2种国产司帕沙星制剂的生物等效性研究

目的 建立反相高效液相色谱法测定血浆中司帕沙星浓度，并研究其片剂与胶囊的人体相对生物利用度。方法 采用随机交叉、自身对照试验设计，20例健康男性志愿受试者单剂口服国产司帕沙星片剂或胶囊剂400mg后在不同时间点采血。用反相高效液相色谱法测定血清中司帕沙星浓度，以方差分析对主要药动学参数进行差别检验，双单侧t检验进行生物等效性判定。结果单剂量口服用400mg司帕沙星胶囊剂和片剂后的药物动力学参数AUC0～96分别为（50．50±6．78）和（50．82±11．57）μg·h·mL^-1，AUC0～∞。分别为（53．44±7．79）和（54．25±12．96）μg·h·mL^-1、tmax分别为（4．22±1．59）和（5．06±2．13）h、Cmax别为（1．46±0．23）和（1．46±0．31）μg·h·mL^-1、t1／2分别为（22．03±4．57）和（23．01±2．94）h。胶囊剂和片剂的相对生物利用度为102．41％±16．77％。2种制剂的药物动力学参数无明显差异。结论RP-HPLC法能快速、准确地测定人血浆中的司帕沙星，受试制剂与参比制剂具有生物等效性。

Bioavailability of 2 sparfloxacin preparations in humans

Objective To determine the concentration of sparfloxacin in the human plasma by High Performance Liquid Chro- matography （HPLC）, and to study its bioequivalence. Methods The pharmaeokinetics of sparfloxacin tablets and capsules were determined following a single oral dose of 400 mg given to 20 healthy volunteers in an open randomized crossover study. The sparfloxacin concentrations in the serum were measured by RP-HPLC. The pharmacokinetic parameters were calculated on the basis of one compartment model using 3P97 program. Results The pharmacokinetic parameters, after the volunteers taking a single dose of 400 mg of the trial preparation or the comparison preparation were as follows： tmax was （4. 22± 1.59） and （5.06±2. 13）h; Cmax was （1.46±0.23） and （1.46±0. 31）μg· mL^-1 ; AUC0～96 was （50. 50±6.78） and （50. 82±11.57） μg·h·mL^-1; AUC0～x was （53. 44±7. 79） and （54. 25±12. 96）μg·h·mL^-1; and t12 was （22. 03 ± 4. 57） and （23.01±2.94） h respectively. The pharmacokinetic parameters obtained from our studies showed no significant differences between the two products. The relative bioavailability of sparfloxacin capsule to tablet was 102. 41%±16. 77%. Conclusion The method can determine sparfloxacin in the plasma quickly and correctly. The two preparations are bioequivalent.