盐酸青藤碱不同晶形在人体的相对生物利用度研究

Study on Relative Bioavailability of Different Sinomenine Hydrochloride Crystal in Healthy Volunteers

目的比较盐酸青藤碱不同晶形在人体的相对生物利用度。方法健康志愿者16名,随机交叉口服给药60mg。采用反相高效液相色谱法测定血药浓度,色谱柱为ODSC18柱(150mm×4.6mm,5μm),流动相为乙腈-0.01mol/L磷酸二氢钾(55∶45),检测波长为263nm。结果盐酸青藤碱纯白色、淡黄色、浅灰色3种纯度晶形的0～12h药时曲线下面积(AUC0→12h)分别为(665.5±118.7),(558.0±101.5),(548.6±98.6)ng·h/mL,相对生物利用度分别为98.5%,82.6%,81.2%。结论纯白盐酸青藤碱为最佳晶形。

Objective To compare the relative bioavailabilities of different sinomenine hydrochloride crystal in healthy volunteers, Methods Sixteen healthy volunteers were given the medicine 60 mg in oral by an open randomized crossover design. The medical concentration of blood was determined by RP-HPLC. An ODS C18（150 mm×4. 6 mm, 5 μm） column with acetonitrile-0.01 mol/L KH2PO4（55：45） as the mobile phase was used, the detective wavelength was 263 nm. Results The AUC（0-12 h） of sinomenine hydrochloride in shape of pure white, light yellow and light grey were （665.5±118.7）, （558.0 ±101.5）, （548.6±98. 6）ng·h/mL respectively,and the relative bioavailabilities were 98.5% ,82.6%, 81.2% respectively. Conclusion The pure white sinomenine hydrochloride is the best crystal.