Studies on Characteristics of Drug Exsorption across the Membrane of Rat Small Intestine

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The exsorption of sulfanilamide into the small intestinal lumen after intravenous administration of the drug was studed with perfusion solution without any drugs having three different tonicities such as hypotonicity (0.45%), isotonicity (0.90%), and hypertonicity (1.35%) with sodium chloride employing an in situ single perfusion method devised by Schanker and his co-workers. The intraluminal single perfusion was conducted principally at a rate of 1 ml/min. The exsorption rate of the drug into the isotonic perfusate was dose-dependent and the rate was decreased with time obeying the first-order kinetics as well as the decrease in blood level of the drug. The amount of the drug exsorbed in the isotonic perfusate for 180 min represented as the percentage of dose was almost constant (about 17%) in the dose rangs from 10 mg/kg to 50 mg/kg used in the present study. The effect of tonicity of perfusion solution on the exsorption was examined and it was found that the exsorption rate and the amount exsorbed in the perfusate of the drug were increased with increasing the tonicity of the perfusate. Although the exsorption rate and the amount exsorbed in the lumen were changed by different experimental conditions, the existence of the drug in the perfusate was not negligible. These evidences suggest that the small intestinal lumen may be an important organ in the distribution of the drug. Moreover, the excretion of the drug in the bile juice was remarkably smaller than the exsorption of the drug into perfusate. Hence it is able to conclude that the distribution of the drug in the small intestinal lumen might be conducted across the intestinal membrane rather than through the agency of bile juice.
公益社団法人日本薬学会の論文
1977-11-25

Studies on Characteristics of Drug Exsorption across the Membrane of Rat Small Intestine

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