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叠氮吗啡及相关物质的吸收、分布和消除。

Absorption, distribution and elimination of azidomorphine and related substances.

作者信息

Knoll J, Magyar K, Zólyomi G

出版信息

Acta Physiol Acad Sci Hung. 1975;46(2):163-72.

PMID:1235233
Abstract

The absorption, distribution and elimination of 14C- and 3H-azidomorphine, 3H-14-OH-azidomorphine, 14C- and 3H-azidocodeine and 3H-azidoethylmorphine were studied in comparison to 14-C-morphine. Whole body autoradiography of pregnant mice, quantitative estimations of tissue radioactivity in male mice, brain autoradiography, subcellular distribution in rat brain and elimination studies in rats were performed. Azidomorphine and morphine are absorbed from the gastrointestinal tract at the same rate but the absorption of 14-OH-azidomorphine, azidocodeine and azidoethylmorphine exceeds that of the formers. The azidomorphines pass across the blood-brain barrier more readily than does morphine. In rats treated with azidomorphines, 30--50% of the doses given were excreted with the urine the first 4 hours and about 90% within 48 hours; whereas 2--5% were recovered from the collected stools.

摘要

与14C-吗啡相比,研究了14C-和3H-叠氮吗啡、3H-14-羟基-叠氮吗啡、14C-和3H-叠氮可待因以及3H-叠氮乙基吗啡的吸收、分布和消除情况。对怀孕小鼠进行了全身放射自显影,对雄性小鼠的组织放射性进行了定量估计,进行了脑放射自显影、大鼠脑亚细胞分布以及大鼠消除研究。叠氮吗啡和吗啡从胃肠道的吸收速率相同,但14-羟基-叠氮吗啡、叠氮可待因和叠氮乙基吗啡的吸收超过前者。叠氮吗啡比吗啡更容易穿过血脑屏障。在用叠氮吗啡治疗的大鼠中,给药剂量的30%-50%在最初4小时随尿液排出,48小时内约90%排出;而从收集的粪便中回收2%-5%。

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