Pharmacokinetics of Compound Amlodipine Besylate/Atorvastatin Calcium Tablets in Healthy Volunteers after Oral Administration of Single Dose vs. Multiple Doses / 中国药房

ABSTRACT

OBJECTIVE:To study the pharmacokinetics of compound amlodipine besylate/atorvastatin calcium tablets(CABACT) following oral administration of single dose vs. multiple doses in healthy volunteers. METHODS:10 volunteers were administered a single dose of Compound amlodipine besylate/atorvastatin calcium tablets(10 mg,p.o.)or multiple doses(10 mg?d-1,p.o.) for 7 days,respectively. Plasma concentrations of amlodipine besylate and atorvastatin calcium were determined by LC-MS/MS and the pharmacokinetic parameters were calculated using DAS software. RESULTS:In single-dose study the pharmacokinetic parameters of amlodipine besylate vs. atorvastatin calcium were as followst1/2?(53.4?12.9)h vs.(15.4?4.6)h; Cmax(6.7?1.8)?g?L-1 vs.(18.5?4.4)?g?L-1; AUC0～120 (298.8?97.1)?g?h?L-1 vs. (118.3?48.9)?g?h?L-1; AUC0～∞(412.2?131.5) ?g?h?L-1 vs. (120.0?55.1)?g?h?L-1. In multiple-dose study the pharmacokinetic parameters were as followst1/2(49.5?10.3)h vs. (14.4?5.3)h; Cmax(8.7?2.5)?g?L-1 vs. (20.3?5.8)?g?L-1; AUC0～120(451.2?127.1)?g?h?L-1 vs. (136.3?54.9)?g?h?L-1; AUC0～∞(569.3?165.8) ?g?h?L-1 vs. (139.0?61.3)?g?h?L-1; Cav(2.7?0.6)、(8.3?1.3)?g?L-1; R(1.7?0.4) vs. (1.1?0.2). CONCLUSION:The elimination rates of amlodipine besylate and atorvastatin calcium do not change after oral administration of multiple doses of CABACT while slight accumulation of amlodipine besylate is founded.