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目的:研究难溶性药物尼群地平共研粉末在大鼠体内的药动学。方法:采用HPLC-UV法,测定大鼠灌胃尼群地平共研粉末(T)和物理混合粉末(R)后不同时间点的血药浓度,绘制药-时曲线,计算药动学参数及相对生物利用度。结果:大鼠灌胃相当于尼群地平20mg的T和R后,血浆中尼群地平的tmax分别为(1.6±0.5)和(2.0±0.7)h;Cmax分别为(496.2±215.1)和(260.6±56.9)μg.L-1;用梯形法计算,AUC0-t分别(4 077.0±1 487.3)μg.h.L-1和(2 438.1±1 039.8)μg.h.L-1。与物理混合粉末R相比,尼群地平共研粉末T的相对生物利用度为209.27%。结论:尼群地平共研粉末与尼群地平物理混合粉末相比,在大鼠体内吸收迅速、生物利用度高。
OBJECTIVE: To study the pharmacokinetics of nitrendipine co-formulation in rats. Methods: HPLC-UV method was used to determine the concentration of nitrendipine co-milled powder (T) and physical mixed powder (R) at different time points after drug administration in rats. The drug-time curve was drawn and the pharmacokinetic parameters Relative bioavailability. Results: After administration of 20 mg of nitrendipine to T and R, tmax in plasma was (1.6 ± 0.5) and (2.0 ± 0.7) h respectively; Cmax was (496.2 ± 215.1) and 260.6 ± 56.9) μg.L-1; AUC0-t was (4 077.0 ± 1 487.3) μg.hL-1 and (2 438.1 ± 1 039.8) μg.hL-1, respectively, calculated by the trapezoidal method. The relative bioavailability of nitrendipine co-powdered T was 209.27% compared with that of the physical mixed powder R. CONCLUSION: Nitrendipine co-produced powder absorbs quickly and has high bioavailability compared with nitrendipine mixed powder.