Liu S, Guo D, Guo Y, Zhou W
College of Veterinary Medicine, Huazhong Agricultural University, Wuhan, Hubei, China.
J Vet Pharmacol Ther. 2011 Feb;34(1):35-41. doi: 10.1111/j.1365-2885.2010.01190.x.
The objective of this study was to prepare ceftiofur sodium liposomes and assess their physical properties, stability, antibacterial effects, and pharmacokinetics. These liposomes appeared as a milky, light yellow suspension with encapsulation efficiency at 57.2 ± 1.17%, and there were no significant changes in all estimated indexes at 4 °C for 90 days. The minimum inhibitory concentrations of liposomes were all 1/4th that of ceftiofur sodium against Streptococcus suis, Staphylococcus aureus, Escherichia coli, and Salmonella enteritidis. Six healthy, adult cows in two treatment groups were dosed intravenously with ceftiofur sodium liposomes and ceftiofur sodium, serial blood samples collected, and plasma concentrations determined by high performance liquid chromatography. Intravenous plasma concentration profiles of liposomes best fit a two-compartment model and the elimination half-life was 2.11 times that of ceftiofur sodium. Thus, this liposome preparation provided therapeutically effective plasma concentrations for a longer duration than with the drug alone, making it more effective and convenient for use in treating bovine mastitis that requires long duration maintenance of therapeutic plasma concentrations.
本研究的目的是制备头孢噻呋钠脂质体，并评估其物理性质、稳定性、抗菌效果和药代动力学。这些脂质体呈乳白色、浅黄色悬浮液，包封率为57.2±1.17%，在4℃下放置90天，所有评估指标均无显著变化。脂质体对猪链球菌、金黄色葡萄球菌、大肠杆菌和肠炎沙门氏菌的最低抑菌浓度均为头孢噻呋钠的1/4。将两个治疗组的六头健康成年奶牛静脉注射头孢噻呋钠脂质体和头孢噻呋钠，采集系列血样，并用高效液相色谱法测定血浆浓度。脂质体的静脉血浆浓度曲线最符合二室模型，消除半衰期是头孢噻呋钠的2.11倍。因此，这种脂质体制剂比单独使用药物能在更长时间内提供治疗有效的血浆浓度，使其在治疗需要长时间维持治疗性血浆浓度的牛乳腺炎时更有效、更方便。
