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卡波姆934基质的药物释放

Drug release from Carbomer 934 matrices.

作者信息

Russo L I, Ghaly E S

机构信息

University of Puerto Rico, School of Pharmacy, San Juan 00936-5067.

出版信息

P R Health Sci J. 2000 Jun;19(2):131-7.

Abstract

The main objective of this investigation was to describe the mechanism of drug release from Carbomer 934 hydrogel matrices and to evaluate the effect of polymer level, diluent type, and matrix restriction using customized device (that permits only one surface of the tablet to be exposed to the dissolution medium) on theophylline release from Carbomer matrices. Formulations containing theophylline (10%), Carbomer (10%, 30, 50%), direct compressible diluent (lactose fast flo, Avicel PH-101, Emcompress) and magnesium stearate (0.75%) were compressed at a target tablet weight of 450 mg and target hardness of 7-9 Kp. USP Apparatus 1, was used to test the drug release and Korsmeyer equation was used to describe the mechanism of drug release from Carbomer matrices. Results show that the release profile and release mechanism from Carbomer matrices were influenced by Carbomer level, diluent type, and matrix restriction. In general the release mechanism was anomalous (non-Fickian) except for 10% and 30% Carbomer level and in Avicel PH-101 matrices, where, the release mechanism appears to follow super case II where, the n exponent has value greater than 0.89. All formulations selected appear to follow zero order release only up to 120 minutes. Restriction of tablet surface resulted in a shift toward Fickian release. This study demonstrated that it is possible to modify the drug release mechanism and rate, by changing polymer level, diluent type, and imposing physical restriction on the surface of the matrix.

摘要

本研究的主要目的是描述卡波姆934水凝胶基质的药物释放机制,并使用定制装置(该装置仅允许片剂的一个表面暴露于溶出介质)评估聚合物水平、稀释剂类型和基质限制对茶碱从卡波姆基质中释放的影响。含有茶碱(10%)、卡波姆(10%、30%、50%)、直接压片稀释剂(乳糖速流、微晶纤维素PH - 101、预胶化淀粉)和硬脂酸镁(0.75%)的制剂在目标片重450 mg和目标硬度7 - 9 Kp下进行压制。使用美国药典装置1测试药物释放,并使用科尔兹迈耶方程描述茶碱从卡波姆基质中的释放机制。结果表明,卡波姆基质的释放曲线和释放机制受卡波姆水平、稀释剂类型和基质限制的影响。一般来说,除了卡波姆水平为10%和30%以及在微晶纤维素PH - 101基质中释放机制似乎遵循超级情况II(n指数大于0.89)外,释放机制为非菲克扩散。所有选定的制剂在120分钟内似乎都遵循零级释放。片剂表面的限制导致向菲克扩散释放的转变。本研究表明,通过改变聚合物水平、稀释剂类型以及对基质表面施加物理限制,可以改变药物释放机制和速率。

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