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新藤黄酸固体脂质纳米粒在大鼠体内药物代谢动力学研究
作者姓名:黄霞  罗晴  朱婷婷  周恺  贾步云  程皓  季兆洁  林彤远  陈卫东
作者单位:安徽中医药大学药学院,安徽,合肥,230031;安徽中医药大学药学院,安徽,合肥,230031;安徽中医药大学药学院,安徽,合肥,230031;安徽中医药大学药学院,安徽,合肥,230031;安徽中医药大学药学院,安徽,合肥,230031;安徽中医药大学药学院,安徽,合肥,230031;安徽中医药大学药学院,安徽,合肥,230031;安徽中医药大学药学院,安徽,合肥,230031;安徽中医药大学药学院,安徽,合肥,230031
摘    要:目的 考察新藤黄酸固体脂质纳米粒(gambogenic acid-solid lipid nanoparticles,GNA-SLN)在大鼠体内的药物代谢动力学特征。方法 对大鼠分别腹腔注射GNA和GNA-SLN,采用高效液相色谱法测定GNA在大鼠体内的血药浓度,DAS 2.1软件拟合计算药物代谢动力学参数。结果 腹腔注射含等量GNA的GNA溶液和GNA-SLN后,GNA-SLN组的峰浓度是GNA溶液组的3.06倍,药时曲线下面积约为GNA溶液组的3倍,体内滞留时间约为GNA溶液组的2倍。GNA-SLN显著增加了GNA的体内吸收,且延长了GNA在体内的作用时间(P<0.05,或P<0.01)。结论 SLN包载可改变GNA的体内行为,提高其血药浓度,延长其体内循环时间,有望改善其治疗效果。

关 键 词:新藤黄酸  固体脂质纳米粒  药物代谢动力学

In Vivo Pharmacokinetics of Gambogenic Acid-Solid Lipid Nanoparticles in Rats
Institution:School of Pharmacy, Anhui University of Chinese Medicine, Anhui Hefei 230031, China
Abstract:Objective Toinvestigate the in vivo pharmacokinetic characteristics of gambogenic acid-solid lipid nanoparticles (GNA-SLNs) in rats. Methods Rats were divided into GNA group and GNA-SLN group. Both groups were intraperitoneally injected with the same amount of GNA in the form of GNA solution or GNA-SLN suspension. The concentration of GNA in plasma was measured by high-performance liquid chromatography, and the pharmacokinetic parameters were calculated by data fitting using DAS 2.1 software. Results The plasma drug concentration-time curve of GNA-SLN group showed two peaks after administration. The peak concentration, area under the curve (AUC), and mean retention time of the GNA-SLN group were approximately 3.06, 3, and 2 times, respectively, those of the GNA group. GNA-SLN significantly increased the internal absorbtion of GNA and extended its action time. Conclusion Compared with GNA, GNA-SLN has different pharmacokinetic characteristics, with increased plasma concentration and prolonged circulation time. GNA-SLN is expected to have an improved therapeutic effect.
Keywords:gambogenic acid  solid lipid nanoparticle  pharmacokinetics
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