氯雷他定血药浓度的HPLC荧光检测法及生物等效性研究(英文)

Determination of loratadine in human plasma by HPLC with fluorescence detector and study on its bioavailability

目的 建立高效液相色谱法荧光检测血浆中氯雷他定 (loratadine)含量的方法 ,以评价氯雷他定的相对生物利用度。方法 色谱柱为AlltechC18,4 6mm× 150mm ;流动相为乙腈 水 冰醋酸 三乙胺 (90∶10 0∶6∶0 15) ;流速为 1mL·min- 1;荧光检测器测定波长 ,Ex=2 74nm ,Em=450nm。结果 HPLC测定线性范围为 0 2～ 3 0 μg·L- 1,最低定量限 0 2 μg·L- 1,方法回收率为 96%～ 98%。人体生物利用度结果表明 ,实验片、胶囊与对照片间的AUC ,Tmax,Cmax和T1 2 β均无显著性差异 (P >0 0 5) ,两者的相对生物利用度分别为 10 7%± 17%和 10 0 %± 14 %。AUC和Cmax经可信区间法检验生物等效。结论

Aim To establish an HPLC-fluorescence method for determination of loratadine in hum an plasma and evaluate its relative bioavailability. Methods An Alltech-C 18 column and a mobile phase of acetonitrile-water-glacial acetic acid-triethylamine (90∶100∶6∶0 15) were used. The fluorescence detec tor was set at E x 274 nm, E m 450 nm. The flow rate was 1 mL·min -1 . Results The calibration curve was linear over a concentration range of 0 2-30 μg·L -1 . The limit of quantification was 0 2 μg·L -1 . The average method recoveries varied from 96% to 98%. The results showed AUC, T max , C max and T 1/2 β between the testing tablets, testing capsules a nd reference tablets had no significant difference (P>0 05). Relative bioav ailabilities were 107%±17% and 100%±14% respectively. Conclusion The three formulations were bioequivalent.