Topical Application of Clobetasol 17-Propionate From Various Cream Bases by Using Wistar Rat as an Animal Model

Clobetasol 17-propionate 為一強效之類固醇藥物，於皮膚治療上其適應症為乾癬及濕疹等，於本研究中將其加入不同處方之乳膏中並以大白鼠做為實驗動物模式進行體外及活體試驗評估。於體外經皮吸收實驗方面，於投與初期由於藥物必須先於皮膚內達到飽合才會通過皮膚障蔽而進入受藥端（即模擬活體中之循環系統），造成投與後期之穿透速率較初期為高，另外於本研究室製備之藥典或專利處方皆顯示較市售處方為高之穿透能力，極有可能是處方中一些經皮吸收促進劑的影響：然而若比較市售處方及自製處方之間的皮內藥物含量及穿透延滯時間則大致上無顯著性差異，因此可推測經皮吸收促進劑並不能使 C10betasol 17-Pr0Pi0nate 之局部藥理療效增加。於大白鼠耳朵之抗發炎活體試驗方面，所有的處方皆能有效地抑制發炎所造成的水腫現象，此實驗結果可能是由於 Clobetasol 17-propionate 為非常強力之類固醇藥物，因此軟膏基劑的不同並不足以影響其療效，另外於體外試驗可知各處方之藥物皮內含量差異並不明顯因此造成在活體試驗中局部抗發炎效應也相當接近，由此可知於本研究中體外及活體試驗之間有一致性，可使用皮內藥物殘餘量當作乳膏品質之參考評估。

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並列摘要

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.

並列關鍵字

clobetasol 17-propionate ； topical qpplication ； Wistar rat

國際替代計量

Topical Application of Clobetasol 17-Propionate From Various Cream Bases by Using Wistar Rat as an Animal Model

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