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安非他酮对大鼠西咪替丁和雷尼替丁吸收的影响。

Effect of bupropion on cimetidine and ranitidine absorption in rats.

作者信息

Tanira M O, Kaka J S, al-Khamis K I

机构信息

Department of Clinical Pharmacy, College of Pharmacy, King Saud University, Riyadh, Saudi Arabia.

出版信息

Biopharm Drug Dispos. 1989 Jan-Feb;10(1):35-41. doi: 10.1002/bdd.2510100105.

DOI:10.1002/bdd.2510100105
PMID:2493822
Abstract

Cimetidine and ranitidine absorption were studied in rats, alone or in combination with concurrent but separate bupropion oral administration. Blood samples were collected before and 0.25, 0.5, 0.75, 1.0, 1.5, 2.0, 3.0, 4.5, and 6.0 h after dosing. In ranitidine-treated rats, an extra blood sample at 8 h was collected. Assays of cimetidine and ranitidine were carried out using a HPLC method. Mean cimetidine plasma concentrations on concurrent bupropion administration at 0.25 and 0.5 h were approximately 2 and 1.5 times compared to the control. Similarly, mean ranitidine plasma concentrations with bupropion combination at 0.25 and 0.5 h were significantly different and approximately 2 and 3 times higher. Time of maximum concentration for cimetidine and ranitidine on combination were reduced to almost half of the control value. However, only the time of maximum concentration for cimetidine showed statistically significant difference. No significant differences were observed between AUCs, maximum concentrations, and half-lives of cimetidine and ranitidine compared to their respective controls. The results suggest that concurrent bupropion administration may affect the rate but not the extent of absorption of cimetidine and ranitidine.

摘要

在大鼠中研究了西咪替丁和雷尼替丁的吸收情况,单独给药或与同时但分开口服的安非他酮联合给药。在给药前以及给药后0.25、0.5、0.75、1.0、1.5、2.0、3.0、4.5和6.0小时采集血样。对于接受雷尼替丁治疗的大鼠,在8小时时额外采集一份血样。使用高效液相色谱法对西咪替丁和雷尼替丁进行测定。与对照组相比,同时给予安非他酮时,0.25小时和0.5小时时西咪替丁的平均血浆浓度分别约为对照组的2倍和1.5倍。同样,与安非他酮联合给药时,0.25小时和0.5小时时雷尼替丁的平均血浆浓度有显著差异,且分别约为对照组的2倍和3倍。联合给药时西咪替丁和雷尼替丁的最大浓度出现时间缩短至对照组值的近一半。然而,只有西咪替丁的最大浓度出现时间显示出统计学上的显著差异。与各自的对照组相比,西咪替丁和雷尼替丁的曲线下面积、最大浓度和半衰期均未观察到显著差异。结果表明,同时给予安非他酮可能会影响西咪替丁和雷尼替丁的吸收速率,但不会影响其吸收程度。

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