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目的:考察并评价辣椒碱亚微乳注射剂在家兔体内的药动学行为。方法:采用HPLC测定家兔血浆中辣椒碱血药浓度,流动相甲醇-水-磷酸(68∶32∶0.1),检测波长281 nm。通过DASTMver1.0药动学智能软件分析家兔耳缘静脉注射辣椒碱亚微乳及其水溶液的房室模型,计算药动学参数。结果:辣椒碱血药浓度在0.500~100 mg·L-1呈良好线性关系(r=0.999 7),萃取回收率96.10%~105.48%。家兔耳缘静脉注射辣椒碱亚微乳及其水溶液的药动学曲线均符合二室模型,消除半衰期分别为(48.501 3±4.011 9),(15.262 5±1.888 2)min,药时曲线下面积分别为(924.09±149.80),(555.36±57.46)mg·min·L-1。结论:建立的HPLC准确、灵敏,适用于辣椒碱血药浓度的测定。与辣椒碱水溶液相比,辣椒碱亚微乳能延长药物的体内半衰期,提高生物利用度。
Objective: To investigate and evaluate the pharmacokinetics of capsaicin submicron emulsion injection in rabbits. Methods: The plasma concentration of capsaicin in rabbit plasma was determined by HPLC. The mobile phase consisted of methanol - water - phosphoric acid (68:32:0.1) and the detection wavelength was 281 nm. Pharmacokinetic parameters were calculated by intravenous injection of capsaicin submicroemulsion and its aqueous solution in rabbits’ ears with DASTMver 1.0 pharmacokinetic software. Results: The concentration of capsaicin in 0.500 ~ 100 mg · L-1 showed a good linear relationship (r = 0.999 7), extraction recovery 96.10% ~ 105.48%. The pharmacokinetic curves of capsaicin submicroemulsion and its aqueous solution in rabbit ear vein were in accordance with the two-compartment model and the elimination half-lives were (48.501 3 ± 4.011 9) and (15.262 5 ± 1.888 2) min, respectively. The area was (924.09 ± 149.80) and (555.36 ± 57.46) mg · min · L-1, respectively. Conclusion: The established HPLC is accurate and sensitive and suitable for the determination of capsaicin in plasma. Compared with capsaicin aqueous solution, capsaicin submicron emulsion can prolong the half-life of the drug in vivo and improve the bioavailability.