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.
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.
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.
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.
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.
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