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影响皮肤渗透性的因素。体内与体外观察结果之间的关系。

Factors affecting the permeability of skin. The relation between in vivo and in vitro observations.

作者信息

Creasey N H, Battensby J, Fletcher J A

出版信息

Curr Probl Dermatol. 1978;7:95-106.

PMID:752461
Abstract

At the same temperature and with adequate circulation of blood or receptor solution beneath it the permeability of the stratum corneum of the rabbit ear to T2O or to 32P-TPP was the same in vivo as in vitro. When skin permeability was measured in vitro, the subcutaneous adipose tissue present in the full-thickness skin of the rat delayed the penetration of CR, a lipophilic substance with a low water solubility, and decreased the permeability constant by nearly 3x. The retardant solvent PEG 300 did not penetrate the stratum corneum; it formed a hydrogen-bonded complex with the cholinesterase inhibitor VX, thereby reducing the thermodynamic activity and penetration rate of this compound through the stratum corneum. The accelerant solvent DMSO removed protein components from the stratum corneum; electron microscope studies showed that the cells of stratum corneum so treated became separated from one another, and their contents became stainable in bulk with Pb++, indicating the creation of new diffusion pathways. When the temperature, clearance of penetrant from the lower surface of the stratum corneum and penetrant formulation were the same in vivo as in vitro, and the surface of the stratum corneum was saturated with the penetrant or its solution, the results of permeability measurements made in vivo were similar to those made in vitro.

摘要

在相同温度下,且其下方有充足的血液或受体溶液循环时,兔耳角质层对T2O或32P - TPP的体内渗透性与体外相同。当在体外测量皮肤渗透性时,大鼠全层皮肤中存在的皮下脂肪组织会延迟亲脂性、低水溶性物质CR的渗透,并使渗透常数降低近3倍。阻滞剂溶剂聚乙二醇300不会穿透角质层;它与胆碱酯酶抑制剂VX形成氢键复合物,从而降低该化合物通过角质层的热力学活性和渗透率。促进剂溶剂二甲基亚砜从角质层中去除蛋白质成分;电子显微镜研究表明,经如此处理的角质层细胞彼此分离,其内容物能用Pb++整体染色,表明形成了新的扩散途径。当体内角质层下表面的渗透物清除率、温度和渗透物制剂与体外相同时,且角质层表面被渗透物或其溶液饱和时,体内渗透性测量结果与体外相似。

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