and a centered drug core. Squeeze-discs were stacked up with different physicochemical properties with gradient such as viscosity, swelling ratio and water absorption ratio using the osmotic agents from a disc of bottom to top. The present work investigated the effect of different preparation factors, such as hydrophilic polymers, the molecular weight of polymers, coating process, orifice size and types of excipient on release performance of nifedipine. With the purpose of delivering water-insoluble nifedipine at an approximate zero-order rate and step-function rate for 24 h, SQT has been successfully prepared, and significantly improved in the release rate and patterns in comparison with the Adalat push-pull system in vitro release features.

摘要

渗透给药系统基于渗透驱动力。硝苯地平片,商品名为络活喜(辉瑞公司)和拜新同(拜耳公司),是一种基本渗透泵型的商业化给药系统,推拉渗透片在递送水不溶性药物方面成功运行。为了改善药物的释放模式和溶解度,我们开发了一种以硝苯地平为模型药物的挤压型渗透片(SQT)。SQT由一个或多个环形挤压 - 推层(挤压盘)和一个居中的药物核心组成。使用渗透剂从底部圆盘到顶部,将具有不同物理化学性质(如粘度、溶胀率和吸水率)的挤压盘以梯度方式堆叠起来。本研究考察了不同制备因素,如亲水性聚合物、聚合物分子量、包衣工艺、孔径和辅料类型对硝苯地平释放性能的影响。为了以近似零级速率和阶跃函数速率递送水不溶性硝苯地平24小时,已成功制备了SQT,并且与拜新同推拉系统的体外释放特征相比,其释放速率和模式有显著改善。

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