盐酸西替利嗪两种制剂在人体内生物利用度比较的研究

Comparision of bioavailability of two preparations of cetirizine dihydrochloride

目的盐酸西替利嗪两种制剂在人体内的生物利用度比较的研究。方法采用改进的高效液相色谱法,以盐酸羟嗪为内标,测定了20名健康男性受试者口眼盐酸西替利嗪胶囊和盐酸西替利嗪片后不同时刻血浆中西替利嗪的浓度,绘制了血药浓度-时间曲线,并求出两种制剂的主要药动学参数。结果两种制剂的主要药动学参数:Cmax分别为(905.7±185.9)和(777.1±105.8)ng/mL,Tmax分别为(0.79±0.26)和(0.90土0.45)h,t1/2分别为(7.59±1.29)和(7.73±1.46)h,AUC0→∞分别为(6774.8±1059.1)和(6603.2±1257.6)ng·h/mL.以AUC0→∞计算相对生物利用度,盐酸西替利嗪胶囊的相对生物利用度平均为(104.0±14.4)%.采用方差分析和双单侧t检验法进行两种制剂生物利用度判断。结论两种制剂生物利用度无显著性差异(P>0.05),可认为两者在人体内生物作用等效.

OBJECTIVE To compare bioavailability of the two preparations of cetirizine dihydrochloride. METHODS The plasma concentrations of cetirizine in 20 healthy male volunteers after oral administration of cetirizine dihydrochlofide capsules and cetirizine dihydrochloride tablets were determined by the improved HPLC, using hydroxyzine dihydrochloride as the internal standard. The plasma concentration-time curves and major pharmacokinetic parameters of tests and reference preparation were obtained. RESULTS The major pharmacokinetic parameters of tests and reference preparation were as follows： Cmax were （905.7 ± 185.9） and （ 777.1 ± 105.8）ng/mL, Tmax were （ 0. 79 ± 0. 26 ） and （0.90±0.45）h, t1/2 were （7.59 ±1.29） and （7.73±1.46）h, AUC0→∞ were （6774.8 ± 1059.1 ） and （6603.2 ± 1257.6） ng·h/mL, respectively. According to AUC0→∞, the relative bioavailability of cetirizine dihydrochloride was （ 104.0 ± 14.4） %. CONCLUSION Results by ANOVA analysis and two-side t-test shows that there is no obvious difference in availability between the two preparations （P 〉 0.05）, and the two preparations are bioequivalent.