scholarly journals Pharmacokinetic parameters of Amoxicillin in Bangladeshi volunteers: a preliminary evaluation

2014 ◽  
Vol 26 (1-2) ◽  
pp. 1-9
Author(s):  
Reefat Zaman Chowdhury ◽  
Md. Saiful Islam ◽  
Md. Sayedur Rahman
Keyword(s):  
Healthy Volunteers ◽  
High Performance ◽  
Oral Route ◽  
Absolute Bioavailability ◽  
Pharmacokinetic Parameters ◽  
Intravenous Route ◽  
Population Pharmacokinetic ◽  
Preliminary Evaluation ◽  
The Difference ◽  
Bangladeshi Population

The present study was designed to get preliminary idea about the pharmacokinetic behavior of the Bangladeshi population through estimating plasma amoxicillin concentration by High-Performance Liquid Chromatography (HPLC) with ultraviolet detection. In this study, Bangladeshi healthy volunteers were divided in two groups, 8 Bangladeshi Bangalee and 7 Bangladeshi Tribal male healthy volunteers. Both the groups received 500 mg of amoxicillin in oral route and blood samples were collected at 0, 30, 60, 120, 180, 360 and 480 minutes after drug administration. After 1 week of washout period, same volunteers of two groups received 500 mg of amoxicillin in intravenous route. In case of oral route, the Cmax, AUC0–8h, Tmax and T1/2 values for Bangladeshi Bangalee and Tribal healthy volunteers were 6.78 ± 1.20 & 9.10 ± 1.34 ìg/mL, 1290.13 ± 158.39 & 1766.06 ± 188.37 ìg min/mL, 82.50 ± 32.05 & 102.86 ± 29.28 min and 96.05 ± 3.80 & 88.15 ± 5.33 min respectively. The difference in Cmax, AUC0–8h and T1/2 values between these two groups of volunteers was significant (p<0.01, p<0.001 and p<0.01 respectively). However, the difference in Tmax was not significant (p>0.05). In case of intravenous route, the C30 min and AUC0–8h values for Bangladeshi Bangalee and Tribal healthy volunteers were 17.88 ± 1.14 & 18.58 ± 0.71 ìg/mL, 2297.96 ± 222.49 & 2376.41 ± 149.99 ìg min/mL respectively and the difference was not significant (p>0.05). The T1/2 for Bangladeshi Bangalee and Tribal healthy volunteers were 97.50 ± 3.33 & 94.40 ± 2.33 min respectively and the difference was significant (p<0.05). The Mean Percent Absolute Bioavailability in Bangladeshi Bangalee and Tribal healthy volunteers was 56.76 ± 5.39 and 74.17 ± 3.90 respectively and the difference was highly significant (p<0.001). The study concluded that the pharmacokinetic parameters of amoxicillin significantly varied among Bangladeshi Bangalee and Bangladeshi Tribal healthy volunteers indicating necessity of further study on population pharmacokinetic to formulate tailor-made drug therapy in these groups of people. http://dx.doi.org/10.3329/bjpp.v26i1-2.19958 Bangladesh J Physiol Pharmacol 2010; 26(1&2) : 1-9

scholarly journals Pharmacokinetic Parameters of Ciprofloxacin in Bangladeshi Volunteers: A Preliminary Evaluation

2014 ◽  
Vol 27 (1-2) ◽  
pp. 1-8
Author(s):  
Reefat Zaman Chowdhury ◽  
Md Saiful Islam ◽  
Md Sayedur Rahman
Keyword(s):  
Healthy Volunteers ◽  
Oral Route ◽  
Absolute Bioavailability ◽  
Pharmacokinetic Parameters ◽  
Intravenous Route ◽  
Population Pharmacokinetic ◽  
Healthy Male ◽  
Healthy Male Volunteers ◽  
Male Volunteers ◽  
The Difference

