摘要
目的:评价坎地沙坦酯片、胶囊与进口参比制剂在健康人体内的药代动力学及其生物等效性。方法:采用三制剂三周期二重3×3拉丁方设计,18名健康男性志愿者交叉单剂量口服受试制剂坎地沙坦酯片、胶囊和参比制剂坎地沙坦酯片各16 mg后,采用高效液相色谱—荧光法测定不同时间血浆中主要代谢产物坎地沙坦浓度,用DAS药动学程序进行药代动力学参数的计算及生物等效性评价。结果:受试制剂坎地沙坦酯片、胶囊和参比制剂坎地沙坦酯片的主要药代动力学参数:tmax分别为(4.6±0.9)、(4.6±1.3)和(4.4±0.9)h,t1/2分别为(8.8±1.9)、(8.3±1.9)、(8.5±1.8)h,Cmax分别为(170±61)、(155±75)和(171±77)ng/mL,AUC0-36分别为(1762±576)、(1684±600)和(1808±662)ng.mL-1.h,AUC0-∞分别为(1886±616)、(1776±600)和(1913±694)ng.mL-1.h。两种受试制剂的相对生物利用度分别为97.8%和93.1%。结论:两种受试制剂和参比制剂具有生物等效性。
AIM： To investigate the pharmacokinetics and bioequivalence of candesartan cilexetic tablets, capsules and imported tablets in healthy volunteers. METHODS： A single oral dose 16 mg of three formulations was randomly given to 18 healthy volunteers in a three cycle duplex 3 × 3 latin square crossover design . The concentration of candesartan in plasma, which is a major metabolite of candesartan cilexetic, was determined by HPLC-FLD at different times. The pharmacokinetics parameters were calculated and the bioequivalence of three formulations were evaluated by DAS program. RESULTS： The main pharmacokinetic parameters of candesartan cilexetic tablets, capsules and imported tablets were as follows： tmax were （4.6±0.9）, （4.6± 1.3） and （4.4 ± 0.9） h, t1/2 were（8.8 ± 1.9）, （8.3 ± 1.9）, （8.5 ± 1.8） h, Cmax were（170± 61）, （155 ± 75） and （171 ± 77） ng/mL, AUC0-36 were（ 1762 ± 576）, （1684 ± 600） and （1808 ± 662） ng.mL^-1.h, AUC0-∞ were （ 1886 ± 616）, （1776 ± 600） and （1913 ± 694） ng.mL^-1.h. The relative bioavailability of tested tablets and capsules were 97.75% and 93.11%. CONCLUSION： The two tested formulations are bioequivalent with reference fomaulation.
出处
《中国临床药理学与治疗学》
CAS
CSCD
2009年第7期794-798,共5页
Chinese Journal of Clinical Pharmacology and Therapeutics
