scholarly journals Bioavailability pharmacokinetics and residues of marbofloxacin in normal and E.coli infected broiler chicken

2016 ◽  
Vol 4 (2) ◽  
pp. 144
Author(s):  
Ashraf El-Komy ◽  
Taha Attia ◽  
Amera Abd El Latif ◽  
Hanem Fathy
Keyword(s):  
Oral Administration ◽  
Half Life ◽  
Broiler Chickens ◽  
Volume Of Distribution ◽  
Pharmacokinetic Parameters ◽  
Maximum Serum ◽  
Elimination Half Life ◽  
Elimination Half ◽  
Total Body

The pharmacokinetics of marbofloxacin was studied following a single intravenous, oral administration in normal broiler chickens and repeated oral administrations in normal and experimentally E.coli infected broiler chickens. The pharmacokinetic parameters following a single intravenous injection of 2 mg/kg b.wt., revealed that marbofloxacin obeyed a two compartments open model, distribution half-life (t0.5(α)) was 0.25±0.02 h, volume of distribution (Vdss) was 0.76±0.08 L/kg, elimination half-life (t0.5(β)) was 5.43±0.87 h and total body clearance (CLtot) was 0.09±0.002 l/kg/h. Following a single oral administration, marbofloxacin was rapidly and efficiently absorbed through gastrointestinal tract of chickens as the absorption half-life (t0.5 (ab): 0.62±0.02 h). Maximum serum concentration (Cmax) was 1.15±0.01 μg/ml, reached its maximum time (tmax) at 2.53±0.04 h, elimination half-life (t0.5 (el)) was 7.36±0.20 h indicating the tendency of chickens to eliminate marbofloxacin in slow rate. Oral bioavailability was 73.57± 1.90 % indicating good absorption of marbofloxacin after oral administration. Serum concentrations of marbofloxacin following repeated oral administration of 2 mg/kg b.wt. once daily for five consecutive days, peaked 2 hours after each oral dose with lower significant values recorded in experimentally infected broiler chickens than in normal ones. Tissues residues of marbofloxacin in slaughtered normal chickens was highly in those tissues lung, liver, and kidneys in chickens and the chicken must not be slaughtered before 3 days of stopping of drug administration. It was concluded that the in- vitro protein binding was 12.33±0.82%.

scholarly journals Pharmacokinetics, tissue residues of tilmicosin phosphate (tilmicor-al®) and its in vitro and in vivo evaluation for the control of Mycoplas-ma gallisepticum infection in broiler chickens

2017 ◽  
Vol 5 (1) ◽  
pp. 11 ◽  
Author(s):  
Mohamed Elbadawy ◽  
Mohamed Aboubakr
Keyword(s):  
Half Life ◽  
Broiler Chickens ◽  
Peak Plasma ◽  
Clinical Signs ◽  
In Vivo Evaluation ◽  
Elimination Half Life ◽  
Elimination Half ◽  
Residue Study

The aim of present study was to determine the pharmacokinetics and tissue residues of tilmicosin phosphate (tilmicoral®) as well as its in vitro and in vivo evaluation for control of Mycoplasma gallisepticum (MG) infection in broiler chickens. Pharmacokinetics (single oral dose) and tissues residues (daily for five days) of tilmicosin (25 mg/kg b.wt) in broilers were investigated. Peak plasma concentration of tilmicosin was 1.25±0.0.09 μg/mL and achieved at 3.15±0.34 h. Elimination half-life was long (44.3±7.22 h) and Vdarea was large (1.25±0.082 L/kg). Residue study revealed a good distribution and penetration of tilmicosine in lung, liver, kidney and muscles. Tilmicosin could not be detected in all tested tissues (except in lung) at 6 days after last administration. The MIC of tilmicosin and tylosin against MG were 0.054 and 0.319 μg/mL, respectively. MG infected chickens and treated by tilmicosin or tylosin showed a significant (p<0.05) improvement in mean body weights gain and a significant (p<0.05) decline in mean clinical signs score, air sac lesion score and mortality rate, however tilmicosin was a superior drug. In conclusion, timicoral® was a very effective medication for controlling MG infection in broiler chickens due to its rapid absorption, long elimination half-life, rapid and extensive penetration from blood into tissues especially lungs and air sacs. Additionally, tilmicoral® had a short withdrawal time. Moreover, its superior efficacy (in vitro and in vivo) against MG.

scholarly journals JPC-2997, a New Aminomethylphenol with HighIn VitroandIn VivoAntimalarial Activities against Blood Stages of Plasmodium

