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Öğe Comparative pharmacokinetics of free and liposome-encapsulated ampicillin after intravenous and subcutaneous administrations(NATL VETERINARY RESEARCH INST, 2004) Yapar, K; Bas, ALPharmacokinetic 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.Öğe Concentrations of sulfadoxine and trimethoprim in plasma, lymph fluids and some tissues 24 H after intramuscular administration to angora goats(TAYLOR & FRANCIS LTD, 1998) Tras, B; Elmas, M; Yazar, E; Bas, AL; Keskin, E; Dasci, ZThis study was carried out to determine the concentrations of sulfadoxine and trimethoprim in plasma, lymph, and some tissues in goats after administration of a single recommended therapeutic dose. Five healthy, adult Angora goats were used. The drug combination, containing 200 mg sulfadoxine and 40 mg trimethoprim per millilitre, was given as a single IM injection at the recommended dose level, 15 mg/kg body weight for sulfadoxine and 3 mg/kg body weight for trimethoprim. The goats were slaughtered 24 hours after drug administration and samples were taken from liver, bone marrow, pelvic limb muscles, hepatic, thoracic duct, and the pelvic limb lymph fluids for analysis of drug concentrations by HPLC. The concentrations of trimethoprim in bone marrow, liver, pelvic limb muscles, hepatic lymph, the pelvic limb lymph, and thoracic duct lymph were found to be 6, 5, 4, 2, 5 and 15 times higher than those of plasma, respectively. Although the sulfadoxine concentrations in bone marrow, pelvic limb muscles, and liver were 2, 3 and 2 times higher than the plasm concentrations, respectively, the sulfadoxine concentrations in hepatic lymph, the pelvic limb lymph, and thoracic duct lymph were lower than those of plasma. The results show that the trimethoprim concentrations in lymph fluids were quite similar to those in tissues. However, the sulfadoxine concentrations in lymph fluids were different in each tissue.Öğe 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, KThis 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.Öğe Effects of different doses of tilmicosin on malondialdehyde and glutathione concentrations in mice(VETERINARNI A FARMACEUTICKA UNIVERZITA BRNO, 2004) Yazar, E; Oztekin, E; Sivrikaya, A; Col, R; Elmas, M; Bas, ALThe aim of this study was to follow the effects of different doses of tilmicosin on malondialdehyde and reduced glutathione levels of heart and liver, and on selected haematological indices. Forty male Balb/C mice were used throughout the experiment. They were divided into four groups (n = 10), and injected subcutaneously as follows: Group I (control), with isotonic saline solution, Group 2 with 25 mg/kg body weight of tilmicosin, Group 3 with 50 mg/kg, and Group 4 with 75 mg/kg of tilmicosin in single injections. After three days, plasma, cardiac and hepatic malondialdehyde and reduced glutathione levels were measured with spectrophotometer. Red blood cell, white blood cell, platelet, haemoglobin, packed cell volume and percentage of leukocytes were also determined. At the end of the experiment, tilmicosin did not cause any statistically significant (P > 0.05) changes in haematological parameters such as red blood cells, white blood cells, platelet, haemoglobin, packed cell volume and percentage of leukocytes. Hepatic malondialdehyde and reduced glutathione levels increased (P < 0.05) only at the highest dose of tilmicosin. The results indicate that tilmicosin did not cause lipid peroxidation in the heart.Öğe Effects of vitamin E and prednisolone on biochemical and haematological parameters in endotoxaemic New Zealand white rabbits(NATL VETERINARY RESEARCH INST, 2004) Yazar, E; Col, R; Konyalioglu, S; Birdane, YO; Elmas, M; Bas, ALEffects of prednisolone and vitamin E on biochemical and haematological values were investigated in endotoxaemic rabbits. Forty rabbits were used and divided into four equal groups. Group I served as the control group; group 2 was infused with lipopolysaccharide (LPS) for 6 h; group 3 was injected with prednisolone before LPS administration; group 4 was injected with vitamin E for 4 consecutive days before LPS administration. Serum and blood samples were collected 8 h after the onset of LPS injection. Serum myoglobin, alanine aminotransferase, gamma glutamyl transferase, amylase, total bilirubin, direct bilirubin, creatinine, blood urea nitrogen, albumin, globulin, total protein, cholesterol, total lipids, triglycerides, low density lipoprotein, very low density lipoprotein, sodium, potassium and magnesium contents were measured. Red blood cell, white blood cell, platelet counts and percentage of differential leukocyte values were determined. It was found that prednisolone and vitamin E had a protective effect in endotoxaemic shock. Prednisolone was more effective in endotoxaemia than vitamin E.Öğe Effects of vitamin E and prednisolone on some oxidative stress markers in endotoxemic rabbits(ECOLE NATIONALE VETERINAIRE TOULOUSE, 2004) Yazar, E; Konyalioglu, S; Col, R; Birdane, YO; Bas, AL; Elmas, MEffects of prednisolone (PR) and vitamin E (VE) on oxidative stress and antioxidant systems were investigated in endotoxemic rabbits. Forty rabbits were used and divided into four equal groups. Group I served as the control group. In group II, lipopolysaccharide (LPS, 100 mug/kg/h) was infused for 6 hours, whereas rabbits of groups III and IV received prior treatments with subcutaneous injection of prednisolone (10 mg/kg) (group III) or with intraperitoneous injections of vitamin E (10 mg/kg) for 4 consecutive days (group IV). Serum, liver, heart and kidney samples were obtained at 8 hours after infusion. Malonedialdehyde (MDA), glutathione (GSH) concentrations and superoxide dismutase (SOD), catalase (CAT) activities were spectrophotometrically determined in tissues plus in serum (for MDA). LPS caused statistically significant (p<0.05) increases of MDA and antioxidants in serum and in all tissues. PR and VE significantly (p<0.05) suppressed increases of MDA, SOD, CAT and GSH. As a consequence, prednisolone and vitamin E had protective effects on oxidative stress in endotoxemic rabbits.Öğe Efficacies of liposome-encapsulated enrofloxacin against Staphylococcus aureus infection in Anatolian shepherd dog monocytes in vitro(M H SCHAPER GMBH CO KG, 2005) Bas, AL; Simsek, A; Erganis, O; Corlu, MThe aim of this study was to evaluate the intracellular activity of two types of liposome-encapsulated enrofloxacin (LE) compared with free enrofloxacin and non-treated control against Staphylococcus aureus, phagocytosed by monocytes in healthy Anatolian Shepherd dogs. Enrofloxacin was encapsulated with two different types of liposome in multilamellar large vesicles (MLV). Type A MLV were composed of 15 mg phosphatidylcholine and 35 mg cholesterol, Type B MLV were composed of phosphatidylcholine, cholesterol and enrofloxacin in a molar ratio of 1:1:1. Intracellular activity was estimated by comparing the numbers of bacteria surviving intracellularly in monocytes exposed to free enrofloxacin and LE for 4 h at the doses of 0.25, 0.5 and 1 mu g/ml, with those surviving intracellularly in untreated control monocytes. All three forms of enrofloxacin (free, Type A and B liposomes) increased the intracellular killing of S. aureus in a concentration dependent manner. Comparison of 1 mu g/ml Type B LE revealed that killing activity was significantly higher than those of other concentrations. The results showed that LE was superior in reducing the number of intracellularly located bacteria compared to the free drug and control. The beneficial effect of liposomal encapsulation is presumably due to the fact that both liposomes and bacteria are localized at the same spot in phagocytic cells.Öğe 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, BIntraphagocytic (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.
