徐佩佩, 任中鲁, 李詠雪, 陆明廉, 李端, 徐红, 赵明霞. 高压液相法测定家兔用吡喹酮后的血药浓度及药代动力学参数J. 药学学报, 1983, 18(6): 401-405.
引用本文: 徐佩佩, 任中鲁, 李詠雪, 陆明廉, 李端, 徐红, 赵明霞. 高压液相法测定家兔用吡喹酮后的血药浓度及药代动力学参数J. 药学学报, 1983, 18(6): 401-405.
XU Pei-pei, REN Zhong-lu, LI Yong-xue, LU Ming-lian, LI Duan, XU Hong , ZHAO Ming-xia, . DETERMINATION OF PRAZIQUANTEL IN RABBIT PLASMA AND IT'S PHARMACOKINETIC PARAMETERS BY HIGH PERFORMANCE LIQUID CHROMATOGRAPHIC METHOD (HPLC)J. Acta Pharmaceutica Sinica, 1983, 18(6): 401-405.
Citation: XU Pei-pei, REN Zhong-lu, LI Yong-xue, LU Ming-lian, LI Duan, XU Hong , ZHAO Ming-xia, . DETERMINATION OF PRAZIQUANTEL IN RABBIT PLASMA AND IT'S PHARMACOKINETIC PARAMETERS BY HIGH PERFORMANCE LIQUID CHROMATOGRAPHIC METHOD (HPLC)J. Acta Pharmaceutica Sinica, 1983, 18(6): 401-405.

高压液相法测定家兔用吡喹酮后的血药浓度及药代动力学参数

DETERMINATION OF PRAZIQUANTEL IN RABBIT PLASMA AND IT'S PHARMACOKINETIC PARAMETERS BY HIGH PERFORMANCE LIQUID CHROMATOGRAPHIC METHOD (HPLC)

  • 摘要: 本文报道用高压液相法测定家兔用吡喹酮后的血药浓度及药代动力学参数。方法条件:青岛硅胶(5~10μm)柱作吸附层析;正丁醇—氯仿—乙酸乙酯—10%氨水(20:20:60:3)作流动相。荧光检测:λex260nm,λem285nm。检测限为20ng吡喹酮,线性范围为0.1~0.9μg/ml血浆。家兔静注吡喹酮后Kα=3.00h-1,t1/2(α)=0.23h,Kel=0.28h-1,t1/2(β)=2.48h。家兔口服吡喹酮片剂及胶囊后,胶囊的相对生物利用度为片剂的74.8%。

     

    Abstract: In recent years, praziquantel has been known to be a new and effective widespectrum antiparasitic. It is particularly effective in the treatmant of Schistosomiasis japanica infection.The high performance liquid chfomatographic method (HPLC) introduced in this paper for the determination of plasma concentration of praziquantel so far has not yet been reported. The specificity of the method was high and the limit of detection was found to be 20 ng,The metabolite distinctly appeared five minutes after intravenous injection to rabbits and was separated chromatographically. The mean value (n=7) of Kα=3.00 h-1,t1/2(α) = 0. 23 h, kel,=0.28h-1, t1/2(β)=2.48 h. This indicates that the drug was metabolized quickly.Following oral administration of tablets or capsules of praziquantel to rabbits (n=13), the time reaching maximum plasma concentration (tm)was found to be about one hour. The relative bioavailability of capsules was 74.8% that of tablets (0.011/2(β) of the tablets was longer than that of capsules, so the tablet of praziquantel used in clinics may be considered reasonable at present.

     

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