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采用模具技术制备的聚乙二醇片剂中吲哚美辛释放特性的研究

Characterization of indomethacin release from polyethylene glycol tablet fabricated with mold technique.

作者信息

Mesnukul A, Yodkhum K, Mahadlek J, 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. 2010 Jan;72(1):92-100. doi: 10.4103/0250-474X.62255.

Abstract

The purpose of this study was to use polyethylene glycol as a carrier to improve the solubility of an aqueous insoluble drug by melting and molding method. The release of dissolved drug was designed to be subsequently sustained with an addition of xanthan gum. The release of indomethacin from the developed system into phosphate buffer pH 6.2 was conducted using the dissolution apparatus. This carrier system could effectively enhance the solubility of indomethacin and an addition of xanthan gum could sustain the drug release. Eudragit L100 film coating could protect the carrier not to be disturbed with HCl buffer pH 1.2 and could dissolve in phosphate buffer pH 6.2, therefore, the drug release from coated tablet was initially very low but subsequently gradually released and prolonged in phosphate buffer pH 6.2. Differential scanning calorimetry study indicated the amorphous state of drug in polyethylene glycol carrier. Scanning electron microscopy photomicrograph indicated the drug diffusion outward through the porous network of matrix tablets into the dissolution fluid and curve fitting signified that the drug release kinetic was Fickian diffusion.

摘要

本研究的目的是使用聚乙二醇作为载体,通过熔融成型法提高水不溶性药物的溶解度。通过添加黄原胶来设计溶解药物的释放,使其具有缓释性。使用溶出装置将吲哚美辛从所开发的体系释放到pH 6.2的磷酸盐缓冲液中。该载体系统可有效提高吲哚美辛的溶解度,添加黄原胶可使药物释放具有缓释性。Eudragit L100薄膜包衣可保护载体不受pH 1.2的HCl缓冲液干扰,并可在pH 6.2的磷酸盐缓冲液中溶解,因此,包衣片在pH 6.2的磷酸盐缓冲液中的药物释放最初非常低,但随后逐渐释放并延长。差示扫描量热法研究表明药物在聚乙二醇载体中呈无定形状态。扫描电子显微镜照片表明药物通过基质片的多孔网络向外扩散到溶出液中,曲线拟合表明药物释放动力学为菲克扩散。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e416/2883233/a56118055b70/IJPhS-72-92-g001.jpg

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