Absorption characteristics of model compounds with different molecular weights from the serosal caecal surface in rats

Absorption characteristics of model compounds with different molecular weights from the serosal caecal surface in rats
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不同分子量模型化合物在大鼠盲肠浆膜表面的吸收特性

DOI:
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发表时间:
2002
期刊:
The Journal of pharmacy and pharmacology
影响因子:
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通讯作者:
J. Nakamura
J. Nakamura
中科院分区:
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文献类型:
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作者:
K. Nishida;Seiichi Nose;A. Kuma;T. Mukai;S. Kawakami;M. Nakashima;H. Sasaki;T. Sakaeda;J. Nakamura

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本研究的目的是阐明药物在大鼠腹腔中占据较大吸收面积的盲肠浆膜的吸收特性。用扩散池研究了模型药物酚磺酞(PSP)和异硫氰酸荧光素葡聚糖(FDs)在大鼠盲肠表面的吸收。PSP从大鼠盲肠粘膜表面吸收,随后出现在血浆和胆汁中。扩散池中剩余PSP量的时间过程符合一级动力学,速率常数Ka计算为8.01 × 10− 3 min −1。PSP的吸收率无显著差异,3个剂量(0.3、0.5和1 mg)6 h内约为90%,表明线性吸收。此外,3 h时大鼠浆膜盲肠表面FD的吸收率随着分子量的增加而降低(FD-4为24.7%,FD-10为12.8%,FD-40为3.4%)。
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 × 10−3min−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 FD‐4, 12.8% for FD‐10 and 3.4% for FD‐40).