The present study has attempted to establish a High-performance liquid chromatography (HPLC) method to determine ciprofloxacin in plasma, in order to evaluate the bioavailability of ciprofloxacin. In this study, initially 8 (eight) Bangladeshi Bangalee healthy male volunteers and 7 (seven) Bangladeshi Tribal healthy male volunteers received 500 mg tablet of pioneer brand of ciprofloxacin in oral route. Blood samples were collected at 0, 30, 60, 120, 180, 360, 540 and 720 minutes after drug administration. After 1 week of washout period, same volunteers of two groups received 200 mg injection of pioneer brand of ciprofloxacin in intravenous route. HPLC with ultraviolet detection was used to quantify plasma ciprofloxacin concentrations. In case of oral route, AUC0–12h, Cmax, Tmax and T1/2 values for Bangladeshi Bangalee and Tribal healthy volunteers were 545.53 ± 32.35 & 655.74 ± 16.57 ?g min/mL, 2.19 ± 0.16 & 2.49 ± 0.20 ?g/mL, 75.00 ± 27.77 & 94.29 ± 32.07 min and 241.96 ± 13.53 & 242.02 ± 19.88 min respectively. In case of intravenous route, the AUC0–12h, Cmax, Tmax and T1/2 values for Bangladeshi Bangalee and Tribal healthy volunteers were 344.07 ± 29.31 & 343.31 ± 25.34 ?g min/mL, 2.47 ± 0.17 & 2.46 ± 0.18 ?g/mL, 30.00 ± 0.00 & 30.0 ± 0.0 min and 278.16 ± 1.74 & 272.74 ± 4.42 min respectively and the difference between these two groups of volunteers was not significant. The difference in AUC0–12h, Cmax, Tmax and T1/2 values between these two groups of volunteers was significant. The mean percent absolute bioavailability in Bangladeshi Bangalee and Tribal healthy volunteers was 64.04 ± 3.21 and 76.81 ± 6.71 respectively. In conclusion, pharmacokinetic parameters of ciprofloxacin significantly varied among Bangladeshi Bangalee and Bangladeshi Tribal healthy volunteers indicating necessity of further study on population pharmacokinetic in these groups of people. DOI: http://dx.doi.org/10.3329/bjpp.v27i1-2.20066 Bangladesh J Physiol Pharmacol 2011;27(1&2):1-8.

Pharmacokinetics of Benzoic Acid, 4-[[(2-Hydroxyethyl)Amino]Carbonyl]- Methyl Ester from Portulaca Oleracea L. in Rats after Intravenous and Oral Administrations Using UHPLC-ESI-Q-TOF/MS

2020 ◽  
Vol 16 (5) ◽  
pp. 601-607
Author(s):  
Haoran Xu ◽  
Zheming Ying ◽  
Lina Wang ◽  
Wenjie Zhang ◽  
Xixiang Ying ◽  
...  
Keyword(s):  
Methyl Ester ◽  
Benzoic Acid ◽  
High Performance ◽  
Internal Standard ◽  
High Performance Liquid Chromatographic ◽  
Absolute Bioavailability ◽  
Pharmacokinetic Parameters ◽  
Pharmacokinetic Data ◽  
Flight Mass Spectrometry ◽  
Tof Ms

Objective: The aim of this study is to investigate the pharmacokinetics of benzoic acid, 4- [[(2-hydroxyethyl)amino]carbonyl], methyl ester in rats after intravenous and oral administrations at doses of 3 mL/kg. Methods: A rapid, high selective ultra-high performance liquid chromatographic electrospray quadrupole- time of flight mass spectrometry (UHPLC-ESI-Q-TOF/MS) method was applied to investigate the pharmacokinetics of benzoic acid, 4-[[(2-hydroxyethyl)amino]carbonyl]-, methyl ester with p-coumaric acid as internal standard (IS) in rats after intravenously and orally dosed. Results: The pharmacokinetic data of benzoic acid, 4-[[(2-hydroxyethyl)amino]carbonyl]-, methyl ester was analyzed in the two-compartment open model. The main pharmacokinetic parameters were, respectively, 36.474 μg·h/mL, 12.59 μg·h/mL (AUC0→∞), and T1/2α was 0.14 h, 0.359 h; T1/2β was 3.046 h, 5.646 h after intravenous and oral administrations. Conclusion: Benzoic acid, 4-[[(2-hydroxyethyl)amino] carbonyl]-, methyl ester was rapidly distributed in rat’s plasma with the absolute bioavailability of 34.5%.

