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通过鼻胃管给药的埃索美拉唑的生物利用度与口服给药相似。

Esomeprazole administered through a nasogastric tube provides bioavailability similar to oral dosing.

作者信息

Sostek M B, Chen Y, Skammer W, Winter H, Zhao J, Andersson T

机构信息

Clinical Research, Biostatistics and Experimental Medicine, AstraZeneca LP, Wilmington, DE 19850-5437, USA.

出版信息

Aliment Pharmacol Ther. 2003 Sep 15;18(6):581-6. doi: 10.1046/j.1365-2036.2003.01667.x.

DOI:10.1046/j.1365-2036.2003.01667.x
PMID:12969084
Abstract

AIM

To determine if nasogastric tube administration of the enteric-coated pellets from an opened esomeprazole capsule provides bioavailability similar to oral dosing with the intact capsule.

METHODS

A randomized, single-centre, open-label, two-period crossover pharmacokinetic study consisting of two 5-day dosing periods separated by a 7- to 14-day washout period was conducted. Healthy subjects between the ages of 18 and 50 years received esomeprazole 40 mg once daily either orally as an intact capsule, or as a suspension of the enteric-coated pellets from an opened capsule in water through a nasogastric tube.

RESULTS

In 47 evaluable subjects, the 90% confidence intervals were 0.87-1.08 and 0.93-1.25 for the geometric mean of the ratio of nasogastric tube administration relative to administration of the intact capsule for the area under the plasma concentration-time curve and for maximum plasma concentration, respectively, on day 1, demonstrating bioequivalence. Oral and nasogastric administration also demonstrated similar bioavailabilities on day 5. Esomeprazole was well tolerated regardless of the mode of administration.

CONCLUSIONS

Nasogastric tube administration of the enteric-coated pellets from an opened esomeprazole 40 mg capsule provides bioavailability similar to oral dosing. Administration of the contents of an opened esomeprazole 40 mg capsule in water through a nasogastric tube is a practical alternative for patients with feeding tubes who require effective gastric acid suppression, but cannot swallow an oral preparation.

摘要

目的

确定经鼻胃管给予打开的埃索美拉唑胶囊中的肠溶微丸是否能提供与完整胶囊口服给药相似的生物利用度。

方法

进行了一项随机、单中心、开放标签、两阶段交叉药代动力学研究,包括两个5天给药期,中间间隔7至14天的洗脱期。18至50岁的健康受试者每天口服一次40毫克埃索美拉唑,剂型为完整胶囊,或通过鼻胃管给予打开胶囊中的肠溶微丸在水中的混悬液。

结果

在47名可评估受试者中,第1天血浆浓度-时间曲线下面积和最大血浆浓度的鼻胃管给药相对于完整胶囊给药的几何平均比值的90%置信区间分别为0.87-1.08和0.93-1.25,表明生物等效性。第5天口服和鼻胃管给药也显示出相似的生物利用度。无论给药方式如何,埃索美拉唑耐受性良好。

结论

经鼻胃管给予打开的40毫克埃索美拉唑胶囊中的肠溶微丸可提供与口服给药相似的生物利用度。对于需要有效抑制胃酸但无法吞咽口服制剂的鼻饲管患者,通过鼻胃管将打开的40毫克埃索美拉唑胶囊内容物溶于水中给药是一种切实可行的替代方法。

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