PREDICTION OF SKIN PERMEABILITIES OF DICLOFENAC AND PROPRANOLOL FROM THEORETICAL PARTITION-COEFFICIENTS DETERMINED FROM COHESION PARAMETERS
PREDICTION OF SKIN PERMEABILITIES OF DICLOFENAC AND PROPRANOLOL FROM THEORETICAL PARTITION-COEFFICIENTS DETERMINED FROM COHESION PARAMETERS
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DOI：
10.1002/jps.2600820416
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发表时间：
1993-04-01
影响因子：
3.8
通讯作者：
NAGAI, T
中科院分区：
文献类型：
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作者：
MAITANI, Y;COUTELEGROS, A;NAGAI, T
实验测定了双氯芬酸与心得安的内聚参数。理论配分系数（P(s,v)）由活度系数（gamma）和溶剂（delta1 = delta(v)）、溶质（delta2）和蒙皮（delta(s)）的内聚参数计算得到。利用扩展的Hildebrand溶解度方程，用双氯芬酸和普萘洛尔在乙醇-水缓冲液中的溶解度数据得出的伽马值来考虑给定溶液中溶质-溶剂相互作用的势能。由通量和溶解度确定的实验渗透率系数（K(p)）值与各自的p （s,v）值进行了比较。在δ (v) = 18-24 (cal/cm3)1/2范围内，由乙醇-水相缓冲液组成的溶剂，由于其黏合参数与溶质相似，其通量增大，K(p)减小。P（s,v）与实验K(P)的差异表明，溶剂中的乙醇影响了膜，双氯芬酸和心得安可能被乙醇溶剂化而穿透膜。
The cohesion parameters of diclofenac and propranolol were determined experimentally. The theoretical partition coefficient (P(s,v)) was calculated from the activity coefficient (gamma) and the cohesion parameters of the solvent (delta1 = delta(v)), solute (delta2), and skin (delta(s)). By using the extended Hildebrand solubility equation, the potential energy of solute-solvent interaction in a given solution was considered to have the gamma value derived from solubility data of diclofenac and propranolol in ethanol-aqueous buffer. Values for experimental permeability coefficients (K(p)), which were determined from flux and solubility, were compared with values for the respective P(s,v). For a solvent that consists of ethanol-aqueous buffer exhibiting cohesion parameters in the range of delta(v) = 18-24 (cal/cm3)1/2, the fluxes increased and the K(p) decreased because of the similarity in cohesion parameters of these solvents to the solute. The difference between P(s,v) and experimental K(p) suggests that ethanol in the solvent affects the membrane and diclofenac and propranolol penetrate through the membrane, possibly solvated by ethanol.