scholarly journals Pharmacokinetic Behaviour of Enrofloxacin after Single Intramuscular Dosage in American Black Vultures (Coragyps atratus)

Antibiotics ◽  
2021 ◽  
Vol 10 (8) ◽  
pp. 957
Author(s):  
Samanta Waxman ◽  
José Julio de Lucas ◽  
Guillermo Wiemeyer ◽  
Laura Torres Bianchini ◽  
Manuel Ignacio San Andrés ◽  
...  
Keyword(s):  
High Performance ◽  
Plasma Concentrations ◽  
Compartmental Analysis ◽  
Intramuscular Administration ◽  
Pharmacokinetic Parameters ◽  
E Coli ◽  
Intramuscular Dose ◽  
Gram Positive Bacteria ◽  
Complete Absorption ◽  
American Black

The aim of the study was to investigate the intramuscular pharmacokinetics of enrofloxacin in black vultures (Coragyps atratus). The pharmacokinetics of a single intramuscular dose (10 mg/kg) of enrofloxacin was studied in six vultures. Plasma concentrations of enrofloxacin and its active metabolite, ciprofloxacin, were determined by high-performance liquid chromatography (HPLCuv). Pharmacokinetic parameters were estimated using non-compartmental and compartmental analysis. After intramuscular administration, enrofloxacin showed a rapid and complete absorption, reaching a Cmax value of 3.26 ± 0.23 μg/mL at 1.75 ± 0.53 h. A long terminal half-life of 19.58 h has been observed. Using previously published MIC values to perform a PK/PD analysis, cumulative fraction responses obtained after Monte Carlo simulation for AUC/MIC > 30, 50 and 125 were 72.93%, 72.34% and 30.86% for E. coli and 89.29%, 88.89% and 58.57% for Mycoplasma synoviae, respectively. Cumulative fraction responses obtained for Cmax/MIC index were 33.93% and 40.18% for E. coli and M. synoviae, respectively. The intramuscular administration of 10 mg/kg could be appropriate to treat infectious diseases caused by gram-positive bacteria with MIC value lower than 1 µg/mL; however, although enrofloxacin showed a slow elimination in black vultures, plasma concentrations were insufficient to reach the gram-negative stablished breakpoints.

scholarly journals Pharmacokinetics and Bioavailability of Carprofen in Rainbow Trout (Oncorhynchus mykiss) Broodstock

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 990
Author(s):  
Kamil Uney ◽  
Duygu Durna Corum ◽  
Ertugrul Terzi ◽  
Orhan Corum
Keyword(s):  
Rainbow Trout ◽  
Oncorhynchus Mykiss ◽  
High Performance ◽  
Peak Plasma ◽  
Peak Plasma Concentration ◽  
Plasma Concentrations ◽  
Compartmental Analysis ◽  
Oral Route ◽  
Pharmacokinetic Parameters ◽  
Rainbow Trout Oncorhynchus Mykiss

The aim of this study was to determine the pharmacokinetics of carprofen following intravenous (IV), intramuscular (IM) and oral routes to rainbow trout (Oncorhynchus mykiss) broodstock at temperatures of 10 ± 1.5 °C. In this study, thirty-six healthy rainbow trout broodstock (body weight, 1.45 ± 0.30 kg) were used. The plasma concentrations of carprofen were determined using high-performance liquid chromatography and pharmacokinetic parameters were calculated using non-compartmental analysis. Carprofen was measured up to 192 h for IV route and 240 h for IM, and oral routes in plasma. The elimination half-life (t1/2λz) was 30.66, 46.11, and 41.08 h for IV, IM and oral routes, respectively. Carprofen for the IV route showed the total clearance of 0.02 L/h/kg and volume of distribution at steady state of 0.60 L/kg. For IM and oral routes, the peak plasma concentration (Cmax) was 3.96 and 2.52 μg/mL with the time to reach Cmax of 2 and 4 h, respectively. The bioavailability was 121.89% for IM route and 78.66% for oral route. The favorable pharmacokinetic properties such as the good bioavailability and long t1/2λz for IM and oral route of carprofen suggest the possibility of its effective use for the treatment of various conditions in broodstock.

scholarly journals Pharmacokinetic Profile of μSMIN Plus™, a new Micronized Diosmin Formulation, after Oral Administration in Rats

