Preparation and Pharmacokinetics of Nevirapine Nanosuspensions in Rats / 中国药师

ABSTRACT

Objective:To prepare nevirapine nanosuspensions ( Nev-NS) and study the pharmacokinetics in rats. Methods:Nev-NS was prepared by a high pressure homogenization technology. The particle size, PDI and Zeta potential of the nanosuspensions were used as the indices to determine the influencing factors in the preparation process. Nevirapine plasma concentration was detected by HPLC and the pharmacokinetic parameters were calculated by 3P97 software. Results: The particle size, PDI and Zeta potential of Nev-NS was (456. 1 ± 72. 1) nm, 0. 441 ± 0. 072 and ( -24. 4 ± 4. 7) mV, respectively. AUC0-12 of Nev and Nev-NS was (7. 57 ± 0.52) and (11.72 ±1.83) mg·h·L-1, t1/2 was (2.45 ±0.31) and (3.16 ±0.39) h, Tmax was (1.43 ±0.38) and (1.61 ± 0. 32) h and Cmax was (1. 62 ± 0. 42) and (3. 15 ± 0. 52) mg·L-1 , respectively. Conclusion:Nev-NS can improve the pharmacoki-netic behavior of Nev in rats significantly, and obviously enhance the bioavailability when compared with nevirapine suspensions.