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静脉注射兰索拉唑的药代动力学和药效学评估。

Evaluation of the pharmacokinetics and pharmacodynamics of intravenous lansoprazole.

作者信息

Freston J W, Pilmer B L, Chiu Y-L, Wang Q, Stolle J C, Griffin J S, Lee C Q

机构信息

University of Connecticut Health Center, 263 Farmington Avenue, Farmington, CT 06030-1111, USA.

出版信息

Aliment Pharmacol Ther. 2004 May 15;19(10):1111-22. doi: 10.1111/j.1365-2036.2004.01942.x.

Abstract

AIM

To compare the pharmacokinetics and pharmacodynamics of lansoprazole 30 mg administered intravenously in 0.9% NaCl or in polyethylene glycol, or orally.

METHODS

Twenty-nine subjects received lansoprazole orally on days 1-7 and intravenous lansoprazole in NaCl on days 8-14. Blood samples were collected on days 1, 7, 8 and 14. Fasting basal acid output and pentagastrin-stimulated maximal acid output were determined on days -1, 8, 9 and 15. Thirty-six different subjects received one of four regimen sequences: intravenous lansoprazole in NaCl, intravenous in polyethylene glycol, per orally, or intravenous placebo, each for 5 days. Twenty-four hour intragastric pH was recorded on days 1 and 5.

RESULTS

Intravenous and per oral lansoprazole for 7 days produced equivalent basal acid output and maximal acid output suppression. Pharmacokinetics and mean pH values with intravenous lansoprazole in NaCl or polyethylene glycol were equivalent. Both produced mean pH and percentages of time pH above 3, 4, 5 and 6 that were significantly greater than did per orally.

CONCLUSIONS

Intravenous lansoprazole inhibits acid secretion as effectively in NaCl as in polyethylene glycol, and its onset of action is faster than per oral lansoprazole.

摘要

目的

比较静脉注射30毫克兰索拉唑于0.9%氯化钠溶液或聚乙二醇中,以及口服给药后的药代动力学和药效学。

方法

29名受试者在第1 - 7天口服兰索拉唑,在第8 - 14天静脉注射于氯化钠溶液中的兰索拉唑。在第1、7、8和14天采集血样。在第-1、8、9和15天测定空腹基础胃酸分泌量和五肽胃泌素刺激的最大胃酸分泌量。36名不同受试者接受四种给药方案序列之一:静脉注射于氯化钠溶液中的兰索拉唑、静脉注射于聚乙二醇中的兰索拉唑、口服给药或静脉注射安慰剂,每种给药5天。在第1和5天记录24小时胃内pH值。

结果

静脉注射和口服兰索拉唑7天对基础胃酸分泌量和最大胃酸分泌量的抑制效果相当。静脉注射于氯化钠溶液或聚乙二醇中的兰索拉唑的药代动力学和平均pH值相当。两者产生的平均pH值以及pH值高于3、4、5和6的时间百分比均显著高于口服给药。

结论

静脉注射兰索拉唑在氯化钠溶液中抑制胃酸分泌的效果与在聚乙二醇中相当,且其起效速度比口服兰索拉唑更快。

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