Ghosh T K, Chiao C S, Gokhale R D
Division of Medicinal Chemistry and Pharmaceutics, School of Pharmacy, Northeast Louisiana University, Monroe 71209.
J Pharm Pharmacol. 1993 Mar;45(3):218-9. doi: 10.1111/j.2042-7158.1993.tb05536.x.
To support the development of a suitable transdermal dosage form for beta-blockers, in-vitro, skin permeation studies of nine beta-blockers were conducted at 37 degrees C across the excised abdominal skin of hairless mouse mounted on the receptor compartment of a two-chambered Valia-Chien glass diffusion cell. The drugs varied in lipophilicity, whereas pKa values were comparable. Permeability coefficients were calculated from the steady-state flux values. Agreement was found between the permeability coefficient and the drug lipophilicity, expressed as the octanol-buffer distribution coefficient.
为了支持开发适合β受体阻滞剂的透皮剂型，在37℃下，将无毛小鼠的腹部离体皮肤安装在两室Valia-Chien玻璃扩散池的受体室上，对9种β受体阻滞剂进行了体外皮肤渗透研究。这些药物的亲脂性各不相同，而pKa值相当。根据稳态通量值计算渗透系数。发现渗透系数与以正辛醇-缓冲液分配系数表示的药物亲脂性之间存在一致性。
