In vitro and in vivo assesemet of sodium norcantharidin lipid microsphere / 药学学报

ABSTRACT

<p><b>AIM</b>To prepare lipid microsphere of sodium norcantharidin (NCTD) and then study their characters and pharmacokinetic behavior.</p><p><b>METHODS</b>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.</p><p><b>RESULTS</b>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.</p><p><b>CONCLUSION</b>The NCTD LM was eligible and the character of it in vivo was not changed.</p>