司帕沙星分散片的人体生物利用度研究

A Study of the Pharmacokinetics and Bioavailability of Sparfloxacin Dispersible Tablet in Humans

目的研究司帕沙星分散片人体内的相对生物利用度。方法18例健康男性受试者交叉口服单剂量司帕沙星分散片(受试制剂)和司帕沙星普通片(参比制剂)各400 mg,用反相高效液相法测定两种制剂在人血清中的司帕沙星浓度。使用SPSS软件对各药物动力学参数进行统计学分析。结果司帕沙星分散片和司帕沙星普通片的AUC0→∞,Cm ax,tm ax分别为(48.11±4.04)h.μg.mL-1,(1.51±0.16)μg.mL-1,(1.86±0.15)h和(47.12±5.23)h.μg.mL-1,(1.49±0.21)μg.mL-1,(4.51±0.21)h。司帕沙星分散片相对普通片生物利用度为(102.10±12.01)%。结论两种司帕沙星制剂的的生物利用度程度差异无显著性,司帕沙星分散片吸收较快。

Objective To study the pharmacokinetics and relative bioavailability of sparfloxacin dispersible tablets in humans. Methods A single oral dose of 400 mg of the 2 sparfloxacin preparations dispersible tablets and common tablets were separately given to each of the 18 healthy male volunteers in an open randomized autologous cross-over test. The interval between the administrations of the 2 preparations was 2 weeks. Venous blood samples were taken from each of the subjects 0.5, 2.0, 3.0, 4.0, 4.5, 5.0, 5.5, 6.0, 8.0, 12.0, 24.0, 48.0, 72.0 and 96.0 h after the medication, respectively. Serum concentrations of sparfloxacin were determined with RP-HPLC. Results The pharmacyokinetics parameters AUC0→∞, Cmax, tmax of sparfloxacin dispersible tablets and common tablets were （48.11±4.04）h·μg·mL^-1, （1.51±0.16）μg·mL^-1, （1.86±0.15） h and （47.12±5.23）h·μg·mL^-1, （1.49±0.21）μg·mL^-1, （4.51±0.21）h, respectively. The bioavailability of dispersible tablets relative to that of common tablets was （102.10±12.01 ）%. Conclusion It was shown by statistical analysis that the difference between the Cmax of the two preparations was significant while the differences between the AUC0→∞ and Cmax were not, suggesting that the bioavailability of the 2 preparations were similar. However, dispersible tablets were absorbed more rapidly.