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弱碱在大鼠胃黏膜的体内和体外转运

Transport of weak bases across rat gastric mucosa in vivo and in vitro.

作者信息

Tai C Y, Jackson M J

出版信息

J Pharmacol Exp Ther. 1982 Aug;222(2):372-8.

PMID:7097557
Abstract

The transport of weak bases (pKa values 1.4 through 10.3) across in vitro and in vivo preparations of rat gastric mucosa have been compared. Asymmetric movements were observed in all cases, and the in vitro and in vivo data showed similar profiles of relation between the degrees of asymmetry and the pKa values of transported compounds. These profiles could be described by an equation based on a three-compartment model system, but it was necessary to postulate two such systems in parallel to give a satisfactory fit to the full range of pKa values tested. One system (I) is analogous to that described previously in small intestine. The properties of this system [(Pi/Pni)a = 2.5 x 10(-3), (Pi/Pni)b = 7.0 x 10(-1)] suggested that the intermediate compartment is a subepithelial extracellular compartment in which an alkaline pH is maintained [pHx = 8.5]. The second system (II) is the opposite polarity [(Pi/Pni)a = 1 x 10(0), (Pi/Pni)b = 3 x 10(-1)], and this system may be represented by the acidic lumen of the gastric tube [pHx = 2.0]. The principal differences between the in vivo and in vitro data could be ascribed to poor stirring of the luminal bulk phase in the in vivo situation. It was concluded that the determinants of weak base transport identified in studies with in vitro preparations are pertinent to the absorptive and secretory processes that occur in the intact stomach.

摘要

对弱碱(pKa值为1.4至10.3)在大鼠胃黏膜的体外和体内制剂中的转运进行了比较。在所有情况下均观察到不对称转运,并且体外和体内数据显示不对称程度与转运化合物的pKa值之间的关系具有相似的曲线。这些曲线可以用基于三室模型系统的方程来描述,但需要假设两个这样的平行系统才能对所测试的整个pKa值范围给出令人满意的拟合。一个系统(I)类似于先前在小肠中描述的系统。该系统的特性[(Pi/Pni)a = 2.5×10(-3),(Pi/Pni)b = 7.0×10(-1)]表明中间室是维持碱性pH值[pHx = 8.5]的上皮下细胞外室。第二个系统(II)具有相反的极性[(Pi/Pni)a = 1×10(0),(Pi/Pni)b = 3×10(-1)],该系统可能由胃管的酸性管腔[pHx = 2.0]表示。体内和体外数据之间的主要差异可归因于体内情况下管腔主体相搅拌不足。得出的结论是,在体外制剂研究中确定的弱碱转运的决定因素与完整胃中发生的吸收和分泌过程相关。

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