Utoguchi N, Watanabe Y, Takase Y, Suzuki T, Matsumoto M
Department of Pharmaceutics, Showa College of Pharmaceutical Sciences, 3-3165 Higashi-Tamagawagakuen, Machida, Tokyo 194-8543, Japan.
J Pharm Sci. 1999 Jan;88(1):142-6. doi: 10.1021/js970412e.
Previously, we found that monocarboxylic acids undergo carrier-mediated transport in primary cultures of oral mucosal epithelial cells.1 In this study, we investigated whether carrier-mediated absorption of a monocarboxylic acid from the oral mucosa occurs in vivo. Salicylic acid was administered to hamster cheek pouch. At predetermined intervals, the concentration of salicylic acid in the fluid remaining in the cheek pouch lumen and the blood salicylic acid concentration were determined. The absorption of salicylic acid was saturable at high salicylic acid concentrations. Sodium azide, a metabolic inhibitor, and carbonylcyanide p-trifluoromethoxyphenylhydrazone (FCCP), a protonophore, significantly inhibited the absorption of salicylic acid but not the absorption of salicylamide from the oral mucosa. Various monocarboxylic acids inhibited the absorption of salicylic acid, whereas dicarboxylic acids had no such effect. Transfer of [14C]salicylic acid from the cheek pouch mucosa to the systemic circulation was observed, and the blood [14C]salicylic acid concentration in the case of coadministration with propionic acid was significantly lower than that in the case of no propionic acid coadministration. These results show that monocarboxylic acids undergo carrier-mediated absorption from the hamster cheek pouch mucosa.
此前，我们发现一元羧酸在口腔黏膜上皮细胞原代培养物中通过载体介导进行转运。1在本研究中，我们调查了一元羧酸在体内是否通过载体介导从口腔黏膜吸收。将水杨酸给予仓鼠颊囊。在预定的时间间隔，测定颊囊腔中残留液体中的水杨酸浓度以及血液中的水杨酸浓度。在高水杨酸浓度下，水杨酸的吸收具有饱和性。代谢抑制剂叠氮化钠和质子载体羰基氰化物对三氟甲氧基苯腙（FCCP）显著抑制了水杨酸的吸收，但未抑制口腔黏膜对水杨酰胺的吸收。各种一元羧酸抑制了水杨酸的吸收，而二元羧酸则没有这种作用。观察到[14C]水杨酸从颊囊黏膜转移到体循环，与丙酸共同给药时的血液[14C]水杨酸浓度显著低于未与丙酸共同给药时的浓度。这些结果表明，一元羧酸通过载体介导从仓鼠颊囊黏膜吸收。
