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含有蟾酥的药物九信的代谢与处置

Metabolism and disposition of kyushin, a drug containing senso (ch'an su).

作者信息

Shimizu Y, Morishita S

机构信息

Research Laboratories Kyushin Pharmaceutical Co., Ltd., Tokyo, Japan.

出版信息

Am J Chin Med. 1996;24(3-4):289-303. doi: 10.1142/S0192415X96000359.

DOI:10.1142/S0192415X96000359
PMID:8982441
Abstract

The method of enzyme immunoassay (EIA) was developed for measurement of anti-resibufogenin IgG reactive substance (RRS) in plasma and urine of healthy volunteers receiving a Senso containing drug, Kyushin (KY). Unchanged bufalin (BF), cinobufagin (CB), and resibufogenin (RB) and their metabolites in plasma and urine were also measured by EIA after the separation of these compounds by high performance liquid chromatography. In a single dosing study, the concentration of BF, CB and RB in plasma reached maximum at 1-2 hr after drug administration, and the half-lives (T1/2 of these were 15.8, 8.94 and 11.5 hr, respectively. In a multiple dosing study, the concentration of BF, CB and RB measured fitted on the estimated curve calculated from data of the single dosing study. These results suggest that BF, CB and RB, important components of Senso, do not have a cumulative nature.

摘要

酶免疫分析法(EIA)用于测定服用含蟾酥制剂的健康志愿者(服用久心(KY))血浆和尿液中的抗脂蟾毒配基IgG反应性物质(RRS)。在通过高效液相色谱法分离血浆和尿液中的未变化蟾毒灵(BF)、华蟾酥毒基(CB)、脂蟾毒配基(RB)及其代谢物后,也用EIA进行了测定。在单剂量研究中,血浆中BF、CB和RB的浓度在给药后1 - 2小时达到最大值,其半衰期(T1/2)分别为15.8、8.94和11.5小时。在多剂量研究中,所测BF、CB和RB的浓度符合根据单剂量研究数据计算出的估计曲线。这些结果表明,蟾酥的重要成分BF、CB和RB不具有蓄积性。

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