2015 ◽  
Vol 10 (9) ◽  
pp. 1934578X1501000 ◽  
Author(s):  
Rosario Russo ◽  
Angelo Mancinelli ◽  
Michele Ciccone ◽  
Fabio Terruzzi ◽  
Claudio Pisano ◽  
...  
Keyword(s):  
Oral Administration ◽  
Plasma Concentrations ◽  
Compartmental Analysis ◽  
Pharmacokinetic Profile ◽  
Pharmacokinetic Parameters ◽  
Maximum Plasma ◽  
Sprague Dawley ◽  
Time Curve ◽  
Maximum Plasma Drug Concentration

Diosmin is a naturally occurring flavonoid present in citrus fruits and other plants belonging to the Rutaceae family. It is used for the treatment of chronic venous insufficiency (CVI) for its pheblotonic and vaso-active properties, safety and tolerability as well. The aim of the current in vivo study was to investigate the pharmacokinetic profile of a branded micronized diosmin (μSMIN Plus™) compared with plain micronized diosmin in male Sprague-Dawley rats. After oral administration by gastric gavage, blood samples were collected via jugular vein catheters at regular time intervals from baseline up to 24 hours. Plasma concentrations were assessed by LC/MS. For each animal, the following pharmacokinetic parameters were calculated using a non-compartmental analysis: maximum plasma drug concentration (Cmax), time to reach Cmax (Tmax), area under the plasma concentration-time curve (AUC0-last), elimination half-life (t1/2), and relative oral bioavailability (%F). The results of the current study clearly showed an improvement in the pharmacokinetic parameters in animals treated with μSMIN Plus™ compared with animals treated with micronized diosmin. In particular, μSMIN Plus™ showed a 4-fold increased bioavailability compared with micronized diosmin. In conclusion, the results from the current study provided a preliminary pharmacokinetic profile for μSMIN Plus™, which may represent a new tool for CVI management.

Exposure to chloroquine in male adults and children aged 9–11 years with malaria due to Plasmodium vivax

2020 ◽  
Author(s):  
Michelle Valeria Dias Ferreira Vieira ◽  
José Luiz Fernandes Vieira
Keyword(s):  
Plasmodium Vivax ◽  
High Performance ◽  
Plasma Concentrations ◽  
Area Under The Curve ◽  
Time Profile ◽  
Pharmacokinetic Parameters ◽  
Older Children ◽  
Asexual Blood Stage ◽  
Adults And Children ◽  
A Prospective Study

Abstract Background Chloroquine is effective against the asexual blood stage of Plasmodium vivax. A high proportion of children are underdosed with the drug, but there are no studies comparing chloroquine exposure in adults and children aged 8–11 years old. The present study intends to compare these populations using the area under the curve (AUC) derived from the plasma concentration-time profile in patients with P. vivax. Methods A prospective study of cases was performed on male children (aged 9–11 years) and adults with vivax malaria. Blood samples were collected after several days of treatment. Chloroquine was measured by high-performance liquid chromatography. A non-compartmental pharmacokinetic model was used to calculate the pharmacokinetic parameters of the drug. Results A total of 20 children and 25 adults were included in the study. Plasma concentrations of chloroquine in older children ranged from 67 to 1112 ng/ml, and in adults the value ranged from 74 to 1147 ng/ml. The AUC to the last measurable concentration and to infinite was significantly lower in children than in adults, indicating a lower exposure to the drug. Conclusion These data demonstrate lower exposure to chloroquine in children, which corroborates the importance of optimising the doses of chloroquine in the study age band to ensure adequate exposure to the drug.

scholarly journals Comparative Study on Pharmacokinetics of Four Long-Acting Injectable Formulations of Enrofloxacin in Pigs

2021 ◽  
Vol 7 ◽  
Author(s):  
Salah Uddin Ahmad ◽  
Jichao Sun ◽  
Fusheng Cheng ◽  
Bing Li ◽  
Safia Arbab ◽  
...  
Keyword(s):  
Comparative Study ◽  
High Performance ◽  
Pasteurella Multocida ◽  
Plasma Concentrations ◽  
Pharmacokinetic Parameters ◽  
Maximum Plasma ◽  
Reference Formulation ◽  
Time Curve ◽  
Drug Concentrations ◽  
Long Acting

