地高辛和主要的药物在健康人体内代谢物/衍生品。
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Hinderling PH值,哈特曼D
地高辛和主要的药物在健康人体内代谢物/衍生品。
其他药物Monit。1991年9月,13 (5):381 - 401。
- PubMed ID
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1957331 (在PubMed]
- 文摘
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三个健康的年轻男性志愿者接受剂量的0.6和1.2毫克的特别标记[3 h]地高辛每个通过静脉注射(注射)丸和口服(订单)政府依照随机四通交叉设计。血浆、尿液和粪便样本接管144 h后药物管理局的间隔。总辐射和个人放射性可转让的地高辛及其代谢物的测定。静脉输液管理后,意味着总辐射的+ / - SD复苏,作为剂量的百分比,是完整的,尿液和粪便81.3 + / - 2.0% 17.1 + / - 2.8%。地高辛的平均恢复及其代谢物在尿地高辛75.6 + / - 3.0%,dihydrodigoxin 2.8 + / - 1.6%, digoxigenin bisdigitoxoside 1.6 + / - 0.1%,和其他代谢物1.5 + / - 0.3%。从尿液中代谢物的数据,考虑到5%的杂质接种剂量,新陈代谢的地高辛输液管理后似乎是无关紧要的。地高辛的总和肾之间的空隙,平均193 + / - 25毫升最低为1和152 + / - 24 ml最低为1。平均稳态分布的体积是489 + / - 73 L和平均停留时间41 + / - 5 h。代谢物dihydrodigoxin和digoxigenin bisdigitoxoside平均停留时间平均35 + / - 9 h和53 + / - 11 h;肾许可79 + / - 13毫升最低为1和100 + / - 26毫升最低为1。范围管理后,平均总辐射的复苏,随着剂量的百分比,也完整,尿液和粪便65.7 + / - 1.98% 31.6 + / - 7.6%。 The mean recovery of digoxin and that of its metabolites, as percent of dose, in urine was digoxin 51.5 +/- 11.4%, dihydrodigoxin 4.5 +/- 3.9%, digoxigenin bisdigitoxoside 1.9 +/- 0.1%, polar metabolites 5.5 +/- 3.8%, and additional metabolites 1.3 +/- 0.6%. After p.o., as compared to i.v. administration, larger amounts of all the metabolites were formed in accordance with first pass metabolism/degradation. Maximum mean plasma concentrations of 4.3 +/- 2.5 ng ml-1 and 9.5 +/- 1.1 ng ml-1 for digoxin were observed at 40 +/- 10 min after p.o. administration of 0.6 and 1.2 mg of the drug. The mean absolute bioavailability of digoxin from an aqueous solution was 0.67 +/- 0.14. Renal clearance and mean oral residence time for digoxin were on average 176 +/- 28 ml min-1 and 37 +/- 4 h after p.o. administration.(ABSTRACT TRUNCATED AT 400 WORDS)
