Nishida Koyo, Nose Seiichi, Kuma Akiko, Mukai Takahiro, Kawakami Shigeru, Nakashima Mikiro, Sasaki Hitoshi, Sakaeda Toshiyuki, Nakamura Junzo
School of Pharmaceutical Sciences, Nagasaki University, Japan.
J Pharm Pharmacol. 2002 Jul;54(7):1005-9. doi: 10.1211/002235702760089144.
The purpose of this study was to clarify the absorption characteristics of drugs across the serosal caecal surface membrane, occupying a large absorption area in the peritoneal cavity in rats. Absorption of phenolsulfonphthalein (PSP) and fluorescein isothiocyanate dextrans (FDs) as model drugs after application to the rat serosal caecal surface was investigated using a cylindrical diffusion cell. PSP was absorbed from the rat serosal caecal surface, followed by appearance in the plasma and bile. The time course of the remaining PSP amount in the diffusion cell obeyed first-order kinetics, and the rate constant, Ka, was calculated to be 8.01 x 10(-3) min(-1). No significant difference was seen in the absorption ratio of PSP, which was approximately 90% in 6 h for three doses (0.3, 0.5 and 1 mg), suggesting linear absorption. Moreover, the absorption ratios of FDs from the rat serosal caecal surface at 3 h decreased with an increase in the molecular weight (24.7% for FD4, 12.8% for FD-10 and 3.4% for FD-40).
本研究的目的是阐明药物在大鼠腹膜腔中占据较大吸收面积的盲肠浆膜表面膜的吸收特性。使用圆柱形扩散池研究了将酚磺酞(PSP)和异硫氰酸荧光素葡聚糖(FDs)作为模型药物应用于大鼠盲肠浆膜表面后的吸收情况。PSP从大鼠盲肠浆膜表面吸收,随后出现在血浆和胆汁中。扩散池中剩余PSP量的时间进程符合一级动力学,计算得出的速率常数Ka为8.01×10(-3)min(-1)。PSP的吸收比率在三剂(0.3、0.5和1mg)给药6小时后约为90%,未见显著差异,提示为线性吸收。此外,3小时时大鼠盲肠浆膜表面FDs的吸收比率随分子量增加而降低(FD4为24.7%,FD-10为12.8%,FD-40为3.4%)。