A comparative study on pharmacokinetics of four long-acting enrofloxacin injectable formulations was investigated in 36 healthy pigs after intramuscular injection according to the recommended single dose @ 2.5 mg/kg body weight. The drug concentrations in the plasma were computed using high-performance liquid chromatography (HPLC) with fluorescence detection. WinNonLin5.2.1 software was used to analyze the experimental data and compared it under one-way ANOVA using SPSS software with a 95% confidence interval (CI). The main pharmacokinetic parameters, that is, the maximum plasma concentrations (Cmax), the time to maximum concentration (Tmax), area under the time curve concentration (AUCall) and Terminal half-life (T1/2) were 733.84 ± 129.87, 917.00 ± 240.13, 694.84 ± 163.49, 621.98 ± 227.25 ng/ml, 2.19 ± 0.0.66, 1.50 ± 0.37, 2.89 ± 0.24, 0.34 ± 0.13 h, 7754.43 ± 2887.16, 8084.11 ± 1543.98, 7369.42 ± 2334.99, 4194.10 ± 1186.62 ng h/ml, 10.48 ± 2.72, 10.37 ± 2.38, 10.20 ± 2.81, and 10.61 ± 0.86 h for 10% enrofloxacin (Alkali), 20% enrofloxacin (Acidic), Yangkang and control drug Nuokang® respectively. There were significant differences among Cmax, Tmax, and AUCall of three formulations compare with that of the reference formulation. No significant differences were observed among the T1/2 for tested formulations compare with the reference formulation. The pharmacokinetic parameters showed that the tested formulations were somewhat better compared to the reference one. The calculated PK/PD indices were effective for bacteria such as Actinobacillus pleuropneumoniae and Pasteurella multocida with values higher than the cut-off points (Cmax/MIC90≥10–12 and AUC/MIC90 ≥ 125). However, they were not effective against bacteria like Haemophilus parasuis, Streptococcus suis, E. coli, and Bordetella bronchiseptica where lower values were obtained.

scholarly journals Bioequivalence of Two Oral Formulations of Ciprofloxacin 250 mg Tablets in Healthy Mexican Volunteers

2019 ◽  
Vol 1 (1) ◽  
pp. 104-109
Author(s):  
Suset J. Tolentino-Hernández ◽  
Leticia Cruz-Antonio ◽  
Irma Torres-Roque ◽  
Jose T. Pérez-Urizar
Keyword(s):  
Confidence Intervals ◽  
Plasma Concentrations ◽  
Compartmental Analysis ◽  
Immediate Release ◽  
Hplc Method ◽  
Pharmacokinetic Parameters ◽  
Test Results ◽  
Oral Formulations ◽  
Acceptance Range ◽  
Bioequivalence Test

Background. There are numerous reports of low-quality formulations of ciprofloxacin in the market, which has been associated with therapeutic failure and the development of microbial resistance. Objective. The aim of this study is evaluating the bioequivalence between two oral immediate-release ciprofloxacin 250 mg tablets. Material and Methods. The study was performed in 24 Mexican healthy volunteers following a randomized cross over 2 × 2 design. Single doses of a test formulation Lemyflox® (Lemery Laboratories, Mexico) and the reference formulation Ciproxina® (Bayer, Mexico) were administered; blood samples were obtained during a 12 h period. Ciprofloxacin plasma concentrations were quantified using a validated High-Pressure Liquid Chromatography (HPLC) method, plasma concentration against time curves were constructed and pharmacokinetic parameters were determined by non-compartmental analysis. In order to determine bioequivalence, test/reference ratios of Cmax, AUC0-t and AUC0-inf were compared using analysis of variance (ANOVA), followed by the 90 % confidence intervals and the Schuirmann bilateral test. Results. The 90 % confidence intervals limits ranged from 82.92 to 100.88 % for Cmax, from 93.05 to 109.15 % for AUC0-t and from 97.76 to 114.99 % for AUC0-inf, all cases were within bioequivalence acceptance range of 80 - 125 %. Schuirmann test confirmed such observation as the probability that Cmax, AUC0-t and AUC0-inf ratios were beyond 80 - 125 % was lower than 0.05. Conclusions. The results obtained demonstrate bioequivalence between the test and reference formulations.

Mivacurium Arteriovenous Gradient during Steady State Infusion in Anesthetized Patients

2002 ◽  
Vol 97 (3) ◽  
pp. 622-629 ◽  
Author(s):  
Samia Ezzine ◽  
François Donati ◽  
France Varin
Keyword(s):  
Steady State ◽  
High Performance ◽  
Sampling Site ◽  
Plasma Concentrations ◽  
Plasma Cholinesterase ◽  
Constant Infusion ◽  
Pharmacokinetic Parameters ◽  
Brachial Vein ◽  
The Difference ◽  
Total Body

