Fang J Y, Shen K L, Huang Y B, Wu P C, Tsai Y H
School of Pharmacy, Kaohsiung Medical College, Taiwan, Republic of China.
Kaohsiung J Med Sci. 1998 May;14(5):286-93.
The effect of clobetasol 17-propionate (CP), a potent corticosteroid, participating in various cream bases on the permeation through rat skin was tested in vitro. Three commercially available formulations and three cream bases prepared in our laboratory according to Pharmacopoeia or registered patent were evaluated in this present study. The amount of CP in the receptor phase of diffusion cell was negligible in the beginning of administration due to the process of saturation of drug in skin reservoir, then the CP molecules pass through the skin directly because of the saturation of receptors in skin reservoir followed the higher flux of CP in the later period. It was suggested that the incorporation of penetration enhancers was the possible reason mainly controlling the flux of CP creams. Nevertheless, CP residue in skin and the lag time of formulations prepared in our laboratory were not significantly higher than those of commercial ones, which indicated penetration enhancer could not dominate the local pharmacological effectiveness of CP though they played a main part on the skin penetration capacity of formulations. The antiinflammatory activity of CP was assessed in the ear of Wistar rat. According to the result of antiinflammatory activity, all formulations showed significant inhibition on oedema suggesting the role of drug itself may be more important than that of vehicle in controlling the therapy efficacy.
在体外测试了强效皮质类固醇丙酸氯倍他索（CP）参与各种乳膏基质时对大鼠皮肤渗透的影响。本研究评估了三种市售制剂以及我们实验室根据药典或注册专利制备的三种乳膏基质。给药开始时，由于药物在皮肤贮库中的饱和过程，扩散池受体相中CP的量可忽略不计，随后由于皮肤贮库中受体的饱和，CP分子直接穿过皮肤，导致后期CP通量更高。有人认为，加入渗透促进剂可能是主要控制CP乳膏通量的原因。然而，我们实验室制备的制剂在皮肤中的CP残留量和滞后时间并不显著高于市售制剂，这表明渗透促进剂虽然对制剂的皮肤渗透能力起主要作用，但并不能主导CP的局部药理作用。在Wistar大鼠耳部评估了CP的抗炎活性。根据抗炎活性结果，所有制剂均显示出对水肿的显著抑制作用，表明在控制治疗效果方面，药物本身的作用可能比载体更为重要。
