Kato A, Iwata S
Tsukuba Research Laboratories, Eisai Co., Ltd., Ibaraki, Japan.
J Pharmacobiodyn. 1988 May;11(5):330-4. doi: 10.1248/bpb1978.11.330.
Various factors influencing corneal permeability to bunazosin were investigated. The permeability of the cornea to bunazosin increased with increasing pH, either in the presence or absence of caprylic acid; the permeability to bunazosin and the partition of bunazosin were both enhanced by caprylic acid and both enhancements became maximal when the molar ratio of bunazosin: caprylic acid became unity; the permeability to methylparaben, a non-ionic permeant, was not increased by caprylic acid or capric acid and the permeability was not increased by the pretreatment of the cornea with caprylic acid. Furthermore, protein-bunazosin interaction was not affected by caprylic acid. The present results suggest that the enhancement of permeability caused by caprylic acid is attributable only to the increased partition of bunazosin to the corneal membrane.
研究了影响角膜对布那唑嗪通透性的各种因素。无论有无辛酸存在,角膜对布那唑嗪的通透性均随pH值升高而增加;辛酸可增强角膜对布那唑嗪的通透性以及布那唑嗪的分配,当布那唑嗪与辛酸的摩尔比为1时,两种增强作用均达到最大;辛酸或癸酸不会增加对非离子渗透剂对羟基苯甲酸甲酯的通透性,用辛酸预处理角膜也不会增加其通透性。此外,辛酸不影响蛋白质与布那唑嗪的相互作用。目前的结果表明,辛酸引起的通透性增强仅归因于布那唑嗪在角膜膜中分配的增加。