Background Mivacurium and isomers undergo rapid hydrolysis by plasma cholinesterase. As this enzyme is largely distributed, it cannot be excluded that these isomers might undergo peripheral elimination. This hypothesis was investigated in patients by measuring the difference between arterial and venous concentrations under a constant-rate continuous infusion of mivacurium. Methods During propofol-remifentanil anesthesia, eight adult consenting patients received an intravenous bolus dose of 0.2 mg/kg mivacurium, followed by a constant infusion (3, 5, or 7 microg. kg. min ) into the brachial vein. One hour after starting the infusion, arterial (radial artery) and venous (contralateral brachial vein) blood samples were drawn simultaneously at 15-min intervals for 45 min. Mivacurium isomers and metabolite plasma concentrations were determined by stereospecific high-performance liquid chromatography. Using the corresponding arterial and venous concentrations, the tissue extraction coefficient as well as total body clearance were calculated. Results During steady state conditions, the venous concentrations of the and isomers were 34 +/- 13% and 42 +/- 11% (mean +/- SD) lower than the corresponding arterial concentrations (P < 0.05), respectively. For the isomer, the difference between venous and arterial concentrations was 3 +/- 4% (P = 0.063). Total body clearances of the and isomers were greater when based on venous sampling (P < 0.05). Conclusion Pharmacokinetic parameters derived from a constant infusion of mivacurium depend heavily on the sampling site (arterial or venous) for the rapidly hydrolyzed isomers. These results strongly suggest a significant metabolism of mivacurium within muscle tissue that may account for the large interpatient variability in response to mivacurium.

PHARMACOKINETICS OF A SINGLE INTRAVENOUS INJECTION OF CEFQUINOME IN RABBITS

2018 ◽  
pp. 307-319
Author(s):  
Mohamed El-Sayed ◽  
Magdy Amer ◽  
Sameh El-nabtity ◽  
Sara El-Azab
Keyword(s):  
Body Weight ◽  
High Performance Liquid Chromatography ◽  
High Performance ◽  
Plasma Concentrations ◽  
Pharmacokinetic Profile ◽  
Pharmacokinetic Parameters ◽  
Post Injection ◽  
Blood Samples ◽  
Single Intravenous Injection ◽  
New Zealand White Rabbits

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.

scholarly journals Validation and Pharmacokinetic Application of a High-Performance Liquid Chromatographic Technique for Determining the Concentrations of Amodiaquine and Its Metabolite in Plasma of Patients Treated with Oral Fixed-Dose Amodiaquine-Artesunate Combination in Areas of Malaria Endemicity

2015 ◽  
Vol 59 (9) ◽  
pp. 5114-5122 ◽  
Author(s):  
Olumuyiwa N. Adedeji ◽  
Oluseye O. Bolaji ◽  
Catherine O. Falade ◽  
Odusoga A. Osonuga ◽  
Olusegun G. Ademowo
Keyword(s):  
Falciparum Malaria ◽  
High Performance ◽  
Limit Of Detection ◽  
Clinical Success ◽  
Plasma Concentrations ◽  
Uncomplicated Falciparum Malaria ◽  
Fixed Dose ◽  
Pharmacokinetic Parameters ◽  
Maximum Plasma ◽  
Chromatographic Technique

ABSTRACTArtemisinin-based combination therapies (ACTs) have been adopted by most African countries, including Nigeria, as first-line treatments for uncomplicated falciparum malaria. Fixed-dose combinations of these ACTs, amodiaquine-artesunate (FDC AQAS) and artemether-lumefantrine (AL), were introduced in Nigeria to improve compliance and achieve positive outcomes of malaria treatment. In order to achieve clinical success with AQAS, we developed and validated a simple and sensitive high-performance liquid chromatography (HPLC) method with UV detection for determination of amodiaquine (AQ) and desethylamodiaquine (DAQ) in plasma using liquid-liquid extraction of the drugs with diethyl ether following protein precipitation with acetonitrile. Chromatographic separation was achieved using an Agilent Zorbax C18column and a mobile phase consisting of distilled water-methanol (80:20 [vol/vol]) with 2% (vol/vol) triethylamine, pH 2.2, at a flow rate of 1 ml/min. Calibration curves in spiked plasma were linear from 100 to 1,000 ng/ml (r> 0.99) for both AQ and DAQ. The limit of detection was 1 ng (sample size, 20 μl). The intra- and interday coefficients of variation at 150, 300, and 900 ng/ml ranged from 1.3 to 4.8%, and the biases were between 6.4 and 9.5%. The mean extraction recoveries of AQ and DAQ were 80.0% and 68.9%, respectively. The results for the pharmacokinetic parameters of DAQ following oral administration of FDC AQAS (612/200 mg) for 3 days in female and male patients with uncomplicated falciparum malaria showed that the maximum plasma concentrations (Cmax) (740 ± 197 versus 767 ± 185 ng/ml), areas under the plasma concentration-time curve (AUC) (185,080 ± 20,813 versus 184,940 ± 16,370 h · ng/ml), and elimination half-life values (T1/2) (212 ± 1.14 versus 214 ± 0.84 h) were similar (P> 0.05).

