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基于气体形成技术的多单元漂浮药物递送系统的制备及体外评价

Preparation and in vitro evaluation of a multiple-unit floating drug delivery system based on gas formation technique.

作者信息

Sungthongjeen Srisagul, Paeratakul Ornlaksana, Limmatvapirat Sontaya, Puttipipatkhachorn Satit

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Naresuan University, Phitsanulok-Nakhonsawan Road, Phitsanulok 65000, Thailand.

出版信息

Int J Pharm. 2006 Nov 6;324(2):136-43. doi: 10.1016/j.ijpharm.2006.06.002. Epub 2006 Jun 9.

Abstract

A multiple-unit floating drug delivery system based on gas formation technique was developed in order to prolong the gastric residence time and to increase the overall bioavailability of the dosage form. The system consists of the drug-containing core pellets prepared by extrusion-spheronization processes, which are coated with double layers of an inner effervescent layer (sodium bicarbonate) and an outer gas-entrapped polymeric membrane of an aqueous colloidal polymer dispersion (Eudragit) RL 30D, RS 30D, NE 30D). Only the system using Eudragit RL 30D as a gas-entrapped polymeric membrane could float. The time to float decreased as amount of the effervescent agent increased and coating level of gas-entrapped polymeric membrane decreased. The optimum system could float completely within 3min and maintained the buoyancy over a period of 24h. The drug release was sustained and linear with the square root of time. Increasing coating level of gas-entrapped polymeric membrane decreased the drug release. Both the rapid floating and the sustained release properties were achieved in the multiple-unit floating drug delivery system developed in this present study.

摘要

为延长剂型的胃滞留时间并提高其整体生物利用度,开发了一种基于气体形成技术的多单元漂浮药物递送系统。该系统由通过挤出滚圆法制备的含药核心微丸组成,微丸涂覆有双层结构,内层为泡腾层(碳酸氢钠),外层为气体截留型聚合物膜,由水性胶体聚合物分散体(Eudragit RL 30D、RS 30D、NE 30D)制成。只有使用Eudragit RL 30D作为气体截留型聚合物膜的系统能够漂浮。随着泡腾剂用量增加和气体截留型聚合物膜包衣水平降低,漂浮时间缩短。最佳系统可在3分钟内完全漂浮,并在24小时内保持漂浮状态。药物释放呈持续线性,与时间的平方根相关。增加气体截留型聚合物膜的包衣水平会降低药物释放。本研究开发的多单元漂浮药物递送系统实现了快速漂浮和持续释放特性。

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