2014 ◽  
Vol 59 (1) ◽  
pp. 170-177 ◽  
Author(s):  
Geoffrey W. Birrell ◽  
Marina Chavchich ◽  
Arba L. Ager ◽  
Hong-Ming Shieh ◽  
Gavin D. Heffernan ◽  
...  
Keyword(s):  
Half Life ◽  
Multidrug Resistant ◽  
Volume Of Distribution ◽  
Parasite Line ◽  
Content Type ◽  
Elimination Half Life ◽  
Highly Active ◽  
Elimination Half

ABSTRACT4-(tert-Butyl)-2-((tert-butylamino)methyl)-6-(6-(trifluoromethyl)pyridin-3-yl)-phenol (JPC-2997) is a new aminomethylphenol compound that is highly activein vitroagainst the chloroquine-sensitive D6, the chloroquine-resistant W2, and the multidrug-resistant TM90-C2BPlasmodium falciparumlines, with 50% inhibitory concentrations (IC50s) ranging from 7 nM to 34 nM. JPC-2997 is >2,500 times less cytotoxic (IC50s > 35 μM) to human (HepG2 and HEK293) and rodent (BHK) cell lines than the D6 parasite line. In comparison to the chemically related WR-194,965, a drug that had advanced to clinical studies, JPC-2997 was 2-fold more activein vitroagainstP. falciparumlines and 3-fold less cytotoxic. The compound possesses potentin vivosuppression activity againstPlasmodium berghei, with a 50% effective dose (ED50) of 0.5 mg/kg of body weight/day following oral dosing in the Peters 4-day test. The radical curative dose of JPC-2997 was remarkably low, at a total dose of 24 mg/kg, using the modified Thompson test. JPC-2997 was effective in curing threeAotusmonkeys infected with a chloroquine- and pyrimethamine-resistant strain ofPlasmodium vivaxat a dose of 20 mg/kg daily for 3 days. At the doses administered, JPC-2997 appeared to be well tolerated in mice and monkeys. Preliminary studies of JPC-2997 in mice show linear pharmacokinetics over the range 2.5 to 40 mg/kg, a low clearance of 0.22 liters/h/kg, a volume of distribution of 15.6 liters/kg, and an elimination half-life of 49.8 h. The highin vivopotency data and lengthy elimination half-life of JPC-2997 suggest that it is worthy of further preclinical assessment as a partner drug.

Dose-Ranging Pharmacokinetic Study of Ciprofloxacin after 200-, 300-, and 400-mg Intravenous Doses

1992 ◽  
Vol 26 (1) ◽  
pp. 8-10 ◽  
Author(s):  
David E. Nix ◽  
J. Michael Spivey ◽  
Allyn Norman ◽  
Jerome J. Schentag
Keyword(s):  
Steady State ◽  
Half Life ◽  
Total Body Clearance ◽  
Volume Of Distribution ◽  
Elimination Half Life ◽  
Elimination Half ◽  
The Mean ◽  
Total Body ◽  
Venous Irritation ◽  
Body Clearance

OBJECTIVE: To assess the pharmacokinetics and tolerance of ciprofloxacin after the administration of single intravenous doses of 200, 300, and 400 mg. DESIGN: Double-blind, three-period, randomized, crossover trial. SETTING: Private, university-affiliated, hospital-based, clinical research center. PATIENTS: Normal healthy male volunteers, 18–40 years of age. INTERVENTIONS: Subjects received 200-, 300-, and 400-mg single intravenous doses of ciprofloxacin via 30-minute infusions in random sequence. MAIN OUTCOME MEASURES: Serum ciprofloxacin concentrations were determined by HPLC after each dose and the results were used to derive pharmacokinetic parameters. Tolerance was assessed by reported and observed adverse events, urine microscopic examinations for crystals, and examination of intravenous infusion sites. RESULTS: The mean area under the time curve (AUC) values displayed linearity with respect to the administered dose. No statistical differences were observed in total body clearance, steady-state volume of distribution, or elimination half-life with respect to dose administered. The mean total body clearance, steady-state volume of distribution, or elimination half-life ranged from 36 to 41 L/h, 146 to 169 L, and 3.5 to 3.7 h for the 200-, 300-, and 400-mg doses, respectively. Adverse effects, including venous irritation (four subjects) and crystalluria (two subjects), were mild and did not require withdrawal of any subject from the study. CONCLUSIONS: Intravenous ciprofloxacin in doses ranging from 200 to 400 mg demonstrated linear pharmacokinetics. These single doses were well tolerated, although cases of transient venous irritation and crystalluria were observed.

