Smith E W, Meyer E, Haigh J M
School of Pharmaceutical Sciences, Rhodes University, Grahamstown, South Africa.
Arzneimittelforschung. 1990 May;40(5):618-21.
The blanching activities of Betnovate cream, lotion, ointment and scalp application (each containing 0.1% betamethasone (as the 17-valerate] were determined using healthy human subjects over a 32 h period in both the occluded and unoccluded modes. Considering that all four formulation types contained the same label concentration of corticosteroid, it may be presumed that the formulations would show similar topical drug availability: this was, however, not found to be the case. The scalp application demonstrated the highest topical availability in both the occluded and unoccluded modes. The lotion formulation showed the greatest increase in topical availability on occlusion and the ointment formulation was the least sensitive to the effects of occlusion. These differences, due solely to the effects of the vehicle, may have important clinical implications.
使用健康人体受试者,在32小时内分别以封包和非封包方式测定了倍他米松乳膏、洗剂、软膏和头皮用制剂(每种均含0.1%倍他米松(以17 - 戊酸酯形式))的变白活性。鉴于所有四种剂型含有相同标示浓度的皮质类固醇,可以推测这些制剂会显示出相似的局部药物可用性:然而,事实并非如此。头皮用制剂在封包和非封包方式下均显示出最高的局部可用性。洗剂剂型在封包时局部可用性增加最大,而软膏剂型对封包效果最不敏感。这些仅由基质效应导致的差异可能具有重要的临床意义。