Pharmacokinetics and Tissue Distribution of Gossypol Nanosuspensions in Mice

WANG Jian-cheng; TANG Hui; YANG Si-tao; YING Xue; LIU Yi-juan

doi:10.13422/j.cnki.syfjx.2015100083

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Pharmacokinetics and Tissue Distribution of Gossypol Nanosuspensions in Mice

更新时间：2024-01-04

- Pharmacokinetics and Tissue Distribution of Gossypol Nanosuspensions in Mice
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 21, Issue 10, Pages: 83-86(2015)
- 作者机构：
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.2015100083
  CLC： R285.5
- Published：2015
- 稿件说明：
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WANG Jian-cheng, TANG Hui, YANG Si-tao, et al. Pharmacokinetics and Tissue Distribution of Gossypol Nanosuspensions in Mice[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(10): 83-86.
DOI：

WANG Jian-cheng, TANG Hui, YANG Si-tao, et al. Pharmacokinetics and Tissue Distribution of Gossypol Nanosuspensions in Mice[J]. Chinese journal of experimental traditional medical formulae, 2015, 21(10): 83-86. DOI： 10.13422/j.cnki.syfjx.2015100083.

摘要

目的: 考察棉酚纳米混悬剂在小鼠体内的药代动力学及组织分布特性. 方法: 采用HPLC测定生物样品中棉酚的含量

流动相甲醇-0.4%磷酸水(85:15)

检测波长238 nm.比较棉酚纳米混悬剂和棉酚溶液经尾静脉给药后体内药代动力学参数与组织分布特点的差异. 结果: 棉酚纳米混剂的血药浓度时间曲线面积、药物体内滞留时间、表观分布容积、消除速率和最大血药浓度分别为(18 792.56±2 304.43) μg ·L-1 ·h-1

(21.82±1.60) h

(0.75±0.16) L ·kg-1

(1.37±0.37) L ·kg-1 ·h-1

(17 589.81±3 034.14) μg ·L-1.棉酚纳米混悬剂在肝、心、脾、肺及肾中的相对摄取率分别为1.44

3.21

12.19

1.88

6.54. 结论: 棉酚纳米混悬剂能显著提高药物在各组织中的浓度水平

且延长了药物在体内组织的滞留时间

提高药物生物利用度

并在一定程度上延长药物在动物体内的循环时间.纳米混悬剂很有可能成为棉酚的一种新型药物传递系统.

Abstract

Objective: To investigate pharmacokinetics and tissue distribution of gossypol nanosuspensions(GP-NS) in mice. Method: HPLC was established to determine the concentration of gossypol in serum and different tissues of mice.After tail administration of GP-NS and gossypol solution

their pharmacokinetics and tissue distribution differences were compared. Result: After administration of GP-NS

area under plasma concentration time curve (AUC0-∞) was (18 792.56±2 304.43) μg · L-1 · h-1

in vivo residence time (MRT0-∞) was (21.82±1.60)h

apparent volume of distribution (V) was (0.75±0.16) L · kg-1

clearance(CL) was (1.37±0.37) L · kg-1 · h-1and maximum plasma concentration (Cmax) was (17 589.81±3 034.14) μg · L-1.Values of relative uptake rate (Re)in the liver

heart

spleen

lung and kidneywere 1.44

3.21

12.19

1.88 and 6.54

respectively. Conclusion: GP-NS can significantly increase the level of gossypol concentration in mice and improve its bioavailability.GP-NS is helpful for gossypol to reach a long circulation time and is hopeful to be its novel drug delivery system.

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