Enhanced skin permeation of a lipophilic drug using supersaturated formulations
Enhanced skin permeation of a lipophilic drug using supersaturated formulations
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DOI：
10.1016/s0168-3659(01)00290-5
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发表时间：
2001-06-15
影响因子：
10.8
通讯作者：
Guy, RH
中科院分区：
文献类型：
--
作者：
Moser, K;Kriwet, K;Guy, RH
使用过饱和来增强亲脂模型化合物（薰衣草素衍生物，LAP）通过体外切除的猪皮肤的渗透。将药物溶解在一系列液体和半固体载体中（其中药物具有不同的溶解度），这些载体可以使用(i)混合助溶剂法，（ii）溶剂蒸发法或（iii）加热溶解药物的方法制备。饱和制剂通过皮肤的渗透率相当，独立于药物在载体中的绝对浓度。饱和度为二的过饱和溶液导致药物渗透速率加倍。因此，这些实验表明，使用过饱和配方可以持续增加LAP的经皮吸收，与载体的类型和组成以及制备方法无关。(C) 2001 Elsevier Science B.V.版权所有
Supersaturation was used to enhance the permeation of a lipophilic model compound (a lavendustin derivative, LAP) through excised pig skin in vitro. The drug was dissolved in a series of liquid and semisolid vehicles (in which it had different solubilities) and which were prepared using either (i) the method of mixed cosolvents, (ii) the method of solvent evaporation, or (iii) the method of dissolving the drug with heating. Saturated formulations showed comparable permeation rates through the skin, independent of the absolute concentration of the drug in the vehicle. Supersaturated solutions at a degree of saturation of two resulted in a doubling of the drug permeation rate. These experiments show, therefore, that the percutaneous absorption of LAP may be consistently increased using supersaturated formulations, independent of the type and composition of the vehicles and independent of their method of preparation. (C) 2001 Elsevier Science B.V. All rights reserved.