摘要
目的评价甲氯芬酯分散片和胶囊在中国健康志愿者体内的生物等效性。方法 18名健康男性受试者随机分为2组,分别单剂量口服甲氯芬酯分散片(试验制剂)或甲氯芬酯胶囊(参比制剂)200 mg。7 d清洗期后再交叉给药。于服药前(0 h)和服药后0.33、0.67、1、1.5、2、2.5、3、4、6、8、10、14、24 h抽取静脉血。采用高效液相色谱法测定血浆中对氯苯氧乙酸的浓度。通过DAS Ver2.0软件计算主要药动学参数,评价2种制剂的生物等效性。结果甲氯芬酯试验制剂与参比制剂的tmax分别为(1.8±s 0.3)和(2.1±0.3)h,ρmax分别为(13.9±2.6)和(12.8±2.8)mg.L-1,t1/2分别为(6.1±2.0)和(6.0±2.1)h,AUC0～t分别为(36±9)和(34±8)mg.h.L-1,AUC0～∞分别为(36±9)和(35±8)mg.h.L-1。以AUC0～t计算,试验制剂中甲氯芬酯对参比制剂的相对生物利用度为(105±10)%。结论甲氯芬酯分散片与胶囊在中国健康志愿者体内具有生物等效性。
AIM To study the pharmacokinetics and bioequivalence of domestic and imported micronized fenofibrate capsule in healthy volunteers.METHODS In a two-treatment,two-period,two-sequence randomized cross-over trial,20 healthy volunteers were given a single 200 mg oral dose of the test preparation and reference preparation.Plasma concentrations were determined by HPLC method.Ketoprofen was used as the internal standard.The pharmacokinetics parameters were calculated statistically to evaluate the bioequivalence between the two preparations by BAPP 2.2 software.RESULTS The pharmacokinetics parameters of test and reference preparation were as follows：ρmax were（5.3 ± s 2.1）mg·L-1 and（4.4 ± 1.5）mg·L-1;tmax were（6.4 ± 2.5）h and（5.8 ± 1.6）h;t1/2 were（23 ± 5）h and（26 ± 8）h;MRT were（35 ± 8）h and（38 ± 11）h;AUC0-72 were（127 ± 34）mg·h·L-1 and（118 ± 28）mg·h·L-1;AUC0-72 were（145 ± 41）mg·h·L-1 and（140 ± 34）mg·h·L-1,respectively.There was no significant difference between the two preparations.The relative bioavailability of tested capsule was（97± 29）%.CONCLUSION The two preparations are bioequivalent.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2010年第11期869-873,共5页
Chinese Journal of New Drugs and Clinical Remedies
