scholarly journals Study of the pharmacokinetics of moxidectin in the body of carnivores using an antiparasitic drug in the form of tablets

2021 ◽  
Vol 15 (2) ◽  
pp. 56-63
Author(s):  
G. B. Arisova

The purpose of the research is studying the pharmacokinetics of moxidectin in the blood serum of cats and dogs after a single administration of antiparasitic drug «Neoterika Protecto tablets».Materials and methods. The studies were performed at the premises of the Kurilovo experimental farm of the VNIIP – FSC VIEV on clinically healthy animals of both sexes aged 1-4 years, namely, 6 cats weighing 1.5–2.0 kg and 6 dogs weighing 10.3–13.8 kg. The drug was administered once orally at the rate of 1.5 mg of moxidectin per 1 kg of body weight. Blood samples were taken in the amount of 2 ml from cats and 4–5 ml from dogs before the drug and after 3, 6, 12, 24 hours, and 3, 6, 10, 20, 45, 60, 75, and 90 days. The study used the high-performance liquid chromatography. We determined the moxidectin content in the blood serum. Based on the results, we calculated the pharmacokinetic parameters of the active substance in the body of cats and dogs.Results and discussion. It was found that the active substance concentration within 3 hours after a single use of the moxidectin-based drug in the form of tablets reached a level of 134.8–498.0 ng/ml in cats and 479.08–1459.4 ng/ml in dogs; moxidectin was present in the bloodstream of cats and dogs for 90 days. Thus, a single administration of the drug at the recommended therapeutic dose of 1.5 mg/kg allows for the therapeutic moxidectin concentration to be maintained for 90 days. 

2021 ◽  
Vol 11 (2) ◽  
pp. 300-306
Author(s):  
Gulnara B. Arisova ◽  
Mikhail V. Arisov ◽  
Irina A. Stepanova

The pharmacokinetic characteristics of the moxidectin-based drugs have been studied in the blood serum of animals after a single oral administration of the drug at the therapeutic dose in form of syrup. The drug is intended to control parasitic diseases of cats and dogs. The present studies on cats and dogs (drug administration and blood sampling) were conducted in the experimental farm of Kurilovo, Russia, for three months. The study involved six dogs and six cats, half breed, aged one to four years. The samples included six dogs (four male and two female) and six cats (three male and three female), and groups were formed according to the principle of analog groups. The drug, moxidectin, was orally administered once at the dose of 1.5 mg per one kg of animal’s weight. The active substance of the drug was identified in the blood serum of animals by High-Performance Liquid Chromatography (HPLC) with fluorescence detection. The result of the current study showed that based on the pharmacokinetics of moxidectin, the concentration of the active substance in the blood serum after three hours reached 134.80-498.09 ng/ml in cats and 479.07-1459.40 ng/ml in dogs. The obtained results indicated that a single administration of the drug at the recommended therapeutic dose could ensure the maintenance of therapeutic concentrations of moxidectin in the blood, and accordingly, the protection of animals from parasites for up to 90 days.


2020 ◽  
Vol 11 (4) ◽  
pp. 7289-7292
Author(s):  
Seema Saini ◽  
Rajeev Garg

In the present study, fast disintegrating tablets of Lercanidipine Hydrochloride (LFDT) were tested in vivo in the buccal cavity of the rabbits. Various pharmacokinetic parameters were analysed in the study, including maximum measured plasma concentration (Cmax), time of maximum measured plasma concentration (tmax) and area under the plasma concentration vs time curve (AUC). Also, the comparative study of the Lercanidipine Hydrochloride fast disintegrating tablets (LFDT) was performed with the marketed conventional tablets of the drug (LMKT). The technique selected for the bioanalytical analysis of the blood samples of the rabbits for pharmacokinetic data computation was High-Performance Liquid Chromatography. An already well-established and validated method was used to analyse the blood samples of the rabbits. The results revealed that the rate of absorption was improved for fast disintegrating tablets of Lercanidipine Hydrochloride (LFDT) as compared to the marketed conventional tablets of the drug (LMKT). This indicated that drug was rapidly absorbed from the fast disintegrating tablet and attained elevated plasma concentration in a short interval after dosing than the marketed formulation. However, the value of tmax was drastically shorter for LFDT than the LMKT. The average peak plasma concentration also designated a rise in the extent of absorption (AUC). From the present study, it was concluded that the fast disintegrating tablet batch (LFDT) had much more improved pharmacokinetic parameters as compared to its conventional marketed counterpart (LMKT).


