scholarly journals Experimental determination of the pharmacokinetic properties of trimethoprim and sulfamethoxazole combination in the blood serum of broiler chickens

Author(s):  
K Putecova ◽  
K Nedbalcova ◽  
I Bartejsova ◽  
M Zouharova ◽  
K Matiaskova ◽  
...  

A rapid, simple and highly efficient analytical method for the targeted determination of trimethoprim and sulfamethoxazole in serum samples has been developed and used to measure the pharmacokinetic curve of these medicinal substances after administration to chicken broilers. The pharmacokinetics properties of trimethoprim and sulfamethoxazole were investigated in clinically healthy broiler chickens after the single oral administration of the commercial preparation Methoxasol (Eurovet Animal Health, B.V., The Netherlands) at a dose of 0.275 ml/kg b.w. After a single dose drug administration, the chickens were sacrificed by decapitation under general anaesthesia by Isoflurin 1 000 mg/g (Vetpharma AH, Spain) and the blood was collected at precisely defined intervals: 15, 30, 45, 60, 90, 120, 180, 360 and 720 min after the administration. The serum concentrations of amoxicillin were determined using Q Exactive tandem mass spectrometer (Thermo Fisher Scientific, USA) in conjunction with liquid chromatography. The detected pharmacokinetic parameters of trimethoprim after the oral administration were C<sub>max</sub> = 2.1 ± 1.0 µg/ml; T<sub>max</sub> = 1.5 h; t<sub>½</sub> = 0.88 h; k<sub>el</sub> = 0.009 3 ± 0.001 1 1/h; AUC<sub>t</sub> = 2.901 ± 1.4 µg.h/ml; AUC<sub>∞</sub> = 2.907 ± 1.5 µg.h/ml; V<sub>d</sub> = 2.632 l/kg; Cl = 2.7 l/h. The pharmacokinetic parameters of sulfamethoxazole after the oral administration were C<sub>max</sub> = 47.1 ± 15.3 µg/ml; T<sub>max</sub> = 1 h; t<sub>½</sub> = 1.92 h; k<sub>el</sub> = 0.004 6 ± 0.000 3 1/h; AUC<sub>t</sub> = 89.676 ± 26.9 µg.h/ml; AUC<sub>∞</sub> = 94.612 ± 28.4 µg.h/ml; V<sub>d</sub> = 0.584 l/kg; Cl = 0.21 l/h. To the best of our knowledge, this is the first pharmacokinetic study of the combination of sulfamethoxazole and trimethoprim in broiler chickens.

2014 ◽  
Vol 58 (4) ◽  
pp. 573-579 ◽  
Author(s):  
Anna Gajda ◽  
Andrzej Posyniak ◽  
Grzegorz Tomczyk

Abstract For the purpose of quantitative determination of doxycycline (DC) residues in tissues, a sensitive liquid chromatography - tandem mass spectrometry (LC-MS/MS) method was developed. The method was used to determine DC residues in chicken tissues (breast and thigh muscle, liver and kidney) after oral administration with drinking water to five-weak-old broiler chickens. The DC was administered for five consecutive days at a therapeutic dose of 10 mg/kg b.w. once a day. The tissues were collected after 6 h, 24 h, 7 d, and 8 d. The method was validated and the decision limit was established for muscle - 109.2 μg/kg, for liver - 326.1 μg/kg, and for kidney - 634.0 μg/kg. The detection limit was 2 μg/kg and the limit of quantification was 5 μg/kg. In a short period after ceasing the treatment, the detected concentrations of DC were much higher than the established maximum residue limit values. The highest residue concentrations of DC were observed in the kidney, followed by the liver and muscle. The lowest concentration of DC was determined in tight muscle.


2021 ◽  
Vol 59 (5) ◽  
pp. 547-554
Author(s):  
B. S. Belov ◽  
L. P. Ananyeva

Lyme disease (LD) or tick-borne borreliosis affects thousands of people every year in different regions of the world, primarily the United States and Europe. In endemic areas, early LD is a common disease that requires high medical vigilance. Considering the extreme relevance of this problem for public health, in November 2020, the committee of experts of three American scientific societies published an updated version of the clinical guidelines for the prevention, diagnosis and treatment of LD, the main provisions of which are presented in this article. It is emphasized that in the absence of vaccines, the risk of LD and other diseases transmitted by ticks can be reduced by using personal protective equipment and repellents. Antibiotic prophylaxis is carried out by a single oral administration of doxycycline. In the laboratory diagnosis of LD, the determination of antibodies to B. burgdorfery in the blood serum is a first-line study. At the second stage, serum samples are examined using an immunoblot for IgM and IgG. The basis of treatment of LD is rational antibiotic therapy. The choice of an antibiotic depends on a number of factors, including the presence of extracutaneous manifestations of LD (neuroborreliosis, carditis, arthritis). The most commonly used are doxycycline, amoxicillin, cefuroxime-axetil and ceftriaxone.


