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以乙基纤维素和尤特奇RS100作为成膜剂制备改性的氟康唑透皮喷雾剂。

Fabrication of modified transport fluconazole transdermal spray containing ethyl cellulose and Eudragit RS100 as film formers.

作者信息

Gohel Mukesh C, Nagori Stavan A

机构信息

Department of Pharmaceutics and Pharmaceutical Technology, L. M. College of Pharmacy, P.O. Box 4011, Navrangpura, Ahmedabad, Gujarat, 380 009, India.

出版信息

AAPS PharmSciTech. 2009;10(2):684-91. doi: 10.1208/s12249-009-9256-8. Epub 2009 May 22.

Abstract

The present investigation was undertaken to fabricate modified transport fluconazole transdermal spray using ethyl cellulose and Eudragit RS100 as film-forming polymers. Eudragit RS100 (X(1)) and ethyl cellulose (X(2)) were selected as independent variables in 3(2) full factorial design, whereas drug transport in first hour (Y (1)) and the time required for 50% drug transport (Y(2)) were selected as dependent variables. Eutectic blend of camphor and menthol was used as permeation enhancer cum solvent for film-forming polymers. The pH, viscosity, volume of solution delivered upon each actuation, spray angle, ex-in vivo physical evaluation and in vitro drug transport of the formulated products were evaluated. The optimized batch B16 containing 5.25% w/w ethyl cellulose and 10.6% w/w Eudragit RS100 was formulated by overlapping the contour plots of Y(1) and Y(2). The pH, viscosity, volume of solution sprayed upon each actuation and spray angle of the batch B16 was 6.3, 52.9 cPs, 0.24 ml and 82.6 degrees respectively. The film of optimized batch was flexible and dermal-adhesive. The responses Y(1) and Y(2) of batch B16 were 7.91 microg/ml and 347 min respectively. The kinetics of drug transport was best explained by the Korsmeyer and Peppas model. The eutectic mixture consisting of equal parts of camphor and menthol showed improved drug permeation through shed snake skin. Short-term stability study demonstrated insignificant changes in performance characteristics.

摘要

本研究旨在使用乙基纤维素和尤特奇RS100作为成膜聚合物制备改性的氟康唑透皮喷雾剂。在3(2)全因子设计中,选择尤特奇RS100(X(1))和乙基纤维素(X(2))作为自变量,而将第1小时的药物转运量(Y(1))和50%药物转运所需时间(Y(2))作为因变量。樟脑和薄荷醇的低共熔混合物用作成膜聚合物的渗透促进剂兼溶剂。对所制备产品的pH值、粘度、每次喷雾喷出溶液的体积、喷雾角度、体外-体内物理评价以及体外药物转运进行了评估。通过叠加Y(1)和Y(2)的等高线图,制备出了优化批次B16,其含有5.25% w/w的乙基纤维素和10.6% w/w的尤特奇RS100。批次B16的pH值、粘度、每次喷雾喷出溶液的体积和喷雾角度分别为6.3、52.9厘泊、0.24毫升和82.6度。优化批次的膜具有柔韧性且对皮肤有粘附性。批次B16的响应Y(1)和Y(2)分别为7.91微克/毫升和347分钟。药物转运动力学最能由Korsmeyer和Peppas模型解释。由等量樟脑和薄荷醇组成的低共熔混合物显示出通过蛇蜕皮肤的药物渗透有所改善。短期稳定性研究表明性能特征无显著变化。

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