2018 ◽  
pp. 307-319
Author(s):  
Mohamed El-Sayed ◽  
Magdy Amer ◽  
Sameh El-nabtity ◽  
Sara El-Azab

The current study was carried out to investigate the pharmacokinetic profile of cefquinome following a single IV injection in ten New Zealand white rabbits (2-2.5 kg body weight). Cefquinome was injected intravenously (2mg/kg body weight) and blood samples were collected before drug administration and up to 24h after injection. Cefquinome plasma concentrations were measured using HPLC (high- performance liquid chromatography). The result showed that the plasma concentration of cefquinome was 9.13 ± 0.43 µg/mL at 5min post-injection then declined gradually to 0.73 ± 0.18µg/mL after 2 hours. No cefquinome concentration could be detected at 4h post injection. The major pharmacokinetic parameters (Mean ± SEM) were T1/2 λz 0.52 ± 0.05h, AUC0-∞ 9.13 ± 0.63 h*µg/mL, Cl 239.25 ±14.61 mL/h/kg, Vz 170.89 ± 9.7 mL/kg and MRT0-∞ 0.75 ±0.06 h.


GYNECOLOGY ◽  
2021 ◽  
Vol 23 (4) ◽  
pp. 335-340
Author(s):  
Mariia V. Iurova ◽  
Vladimir E. Frankevich ◽  
Stanislav V. Pavlovich ◽  
Vitali V. Chagovets ◽  
Nataliya L. Starodubtseva ◽  
...  

Background. Ovarian cancer is the first fatal malignancy of the female reproductive system. Early detection is associated with better outcomes, but is significantly difficult because of asymptomatic or low-symptomatic course. Aim. To study the possibility of detecting of OC in early stages (IaIc) by the lipid profile of blood serum obtained using high-performance liquid chromatography with mass spectrometric (MS) detection. Materials and methods. An observational "case-control" study was conducted in period November 2019 July 2020 in the Kulakov National Medical Research Center for Obstetrics, Gynecology and Perinatology. 41 patients were included: group 1 (main) 28 patients with histologically verified high grade serous ovarian cancer of IIV FIGO stage, group 2 (control) 13 conditionally healthy women. Venous blood samples were collected immediately before the operation. Extracts of serum lipids were obtained in accordance with the modified Folch method. The composition of the samples was analyzed by electrospray ionization MS. Using the method of discriminant analysis and orthogonal projections to latent structures (OPLS-DA) were building OPLS-models based on profile of significant lipids. The comparison based on the non-parametric MannWhitney test. Results. The presence of 128 lipids in blood serum samples makes a major contribution to the OPLS-models, that are different for patients with IIV OC stage and controls. The OPLS-model parameters are: R2=0.87 and Q2=0.80, the area under the ROC curve reached 1, sensitivity and specificity of the model 100%. The second OPLS-model was developed to assign patients to 13 blood serum samples of the control group or to 5 blood samples of patients with I-II stages of OC: 108 lipids made the main contribution to this model (R2=0.97, Q2=0.86). The third OPLS-model was constructed to distinguish patients with earlier (IaIa stages; n=5) and advanced (IIaIVa; n=23) stages: R2=0.96 and Q2=1.00, AUC=0.99. Diglycerides, triglycerides, phosphatidylcholines, ethanolamines, sphingomyelins, ceramides, phosphatidylserines, phosphoinositols and prostaglandins significantly differ in the blood serum samples of patients with IaIc stages of OC and patients with IIIV stages and controls, that indicates the diagnostic value. Conclusion. It is possible to distinguish a healthy person from patient with IaIc or IIIV stages of OC. Serum oncolipids profile obtained by high-performance liquid chromatography with MS detection can be used as markers of early stages of OC, that are associated with better prognosis.


