Malzfeldt E, Lehmann P, Goerz G, Lippold B C
Department of Dermatology, University of Düsseldorf, FRG.
Arch Dermatol Res. 1989;281(3):193-7. doi: 10.1007/BF00456392.
In a bilateral paired comparison (randomized double-blind study) 31 dermatitis patients (atopic and contact dermatitis) were tested with two ointments containing 0.0056% betamethasone-17-benzoate. One ointment was applied on each side of the body. The topical formulations differed in their solution capacities for the drug by a factor of about 50 (solution-type: high mutual affinity between drug and vehicle; suspension-type: low affinity). The different antiinflammatory effects were studied visually by assessing five symptoms: erythema, scaling, infiltration, lichenification, and excoriation. On the 5th day, 73% of the patients showed significant differences between the sides in favor of the suspension-type ointment (Wilcoxon test). Blanching tests on 30 volunteers confirmed the result. The in vitro drug release, however, was faster with the solution-type ointment. The efficacy of an ointment can be increased greatly, if the solution capacity for the drug is low, and thus the partition coefficient between the stratum corneum (barrier of the skin) and the vehicle is high. As long as the barrier is not damaged completely, the difference in drug release is not the determining factor for the effect.
在一项双侧配对比较（随机双盲研究）中，31名皮炎患者（特应性皮炎和接触性皮炎）使用两种含有0.0056%倍他米松-17-苯甲酸酯的软膏进行测试。每种软膏分别涂抹于身体的一侧。两种外用制剂的药物溶解能力相差约50倍（溶液型：药物与赋形剂之间具有高相互亲和力；混悬型：低亲和力）。通过评估红斑、脱屑、浸润、苔藓化和擦伤这五种症状，直观地研究不同的抗炎效果。在第5天，73%的患者两侧出现显著差异，混悬型软膏更具优势（Wilcoxon检验）。对30名志愿者进行的皮肤苍白试验证实了这一结果。然而，溶液型软膏的体外药物释放更快。如果药物的溶解能力较低，因此角质层（皮肤屏障）与赋形剂之间的分配系数较高，软膏的疗效可大大提高。只要屏障未被完全破坏，药物释放的差异就不是疗效的决定性因素。
