二代COX-II抑制剂溶解度增强三元体系的开发与表征

Santosh Girani, Shidallingapa Zalki, Mahantesh G. Kavatekar, Ajay S. Shahapur, Vitthal K. Vijapure
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引用次数: 3

摘要

依托妥昔布是一种高选择性COX-II抑制剂,用于治疗不同病因的疼痛。依托妥昔布水溶性低(201µg/ml),渗透性高,属于BCS II类药物。用环糊精作为包合物配制这些药物可以提高生物利用度。环糊精用作络合剂时,可提高水溶性较差的亲脂性药物的溶解度。本文以柠檬酸、酒石酸和PVP K-30为三元体系,制备依托昔布环糊精配合物,以提高其溶解度,并通过体外溶出评价其溶解度。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development and characterization of ternary system for solubility enhancement of a second-generation COX-II inhibitor
Etoricoxib is a highly selective COX-II inhibitor, used to treat pains of different etiologies. Etoricoxib has low aqueous solubility (201 µ g/ml) and high permeability and therefore classified as BCS class II drug. By formulating these drugs with cyclodextrins as inclusion complexes have shown to increase the bioavailability. Cyclodextrins when used as complexing agents, enhance the solubility of poor water soluble lipophilic drugs. The objective of the present work is to formulate Etoricoxib cyclodextrin complexes by using ternary systems as Citric acid, Tartaric acid and PVP K-30 in order to enhance solubility and evaluate the enhanced solubility by in-vitro dissolution.
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