Separations ◽  
2021 ◽  
Vol 8 (6) ◽  
pp. 78
Author(s):  
Sevasti Karampela ◽  
Jessica Smith ◽  
Irene Panderi

An ever-increasing need exists within the forensic laboratories to develop analytical processes for the qualitative and quantitative determination of a broad spectrum of new psychoactive substances. Phenylethylamine derivatives are among the major classes of psychoactive substances available on the global market and include both amphetamine analogues and synthetic cathinones. In this work, an ultra-high-performance liquid chromatography-positive ion electrospray ionization tandem mass spectrometric method (UHPLC-ESI-MS/MS) has been developed and fully validated for the determination of 19 psychoactive substances, including nine amphetamine-type stimulants and 10 synthetic cathinone derivatives, in premortem and postmortem whole blood. The assay was based on the use of 1 mL premortem or postmortem whole blood, following solid phase extraction prior to the analysis. The separation was achieved on a Poroshell 120 EC-C18 analytical column with a gradient mobile phase of 0.1% formic acid in acetonitrile and 0.1% formic acid in water in 9 min. The dynamic multiple reaction monitoring used in this work allowed for limit of detection (LOD) and lower limit of quantitation (LOQ) values of 0.5 and 2 ng mL−1, respectively, for all analytes both in premortem and postmortem whole blood samples. A quadratic calibration model was used for the 12 quantitative analytes over the concentration range of 20–2000 ng mL−1, and the method was shown to be precise and accurate both in premortem and postmortem whole blood. The method was applied to the analysis of real cases and proved to be a valuable tool in forensic and clinical toxicology.


2020 ◽  
Vol 10 (1) ◽  
Author(s):  
Fiona Li ◽  
Justin W. Hicks ◽  
Lihai Yu ◽  
Lise Desjardin ◽  
Laura Morrison ◽  
...  

Abstract Background In molecular imaging with dynamic PET, the binding and dissociation of a targeted tracer is characterized by kinetics modeling which requires the arterial concentration of the tracer to be measured accurately. Once in the body the radiolabeled parent tracer may be subjected to hydrolysis, demethylation/dealkylation and other biochemical processes, resulting in the production and accumulation of different metabolites in blood which can be labeled with the same PET radionuclide as the parent. Since these radio-metabolites cannot be distinguished by PET scanning from the parent tracer, their contribution to the arterial concentration curve has to be removed for the accurate estimation of kinetic parameters from kinetic analysis of dynamic PET. High-performance liquid chromatography has been used to separate and measure radio-metabolites in blood plasma; however, the method is labor intensive and remains a challenge to implement for each individual patient. The purpose of this study is to develop an alternate technique based on thin layer chromatography (TLC) and a sensitive commercial autoradiography system (Beaver, Ai4R, Nantes, France) to measure radio-metabolites in blood plasma of two targeted tracers—[18F]FAZA and [18F]FEPPA, for imaging hypoxia and inflammation, respectively. Results Radioactivity as low as 17 Bq in 2 µL of pig’s plasma can be detected on the TLC plate using autoradiography. Peaks corresponding to the parent tracer and radio-metabolites could be distinguished in the line profile through each sample (n = 8) in the autoradiographic image. Significant intersubject and intra-subject variability in radio-metabolites production could be observed with both tracers. For [18F]FEPPA, 50% of plasma activity was from radio-metabolites as early as 5-min post injection, while for [18F]FAZA, significant metabolites did not appear until 50-min post. Simulation study investigating the effect of radio-metabolite in the estimation of kinetic parameters indicated that 32–400% parameter error can result without radio-metabolites correction. Conclusion TLC coupled with autoradiography is a good alternative to high-performance liquid chromatography for radio-metabolite correction. The advantages of requiring only small blood samples (~ 100 μL) and of analyzing multiple samples simultaneously, make the method suitable for individual dynamic PET studies.


2010 ◽  
Vol 55 (1) ◽  
pp. 326-330 ◽  
Author(s):  
José Moltó ◽  
Marta Valle ◽  
Cristina Miranda ◽  
Samandhy Cedeño ◽  
Eugenia Negredo ◽  
...  

