替诺昔康凝胶剂的制备及其经皮吸收研究

 目的 制备了替诺昔康(TxM)凝胶剂,研究其经皮吸收过程。方法 测定药物溶解度和油水分配系数,采用双室渗透扩 散装置,进行小鼠离体皮肤体外渗透实验。结果月桂氮　酮对替诺昔康的渗透有明显促透作用,其渗透系数和增渗倍数比 其他促透剂大,分别为(28．12±4．39)×10^-6cm·s^-1和(58．71±9．17),基质中凝胶骨架种类和比例是影响药物经皮吸收的重要 因素。结论凝胶剂的最佳处方含2％TXM,5％月桂氮　酮和卡波普-HPME为3:1。

Preparation and evalution of tenoxicam gels for transdermal absorption

OBJECTIVE To prepare the tenoxicam gels using hydrophilic gel system and to investigate the transdermal absorption preparation containing tenoxicam.METHODS The solubility and oil/water distribution coefficient of drugs were determined by UV method. In vitro drug diffusion from gel matrix and the permeation tests in mouse skin were carried out by a two-compartment diffusion cells.RESULTS The permeation rale of tenoxicam was effectively enhanced by azone. Azone showed the highest permeation coefficient and the enhancement ratios. The permeation coefficient and enhancement ratios of azone were(28.12±4.39)×10^-6 cm·s^-1 and(58.71±9.17) .The important factors effecting the permeation of tenoxicam through mouse skin included gels matrix and the proportion of excipients. CONCLUSION The optimum formulation of the gels consists of 2% tenoxicam,5% azone and Carborpol-HPMC(3:1) mixture.