Ohsako M, Matsumoto Y, Goto S
Department of Pharmacy, Daiichi College of Pharmaceutical Sciences, Fukuoka, Japan.
Biol Pharm Bull. 1993 Feb;16(2):154-7. doi: 10.1248/bpb.16.154.
The transport of aspirin (ASP) and its metabolites (salicylic acid (SA), salicyluric acid (SAU), gentisic acid (GA) and gentisuric acid (GAU)) through human erythrocyte membrane was investigated. ASP permeated rapidly into the erythrocytes and the concentration dwindled gradually after the maximum concentration was attained almost within one minute. It was suggested that SA is released from the erythrocytes after ASP transported into the erythrocytes is hydrolyzed in them. In both an inward and outward direction, the transport rates of SA and GA were rapid, while those of SAU and GAU were lower by conjugating glycine. It was suggested that GAU remains for a long time in a living body. The rate of transport of GA and GAU were markedly obstructed by the band 3 protein inhibitor 4,4'-diisothiocyanostilbene-2,2'-disulfonate, although the transport rates of SA and SAU were obstructed only slightly. It was suggested that the transport of GA and GAU are mediated through band 3 protein.
研究了阿司匹林（ASP）及其代谢产物（水杨酸（SA）、水杨尿酸（SAU）、龙胆酸（GA）和龙胆尿酸（GAU））通过人红细胞膜的转运情况。ASP迅速渗透进入红细胞，在几乎一分钟内达到最大浓度后，其浓度逐渐下降。有人提出，进入红细胞的ASP在细胞内水解后，SA从红细胞中释放出来。在向内和向外两个方向上，SA和GA的转运速率都很快，而SAU和GAU通过与甘氨酸结合，转运速率较低。有人提出，GAU在生物体内会长时间留存。尽管SA和SAU的转运速率仅略有受阻，但带3蛋白抑制剂4,4'-二异硫氰酸芪-2,2'-二磺酸盐显著阻碍了GA和GAU的转运速率。有人提出，GA和GAU的转运是通过带3蛋白介导的。
