Zhang S, Dai W, Lu Z, Lei Z, Yang B, He B, Zhou H, Cao J
College of Veterinary Medicine, Huazhong Agricultural University, Wuhan, Hubei, China.
Unit of Animal Infectious Diseases, State Key Laboratory of Agricultural Microbiology, Huazhong Agricultural University, Wuhan, Hubei, China.
J Vet Pharmacol Ther. 2018 Feb;41(1):117-124. doi: 10.1111/jvp.12429. Epub 2017 Jun 27.
Cefquinome (CEF) is widely used for veterinary clinical applications because of its broad spectrum and high efficiency. However, frequent administrations are required due to its short elimination half-life. In this study, cefquinome sulfate gelatin microspheres (CEF-GMS) were prepared as a sustained-release formulation using emulsion chemical cross-linking technique. Physical properties, stability, sustained-release property in vitro, and pharmacokinetics in pigs were assessed. The morphology of CEF-GMS showed a good sphericity with porous structure on the surface, and the mean diameter was 8.80 ± 0.78 μm, with 90.60 ± 3.98% of the total in the range of 5-20 μm. There were no significant changes of all estimated indexes in the stability tests. In vitro drug release study showed that the release of CEF from CEF-GMS was much slower than that from crude CEF in a release medium. Pharmacokinetic characteristics were evaluated following intramuscular administration of CEF-GMS or Cefquinome sulfate injection (CEF-Inj) in pigs at a dosage of 4 mg CEF/kg body weight. The plasma drug concentration-time data of CEF-GMS and CEF-Inj were both best fitted by two-compartment models with first-order absorption, and the elimination half-life of CEF-GMS was almost 10 times that of CEF-Inj. Overall, CEF-GMS might be used as a sustained-release formulation of CEF for veterinary clinical applications.
头孢喹肟（CEF）因其广谱高效而被广泛应用于兽医临床。然而，由于其消除半衰期短，需要频繁给药。在本研究中，采用乳液化学交联技术制备了硫酸头孢喹肟明胶微球（CEF-GMS）作为缓释制剂。评估了其物理性质、稳定性、体外缓释性能以及在猪体内的药代动力学。CEF-GMS的形态呈良好的球形，表面具有多孔结构，平均直径为8.80±0.78μm，5-20μm范围内的占总量的90.60±3.98%。稳定性试验中所有评估指标均无显著变化。体外药物释放研究表明，在释放介质中，CEF从CEF-GMS中的释放比从粗品CEF中的释放要慢得多。以4mg CEF/kg体重的剂量对猪肌肉注射CEF-GMS或硫酸头孢喹肟注射液（CEF-Inj）后评估药代动力学特征。CEF-GMS和CEF-Inj的血浆药物浓度-时间数据均最适合一级吸收的二室模型，且CEF-GMS的消除半衰期几乎是CEF-Inj的10倍。总体而言，CEF-GMS可作为CEF的缓释制剂用于兽医临床。
