中国药理学通报2003，Vol.19Issue(8)：944-949,6.
猕猴硬膜外及静脉注射[125I]虎纹毒素-1的药代动力学
Pharmacokinetics of [125I]Huwentoxin-1 after epidural and intravenous administration to rhesus monkeys
摘要
Abstract
AIM To study and compare pharmacokinetics (PK) after epidural or intravenous (iv) administration of [125I]labeled Huwentoxin-1 ([125I]HWTX-1) in rhesus monkeys. METHODS Huwentoxin-1 was labeled by iodogen method and was administered at a dose of 0.388 MBq*kg-1 by lumbar puncture at the third lumbar (L3) and the forth lumbar (L4) interspaces using a 12-gauge paracentetic needle into epidural space of rhesus monkeys or iv at the same dose. Reverse Phase High Performance Liquid Chromatography (RP-HPLC) determined serum [125I]Huwentoxin-1 with an automatic gamma counter. RESULTS The puriation of [125I]Huwentoxin-1>96% and with the same bio-activity as unlabeled Huwentoxin-1; Radioactivity detected in epidural space was 38% of injected radioactivity at 10 min after epidural injection, which demonstrated successful administration into epidural space; The maximum serum concentration after epidural or iv administration of [125I]labeled Huwentoxin-1 were determined to be (0.70±0.04) MBq*L-1 and (4.98±0.58) MBq*L-1, respectively, at the maximum serum concentration times of 30 min and 2 min. Terminal T1/2 after epidural or iv administration were (10.36±0.27) h or (11.03±1.16) h, respectively. Cls was (1.29±0.07) L*h-1*kg-1 or (1.25±0.23) L*h-1*kg-1, respectively. Bioavailability after epidural administration was(95±5)%. CONCLUSION Concentration-time curves of [125I] labeled Huwentoxin-1 after two routes were different. The degradation profiles after epidural and iv injection supported the using of HWTX-1 as analgesic by epidural administration.关键词
虎纹毒素-1/药代动力学/硬膜外注射Key words
huwentoxin-1/pharmacokinetics/epidural administration分类
医药卫生引用本文复制引用
廖智,戴舒佳,刘秀文,汤仲明,梁宋平..猕猴硬膜外及静脉注射[125I]虎纹毒素-1的药代动力学[J].中国药理学通报,2003,19(8):944-949,6.基金项目
国家自然科学基金重点资助项目,No 39930180 （）
