活性炭延迟给药对常规释放型和缓释型维拉帕米吸收的影响。

Effect of delayed administration of activated charcoal on the absorption of conventional and slow-release verapamil.

作者信息

Laine K, Kivistö K T, Neuvonen P J

机构信息

University of Turku, Finland.

出版信息

J Toxicol Clin Toxicol. 1997;35(3):263-8. doi: 10.3109/15563659709001210.

DOI:10.3109/15563659709001210

PMID:9140320

Abstract

OBJECTIVE

To investigate the effect of simultaneous and delayed administration of activated charcoal on the absorption of two verapamil formulations.

METHODS

In the first study, 9 healthy volunteers received the following treatments: 1) verapamil 80 mg (conventional formulation) with 50 mL water only, 2) verapamil 80 mg and 25 g activated charcoal immediately afterwards, and 3) verapamil 80 mg with 50 mL water, followed by 25 g charcoal 2 h after verapamil ingestion. In the second study, 8 healthy volunteers received the following treatments: 1) verapamil 240 mg (slow-release formulation) with 50 mL water only, 2) verapamil slow-release 240 mg and 25 g activated charcoal immediately afterwards, 3) verapamil slow-release 240 mg with 50 mL water, followed by 25 g charcoal 2 h after verapamil ingestion, and 4) verapamil slow-release 240 mg with 50 mL water, followed by 25 g charcoal 4 h later. Plasma verapamil concentrations over 24 h were measured by high performance liquid chromatography.

RESULTS

Activated charcoal given immediately after the conventional formulation of verapamil reduced the AUC0-24 h by 99% (p < 0.0005) and the Cmax by 98% (p < 0.0005). When the administration of charcoal was delayed 2 h, no significant change in verapamil absorption was observed. With the slow-release formulation of verapamil, charcoal given immediately after verapamil ingestion reduced the verapamil AUC0-24 h by 86% (p = 0.001) and the Cmax by 82% (p = 0.002). When the administration of charcoal was delayed 2 or 4 h, the AUC0-24 h was reduced by 35% (p = 0.04) and 32% (p = 0.001), respectively, but the Cmax was decreased by 13% (p = NS) and 9% (p = NS) only.

CONCLUSIONS

Activated charcoal was effective in preventing absorption of verapamil when it was administered immediately after verapamil ingestion. In the case of slow-release formulation, charcoal reduced verapamil absorption by over 30% even when given 4 h after verapamil.

摘要

目的

研究同时给予和延迟给予活性炭对两种维拉帕米制剂吸收的影响。

方法

在第一项研究中，9名健康志愿者接受了以下治疗：1）仅用50毫升水服用80毫克维拉帕米（常规制剂）；2）服用80毫克维拉帕米后立即服用25克活性炭；3）用50毫升水服用80毫克维拉帕米，在摄入维拉帕米2小时后服用25克活性炭。在第二项研究中，8名健康志愿者接受了以下治疗：1）仅用50毫升水服用240毫克维拉帕米（缓释制剂）；2）服用240毫克维拉帕米缓释剂后立即服用25克活性炭；3）用50毫升水服用240毫克维拉帕米缓释剂，在摄入维拉帕米2小时后服用25克活性炭；4）用50毫升水服用240毫克维拉帕米缓释剂，4小时后服用25克活性炭。采用高效液相色谱法测定24小时内血浆维拉帕米浓度。

结果

维拉帕米常规制剂服用后立即给予活性炭，使AUC0 - 24小时降低99%（p < 0.0005），Cmax降低98%（p < 0.0005）。当活性炭给药延迟2小时时，维拉帕米吸收未观察到显著变化。对于维拉帕米缓释制剂，维拉帕米摄入后立即给予活性炭，使维拉帕米AUC0 - 24小时降低86%（p = 0.001），Cmax降低82%（p = 0.002）。当活性炭给药延迟2小时或4小时时，AUC0 - 24小时分别降低35%（p = 0.04）和32%（p = 0.001），但Cmax仅降低13%（p = 无显著性差异）和9%（p = 无显著性差异）。