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目的:研究兰索拉唑在健康受试者体内的药动学和药效学。方法:选择健康受试者20名,男女各半,随机分为兰索拉唑组(30mg)和奥美拉唑组(40mg),给药后监测24h胃内pH,并用高效液相色谱法测定兰索拉唑和奥美拉唑血药浓度,数据分别用SPSS11.5和DAS2.0处理。结果:兰索拉唑药动学参数为AUC0-t:(7.2±3.9)mg.h.L-1;AUC0-∞(7.7±4.6)mg.h.L-1;AUMC0-t(24.0±21.2);AUMC0-∞(33.2±35.6);MRT0-t(2.8±1.1)h;MRT0-∞(3.4±1.8)h;t1/2(2.2±1.3)h;CL(5.3±3.1)L.h-1;Cmax(2.3±0.4)mg.L-1。奥美拉唑药动学参数为:AUC0-t(4.8±4.1)mg.h.L-1;AUC0-∞(4.6±4.2)mg.h.L-1;AUMC0-t(11.0±15.1);AUMC0-∞(12.2±17.1);MRT0-t:(1.8±0.8)h;MRT0-∞(1.9±0.9)h;t1/2(1.1±0.6)h;CL(13.6±7.4)L.h-1;Cmax(2.1±0.8)mg.L-1;给药后胃内pH明显升高,给药结束后12h胃内pH仍分别达(5.1±1.6)和(3.9±1.9)。结论:健康受试者体内血药浓度未能实时反映该药在人体胃组织中的浓度及抑酸效果,该药能蓄积在人体胃组织中并维持较长时间的抑酸作用。
Objective: To study the pharmacokinetics and pharmacodynamics of lansoprazole in healthy subjects. Methods: Twenty healthy subjects were selected and divided into two groups: male and female, randomly divided into two groups: lansoprazole group (30mg) and omeprazole group (40mg). After intragastric administration, the intragastric pH was monitored and analyzed by high performance liquid chromatography The plasma concentration of lansoprazole and omeprazole was determined and the data were treated with SPSS 11.5 and DAS 2.0 respectively. Results: The pharmacokinetic parameters of Lansoprazole were AUC0-t (7.2 ± 3.9) mg.hL-1, AUC0-∞ (7.7 ± 4.6) mg.hL-1, AUMC0-t (33.2 ± 35.6), MRT0-t (2.8 ± 1.1) h, MRT0-∞ (3.4 ± 1.8) h, t1 / 2 (2.2 ± 1.3) h, CL (5.3 ± 3.1) Lh- 2.3 ± 0.4) mg.L-1. The pharmacokinetic parameters of omeprazole were AUC0-t (4.8 ± 4.1) mg.hL-1, AUC0-∞ (4.6 ± 4.2) mg.hL-1, AUMC0-t (12.2 ± 17.1), MRT0-t: (1.8 ± 0.8) h, MRT0-∞ (1.9 ± 0.9) h, t1 / 2 (1.1 ± 0.6) h, CL (13.6 ± 7.4) Lh- ± 0.8) mg.L-1. After administration, the intragastric pH was significantly increased (5.1 ± 1.6) and (3.9 ± 1.9) after 12 h of administration. Conclusion: The plasma concentration of healthy volunteers in vivo can not reflect the concentration of the drug in human gastric tissue and the effect of inhibiting acid in real time. The drug can accumulate in human gastric tissue and maintain acid suppression for a long time.