摘要
目的 :研究多西环素肠溶微粒胶囊和多西环素片的人体生物等效性与药动学。方法 :2 0名男性健康志愿者随机分 2组 ,按双周期交叉口服单剂量 2 0 0mg多西环素的 2种制剂 ,分别于服药前及服药后 0 5 ,1,1 5 ,2 ,2 5 ,3,4,6 ,8,12 ,2 4,48,72h取血样 ,以HPLC法测定血浆中多西环素浓度 ,计算 2种制剂相对生物利用度参数 ,并评价其生物等效性。结果 :口服受试制剂多西环素肠溶微粒胶囊和参比制剂多西环素片的药动学参数 :cmax分别为 (3 6 5± 0 81) μg·mL-1和 (3 6 5± 0 73) μg·mL-1,tmax分别为 (2 5± 0 3)h和 (2 2± 0 7)h ,T1/ 2 (消除半衰期 )分别为 (2 1 4 8± 3 2 0 )h和 (2 1 85± 3 11)h ,AUC0→ 72 分别为 (72 18±2 2 6 8) μg·h·mL-1和 (72 0 6± 2 1 0 8) μg·h·mL-1,AUC0→∞ 分别为 (81 4 4± 2 4 94) μg·h·mL-1和 (81 82± 2 3 19) μg·h·mL-1,多西环素肠溶微粒胶囊相对生物利用度为 (10 1 9± 2 5 2 ) %,对参数cmax,AUC0→ 72 先进行方差分析 ,再进行双单侧t检验 ,表明 2种制剂的参数生物等效 ,tmax经非参数检验表明无统计学差异。结论 :多西环素肠溶微胶囊和多西环素片具有生物等效性。
AIM: To study the bioequivalence and pharmacokinetics of doxycycline enteric-coated microsomes capsules and doxycycline tablets. METHODS: A single oral dose of 200 mg doxycycline enteric-coated microsomes capsules and doxycycline tablets was given to 20 healthy male volunteers in an open randomized cross-over test. The plasma drug concentration was determined by high performance liquid chromatography (HPLC) method. The relative bioavailability and bioequivalence of 2 doxycycline were calculated and compared. RESULTS: The pharmacokinetic parameters of doxycycline enteric-coated microsomes capsules and doxycycline tablets were as follows: c max: (3.65±0.81) μg·mL -1 and (3.65±0.73) μg·mL -1, t max: (2.5±0.3) h and (2.2±0.7) h, T 1/2ke: (21.48±3.20) h and (21.85±3.11) h, AUC 0→72: (72.18±22.68) μg·h·mL -1 and (72.06±21.08) μg·h·mL -1,AUC 0→∞: (81.44±24.94) μg·h·mL -1 and (81.82±23.19) μg·mL -1, respectively. The relative bioavailability of doxycycline enteric-coated microsomes capsules was (101.9±25.2)% compared with the tablet. Variance analysis and two one-sided t test were performed to parameters: c max, AUC 0→72 and AUC 0→∞. The results showed that the parameters were no significant statistical differences. CONCLUSION: The 2 preparations of doxycycline are bioequivalent.
出处
《中国临床药学杂志》
CAS
2003年第1期16-19,共4页
Chinese Journal of Clinical Pharmacy
关键词
多西环素肠溶微粒胶囊
多西环素片
高效液相色谱法
生物等效性
doxycycline enteric-coated microsome capsule
doxycycline tablet
high performance liquid chromatography
bioequivalence
