盐酸氟西汀口腔崩解片人体生物等效性研究

Bioequivalence of Fluoxetine Hydrochloride Orally Disintegrating Tablets in Healthy Volunteers

目的:研究盐酸氟西汀口腔崩解片在健康人体内的药动学及相对生物利用度。方法:18名健康志愿者分别单剂量交叉口服盐酸氟西汀口腔崩解片(受试制剂)和盐酸氟西汀胶囊(参比制剂)40mg,用高效液相色谱法测定血药浓度,以3p97程序计算药动学参数并进行生物等效性评价。结果:受试制剂与参比制剂在体内血药浓度药-时曲线呈一室模型,tmax分别为(5·17±1·10)、(5·11±1·02)h,Cmax分别为(76·24±38·42)、(77·92±34·97)ng·mL-1,AUC0～150分别为(3216·21±899·69)、(3220·62±1275·57)ng·h·mL-1,AUC0～∞分别为(3570·60±1299·29)、(3662·49±1444·69)ng·h·mL-1。经组间t检验,受试制剂与参比制剂药动学参数无显著性差异(P>0·05),受试制剂的相对生物利用度为(96·47±10·43)%。结论:盐酸氟西汀口腔崩解片与盐酸氟西汀胶囊具有生物等效性。

OBJECTIVE： To study the pharmacokinetics and the relative bioavailability of fluoxetine hydrochloride orally disintegrating tablets in healthy volunteers.METHODS：A single oral dose of 40 mg fluoxetine hydrochloride orally integrating tablets（test preparation） and 40 mg fluoxetine hydrochloride capsules（reference） were given to 18 healthy volunteers by a randomized crossover way.The concentrations of fluoxetine hydrochloride in plasma were determined by HPLC; the pharmacokinetic parameters were calculated with 3p97 pharmacokinetic program and bioequivalence was evaluated.RESULTS： The time concentration curves of test and reference preparations of fluoxetine hydrochloride fitted two compartment model with the main pharmacokinetic parameters stated as follows： tmax were （5.17±1.10） h and （5.11±1.02） h; Cmax were （76.24±38.42） ng·mL^-1 and （77.92±34.97） ng·mL^-1;AUC0-150 were （3 216.21±899.69） ng·h·mL^-1 and （3 220.62±1 275.57） ng·h·mL^-1,and AUC0-∞ were （3 570.60±1 299.29） ng·h·mL^-1 and （3 662.49±1 444.69） ng·h·mL^-1,respectively. The t test results showed that the two preparations had no significant difference in pharmacokinetic parameters（P 〉 0.05） . The relative bioavailability of the test preparation was （96.47± 10.43）% .CONCLUSION： The result demonstrated that the two formulations were bioequivalent.