FU, Q., FU, H., Huan, L., Zhang, W., Shu, G., Liu, M., Deng, F., Hu, J. (2013). Preparation of Cefquinome Sulfate Proliposome and
its Pharmacokinetics in Rabbit. Iranian Journal of Pharmaceutical Research, 12(4), 611-621. doi: 10.22037/ijpr.2013.1392
Qiang FU; Hua-Lin FU; LUO Huan; Wei Zhang; Guang Shu; Meng-Jiao Liu; Feng-Ying Deng; Jun Hu. "Preparation of Cefquinome Sulfate Proliposome and
its Pharmacokinetics in Rabbit". Iranian Journal of Pharmaceutical Research, 12, 4, 2013, 611-621. doi: 10.22037/ijpr.2013.1392
FU, Q., FU, H., Huan, L., Zhang, W., Shu, G., Liu, M., Deng, F., Hu, J. (2013). 'Preparation of Cefquinome Sulfate Proliposome and
its Pharmacokinetics in Rabbit', Iranian Journal of Pharmaceutical Research, 12(4), pp. 611-621. doi: 10.22037/ijpr.2013.1392
FU, Q., FU, H., Huan, L., Zhang, W., Shu, G., Liu, M., Deng, F., Hu, J. Preparation of Cefquinome Sulfate Proliposome and
its Pharmacokinetics in Rabbit. Iranian Journal of Pharmaceutical Research, 2013; 12(4): 611-621. doi: 10.22037/ijpr.2013.1392
Preparation of Cefquinome Sulfate Proliposome and
its Pharmacokinetics in Rabbit
Department of Pharmacy, College of Veterinary Medicine, Sichuan Agriculture University, Ya, an, Sichuan, 625014,China.
Abstract
Cefquinome Sulfate (CS) is a fourth-generation cephalosporin, which has been developed solely for veterinary use. It shows potent antibacterial activity against a broad spectrum of bacterial species. However, Cefquinome is susceptible to hydrolysis, which limiting its clinical employment efficacies to some extent. So, in this study, to increase Cefquinome Sulfate biological half-life, a novel Cefquinome Sulfate proliposome was prepared by solid dispersion and effervescent techniques and characterized for morphology, particle size, entrapment efficiency and in vitro release. A Reversed Phase-High Performance Liquid Chromatography (RP–HPLC) method was first chosen and established to determine the drug concentration in plasma after intra muscular (IM) administrating Cefquinome Sulfate solution and liposome at a single dosage of 18 mg/kg in rabbit. Then their pharmacokinetics in vivo was compared. Results showed that the received liposome was milky white suspension, spherical or ellipsoidal in shape. The mean particle size was 203±5 nm and the entrapment efficiency was 53.5±0.16%. The cefaquinom sulfate solution and liposome both followed a two compartment model, in vivo. The pharmacokinetic parameters for the solution and liposomal formulations were measured as follows: t1/2αwere (1.214 ± 0.135) h and (1.395 ± 0.113) h, t1/2βwere (8.752 ± 0.846) h and (16.503 ± 1.275) h, AUC(0-24) were (49.582 ± 9.173) (mg·h)/L and (138.727 ± 11.034) (mg·h)/L, CL/F were (0.357 ± 0.015) L/(h·kg) and (0.127 ± 0.012) L/(h·kg), MRT(0-24) were (2.68 ± 0.229) h and (5.945 ± 0.479) h, respectively. It could be clearly seen that t1/2β of liposome prolonged (p < 0.05), AUC and MRT both increased remarkably (p < 0.01), CL/F decreased. Results indicated that this preparation has more residence time and exhibits some sustained–release tendency.
Top