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成膜聚合物颗粒辅料作为控释剂型的基质材料。

Film-forming polymer-granulated excipients as the matrix materials for controlled release dosage forms.

作者信息

Tsai T, San Y P, Ho H O, Wu J S, Sheu M T

机构信息

Graduate Institute of Pharmaceutical Sciences, Taipei Medical College, Taiwan, ROC.

出版信息

J Control Release. 1998 Feb 12;51(2-3):289-99. doi: 10.1016/s0168-3659(97)00183-1.

Abstract

Lactose and dibasic calcium phosphate (DCP) were granulated with various concentrations of film-forming polymers by a stepwise spraying method to prepare a directly compressible matrix excipient. The film-forming polymeric latex of Eudragit RS-30D, Eudragit RL-30D, and Surelease (ethylcellulose) were used in this study as the source of the granulating materials. Better flowability and compressibility were observed for all the granulated particles than the polymer-free granules. Most tablets prepared from the polymer-granulated particles exhibited satisfactory friability of less than 1% except for those prepared from lactose particles granulated with low concentrations of ethylcellulose and from plain lactose granules. Change in tensile strength and tablet thickness were in good agreement with the plasticity of the granulating polymer. Polymer-granulated lactose and DCP provided for controlled release of captopril from matrix tablets. This investigation suggests that conventional excipients can be modified by a simple granulating procedure to provide better physical properties for being used as a matrix material.

摘要

通过逐步喷雾法,将乳糖和磷酸氢钙(DCP)与不同浓度的成膜聚合物制粒,以制备可直接压片的基质辅料。本研究使用了尤特奇RS - 30D、尤特奇RL - 30D和Surelease(乙基纤维素)的成膜聚合物乳胶作为制粒材料的来源。与无聚合物颗粒相比,所有制粒颗粒均表现出更好的流动性和可压性。除了由低浓度乙基纤维素制粒的乳糖颗粒和平乳糖颗粒制备的片剂外,大多数由聚合物制粒颗粒制备的片剂表现出令人满意的脆碎度,小于1%。抗张强度和片剂厚度的变化与制粒聚合物的可塑性高度一致。聚合物制粒的乳糖和DCP可实现卡托普利从基质片剂中的控释。本研究表明,传统辅料可通过简单的制粒程序进行改性,以提供更好的物理性质用作基质材料。

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