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目的 研究与比较猕猴硬膜外 (ed)及静脉 (iv)注射虎纹毒素 1后的药代动力学过程。方法 Iodogen法标记虎纹毒素 1 ,按 0 388MBq·kg- 1 的剂量向猕猴第 3和第 4腰椎之间硬膜外腔及静脉注射标记后虎纹毒素 1 ,用反相高效液相色谱检测猴血清中的药物放射性活度 ;γ 计数仪检测猴第 3和第 4腰椎硬膜外腔的药物放射性活度。结果 制备了具有生物活性的 [1 2 5I]虎纹毒素 1。硬膜外给药 1 0min后 ,给药部位局部硬膜外腔的药物放射性占总给药量的0 38,说明硬膜外给药是成功的 .硬膜外及静脉给药后 ,血药浓度分别在 30min和 2min达峰 ,分别为 (0 70± 0 0 4 )MBq·L- 1 和 (4 98± 0 58)MBq·L- 1 。两种给药途径的药时曲线不同 :猕猴硬膜外和静脉给药后 ,末端T12 分别为(1 0 36± 0 2 7)h和 (1 1 0 3± 1 1 6)h ;ClS 分别为 (1 2 9±0 0 7)L·h- 1 ·kg- 1 和 (1 2 5± 0 2 3)L·h- 1 ·kg- 1 ,硬膜外给予 [1 2 5I]HWTX 1的绝对生物利用度 (95± 5) %。结论 硬膜外和静脉两种给药方式下 ,[1 2 5I]虎纹毒素 1在猕猴体内的药代动力学过程具有差异性 ,两种给药方式下 [1 2 5I]在猕猴体内的分布与吸收特点对于虎纹毒素 I的临床药效学和毒理学研究提供了参考数据。
Objective To study and compare the pharmacokinetics of tiger toxin 1 after epidural (ed) and intravenous (iv) injection in rhesus monkeys. Methods Iodogen method was used to label tiger toxin 1. The labeled tiger toxin 1 was injected into the epidural space between the third and fourth lumbar vertebrae at the dosage of 388MBq · kg-1. The reverse transcription-phase high performance liquid chromatography The radioactivity of the drug in the serum of the monkey was measured. The radioactivity of the drug in the third and fourth lumbar epidural space of the monkey was detected by gamma counter. As a result, a biologically active [125 I] tiger toxin 1 was prepared. Epidural administration of 10min, the drug delivery site of the local epidural radioactivity accounted for 38% of the total dose, indicating that the epidural delivery is successful. Epidural and intravenous administration, blood drug The concentrations peaked at 30 min and 2 min respectively, and were (0 70 ± 0 0 4) MBq · L -1 and (988 ± 0 58) MBq · L -1, respectively. The drug-delivery curves of the two routes of administration were different: after the epidural and intravenous administration, the terminal T12 were (1 0 36 ± 0 2 7) h and (1 1 0 3 ± 1 1 6) h, respectively; (1 2 9 ± 0 0 7) L · h -1 · kg -1 and (1 2 5 ± 0 2 3) L · h -1 · kg -1, and epidural administration of [125 I] HWTX 1 The absolute bioavailability (95 ± 5)%. Conclusion Both epidural and intravenous modes of administration [1 2 5 I] tiger toxin 1 have different pharmacokinetic processes in rhesus monkeys. In the two modes of administration, [125 I] Distribution and absorption characteristics of tiger toxin I clinical pharmacodynamic and toxicological studies provide reference data.