scholarly journals Disposition Kinetic of Moxifloxacin following Intravenous, Intramuscular, and Subcutaneous Administration in Goats

2011 ◽  
Vol 2011 ◽  
pp. 1-5
Author(s):  
Harshad B. Patel ◽  
Shailesh K. Mody ◽  
Hitesh B. Patel ◽  
Vipul A. Patel ◽  
Urvesh D. Patel
Keyword(s):  
Drug Concentration ◽  
Half Life ◽  
Total Body Clearance ◽  
Volume Of Distribution ◽  
The Body ◽  
Maximum Plasma ◽  
Elimination Half Life ◽  
Elimination Half ◽  
Total Body ◽  
Body Clearance

The present study was carried out to investigate disposition kinetics of moxifloxacin following single-dose intravenous (i.v.), intramuscular (i.m.), and subcutaneous (s.c.) administration at a dose rate of 5 mg/kg of body weight (b.wt.) in goats. Plasma samples collected after treatments were analyzed for drug concentration using high-performance liquid chromatography (HPLC). After i.v. administration, distribution of the drug was rapid and wide as reflected by high steady-state volume of distribution. Drug elimination was relatively faster with a total body clearance of 0.59±0.03 L/h/kg. Following i.m. injection, the drug has shown the rapid and near-to-complete absorption with bioavailability of 98.20±3.96 per cent. The maximum plasma drug concentration (Cmax) of 1.21±0.04 μg/mL was attained at 1 h (Tmax). The drug was widely distributed as reflected by high apparent volume of distribution. The elimination half-life (t1/2β) of the drug was 6.26±0.08  h. Following s.c. administration, the drug was rapidly absorbed (Cmax: 1.16±0.02 μg/mL; tmax: 1 h) and slowly eliminated from the body. The elimination half-life and total body clearance (ClB) were 5.61±0.10 h and 0.60±0.03 L/h/kg, respectively. The bioavailability of moxifloxacin following s.c. administration was 90.44±3.96 per cent.

scholarly journals Pharmacokinetics of Isepamicin during Continuous Venovenous Hemodiafiltration

1999 ◽  
Vol 43 (10) ◽  
pp. 2409-2411 ◽  
Author(s):  
Dominique Breilh ◽  
Bernard Allaouchiche ◽  
Hélène Jaumain ◽  
Paul Boulétreau ◽  
Dominique Chassard ◽  
...  
Keyword(s):  
Half Life ◽  
Initial Dosage ◽  
Volume Of Distribution ◽  
Elimination Half Life ◽  
Continuous Venovenous Hemodiafiltration ◽  
Concentration Peak ◽  
Elimination Half ◽  
The Mean ◽  
Total Body ◽  
Body Clearance

ABSTRACT The objective of this study was to analyze the pharmacokinetics of isepamicin during continuous venovenous hemodiafiltration. Six patients received 15 mg of isepamicin per kg of body weight. The mean isepamicin concentration peak in serum was 62.88 ± 18.20 mg/liter 0.5 h after the infusion. The elimination half-life was 7.91 ± 0.83 h. The mean total body clearance was 1.75 ± 0.28 liters/h, and dialysate outlet (DO) clearance was 2.76 ± 0.59 liters/h. The mean volume of distribution was 19.83 ± 2.95 liters. The elimination half-life, DO clearance, and volume of distribution were almost constant. In this group of patients, the initial dosage of 15 mg/kg appeared to be adequate, but the dosage interval should be determined by monitoring residual isepamicin concentrations in plasma.

scholarly journals Disposition of intravenous metronidazole in Asian surgical patients.

1996 ◽  
Vol 40 (10) ◽  
pp. 2248-2251 ◽  
Author(s):  
T Y Ti ◽  
H S Lee ◽  
Y M Khoo
Keyword(s):  
Half Life ◽  
Inverse Correlation ◽  
Volume Of Distribution ◽  
Population Based ◽  
Surgical Patients ◽  
Pharmacokinetic Analysis ◽  
Elimination Half Life ◽  
Elimination Half ◽  
The Mean ◽  
Total Body

