非诺洛芬钙凝胶剂的制备及其体外透皮吸收研究

Studies on preparation of fenoprofen calcium gels and its percutaneous absorption in vitro

目的：对非诺洛芬钙凝胶剂制备，以及该剂型对小鼠皮肤的渗透作用进行研究。方法：建立了凝胶剂含量测定的三波长紫外法。结果：高分子辅料的种类、比例及透皮吸收促进剂的用量均对凝胶剂的物理性质有影响。首次发现，凝胶剂中加入２％按叶油为透皮吸收促进剂，其体外累积渗透量和渗透速率均最大。非诺洛芬钙凝胶剂的体外渗药动力学可用Ｈｉｇｕｃｈｉ方程来表述。结论：凝胶基质的最佳配比为５％Ｃａｐ与２０％ＰＶＡ（２∶１）混合。２％桉叶油可明显增加非诺洛芬钙凝胶剂的透皮吸收。

OBJECTIVE :The purpose of this paper is to investigate the preparation of fenoprofen calcium gels. The effect of the dosage form on the permeation through excised mouse skin was developed. METHODSZ:The content of fenoprofen calcium in gel was determined by triple wavelength UV spectrophotometry. RESULTS :The effect of different kinds,proportion of highpolymer excipient and the amount of enhancer through mouse skin on the physical properties of gels was observed.In this study gelmatrix consisting of 2% eucalyptus oil was found to be an optimal enhancer for the penetration of fenoprofen calcium.Its cumulative amount permeated and the pemeation rate were greater than those of the others. The permeation process of fenoprofen calcium gels in vitro could be described by Higuchi's Equation. CONCLUSIONS :The gel base was prepared by mixing 5% Cap with 20% PVA(21) for the formulation. 2% Ecucalyptus oil as the enhancer could significantly increase percutaneous absorption of fenoprofen calcium.