| 英文摘要 |
Semisolid creams and ointments containing 0.05% w/w clobetasol 17-propionate (CP) as active ingredient are categorized as superpotent topical dermatological corticosteroids. The objective of the study was to evaluate the content and transdermal delivery of CP from eleven commercial dosage forms, including three ointments and eight creams. It was found that the CP content of the ointments ranged from 77.5 to 96.1% of the labeled amount, and that of the creams ranged from 84.0 to 105.6%. In vitro transdermal flux of CP through nude mouse skin ranged from 0.156 to 0.270 μg/cm2/h for ointments, and 0.100 to 0.521 μg/cm2/h for creams. Total amount of CP penetrated in 8 h ranged from 1.03 to 1.75 μg for ointments, and 0.67 to 2.95 μg for creams. Lag time to reach steady-state of delivery ranged from 1.48 to 1.63 h for ointments, and 1.53 to 3.19 h for creams. In comparison with the brand name products, transdermal flux of CP from the generic ointments was 57.7% and 83.5% of Dermovate ointment, and that from the generic creams ranged from 19.2 to 94.8% of Dermovate cream. The results demonstrated that commercial 0.05% CP creams and ointments were highly variable in the transdermal delivery of CP, which may influence their bioavailability and clinical efficacy.
氯貝他索丙酸（Clobetasol 17-propionate, CP）乳軟膏製劑是外用皮質類固醇中效價最強的藥品，本研究之目的在評估市售11種含0.05% clobetasol 17-propionate的外用製劑（包括3種軟膏和8種乳膏）的含量及體外穿皮速率。含量測定結果得3種軟膏的CP含量在標示量的77.5 - 96.1%之間，而8種乳膏的含量則在標示量的84.5-105.6%之間。體外裸鼠皮滲透試驗結果得軟膏的穿皮速率介於0.156與0 .270μg／cm2／h之間，而乳膏則為0.100-0.521μg／cm2／h；8小時總穿透量在軟膏為1.03 - 1.75μg／cm2，乳膏則為0.67 - 2.95μg／cm2；其滯留時間在軟膏為介於1.48和1. 63小時間，乳膏則在1.53 - 3.19小時間。如與商品名製劑比較，兩種學名軟膏的穿皮速率分別為Dermovate軟膏的57.7%和83.5%，而學名乳膏的穿皮速率則為Dermovate乳膏的19.2 - 94.8%。研究結果顯示市售0.05%CP乳軟膏製劑的穿皮速率差距差大，可能嚴重影響這些製劑的生體可用率和臨床療效。 |
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