Steady-state peak and trough concentrations of metronidazole and its metabolites were measured in the sera of 54 surgical patients who were on intravenous metronidazole, 500 mg every 8 h. These patients had no significant renal or hepatic impairment. High-pressure liquid chromatography was used to determine the concentrations of metronidazole and its metabolites. The mean peak and trough metronidazole concentrations were 28.9 +/- 11.0 and 18.0 +/- 9.9 micrograms/ml, respectively. The acid metabolite was not detectable in all the blood specimens. The mean peak concentration of the hydroxy metabolite (MH) was 6.6 +/- 4.3 micrograms/ml, the mean trough concentration of MH was 6.2 +/- 4.2 micrograms/ml, and the MH concentration/metronidazole concentration ratio was 0.4 +/- 0.24. Using a population-based method for the pharmacokinetic analysis and stepwise regression between parameters and covariables (sex, age, and weight), we found that weight showed the highest correlation with the total body clearance (CL). The mean CL was 0.89 +/- 0.3 ml min-1 kg-1 (3.029 liters/h), the mean volume of distribution was 0.73 +/- 0.14 liter/kg, and the mean elimination half-life was 10.6 +/- 4.5 h. For the patients in our study, the CL was lower and the elimination half-life was longer compared with those for healthy volunteers, but the values of these parameters were comparable to those found for hospitalized patients. There was an inverse correlation between age and CL.

scholarly journals Formulation And In-Vitro Evaluation Of Cocrystals Of Pantoprazole Sodium For Immediate Release

2021 ◽  
Vol 9 (1) ◽  
Author(s):  
Shiwangi Jain ◽  
Mayank Bansal ◽  
Ashutosh Sharma
Keyword(s):  
Half Life ◽  
Serum Proteins ◽  
Immediate Release ◽  
Volume Of Distribution ◽  
Current Approach ◽  
Total Serum ◽  
Elimination Half Life ◽  
Elimination Half ◽  
Acid Labile

Pantoprazole is extensively metabolized in the liver and has a total serum clearance of 0.1 l/h/kg, a serum elimination half-life of about 1.1 h, and an apparent volume of distribution of 0.15 L/kg. 98% of pantoprazole is bound to serum proteins. Elimination half-life, clearance, and volume of distribution are independent of the dose. Almost 80% of an oral or intravenous dose is excreted as metabolites in urine; the remainder is found in feces and originates from biliary secretion. The clearance of pantoprazole is only slightly affected by age, with its half-life being approximately 1.25 h in the elderly. Pantoprazole is an acid labile drug that requires protection from degradation in acidic media. Hence, co-crystallization of pantoprazole sodium with appropriate co-formers will inhibit its degradation in acidic medium ensuring fast release in the stomach. The acid-labile drugs for oral administration may also be protected from gastric acidity by inhibiting its degradation upon entering into acidic environment. So, the current approach includes co-crystallization of the provided drug with appropriate co-former which prevents degradation of drug by quick absorption and protects the drug from low pH. Apart from that, the formulations also modulate or control the drug release for an immediate action. Keywords: Pantoprazole sodium, Co-crystal, solvent drop method, Co-former.

scholarly journals Propofol

2008 ◽  
Vol 109 (6) ◽  
pp. 1132-1136 ◽  
Author(s):  
Paul F. White ◽  
David S. Warner
Keyword(s):  
Half Life ◽  
Compartment Model ◽  
Volume Of Distribution ◽  
Major Surgery ◽  
Anesthetic Technique ◽  
General Anesthetic ◽  
Clearance Rates ◽  
Elimination Half Life ◽  
Elimination Half ◽  
Total Body

Pharmacokinetics and pharmacodynamics of propofol infusions during general anesthesia. By Audrey Shafer, Van A. Doze, Steven L. Shafer, and Paul F. White. Anesthesiology 1988; 69:348-56. Reprinted with permission.The pharmacokinetic and pharmacodynamic properties of propofol (Diprivan) were studied in 50 elective surgical patients. Propofol was administered as a bolus dose, 2 mg/kg iv, followed by a variable-rate infusion, 0-20 mg/min, and intermittent supplemental boluses, 10-20 mg iv, as part of a general anesthetic technique that included nitrous oxide, meperidine, and muscle relaxants. For a majority of the patients (n = 30), the pharmacokinetics of propofol were best described by a two-compartment model. The propofol mean total body clearance rate was 2.09 +/- 0.65 l/min (mean +/- SD), the volume of distribution at steady state was 159 +/- 57 l, and the elimination half-life was 116 +/- 34 min. Elderly patients (patients older than 60 yr vs. those younger than 60 yr) had significantly decreased clearance rates (1.58 +/- 0.42 vs. 2.19 +/- 0.64 l/min), whereas women (vs. men) had greater clearance rates (33 +/- 8 vs. 26 +/- 7 ml x kg x min ) and volumes of distribution (2.50 +/- 0.81 vs. 2.05 +/- 0.65 l/kg). Patients undergoing major (intraabdominal) surgery had longer elimination half-life values (136 +/- 40 vs. 108 +/- 29 min). Patients required an average blood propofol concentration of 4.05 +/- 1.01 micrograms/ml for major surgery and 2.97 +/- 1.07 micrograms/ml for nonmajor surgery. Blood propofol concentrations at which 50% of patients (EC50) were awake and oriented after surgery were 1.07 and 0.95 microgram/ml, respectively. Psychomotor performance returned to baseline at blood propofol concentrations of 0.38-0.43 microgram/ml (EC50). This clinical study demonstrates the feasibility of performing pharmacokinetic and pharmacodynamic analyses when complex infusion and bolus regimens are used for administering iv anesthetics.

