原人参二醇脂质立方液晶纳米粒在大鼠体内的药动学研究  

Study on pharmacokinetics of 20(S)-protopanaxadiol lipid cubic nanoparticles

作　　者：金鑫[1] 张振海[1] 孙娥[1] 刘其媛[1] 贾晓斌[1] 

机构地区：[1]南京中医药大学附属中西医结合医院,江苏南京210028

出　　处：《中国中药杂志》2013年第2期263-268,共6页China Journal of Chinese Materia Medica

基　　金：国家中医药管理局重点研究室开放基金项目(2011NDDCM01001)

摘　　要：目的:本研究旨在建立高效液相色谱-串联质谱测定大鼠血浆中原人参二醇的方法,分析原人参二醇脂质立方液晶纳米粒、原人参二醇原料药的药代动力学特征。方法:SD大鼠分别灌胃给予原人参二醇(PPD)、原人参二醇脂质立方液晶纳米粒后,定时眼眶取血,0.05%甲酸甲醇-0.05%甲酸水(95∶5)为流动相。采用电喷雾离子化四极杆串联质谱,以全扫描检测(SCAN)方式进行检测,用于定量分析的二级碎片离子分别为m/z 460.4/425.3(PPD)和m/z 622.9/587.4(Rh2,内标),检测血浆中的原人参二醇含量,绘制药时曲线,DAS程序计算药动学参数。结果:PPD血浆浓度测定方法的线性范围为10～1 407μg·L-1,定量限为2.5μg·L-1。日内、日间精密度(RSD)均小于13%,准确度(RE)在±8.5%之内。结论:该方法专属性强,灵敏度高,血浆用量少,适用于药代动力学研究。制备成原人参二醇脂质立方液晶纳米粒可以促进原人参二醇在体内的吸收,其相对生物利用度为原料药的166%。Objective： To establish a high-performance liquid chromatographic/tandem mass spectrometry （HPLC-MS/MS） method for determining 20（S）-protopanaxadiol （PPD） in rat plasma, in order to analyze pharmacokinetic characteristics of PPD and PPD cubic nanoparticles. Method： Sprague-Dawley rats were administered orally with PPD and PPD cubic nanoparticles, respectively. Their blood samples were obtained from fossa orbitalis at regular time points. The mobile phase was 0. 05% formic acidac etonitrile- 0. 05% formic acidac water （95：5）. Electrospray ionization （ESI） was adopted for the quadrupole tandem mass spectrum. SCAN mode was used for the quantitative analysis, with m/z 460. 4/425.3 and m/z 622. 9/318.3 （ Rh2, interior label） as secondary frag- ment ions. The concentration of PPD in plasma was analyzed. The concentration-time curve was mapped. The data were calculated by DAS program. Result： The linearity of the PPD plasma concentration determination method ranged between 10-1 407μg·L^-1, with the limit of quantification of 2. 5μg·L^-1. Both of the inter-day and intra-day precisions （RSD） were less than 13.25% , and the ac- curacy （relative error） was between ± 8.50%0. Conclusion： The method was so highly specific and sensitive with less plasma that it is suitable for pharmacokinetic studies. The prepared 20（S）-protopanaxadiol lipid cubic nanoparticles can enhance its absorption in vivo. Its relative bioavailability is 166% of the raw material.

关 键 词：原人参二醇 立方液晶 生物利用度 高效液相色谱-串联质谱法 

分 类 号：R96[医药卫生—药理学]