头孢克洛胶囊及分散片在健康人体内的生物等效性研究

Bioequivalence of Oral Cefaclor Capsule and Dispersible Tablets in Healthy Volunteers

目的评价头孢克洛胶囊及分散片在健康人体内相对生物利用度及生物等效性。方法受试者采用3处理、3周期、随机、自身交叉对照方法口服受试制剂头孢克洛胶囊、头孢克洛分散片和参比制剂500mg,采用反相高效液相色谱(RP-HPLC)法测定血浆中药物浓度,药代动力学参数采用DAS软件处理。结果头孢克洛胶囊、分散片及参比制剂分散片峰浓度(Cmax)分别为(11.79±2.85)μg/mL,(13.07±3.53)μg/mL和(12.59±3.34)μg/mL;达峰时间(tmax)分别为(0.75±0.20)h,(0.62±0.17)h和(0.55±0.11)h;半衰期(t1/2)分别为(0.60±0.11)h,(0.56±0.08)h和(0.57±0.10)h;0→t药-时曲线下面积(AUC0→t)分别为(15.37±2.23)μg·h/mL,(16.15±3.75)μg·h/mL和(15.66±2.98)μg·h/mL;0→∞药-时曲线下面积(AUC0→∞)分别为(15.67±2.26)μg·h/mL,(16.43±3.74)μg·h/mL和(15.93±3.02)μg·h/mL;受试制剂的相对生物利用度F0→t和F0→∞分别为(100.51±19.19)%,(100.70±19.00)%和(105.96±29.16)%,(105.87±28.52)%。受试制剂与参比制剂符合生物等效标准。结论头孢克洛胶囊、头孢克洛分散片与参比制剂具有生物等效性。

Objective To study the bioavailability and bioequivalenee of eefaelor （capsule and dispersible tablets） in healthy volunteers. Methods According to the 3- way crossover design, each volunteer was orally given 500 mg eefaelor. The plasma concentrations were determined by RP-HPLC. The pharmaeokinetie parameters were obtained using DAS program. Results Cmax of eefaelor（eapsule and dispersible tablets） was（11. 79 ± 2. 85）μg/mL, （13.07 ± 3.53）μg/mL and （12.59 ± 3.34）μg/mL; Tmax was （0.75 ±0. 20）h, （0.62 ±0.17）h and （0.55±0.11）h; t1/2： was （0.60±0.11）h,（0.56±0.08）h and （0.57±0.10）h; AUC0→t, was （15.37 ±2.23）μg· h/mL,（16.15±3.75）μg · h/mL and （15.66±2.98）μg · h/mL;AUC0→∞ was （15.67±2.26）μg · h/mL, （16. 43 ± 3. 74） μg · h/mL and （15.93± 3.02）μg ·h/mL,respeetively. The relative bioavailability was （100. 51 ± 19. 19）% and （105.96 ±29. 16）%. The data of the reference and tested drugs were up to the standard of bioequivalenee as shown by F test. Conclusion The results show that one eefaclor capsule and two cefaclor dispersible tablets made in three different dosage forms are bioequivalent.