目的 采用高效液相色谱-质谱联用法研究盐酸多奈哌齐口腔崩解片的人体药物代谢动力学，并评价其生物等效性。 方法 2009年9月－11月对22例健康男性受试志愿者单次交叉口服盐酸多奈哌齐口腔崩解片（试验制剂）和盐酸多奈哌齐普通片（参比制剂），测定给药后不同时间点血浆中多奈哌齐经时血药浓度，采用DAS 2.0软件进行药物代谢动力学参数计算和生物等效性评价。 结果 受试者单次口服试验制剂与参比制剂后，达峰时间分别为（2.95 ± 1.16）、（3.19 ± 0.98） h，峰浓度分别为（9.98 ± 2.93）、（9.13 ± 2.05） ng/mL，药时曲线下面积（0-t）分别为（470.76± 142.64）、（446.57 ± 137.30）ng/mL·h；药时曲线下面积（0-∞）分别为（517.74 ± 169.79）、（489.47 ± 162.13）ng/mL·h。试验制剂与参比制剂的生物等效性结果为104.7%，其90%置信区间为（98.4%，111.4%）。结论 盐酸多奈哌齐口腔崩解片与普通片生物等效。
目的 采用高效液相色谱-质谱联用法（HPLC-MS/MS）研究普罗布考片的人体药物代谢动力学变化规律。 方法 2010年10月－11月，24例健康男性受试者单次口服普罗布考片0.5 g，采用HPLC-MS/MS法测定给药后不同时间点血浆中普罗布考的经时血药浓度，采用DAS 2.0软件进行药动学参数计算。 结果 受试者单次口服普罗布考片，达峰时间为（11.50 ± 6.66）h，峰浓度为（2 894.72 ± 1 320.53）ng/mL，药-时曲线下面积（AUC）0-t为（238 876.96 ± 131 873.67） ng/mL· h，AUC0-∞为（259 989.08 ± 146 112.88）ng/mL· h，半衰期为（278.52 ± 164.72） h。结论 普罗布考片体内过程符合二室模型，单次口服具有较好的安全性。
ObjectiveTo study the pharmacokinetics of lovastatin/niacin sustained-release tablets in healthy Chinese volunteers. MethodsEligible subjects were enrolled to receive a single dose of 20/500, 20/750 and 20/1 000 mg lovastatin/niacin sustained-release tablets and multiple dose of 20/1 000 mg lovastatin/niacin sustainedrelease tablets, one time per day, sustained for 5 days, respectively. Blood samples were obtained before dosing and up to 10, 20, 30, and 45 minutes, and 1 hour, 1.5, 2, 2.5, 3, 3.5, 4, 5, 7, 9, 12, and 15 hours after dosing. Niacin, niacinamide, nicotinuric acid and lovastatin were detected by high performance liquid chromatography-tandem mass spectrometry method. ResultsThe peak concertration and the area under the plasma concentration-time curve (0-t) of nicotinuric acid had linear dynamics characteristics with the dosage when the dose of niacin was between 500 and 1 000 mg. After multiple dosing, pharmacokinetics parameters of nicotinuric acid and lovastatin were close. No significant diTherence was found between male and female subjects. ConclusionLovastatin/niacin sustained-release tablets possess linear kinetics. Accumulation is not significant after multiple dosing. Gender doesn't affect the pharmacokinetics parameters.