去甲斑蝥酸钠脂质微球的体外与体内评价
[In vitro and in vivo assesemet of sodium norcantharidin lipid microsphere].
作者信息
Wang Li-xin, He Hai-bing, Tang Xing, Shao Rui-ying, Wang Juan, Chen Da-wei
机构信息
School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China.
出版信息
Yao Xue Xue Bao. 2006 Aug;41(8):784-8.
AIM
To prepare lipid microsphere of sodium norcantharidin (NCTD) and then study their characters and pharmacokinetic behavior.
METHODS
Dynamic Light Scattering, HPLC and retrodialysis technique were used to determine the in vitro characters of the NCTD loaded lipid microsphere (LM), such as the particle size, xi-potential, content, incorporation ratio, release profile and changes after dilute. And the plasma concentration was determined by HPLC-MS, compared with NCTD aqueous solution at the same time.
RESULTS
Every property showed that the LM was preferable. The average diameter was about 200 nm. The xi-potential was - 38 mV. The content was close to 100%. And the incorporation ratio exceeded 80%. After i. v. administration of single dose, the pharmacodynamic parameter of LM AUC was 111.28 microg x mL(-1) x h(-1). The data of plasma concentrations showed that the NCTD LM was of two compartment. There was no obvious difference between in vivo parameters of LM and reference solution.
CONCLUSION
The NCTD LM was eligible and the character of it in vivo was not changed.
目的
制备去甲斑蝥素（NCTD）脂质微球，研究其性质及药代动力学行为。
方法
采用动态光散射、高效液相色谱和反透析技术测定载药脂质微球（LM）的体外性质，如粒径、ζ电位、含量、包封率、释放曲线及稀释后的变化。同时用高效液相色谱 - 质谱法测定血浆浓度，并与NCTD水溶液进行比较。
结果
各项性质表明LM性能良好。平均直径约为200 nm，ζ电位为 - 38 mV，含量接近100%，包封率超过80%。单剂量静脉给药后，LM的药代动力学参数AUC为111.28 μg·mL⁻¹·h⁻¹。血浆浓度数据表明NCTD脂质微球呈二室模型。LM与参比溶液的体内参数无明显差异。
结论
NCTD脂质微球合格，其体内性质未改变。
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