Phase I clinical and pharmacokinetic study of oral etoposide phosphate.

1995 ◽  
Vol 13 (1) ◽  
pp. 200-209 ◽  
Author(s):  
C Sessa ◽  
M Zucchetti ◽  
T Cerny ◽  
O Pagani ◽  
F Cavalli ◽  
...  
Keyword(s):  
Phase I ◽  
Intravenous Administration ◽  
High Performance ◽  
Plasma Concentrations ◽  
Area Under The Curve ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Studies ◽  
Oral Etoposide ◽  
Validation Data ◽  
Etoposide Phosphate

PURPOSE To determine the bioavailability (F) and the pharmacokinetic profile of both etoposide and its prodrug, etoposide phosphate, after oral and intravenous administration of etoposide phosphate, and to determine the maximum-tolerable dose (MTD) of oral etoposide phosphate administered daily for 5 consecutive days every 3 weeks. In addition, we sought to develop and validate two limited-sampling models (LSMs) to predict the etoposide area under the curve (AUC) 24 hours after administration of oral and intravenous etoposide phosphate. PATIENTS AND METHODS In the F part of the study, patients were assessed for pharmacokinetic studies after one oral and one intravenous administration of the same dose of etoposide phosphate. Etoposide phosphate and etoposide plasma concentrations were assayed by high-performance liquid chromatography (HPLC). To develop LSMs after oral and intravenous administration, patients were randomized between the training and validation data sets. In the phase I part of the study, which followed the F part, the dose of etoposide phosphate was escalated from 50 mg/m2/d for etoposide equivalents for 5 days to 220 mg/m2/d for 5 days. RESULTS Forty adult patients with solid tumors or lymphoma entered the study and 35 were assessable for toxicity. The MTDs were defined as 175 mg/m2 and 220 mg/m2 in previously treated and untreated patients, respectively. Neutropenia was dose-limiting, with high interpatient variability. Within 15 minutes after intravenous administration, etoposide phosphate was no longer detectable in plasma, and it was never detectable after oral administration. Plasma concentrations and pharmacokinetic parameters of etoposide following etoposide phosphate were comparable to those reported for etoposide. The relative F (mean +/- SD) of etoposide after oral etoposide phosphate was 76 +/- 27%, with a range of 37% to 144%. CONCLUSION The clinical and pharmacokinetic results of this study confirm the prodrug hypothesis of etoposide phosphate. Although firm conclusions cannot be drawn, the F of oral etoposide phosphate seems to be comparable to or only slightly better than that of oral etoposide.

scholarly journals FARMACOCINÉTICA Y BIODISPONIBILIDAD ABSOLUTA DE MARBOFLOXACINA EN BÚFALOS (Bubalus bubalis)

2021 ◽  
Vol 19 (suplemento) ◽  
Author(s):  
A Anadón
Keyword(s):  
Half Life ◽  
Therapeutic Dose ◽  
Plasma Concentrations ◽  
Compartmental Analysis ◽  
Bubalus Bubalis ◽  
Absolute Bioavailability ◽  
Pharmacokinetic Analysis ◽  
Pharmacokinetic Parameters ◽  
Maximum Plasma ◽  
Water Buffaloes

The aim of this study was to evaluate the pharmacokinetic behaviour and the absolute bioavailability of marbofloxacin (MFX) in adult water buffaloes and to estimate the pharmacokinetic parameters for calculating the therapeutic dose in this animal species. Six adult buffaloes (3 males and 3 females) where treated by intravenous (IV) and subcutaneous (SC) route with a 10% experimental MFX injectable formulation at the dose of 2 mg/kg. After administration blood samples were drawn at pre-established times and MFX plasma concentrations where determined by microbiologic method. The pharmacokinetic analysis was made by compartmental analysis. After IV administration MFX presented a clearance of 198.4 ± 21.0 mL.kg.h and a half-life of elimination of 7.64 ± 3.29 h. After SC administration marbofloxacin presented a half-life of elimination of 8.5 ± 2.42 h, reaching it maximum plasma concentration (1.67 ± 0.516 μg/mL) at 1.69 ± 0.231 h, with a bioavailability of 80.8 ± 11.2 %. The estimated values of clearance and bioavailability will be employed in further studies for calculating the therapeutic dose of MFX in water buffaloes.    

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