Authors: ZHANG, Yi-fan¹; CHEN, Xiao-yan¹; DAI, Xiao-jian¹; ZHANG, Yi-ni; LIU, Qi-zhi²; YU, Hua-ling³; ZHONG, Da-fang

Source: Acta Pharmacologica Sinica, Volume 28, Number 8, August 2007 , pp. 1243-1246(4)

Publisher: Wiley-Blackwell

Abstract:

Aim: To investigate the influence of omeprazole on the pharmacokinetics of domperidone given as free base and maleate salt. Methods: An open, randomized, 2-period crossover study with a washout period of 7 d was conducted in 10 healthy Chinese, male patients. In each study period, the patients were administered a single oral dose of 10 mg domperidone as free base or maleate salt on d 1, 20 mg omeprazole twice daily on d 2 and 3, and once on d 4. A single dose of 10 mg domperidone as free base or maleate salt was taken at 4 h after administration of omeprazole on d 4. Plasma samples were collected on d 1 and 4 after the administration of domperidone, and the plasma concentrations of domperidone were determined by a sensitive liquid chromatography-tandem mass spectrometry method. Results: For free-base domperidone, pretreatment with omeprazole resulted in a 16% decrease in maximum concentration (C_max), compared with administration alone (P < 0.05). However, for maleate salt, with the exception of an increase in t_1/2, no pharmacokinetic parameters were significantly changed. When the free base and maleate salt were administered alone, no differences were found in any parameters between the 2 formulations. In contrast, when they were administered in the presence of omeprazole, the C_max of domperidone given as free base was lower (25.9%) than that given as maleate salt (P < 0.05). Conclusion: Pretreatment of omeprazole does not affect the absorption of domperidone maleate, but leads to a moderately decreased rate of absorption of the free base.

Keywords: domperidone; omeprazole; maleate salt; free base; pharmacokinetics

Document Type: Research article

DOI: http://dx.doi.org/10.1111/j.1745-7254.2007.00596.x

Affiliations: 1: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China 2: Beijing Hanmi Pharm, Beijing 101312, China 3: Shenyang Pharmaceutical University, Shenyang 110016, China

Publication date: 2007-08-01

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