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新型酮洛芬透皮贴剂的研制:杏仁油作为渗透促进剂对酮洛芬经兔皮体外和离体渗透的影响。

Development of a novel ketoprofen transdermal patch: effect of almond oil as penetration enhancers on in-vitro and ex-vivo penetration of ketoprofen through rabbit skin.

作者信息

Hussain Abid, Khan Gul Majid, Shah Shefaat Ullah, Shah Kifayat Ullah, Rahim Nauman, Wahab Abdul, Rehman Asim-Ur

机构信息

Drug Delivery Research Center, Gomal University, Dera Ismail Khan, Pakistan.

出版信息

Pak J Pharm Sci. 2012 Jan;25(1):227-32.

Abstract

The aim of the study was to formulate and evaluate topically applied ketoprofen gels and patches and to see the effect of naturally occurring almond oil as penetration enhancer on the penetration of ketoprofen through artificial membrane/rabbit skin. Prior to ketoprofen gel and patch formulation, the particle size and particle size determination of ketoprofen was analyzed by Particle size analyzer (Horiba LA300). Ketoprofen gels and patches were formulated and almond oil was added in several concentrations i.e. 0.5%, 1%, 1.5%, 2%, 2.5% and 3%. The formulated gels were evaluated by several parameters like pH, spreadibility, consistency, homogeneity, skin irritation and drug content determination. In vitro drug permeation studies from transdermal gels and patches were carried out across artificial membrane and rabbit skin by using Franz Cell Apparatus (PermeGear, USA). Kinetics model was employed to the release patterns of ketoprofen from gel and patches in order to investigate the drug transport mechanism. The cumulative amount of drug penetrated from different formulations was statistically evaluated by using One-way analysis of variance (ANOVA). Stability study was performed for various batches of ketoprofen transdermal gel. Almond oil as penetration enhancer in various concentrations significantly enhances the penetration of drug from transdermal gels and patch across synthetic membrane/rabbit skin but was most significant when used in 3% concentration.

摘要

本研究的目的是制备并评估局部应用的酮洛芬凝胶和贴剂,并观察天然杏仁油作为渗透促进剂对酮洛芬透过人工膜/兔皮的渗透作用。在制备酮洛芬凝胶和贴剂之前,使用粒度分析仪(Horiba LA300)分析酮洛芬的粒度和粒度测定。制备了酮洛芬凝胶和贴剂,并添加了几种浓度的杏仁油,即0.5%、1%、1.5%、2%、2.5%和3%。通过pH值、铺展性、稠度、均匀性、皮肤刺激性和药物含量测定等几个参数对制备的凝胶进行评估。使用Franz细胞装置(美国PermeGear公司)在人工膜和兔皮上进行了透皮凝胶和贴剂的体外药物渗透研究。采用动力学模型研究酮洛芬从凝胶和贴剂中的释放模式,以探讨药物转运机制。使用单向方差分析(ANOVA)对不同制剂中渗透的药物累积量进行统计学评估。对不同批次的酮洛芬透皮凝胶进行了稳定性研究。不同浓度的杏仁油作为渗透促进剂可显著提高药物从透皮凝胶和贴剂透过合成膜/兔皮的渗透率,但在3%浓度下使用时效果最为显著。

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