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目的评价高脂餐对阿雷地平及其活性代谢产物羟基阿雷地平在健康中国人体内药动学的影响。方法10名健康男性受试者空腹口服阿雷地平10 mg,经过1 wk清洗期后,受试者高脂餐后口服阿雷地平10 mg。采用液相色谱-串联质谱联用法测定血浆中阿雷地平及其活性代谢产物羟基阿雷地平的浓度。结果空腹和高脂餐后口服阿雷地平,阿雷地平的c_(max)分别为(2.4±s0.8)和(4.4±2.9)μg·L~(-1),羟基阿雷地平的c_(max)分别为(41±10)和(51±19)μg·L~(-1);空腹和高脂餐后阿雷地平和羟基阿雷地平的c_(max)无显著差异。空腹和高脂餐后口服阿雷地平,阿雷地平的AUC_(0～36)分别为(10.3±2.3)和(15±7)μg·h·L~(-1),羟基阿雷地平的AUC_(0～36)分别为(305±108)和(389±129)μg·h·L~(-1);阿雷地平的t_(max)分别为(4.4±1.0)和(9±6)h,羟基阿雷地平的f_(max)分别为(5.0±1.6)和(11±7)h;空腹和高脂餐后阿雷地平和羟基阿雷地平的AUC_(0～36)和t_(max)均存在显著差异,AUC显著增加,t_(max)显著延长。结论高脂餐后,阿雷地平的吸收出现延迟现象,吸收程度有所增加;羟基阿雷地平的体内生成延迟,但生成的量增加。
Objective To evaluate the effect of high fat diet on the pharmacokinetics of Areradipine and its active metabolite hydroxy Arelipine in healthy Chinese. Methods Ten healthy male subjects were treated with oral 10 mg of andrographolide 10 mg orally fasting for 1 wk. The plasma concentration of Areradipine and its active metabolite hydroxyareline was determined by liquid chromatography-tandem mass spectrometry. RESULTS: After oral fasting and high fat oral aredipine, the average maximal concentrations of isradipine were (2.4 ± s0.8) and (4.4 ± 2.9) μg · L -1, respectively. The c_ (max) were (41 ± 10) and (51 ± 19) μg · L -1, respectively. There was no significant difference in c max of Aretrianidipine and Hydroxyaretinid after fasting and high fat meal. The AUC_ (0 ~ 36) of oral aredipine and areleidipine after fasting and high fat meal were (10.3 ± 2.3) and (15 ± 7) μg · h · L -1, AUC_ (0 ~ 36) were (305 ± 108) and (389 ± 129) μg · h · L -1, respectively, and the t max of Arerampine were (4.4 ± 1.0) and ) h, and the f_ (max) of hydroxylysine was (5.0 ± 1.6) and (11 ± 7) h respectively. The AUC_ (0 ~ 36) and t_ (max), there was a significant difference, AUC increased significantly, t_ (max) significantly prolonged. Conclusion After high-fat diet, the absorption of Areradip lags behind and the degree of absorption increases. The production of hydroxy-Areradipine is delayed but the amount of Alkaliplatin is increased.