DETERMINATION OF FIRST PASS INTESTINAL METABOLISM OF MIDAZOLAM IN HUMAN SUBJECTS
DETERMINATION OF FIRST PASS INTESTINAL METABOLISM OF MIDAZOLAM IN HUMAN SUBJECTS
批准号:
6115617
负责人:
ALASTAIR J. J. WOOD
金额:
$3.64万
依托单位:
依托单位国家:
美国
项目类别:
财政年份:
1998
资助国家:
美国
项目状态:
已结题
起止时间:
1998-12-01 至 1999-11-30
中文摘要
为了估计肠道对首过代谢的贡献,
口服咪唑安定。假设咪达唑仑是
由肠细胞色素P450 3A(P450 3A)酶代谢为
临床显著量。
为了测量P450 3A抑制的效果,通过口服给予
酮康唑对口服给药的药代动力学参数和
静脉注射咪达唑仑假设是口服
酮康唑对口服剂量分布的影响大于
静脉注射咪唑安定初步分析显示,
咪达唑仑代谢的差异。继续分析将
确定其重要性到什么程度。
英文摘要
To estimate the intestinal contribution to the first pass metabolism of
orally administered midazolam. The hypothesis is that midazolam is
metabolized by intestinal cytochrome P450 3 A (P450 3A) enzymes to a
clinical significant amount.
To measure the effect of P450 3A inhibition by orally administered
ketoconazole on the pharmacokinetic parameters of orally and
intravenously administered midazolam. The hypothesis is that oral
ketoconazole affects the disposition of the oral dose more than that of
the intravenous midazolam. Preliminary analysis has shown some racial
differences in the metabolism of midazolam. Continued analysis will
determine to what extent the significance.
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