The effect of vehicle on the diffusion of salicylic acid through hairless mouse skin.
The effect of vehicle on the diffusion of salicylic acid through hairless mouse skin.
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载体对水杨酸通过无毛小鼠皮肤扩散的影响。
DOI：
10.1002/jps.2600750804
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发表时间：
1986
影响因子：
3.8
通讯作者：
Koch,SA
中科院分区：
文献类型：
--
作者：
Sloan,KB;Siver,KG;Koch,SA
水杨酸的溶解度，并通过，无毛小鼠皮肤从肉豆蔻酸异丙酯，1-辛醇，1-丙醇，丙二醇，甲酰胺的流量已被实验确定。根据通量/溶解度=Kp确定相应通量的渗透系数（Kp）值。然后将这些值与根据溶剂（δv）、水杨酸（δi）和皮肤（δs）的已知溶解度参数计算的相应分配系数（P）值进行比较。使用两种不同的δi值计算理论P值，一种基于峰值溶解度方法，另一种基于基团贡献的计算（分别为11和14.4（cal/cm 3）1/2）。从溶剂中递送水杨酸的理论logP-1.42和实验logKP值之间存在良好的相关性，溶剂的溶解度参数范围为δv= 10-18（cal/cm 3）1/2，当δ i为14.4（cal/cm ~ 3）~（1/2.对于表现出溶解度参数的溶剂，理论logP-2.09和实验logKp值之间也存在良好的相关性在δv= 7.6-10（cal/cm ~ 3）~（1/2）范围内，当假定δ i为11（cal/cm ~ 3）~（1/2）时，使用了两个不同的δi值，因为水杨酸在极性溶剂中表现出极性分子的性质，而在非极性溶剂中表现出非极性分子的性质。发现质量、通量和渗透系数与药物在溶媒中的溶解度成反比，最小值大致对应于δv=δi的点，最小值在理论P曲线内。可溶性很强的分子的这些结果与可溶性较差的分子茶碱获得的结果几乎相同。
The solubilities of salicylic acid in, and the fluxes through, hairless mouse skin from isopropyl myristate, 1-octanol, 1-propanol, propylene glycol, and formamide have been determined experimentally. Values for permeability coefficients (Kp) corresponding to the respective fluxes were determined from: flux/solubility =Kp.These values were then compared with values for the respective partition coefficients (P) which were calculated from the known solubility parameters for the vehicles (δv), salicylic acid (δi), and skin (δs). Two differentδi, values were used to calculate theoreticalPvalues, one based on the peak solubility method and the other based on calculation from group contributions (11 and 14.4 (cal/cm3)1/2, respectively). There was good correlation between the values for theoretical logP−1.42 and experimental logKpfor the delivery of salicylic acid from vehicles exhibiting solubility parameters in the range ofδv= 10–18 (cal/cm3)1/2, whenδiwas assumed to be 14.4 (cal/cm3)1/2.There was also a good correlation between the values for theoretical logP−2.09 and experimental logKpfor vehicles exhibiting solubility parameters in the range ofδv= 7.6–10 (cal/cm3)1/2, whenδiwas assumed to be 11 (cal/cm3)1/2.Two differentδi, values were used because salicylic acid apparently behaves like a polar molecule in polar vehicles and a nonpolar molecule in nonpolar vehicles. Qualitatively, fluxes and permeability coefficients were found to be inversely dependent on drug solubility in the vehicles, with a minimum that corresponded approximately to the point whereδv=δi, and the minimum within the theoretical Pcurve. These results with a very soluble molecule are almost the same as those obtained with the poorly soluble molecule, theophylline.