Endo T, Nakaya S, Kimura R
Faculty of Pharmaceutical Science, Higashi Nippon Gakuen University, Hokkaido, Japan.
Pharmacol Toxicol. 1989 Aug;65(2):128-35. doi: 10.1111/j.1600-0773.1989.tb01142.x.
A correlation between absorption of organic mercuric compounds and their molecular weight or lipophilicity was investigated by the perfusion of rat small intestine. The intestine was perfused for 1.0 hr at different osmolarity and different pH with buffers containing 10(-4) M organic mercuric compounds, methyl mercuric chloride (MMC), phenyl mercuric chloride (PMC), p-chloromercuribenzoic acid (PCMB) and p-chloromercuriphenylsulfonic acid (PCMBS). The order of absorption of these compounds at several osmolarities and pHs (MMC greater than PMC greater than PCMB greater than PCMBS) was inversely correlated to their molecular weight. The increase in pH decreased markedly the absorption and n-octanol/water partition coefficient of PCMB, and it decreased scarcely those of MMC, PMC and PCMBS. The order of the coefficients at each pH was as follows; PMC greater than MMC greater than PCMB greater than PCMBS, in disagreement with the order of absorption. These results suggest that the molecular weight is more important factor in the intestinal absorption of organic mercuric compounds than the lipophilicity.
通过大鼠小肠灌注研究了有机汞化合物的吸收与其分子量或亲脂性之间的相关性。用含有10(-4)M有机汞化合物、甲基汞氯化物(MMC)、苯基汞氯化物(PMC)、对氯汞苯甲酸(PCMB)和对氯汞苯磺酸(PCMBS)的缓冲液在不同渗透压和不同pH值下对小肠进行1.0小时的灌注。这些化合物在几种渗透压和pH值下的吸收顺序(MMC>PMC>PCMB>PCMBS)与其分子量呈负相关。pH值的升高显著降低了PCMB的吸收和正辛醇/水分配系数,而对MMC、PMC和PCMBS的吸收和分配系数几乎没有影响。各pH值下系数的顺序如下:PMC>MMC>PCMB>PCMBS,与吸收顺序不一致。这些结果表明,分子量在有机汞化合物的肠道吸收中比亲脂性更重要。