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目的:制备奈韦拉平纳米混悬剂,考察其在大鼠口服给药后体内的药动学特征。方法:采用高压均质法制备奈韦拉平纳米混悬剂,以纳米混悬剂粒径分布、Pd I和Zeta电位为指标,考察了奈韦拉平纳米混悬剂的影响因素,并对制得的纳米粒进行表征;采用高效液相色谱法测定大鼠血浆中的奈韦拉平浓度,使用3P97软件计算相应的药动学参数。结果:奈韦拉平纳米混悬液平均粒径为(456.1±72.1)nm,Pd I为(0.441±0.072),Zeta电位为(-24.4±4.7)m V。奈韦拉平混悬液和奈韦拉平纳米混悬剂在大鼠体内的AUC0-12分别为(7.57±0.52)和(11.72±1.83)mg·h·L-1;t1/2分别为(2.45±0.31)和(3.16±0.39)h;Tmax分别为(1.43±0.38)和(1.61±0.32)h;Cmax分别为(1.62±0.42)和(3.15±0.52)mg·L-1。结论:奈韦拉平纳米混悬液能够明显改善大鼠体内奈韦拉平的药动学行为,与奈韦拉平混悬液相比显著提高了药物的生物利用度。
OBJECTIVE: To prepare nevirapine nanosuspension and study its pharmacokinetics in rats after oral administration. Methods: Nilavelin nanosuspension was prepared by high pressure homogenization method. Influencing factors of the nanoezolamine nanosuspension were investigated by the particle size distribution of nanosuspension, Pd I and Zeta potential. The concentration of nevirapine in rat plasma was determined by HPLC, and the corresponding pharmacokinetic parameters were calculated by 3P97 software. Results: The mean particle size of nevirapine nanospheres was (456.1 ± 72.1) nm, the Pd I was (0.441 ± 0.072) and the zeta potential was (-24.4 ± 4.7) mV. The AUC0-12 of nevirapine suspension and nevirapine nanosuspension in rats were (7.57 ± 0.52) and (11.72 ± 1.83) mg · h · L-1, respectively; t1 / 2 were (2.45 ± 0.31) and (3.16 ± 0.39) h respectively; Tmax was (1.43 ± 0.38) and (1.61 ± 0.32) h respectively; Cmax was (1.62 ± 0.42) and (3.15 ± 0.52) mg · L-1, respectively. CONCLUSIONS: The nevirapine nanosuspension can significantly improve the pharmacokinetics of nevirapine in rats, and significantly improve the bioavailability of the drug compared with the nevirapine suspension.