Sato K, Sugibayashi K, Morimoto Y
Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan.
J Pharm Sci. 1991 Feb;80(2):104-7. doi: 10.1002/jps.2600800203.
The species difference in skin permeability, Kp, of nicorandil was determined by using excised skin samples from hairless mouse, hairless rat, guinea-pig, dog, pig, and human. The Kp value of nicorandil in hairless mice was the greatest among the six species, and those in pigs and humans were in good agreement. To clarify the reasons for the species difference, various skin characteristics in each species were measured. It was suggested that the difference of skin surface lipids in each species affected the partitioning of nicorandil from vehicle to stratum corneum, and that such a difference would be a main factor for the species difference in nicorandil permeability. Since pig and human skins had similar surface lipids, barrier thickness, and morphological aspects, percutaneous absorption studies using excised pig skin samples would be useful for the estimation of in vitro human skin permeation behavior.
采用来自无毛小鼠、无毛大鼠、豚鼠、犬、猪和人类的离体皮肤样本，测定了尼可地尔的皮肤渗透系数（Kp）的种属差异。在这六个物种中，尼可地尔在无毛小鼠中的Kp值最大，而在猪和人类中的Kp值较为一致。为阐明种属差异的原因，对每个物种的各种皮肤特性进行了测量。结果表明，各物种皮肤表面脂质的差异影响了尼可地尔从载体向角质层的分配，这种差异可能是尼可地尔渗透性种属差异的主要因素。由于猪和人类皮肤具有相似的表面脂质、屏障厚度和形态学特征，因此使用离体猪皮肤样本进行经皮吸收研究将有助于评估体外人类皮肤的渗透行为。
