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    Comparative pharmacokinetics of free and liposome-encapsulated ampicillin after intravenous and subcutaneous administrations
    (NATL VETERINARY RESEARCH INST, 2004) Yapar, K; Bas, AL
    Pharmacokinetic properties of liposome-encapsulated (LEA) and free (FA) ampicillin after intravenous (IV) and subcutaneous (SC) administrations were compared in sheep. Six healthy adult sheep were used in this study. Ampicillin was encapsulated in multilamellar large vesicles (MLV). FA and LEA were administered at a single recommended dose (5 mg/kg) to the same individual sheep at 1-week interval. Concentrations of the drug in serum were determined by HPLC. Results indicated that, when LEA was administered IV and SC, mean residence time (MRT), elimination half-life (t(1/2beta)) and the volume of distribution (V-d) were higher (P<0.05), and clearance (Cl) was lower (P<0.05) than in the case of the free form. When the drug was administered SC, the area under the curve (AUC) and the time to peak concentration (t(max)) were significantly higher (P<0.05), and maximum concentration (C-max) of LEA was lower than those of the free form. The results obtained in the present study shown that liposome encapsulated ampicillin provided the effective and prolonged serum concentration after IV and SC administration.
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    Disposition and milk levels of sulfadiazine-trimethoprim combination following intrauterine bolus administration in lactating cows during postpartum
    (ECOLE NATIONAL VET TOULOUSE, 1999) Elmas, M; Tras, B; Bas, AL; Yazar, E; Nizamlioglu, F; Colak, M; Yapar, K
    This study was carried out to describe the disposition and milk levels of sulfadiazine (SDZ)-trimethoprim (TMP) combination following intrauterine bolus administration in cows during postpartum. Six cows were used as materials. SDZ-TMP combination bolus was given through intrauterine administration at the recommended dose of 4 g of SDZ plus 0.8 g of TMP to each animal during postpartum. Concentrations of SDZ and TMP were determined by HPLC. The absorption half-lives of SDZ and TMP were 1.44 and 1.68 hours, respectively. The elimination half-life of SDZ was 3.74 hours, while it was 11.04 hours for TMP. SDZ did not reach to MIC levels in plasma and milk after the intrauterine administration. After intrauterine administration, TMP was detected at the effective levels in milk. These results suggest that passing ratio of antimicrobials into milk should be taken into consideration for drug administrations into uterine in lactating cows during postpartum.
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    Intraphagocytic concentrations of free and liposome encapsulated ampicillin in sheep after intravenous infusion
    (NATL VETERINARY RESEARCH INST, 2006) Yazar, E; Bas, AL; Yapar, K; Birdane, YO; Elmas, M; Tras, B
    Intraphagocytic (neutrophil and monocyte) concentrations of free and liposome encapsulated ampicillin were investigated in sheep. The ampicillin (5 mg/kg b.wt.) was administered as intravenous infusion. Blood samples were collected at 0, 10, 30, and 60 min, and 2 and 4 h after the infusion. Neutrophils and monocytes were isolated and lysed. Ampicillin concentrations were measured by high performance liquid chromatography. As results, liposome encapsulated ampicillin caused higher intracellular concentrations in neutrophils (ratio of liposome encapsulated ampicillin/free ampicillin; from 1.736 to 2.511) and monocytes (ratio of liposome encapsulated ampicillin/free ampicillin from 2.041 to 4.384) than free ampicillin. Liposome encapsulated ampicillin also existed longer time within neutrophils (2 h) and monocytes (2 h) than free ampicillin (60 min). This formulation may be beneficial in the treatment of intracellular bacterial infections.