2018 ◽  
Vol 15 (1) ◽  
pp. 74-81 ◽  
Author(s):  
Shuo Sun ◽  
Xue Zhang ◽  
Linda Luo ◽  
Ping Wang ◽  
Mengxuan Bai ◽  
...  

Introduction: A rapid, sensitive and convenient ultra-performance liquid chromatography with tandem mass spectrometric detection (UPLC-MS/MS) method has been validated and applied to the simultaneous determination of kirenol, rosmarinic acid and caffeic acid after oral administration of the extract of Manxingshizhen preparation in rat plasma. Materials and Methods: Puerarin was selected as the internal standard (IS). The plasma sample preparation was pretreated by liquid-liquid extraction of the mixture with ethyl acetate. All analytes were simultaneously detected in multiple reaction monitoring (MRM) mode via both the positive electrospray ionization (ESI+) and negative electrospray ionization (ESI). In the experiment, all calibration curves revealed good linearity (r > 0.999). The LLOQ were between 0.80-2.00 ng/mL, respectively. Besides, the intra-day and inter-day precision ranged from 6.4 to 13.8%, respectively. Moreover, the accuracy was within - 11.4% and 12.8% for all the QC levels of all analytes. The extraction recoveries of the analytes and IS in plasma at three concentration levels ranged from 88.5 to 103.2%, moreover, the matrix effects of all the analytes and the IS were found to be satisfied with the acceptable range of 89.8%-101.7%. Meanwhile, the RSD values of stability met the requirement of not more than 15%. Furthermore, the pharmacokinetic parameters of three compounds were analyzed using concentrationtime profiles. Conclusion and Results: Plasma concentrations of the three compounds were determined up to 24 h after oral administration, and their pharmacokinetic parameters were in agreement with previous studies. The validated method was successfully applied in a pharmacokinetic study in rat plasma after oral administration of Manxingshizhen preparation.


PLoS ONE ◽  
2017 ◽  
Vol 12 (7) ◽  
pp. e0181755 ◽  
Author(s):  
Arina Lopes de Lima ◽  
Fabiano Barreto ◽  
Renata Batista Rau ◽  
Guilherme Resende da Silva ◽  
Leonardo José Camargos Lara ◽  
...  

Author(s):  
H.B. Patel ◽  
U.D. Patel ◽  
C.M. Modi ◽  
V.C. Ladumor ◽  
C.N. Makwana ◽  
...  

Background: Various antibacterial drugs are substrates for drug metabolizing enzymes. They suffer from reduced bioavailability after oral administration in chickens. Herbal bio-enhancers increased the absorption of co-administered drugs. Hence, present study was planned to explore the bio-enhancing effect of piperine and quercetin pretreatment on pharmacokinetics of marbofloxacin after oral administration in broiler chickens.Methods: The pharmacokinetics of marbofloxacin was investigated following single dose (5 mg/kg) oral administration in piperine, quercetin alone and both in combination pretreated (10 mg/kg each, oral, 3 days) broiler chickens. The concentrations of marbofloxacin in plasma samples were analyzed by high performance liquid chromatography.Result: Following single oral administration of marbofloxacin, elimination half-lives (t1/2β) were 6.23 ± 1.01, 5.69 ± 0.39 and 7.71 ± 0.59 h in piperine, quercetin and both in combination pretreated chickens, respectively. The elimination half-life (t1/2β), apparent volume of distribution (Vd(area)/F) and mean residence time (MRT) were significantly (p less than 0.05) higher in combination pretreated chickens as compared to piperine and quercetin alone groups. Piperine and quercetin combined pretreatment has improved the pharmacokinetics profile of marbofloxacin after oral administration in broiler chickens. Findings of the study are expedient for the development of protocol for use of bio-enhancers with antibiotics in broiler chickens.


