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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。
Objective: To investigate the pharmacokinetics and tissue distribution of gossypol nanosuspensions in mice. Methods: The content of gossypol in the biological samples was determined by HPLC. The mobile phase was methanol-0.4% phosphoric acid water (85:15). The detection wavelength was 238 nm. Comparison of the pharmacokinetic parameters and tissue distribution characteristics between gossypol nanosuspension and gossypol solution after tail vein administration. Results: The area of blood concentration and time curve, the residence time in the drug, the apparent volume of distribution, the elimination rate and the maximum plasma concentration of the gossypol nanomixture were (18 792.56±2 304.43) μg·L -1 ·h -1, respectively. , (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. The relative uptake rates of gossypol nanosuspensions in the liver, heart, spleen, lung, and kidney were 1.44, 3.21, 12.19, 1.88, and 6.54, respectively. Conclusion: Gossypol nanosuspension can significantly increase the concentration of drugs in various tissues, prolong the residence time of drugs in vivo, increase the bioavailability of drugs, and extend the circulation time of drugs in animals to some extent. . Nanosuspensions are likely to become a novel drug delivery system for gossypol.