高效液相色谱法研究人体内格列齐特片药动学和生物等效性

目的研究健康人口服格列齐特片后的药动学和生物等效性。方法19个健康受试者采用随机分组自身交叉对照试验设计，口服格列齐特片80mg后用HPLC法测定血浆中格列齐特浓度，以DAS软件计算其药动学参数和评价生物等效性。结果在选定的色谱条件下格列齐特与内标及血浆杂质分离良好，在0．1～10．0μg·mL^-1范围内线性良好。相对回收率〉95．58％，日内和日间RSD〈10．7％。格列齐特片受试制剂和参比制剂的主要药动学参数：Tmax分别为（1．85±0．49）h和（1．65±0．46）h，Cmax分别为（11．107±3．184）μg·mL^-1和（11．439±3．388）μg·mL^-1；t1/2分别为（1．63±0．28）h和（1．57±0．42）h；AUC0→t分别为（38．9±9．6）μg·h·mL^-1和（37．4±10．4）μg·h·mL^-1；用面积法（AUC0→t）估算的格列齐特片相对生物利用度为（105．7±12．8）％。结论用HPLC法测定血浆中格列齐特浓度，杂质无干扰，定量限低，重复性好，准确度高。受试的格列齐特片与参比的格列齐特片生物等效。

Determination of Gliclazide Tablets in Human Plasma by HPLC:Application to Bioequivalence and Pharmacokinetics Study

Aim To study the pharmacokinetics of gliclazide tablets in human plasma. Methods Nineteen volunteers were given the gliclazide tablets by oral administration with 2-way crossover design. The concentration of gliclazide in plasma was determined by HPLC and the pharmacokinetic parameters were calculated by DAS software. Results The calibration curve was linear in the range from 0. 1μg·mL^-1 to 10.0μg·mL^-1. The relative recovery enceeded 95.58%. The intra and inter-day RSD was less than 10.7%. The main pharmacokinetic parameters t1/2, Cmax, Tmax and AUC0→t for the test preparations were （ 1.63±0.28 ） h, （ 11. 107 ± 3.184 ） μg ·mL^-1, （ 1.85±0.49） h and （38.9± 9.6） μg·h·mL^-1, respectively. Those for the reference preparations were （ 1.57±0.42） h, （ 11. 439±3. 388） μg·mL^-1, （ 1.65±0.46） h and （37.4±10.4） μg·h·mL^-1 ,respectively. The relative bioavalability of the test preparations was （ 105.7 ± 12.8） %. Conclusion The HPLC method for determination of gliclazide in plasma was proved to be sensitive accurate and convenient. The reference and test preparations are bioequivalent.