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影响抗胆碱能药物作用的生物药剂学因素:丙胺太林、己环铵和异丙胺的比较

Biopharmaceutic factors that influence effects of anticholinergic drugs: comparison of propantheline, hexocyclium, and isopropamide.

作者信息

Grundhofer B, Gibaldi M

出版信息

J Pharm Sci. 1977 Oct;66(10):1433-5. doi: 10.1002/jps.2600661021.

Abstract

The antisecretory (determined from salivary flow rates) and antimotility (determined from riboflavin absorption) effects of usually recommended doses of propantheline, hexocyclium, and isopropamide were compared in four adult volunteers. Both propantheline and hexocyclium significantly decreased salivary flow and increased riboflavin absorption. Although the usual dose of propantheline was about twice as effective as the usual dose of hexocyclium in suppressing salivary flow, these doses produced comparable effects on riboflavin absorption. Isopropamide had little or no effect on either the salivary flow rate or riboflavin absorption. Propantheline and hexocyclium elicited little effect on salivary flow when administered after a meal. Prolonged-release dosage forms of these drugs produced effects comparable to those produced by much smaller doses in conventional tablets and gave no indication of providing prolonged anticholinergic effects.

摘要

在四名成年志愿者中比较了通常推荐剂量的丙胺太林、己环铵和异丙胺的抗分泌作用(根据唾液流速确定)和抗蠕动作用(根据核黄素吸收情况确定)。丙胺太林和己环铵均显著降低唾液流速并增加核黄素吸收。虽然丙胺太林的常用剂量在抑制唾液分泌方面的效果约为己环铵常用剂量的两倍,但这些剂量对核黄素吸收产生的效果相当。异丙胺对唾液流速或核黄素吸收几乎没有影响。丙胺太林和己环铵在餐后给药时对唾液流速几乎没有影响。这些药物的缓释剂型产生的效果与常规片剂中剂量小得多时产生的效果相当,且未显示出具有延长的抗胆碱能作用。

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