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依替膦酸钙镁对大鼠水杨酸吸收的剂量依赖性效应。

Dose-dependent effect of calcium and magnesium etidronate on salicylic acid absorption in the rat.

作者信息

Shrewsbury R P, Wurster D E, Dittert L W

出版信息

J Pharm Pharmacol. 1985 Jun;37(6):440-2. doi: 10.1111/j.2042-7158.1985.tb03034.x.

Abstract

Disodium etidronate affected salicylic acid absorption from the rat small intestine, in-situ, when instilled into a jejunal segment for different exposure times before the salicylic acid absorption was measured. At low etidronate concentrations and short exposure times, the salicylic acid absorption rate was significantly increased compared with saline controls. At high etidronate concentrations and longer exposure times, the absorption rate was reduced. Etidronate precomplexed with calcium or magnesium ions at low concentrations still enhanced salicylic acid absorption but at high concentrations absorption of salicylic acid was close to saline controls. Intestinal mucosa exposed to high etidronate concentrations showed a progressive structural destruction but with the complexes, there was no visible alteration. It is proposed that a solubilized etidronate complex, formed either in-situ or administered as such, is responsible for enhancing salicylic acid absorption. This effect is hidden at high etidronate concentrations because of the deterioration of the mucosal surface and at high complex concentrations because these decrease the absorbing surface area and increase the viscosity of the lumen contents.

摘要

依替膦酸二钠在测量水杨酸吸收之前,于大鼠空肠段原位注入不同暴露时间,会影响水杨酸从大鼠小肠的吸收。在低依替膦酸浓度和短暴露时间下,与生理盐水对照组相比,水杨酸吸收速率显著增加。在高依替膦酸浓度和较长暴露时间下,吸收速率降低。低浓度下与钙或镁离子预络合的依替膦酸仍能增强水杨酸吸收,但在高浓度下,水杨酸吸收接近生理盐水对照组。暴露于高依替膦酸浓度的肠黏膜显示出渐进性结构破坏,但与络合物一起时,未见明显改变。有人提出,原位形成或原样给药形成的可溶性依替膦酸络合物是增强水杨酸吸收的原因。在高依替膦酸浓度下,由于黏膜表面恶化,这种作用被掩盖;在高络合物浓度下,由于它们减小了吸收表面积并增加了肠腔内容物的粘度,这种作用也被掩盖。

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Dose-dependent absorption of disodium etidronate.依替膦酸二钠的剂量依赖性吸收。
J Pharm Pharmacol. 1985 Jun;37(6):443-5. doi: 10.1111/j.2042-7158.1985.tb03035.x.
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In vivo absorption of theophylline and salicylic acid from rat small intestine.茶碱和水杨酸在大鼠小肠内的体内吸收情况。
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