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

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 follows:t1/2β(53.4±12.9)h vs.(15.4±4.6)h; Cmax(6.7±1.8)μg·L-1 vs.(18.5±4.4)μg·L-1; AUC0～120 (298.8±97.1)μg·h·L-1 vs. (118.3±48.9)μg·h·L-1; AUC0～∞(412.2±131.5) μg·h·L-1 vs. (120.0±55.1)μg·h·L-1. In multiple-dose study the pharmacokinetic parameters were as follows:t1/2(49.5±10.3)h vs. (14.4±5.3)h; Cmax(8.7±2.5)μg·L-1 vs. (20.3±5.8)μg·L-1; AUC0～120(451.2±127.1)μg·h·L-1 vs. (136.3±54.9)μg·h·L-1; AUC0～∞(569.3±165.8) μg·h·L-1 vs. (139.0±61.3)μg·h·L-1; Cav(2.7±0.6)、(8.3±1.3)μg·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.