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采用热熔和模压技术制备的含吲哚美辛-聚乙二醇-羟丙基甲基纤维素的固体分散体骨架片

Solid Dispersion Matrix Tablet Comprising Indomethacin-PEG-HPMC Fabricated with Fusion and Mold Technique.

作者信息

Mesnukul A, Yodkhum K, Phaechamud T

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Silpakorn University, Nakhon Pathom 73000, Thailand.

出版信息

Indian J Pharm Sci. 2009 Jul;71(4):413-20. doi: 10.4103/0250-474X.57290.

Abstract

The purpose of this study is to fabricate the polyethylene glycol matrix tablet by mold technique. Indomethacin and hydroxypropylmethylcellulose were used as model drug and polymer, respectively, in PEG matrix system. The physical and drug release characteristics of developed matrix tablet were studied. This inert carrier system comprising 7:3 polyethylene glycol 4000: polyethylene glycol 400 could effectively enhance the solubility of indomethacin and an addition of hydroxypropylmethylcellulose could sustain the drug release. Scanning electron microscope photomicrograph indicated the drug diffusion outward through the porous network of this developed matrix tablet into the dissolution fluid. Least square fitting the experimental dissolution data to the mathematical expressions (power law, first-order, Higuchi's and zero-order) indicated the drug release kinetics primarily as Fickian diffusion. Both the enhancement of drug dissolution and the prolongation of the drug release could be achieved for aqueous insoluble drug such as, indomethacin, by using polyethylene glycol-hydroxypropylmethylcellulose matrix system prepared with melting and mold technique.

摘要

本研究的目的是通过模压技术制备聚乙二醇基质片剂。在聚乙二醇基质体系中,分别使用吲哚美辛和羟丙基甲基纤维素作为模型药物和聚合物。对所制备的基质片剂的物理性质和药物释放特性进行了研究。这种由7:3的聚乙二醇4000:聚乙二醇400组成的惰性载体系统能够有效提高吲哚美辛的溶解度,添加羟丙基甲基纤维素可以维持药物释放。扫描电子显微镜照片显示药物通过所制备的基质片剂的多孔网络向外扩散到溶出液中。将实验溶出数据用数学表达式(幂律、一级、Higuchi方程和零级)进行最小二乘拟合,结果表明药物释放动力学主要为菲克扩散。通过采用熔融和模压技术制备的聚乙二醇-羟丙基甲基纤维素基质体系,对于吲哚美辛这种水不溶性药物,既能提高药物溶出度,又能延长药物释放时间。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b20e/2865813/ca84f52595e6/IJPhS-71-413-g001.jpg

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