Pharmacokinetics of Hydroxycamptothecin Magentolipsomes in Rats Based on Microdialysis Sampling Technique

ZHU Hai-mei; XIE Yi; XIE Bo; LING Jia-jun

doi:10.13422/j.cnki.syfjx.2017180064

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Pharmacokinetics of Hydroxycamptothecin Magentolipsomes in Rats Based on Microdialysis Sampling Technique

更新时间：2024-01-04

- Pharmacokinetics of Hydroxycamptothecin Magentolipsomes in Rats Based on Microdialysis Sampling Technique
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 23, Issue 18, Pages: 64-70(2017)
- 作者机构：
- 作者简介：
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- DOI：10.13422/j.cnki.syfjx.2017180064
  CLC： R285.5
- Published：2017
- 稿件说明：
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ZHU Hai-mei, XIE Yi, XIE Bo, et al. Pharmacokinetics of Hydroxycamptothecin Magentolipsomes in Rats Based on Microdialysis Sampling Technique[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(18): 64-70.
DOI：

ZHU Hai-mei, XIE Yi, XIE Bo, et al. Pharmacokinetics of Hydroxycamptothecin Magentolipsomes in Rats Based on Microdialysis Sampling Technique[J]. Chinese journal of experimental traditional medical formulae, 2017, 23(18): 64-70. DOI： 10.13422/j.cnki.syfjx.2017180064.

摘要

目的：探究羟基喜树碱（HCPT）磁性脂质体在大鼠体内药代动力学特征，为该药物的制剂开发提供参考。方法：建立微透析样品中开环HCPT（C-HCPT），闭环HCPT（L-HCPT）的HPLC，SD大鼠尾静脉注射HCPT磁性脂质体和HCPT注射液，腹腔注射HCPT注射液（剂量以HCPT计均为10 mg · kg-1），于给药后采用微透析技术定时采样。微透析样品经各样本自身体内回收率校正，利用DAS 2.1.1软件计算相关药物动力学参数。结果： HCPT磁性脂质体尾静脉给药组，HCPT注射液尾静脉给药组和HCPT注射液腹腔给药组的药峰浓度（Cmax）分别为（2.789±0.158），（4.537±0.092），（0.340±0.066） mg · L-1，达峰时间（tmax）分别为（24±0），（6±0.127），（24±0.127） min，平均滞留时间（MRT0-∞）分别为（72.255±4.668），（20.325±4.288），（112.630±29.969） min，药时曲线下面积（AUC0-∞）分别为（216.870±3.271），（150.668±7.306），（34.883±10.245） mg · L-1 · min；与HCPT注射液尾静脉给药组相比，HCPT磁性脂质体尾静脉给药组的t>，MRT0-∞较大，差异有统计学意义；与HCPT注射液腹腔给药组相比，HCPT磁性脂质体尾静脉给药组的Cmax，AUC0-∞较大，差异有统计学意义。结论： HCPT磁性脂质体尾静脉注射能显著提高药物血药浓度、生物利用度及其在体内的滞留时间；且脂质体可保护HCPT活性必需基团内酯环不被破坏，从而保证HCPT的抗肿瘤活性。

Abstract

Objective: To study on the pharmacokinetics of hydroxycamptothecin(HCPT) magentolipsomes in rats.Method: The detection method for open-loop HCPT(C-HCPT) and closed-loop HCPT(L-HCPT) in microdialysis samples were established by HPLC.The microdialysis samples were collected after they were treated with HCPT magentolipsomes(intravenous injection)

HCPT injection(intravenous injection) and HCPT injection(intraperitoneal injection) at a concentration of 10 mg · kg-1 for HCPT.The microdialysis samples were corrected with in vivo recoveries

the pharmacokinetic parameters were calculated by DAS 2.1.1 software.Result: The pharmacokinetic parameters of HCPT magentolipsomes(intravenous injection)

HCPT injection(intravenous injection)and HCPT injection(intraperitoneal injection) were calculated as follows:Cmax of (2.789±0.158)

(4.537±0.092)

(0.340±0.066) mg · L-1

tmax of (24±0)

(6±0.127)

(24±0.127) min

MRT0-∞ of (72.255±4.668)

(20.325±4.288)

(112.630±29.969) min

AUC0-∞ of (216.870±3.271)

(150.668±7.306)

(34.883±10.245) mg · L-1 · min.The tmax and MRT0-∞ of HCPT magentolipsomes(intravenous injection) were significantly longer than those of HCPT injection(intravenous injection);the Cmax and AUC0-∞ of HCPT magentolipsomes(intravenous injection) were significantly higher than those of HCPT injection(intraperitoneal injection).Conclusion: HCPT magentolipsomes(intravenous injection) can evidently raise plasma concentration

bioavailability and its residence time in the body of rats

and it can protect L-HCPT from blood

which is good for the anti-tumor activity.

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