Author(s):  
Shi-tang Ma ◽  
Xin-yuan Zhang ◽  
Ning Zhang ◽  
Xiao-lin Bi ◽  
Cheng-Tao Feng

Background: Quercitrin is widely found in herbal medicines, and it is particularly important in the design of new therapeutic agents. Because of its wide range of biological activities, methods for detecting quercitrin and its pharmacokinetics in biological samples must be investigated. Objective: To develop and validate a sensitive and reliable ultra-high-performance liquid chromatography-tandem mass spectrometry (UHPLC-MS/MS) method for the quantitative determination of quercitrin levels in rat plasma and test its application in a pharmacokinetic investigation after the oral administration of Polygoni cuspidati folium capsules (HC). Methods: First, a rapid analytical method implementing UHPLC-MS/MS for the quantification of quercitrin levels in rat plasma was developed and validated. The analyte and internal standard (IS) tinidazole were extracted from rat plasma via protein precipitation with 800 μL of methanol and 50 μL of 1% formic acid solution. Chromatographic separation was performed using an Agilent ZORBAX C18 column within 4 min. Mass spectrometry was performed for quantification using a triple-quadrupole mass spectrometer employing electrospray ionization in the negative ion mode. The MRM transitions for quercitrin and IS were m/z 447.2→229.9 and m/z 246.0→125.8, respectively. The UHPLC-MS/MS method for the quantitative determination of quercitrin levels in rat plasma was then applied to investigate its pharmacokinetics after the oral administration of HC in rats. Results: The developed UHPLC-MS/MS method for detecting quercitrin in rat plasma was linear over the range of 0.1–160 ng/mL. The linear regression equation was Y = (0.7373 ± 0.0023)X − (0.0087 ± 0.0021) (r2 = 0.9978). The intra- and interday precision values were within 7.8%, and the recoveries of quercitrin and IS exceeding 67.3%. The UHPLC-MS/MS method was successfully applied to characterize the pharmacokinetic profile of quercitrin in eight rats after the oral administration of HC. The experimentally obtained values were fit to a one-compartment, first-order pharmacokinetic model, and they appeared to fit the concentration-time curve. Conclusion: Quercitrin was proven to be stable during sample storage, preparation, and analytical procedures. The pharmacokinetic parameters suggested that quercitrin may be present in the peripheral tissues of rats.


2007 ◽  
Vol 51 (9) ◽  
pp. 3063-3066 ◽  
Author(s):  
David E. Martin ◽  
Robert Blum ◽  
John Wilton ◽  
Judy Doto ◽  
Hal Galbraith ◽  
...  

ABSTRACT Bevirimat (BVM; formerly known as PA-457) is a novel inhibitor of human immunodeficiency virus (HIV) maturation that is being developed for the treatment of HIV infection. The pharmacokinetics of this agent in healthy male volunteers were studied in a randomized, double-blind study in which the participants received single oral doses of placebo (n = 8) or escalating doses of BVM at 25, 50, 100, or 250 mg (n = 6 per dose); escalation was performed only after the pharmacokinetics and safety of the preceding dose had been evaluated. Plasma was collected over 480 h after dosing and urine was collected over 48 h after dosing for determination of the values of pharmacokinetic parameters. BVM was well absorbed after oral administration, with peak plasma concentrations being achieved 1 to 3 h after dosing. The half-life was 60 to 80 h. The exposure assessed by determination of the peak concentration and the area under the concentration-time curve was dose proportional. Single oral doses of BVM were well tolerated: there were no dose-limiting toxicities, and no serious adverse events were reported. These findings suggest that that BVM offers a favorable pharmacokinetic profile, with predictable pharmacokinetics following the oral administration of single doses. The long half-life of BVM may facilitate once-daily dosing.


2020 ◽  
Vol 8 (1) ◽  
pp. 60
Author(s):  
Ashraf Elkomy ◽  
Mohamed Aboubakr

The present study was designed to assess the comparative bio-equivalence of Lincopharm 800® and Lincoyosr® in healthy broiler chicken after oral administration of both products in a dose of 20 mg lincomycin base/kg b.wt. Twenty four broiler chickens were divided into two groups. The first group was designed to study the pharmacokinetics of Lincopharm 800®, while the 2nd group was designed to study the pharmacokinetics of Lincoyosr®. Each broiler chicken in both groups was orally administered with 20 mg lincomycin base/kg b.wt. Blood samples were obtained from the wing vein and collected immediately before and at 0.08, 0.16, 0.25, 0.5, 1, 2, 4, 8, 12 and 24 hours after a single oral administration. The disposition kinetics of Lincopharm 800® and Lincoyosr® following oral administration of 20 mg lincomycin base /kg b.wt, revealed that the maximum blood concentration of lincomycin [Cmax] were 4.81 and 4.62 μg/ml and attained at [tmax] of 1.36 and 1.35 hours, respectively. In conclusion: Lincoyosr® is bioequivalent to Lincopharm 800® since the ratios of Cmax, AUC0-24 and AUC0-∞ (T/R) was 0.96, 0.92 and 0.91 respectively. These are within the bioequivalence acceptance range. Lincoyosr® and Lincopharm 800® are therefore bioequivalent and interchangeable.   


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