ABSTRACTThe aim of this open-label, fixed-sequence study was to investigate the potential ofEchinacea purpurea, a commonly used botanical supplement, to interact with the boosted protease inhibitor darunavir-ritonavir. Fifteen HIV-infected patients receiving antiretroviral therapy including darunavir-ritonavir (600/100 mg twice daily) for at least 4 weeks were included.E. purpurearoot extract capsules were added to the antiretroviral treatment (500 mg every 6 h) from days 1 to 14. Darunavir concentrations in plasma were determined by high-performance liquid chromatography immediately before and 1, 2, 4, 6, 8, 10, and 12 h after a morning dose of darunavir-ritonavir on days 0 (darunavir-ritonavir) and 14 (darunavir-ritonavir plus echinacea). Individual darunavir pharmacokinetic parameters were calculated by noncompartmental analysis and compared between days 0 and 14 with the geometric mean ratio (GMR) and its 90% confidence interval (CI). The median age was 49 (range, 43 to 67) years, and the body mass index was 24.2 (range, 18.7 to 27.5) kg/m2. Echinacea was well tolerated, and all participants completed the study. The GMR for darunavir coadministered with echinacea relative to that for darunavir alone was 0.84 (90% CI, 0.63-1.12) for the concentration at the end of the dosing interval, 0.90 (90% CI, 0.74-1.10) for the area under the concentration-time curve from 0 to 12 h, and 0.98 (90% CI, 0.82-1.16) for the maximum concentration. In summary, coadministration ofE. purpureawith darunavir-ritonavir was safe and well tolerated. Individual patients did show a decrease in darunavir concentrations, although this did not affect the overall darunavir or ritonavir pharmacokinetics. Although no dose adjustment is required, monitoring darunavir concentrations on an individual basis may give reassurance in this setting.


Author(s):  
Yan Xiong ◽  
Yong-Hong Liu ◽  
Jian-Sha Li ◽  
Yu-Ying Zhang ◽  
Jing Zhang ◽  
...  

Abstract A simple high performance liquid chromatography (HPLC) method was developed and validated for the determination of coumarin-3-carboxylic acid analogues (C3AA) in rat plasma and a preliminary study on pharmacokinetics. Ferulic acid (FA) was used as the internal standard substance, and coumarin-3-carboxylic acid (C3A) was used as a substitute for quantitative C3AA. After protein precipitation with methanol, the satisfactory separation was achieved on an ODS2 column when the temperature was maintained at 30 ± 2°C. The correlation coefficient r in the C3A linear equation is equal to 0.9990. Pharmacokinetic parameters for t1/2, Tmax, Cmax, area under the curve (AUC)0-t, average residence time (MRT), apparent volume of distribution (V z/F) and clearance (Cl/F) were 1.89 ± 0.03 h, 0.39 ± 0.14 h, 1.81 ± 0.10 g· mL−1 ·h, 7.88 ± 0.24 g·mL−1·h, 3.23 ± 0.14 h, 0.43 ± 0.03 (mg·kg−1)·(g·mL−1)−1·h−1, respectively. The high performance liquid chromatography-photo diode array detector (HPLC-PDA) method established in this study can be used to separate and determine the content of C3AA in plasma of rats after 60% ethanol extraction by gavage. The plasma concentration-time curve and pharmacokinetic parameters reflect the absorption of C3AA in rat blood after oral administration to some extent.


2020 ◽  
Vol 11 (SPL4) ◽  
pp. 2756-2767
Author(s):  
Vijaya Vemani ◽  
Mounika P ◽  
Poulami Das ◽  
Anand Kumar Tengli

In the preservation of normal physiological functions, the building blocks of the body called amino acids play a crucial role. A number of valuable and nutritional phytoconstituents are contained in fruit juices, such as vitamins, minerals, microelements, organic acids, antioxidants, flavonoids, amino acids and other components. Due to the growing population and demand, the quality of fruit juices is decreasing. One of the unethical and harmful practices called adulteration or food fraudulence has been adopted by most food and beverage industries. The amino acids which is one of the most important phytochemicals of fruit and fruit juices which affects the organoleptic properties like color, odor, and taste of juices and also helps in authenticity process from governing bodies by providing total amino acid content. Consequently, the main aim of the present review work is to provide information regarding the importance of amino acids, how they are adulterated, the potential analytical approach to detected amino acids and which methods are generally accepted method by the food industries. According to the literature review, we presume that reverse phased high-performance liquid chromatography with pre-column derivatization was the most adopted method for quality checking due to its advantages over other old and recent analytical approaches like simple, rapid, cost-effective nature, less / no sample matrix effect with high sensitivity, accuracy, and precision.


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