scholarly journals Plasma disposition of cefoperazone after single intravenous and intramuscular administrations in camels (Camelus dromedarius)

2018 ◽  
Vol 66 (3) ◽  
pp. 444-450
Author(s):  
Mohamed Aboubakr ◽  
Ahmed Soliman ◽  
Kamil Uney ◽  
Muammer Elmas
Keyword(s):  
Half Life ◽  
High Performance ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Volume Of Distribution ◽  
Camelus Dromedarius ◽  
Promising Alternative ◽  
Elimination Half Life ◽  
Elimination Half ◽  
Total Body

The plasma disposition of cefoperazone was investigated after intravenous (IV) and intramuscular (IM) administrations of 20 mg/kg as a single dose in six camels (Camelus dromedarius) in a crossover design. Blood plasma samples were analysed by high-performance liquid chromatography (HPLC). After IV administration, elimination half-life (t1/2β), volume of distribution at steady state (Vdss), total body clearance (Cltot) and mean residence time (MRT) of cefoperazone were 1.95 h, 0.38 L/kg, 0.17 L/h/kg and 2.16 h, respectively. After IM administration of cefoperazone, peak plasma concentration (Cmax) was 21.95 μg/mL and it was obtained at (tmax) 1.23 h. Absorption half-life (t1/2ab), elimination half-life and mean absorption time were 0.45 h, 2.84 h and 2.07 h, respectively. The bioavailability of cefoperazone was 89.42%. The lack of local reaction or any other adverse effects and the very good bioavailability following IM administration indicate that cefoperazone might be a promising alternative treatment for a variety of infectious diseases in camels.

scholarly journals Pharmacokinetics and bioavailability of doxycycline in fasted and nonfasted broiler chickens

2001 ◽  
Vol 49 (1) ◽  
pp. 31-37 ◽  
Author(s):  
P. Laczay ◽  
G. Semjén ◽  
J. Lehel ◽  
G. Nagy
Keyword(s):  
Half Life ◽  
Broiler Chickens ◽  
Volume Of Distribution ◽  
The Body ◽  
Absolute Bioavailability ◽  
Elimination Half ◽  
Influence Of Food ◽  
Maximal Plasma ◽  
The Absolute ◽  
Total Body

The pharmacokinetics and the influence of food on the kinetic profile and bioavailability of doxycycline was studied after a single intravenous (i.v.) and oral dose of 10.0 mg/kg body weight in 7-week-old broiler chickens. Following i.v. administration the drug was rapidly distributed in the body with a distribution half-life of 0.21 ± 0.01 h. The elimination half-life of 6.78 ± 0.06 h was relatively long and resulted from both a low total body clearance of 0.139 ± 0.007 L/h·kg and a large volume of distribution of 1.36 ± 0.06 L/kg. After oral administration to fasted chickens, the absorption of doxycycline was quite fast and substantial as shown by the absorption half-life of 0.39 ± 0.03 h, the maximal plasma concentration of 4.47 ± 0.16 —g/mL and the time to reach the Cmax of 1.73 ± 0.06 h. The distribution and the final elimination of the drug were slower than after i.v. administration. The absolute bioavailability was 73.4 ± 2.5%. The presence of food in the intestinal tract reduced and extended the absorption (t1/2a = 1.23 ± 0.21 h; Cmax = 3.07 ± 0.23 µg/mL; tmax = 3.34 ± 0.21 h). The absolute bioavailability was reduced to 61.1% ± 4.4%.

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