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以溶解度参数为基础,通过悬浮聚合和溶液聚合设计、表征和评价美洛昔康凝胶的制备。

Design, characterization, and evaluation of meloxicam gel prepared by suspension and solution polymerization using solubility parameter as the basis for development.

机构信息

Department of Pharmaceutics, Rajiv Academy for Pharmacy, National Highway #2, P.O. Chhatikara, Mathura, Uttar Pradesh 281001, India.

出版信息

AAPS PharmSciTech. 2010 Mar;11(1):133-42. doi: 10.1208/s12249-009-9369-0. Epub 2010 Jan 15.

Abstract

Meloxicam gel was designed based on the matching of the solubility parameter (delta) of the drug with that of the polymer and subsequently with skin for improved dermal delivery of meloxicam. The delta of meloxicam (11.48 (cal/cm(3))(0.5)) determined by solubility measurement was matched statistically to the solubility parameter of monomers, n-vinyl-2-pyrrolidone, polyvinyl alcohol (PVA), hydroxyl ethyl methacrylate, ethylene glycol methacrylate (EGMA) determined by intrinsic viscosity measurement. Consequently gels were formulated by polymerization in selected solvent blend of water/ethyl acetate (20:80) in which the drug showed maximum solubility. Thus, F1-F16 formulations designed were evaluated for physicochemical properties, textural analysis, and in vitro drug release. On the basis of optimum characteristics, F2 (PVA, delta = 16.96 (cal/cm(3))(0.5)) and F8 (EGMA, delta = 18.35 (cal/cm(3))(0.5)) formulated by suspension polymerization were selected and subjected to skin irritation and topical anti-inflammatory studies. The formulation F8 demonstrated significant (p < 0.05) of anti-inflammatory activity in comparison to marketed piroxicam gel and was free from irritation.

摘要

美洛昔康凝胶是基于药物的溶解度参数(δ)与聚合物和皮肤的匹配而设计的,以改善美洛昔康的经皮传递。通过溶解度测量确定的美洛昔康的 δ(11.48(cal/cm(3))(0.5))通过统计方法与单体、N-乙烯基-2-吡咯烷酮、聚乙烯醇(PVA)、羟乙基甲基丙烯酸酯、乙二醇甲基丙烯酸酯(EGMA)的溶解度参数相匹配,通过特性粘度测量确定。因此,在药物在所选水/乙酸乙酯(20:80)溶剂混合物中具有最大溶解度的情况下,通过聚合在选定的溶剂混合物中进行凝胶的配方设计。因此,对 F1-F16 制剂进行了理化性质、质地分析和体外药物释放评价。基于最佳特性,选择悬浮聚合制备的 F2(PVA,δ=16.96(cal/cm(3))(0.5))和 F8(EGMA,δ=18.35(cal/cm(3))(0.5))进行皮肤刺激和局部抗炎研究。与市售吡罗昔康凝胶相比,制剂 F8 表现出显著的抗炎活性(p<0.05),且无刺激性。

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