Pharmacokinetics of neostigmine bromide multivesicular liposomes in rats / 第二军医大学学报

ABSTRACT

Objective To study the pharmacokinetics of neostigmine bromide multivesicular liposomes (NB-MVLs) and conventional neostigmine bromide (NB) injection in rats. Methods Twelve healthy rats, half male and half female, were randomly divided into two groups. One group was injected with NB-MVLs and the other with reference NB (0.15 mg/kg). RP-HPLC was used to examine neostigmine concentrations in rat plasma at different time points, and the pharmacokinetic parameters and relative bio-availability were calculated. Results Pharmacokinetic parameters of NB-MVLs and NB were as follows AUC0-t (35.56±4.62) mg·h·L-1 vs (15.97±5.22) mg·h·L-1;Tmax(2.40±0.89) h vs (0.45±0.11) h; Cmax (2.49±0.31) mg/L vs (4.61±0.91) mg/L; and t1/2 (15.14± 6.81) h vs (1.79±0.27) h, respectively. AUC0-t, AUC0-∞ and Cmax were studied by DAS 2.1.1 software for double unilateral t test and [1-2α] 90% confidence interval, and Tmax was precessed by Wilcoxon nonparametric test to evaluate the bioequivalence of NB-MVLs and NB. The result showed that NB-MVLs and NB were not bioequivalent. Conclusion Neostigmine in the form of multivesicular liposomes has improved bioavailability and stable drug release; NB-MVLs and NB are not bioequivalent.