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 &lt; 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 &lt; 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.

scholarly journals Pharmacokinetics of Ganciclovir during Continuous Venovenous Hemodiafiltration in Critically Ill Patients

2013 ◽  
Vol 58 (1) ◽  
pp. 94-101 ◽  
Author(s):  
Thomas Horvatits ◽  
Reinhard Kitzberger ◽  
Andreas Drolz ◽  
Christian Zauner ◽  
Walter Jäger ◽  
...  
Keyword(s):  
Critically Ill ◽  
Critically Ill Patients ◽  
High Performance ◽  
Area Under The Curve ◽  
Antiviral Agent ◽  
Pharmacokinetic Analysis ◽  
Pharmacokinetic Parameters ◽  
Population Pharmacokinetic ◽  
Target Area ◽  
Continuous Venovenous Hemodiafiltration

ABSTRACTGanciclovir is an antiviral agent that is frequently used in critically ill patients with cytomegalovirus (CMV) infections. Continuous venovenous hemodiafiltration (CVVHDF) is a common extracorporeal renal replacement therapy in intensive care unit patients. The aim of this study was to investigate the pharmacokinetics of ganciclovir in anuric patients undergoing CVVHDF. Population pharmacokinetic analysis was performed for nine critically ill patients with proven or suspected CMV infection who were undergoing CVVHDF. All patients received a single dose of ganciclovir at 5 mg/kg of body weight intravenously. Serum and ultradiafiltrate concentrations were assessed by high-performance liquid chromatography, and these data were used for pharmacokinetic analysis. Mean peak and trough prefilter ganciclovir concentrations were 11.8 ± 3.5 mg/liter and 2.4 ± 0.7 mg/liter, respectively. The pharmacokinetic parameters elimination half-life (24.2 ± 7.6 h), volume of distribution (81.2 ± 38.3 liters), sieving coefficient (0.76 ± 0.1), total clearance (2.7 ± 1.2 liters/h), and clearance of CVVHDF (1.5 ± 0.2 liters/h) were determined. Based on population pharmacokinetic simulations with respect to a target area under the curve (AUC) of 50 mg · h/liter and a trough level of 2 mg/liter, a ganciclovir dose of 2.5 mg/kg once daily seems to be adequate for anuric critically ill patients during CVVHDF.

scholarly journals Pharmacokinetics study of Pioglitazone (30 mg) tablets in healthy volunteers

2015 ◽  
Vol 13 (2) ◽  
pp. 181-186 ◽  
Author(s):  
Sajal K Saha ◽  
AK Azad Chowdhury ◽  
Sitesh C Bachar
Keyword(s):  
High Performance ◽  
Reversed Phase ◽  
Pharmacokinetic Parameters ◽  
German Population ◽  
Polymorphic Variation ◽  
Healthy Male ◽  
Insulin Sensitizer ◽  
Bangladeshi Population ◽  
Randomized Protocol

Pioglitazone, an excellent insulin sensitizer, is used for the treatment of type 2 diabetes mellitus (T2DM). The present investigation demonstrated a single dose pharmacokinetic study of pioglitazone tablet in 24 healthy male volunteers in a randomized protocol. Blood samples were collected before and 0.5 to 24.0 h after a single oral dose of a 30 mg pioglitazone tablet. Plasma pioglitazone level was determined using a validated method of reversed phase binary high performance liquid chromatography (HPLC). The pharmacokinetic parameters determined were 1.117 ± 0.315 (?g/ml), 2.5 ± 0.735 (h), 9.014 ± 3.385 (?g.h/ml), 8.081 ± 3.407 (?g. h/ml), 1.315 ± 0.964 (h), 0.707 ± 1.636 (h-1), 0.078 ± 0.02 (h-1) and 8.884 ± 03.808 (h) for Cmax, Tmax, AUC0-?, AUC0-24, Ka, T1/2 (?), Kel, and T1/2(?), respectively. Variation of pioglitazone pharmacokinetic parameters in Bangladeshi population compared to Chinese, Thai and German population may indicate the polymorphic variation in the pioglitazone responsive metabolizing gene CYP3A4 and CYP2C19 in our population. DOI: http://dx.doi.org/10.3329/dujps.v13i2.21896 Dhaka Univ. J. Pharm. Sci. 13(2): 181-186, 2014 (December)

scholarly journals Dissolution efficiency and bioequivalence study using urine data from healthy volunteers: a comparison between two tablet formulations of cephalexin

2015 ◽  
Vol 51 (2) ◽  
pp. 383-392
Author(s):  
Cristina Helena dos Reis Serra ◽  
Kyung Hee Chang ◽  
Thaisa Marinho Dezani ◽  
Valentina Porta ◽  
Sílvia Storpirtis
Keyword(s):  
Urinary Excretion ◽  
Healthy Volunteers ◽  
High Performance ◽  
Bioequivalence Study ◽  
Immediate Release ◽  
International Standards ◽  
Pharmacokinetic Parameters ◽  
Tablet Formulations ◽  
Dissolution Efficiency

<p>The aim of the present study was to assess the bioequivalence of two cephalexin tablet formulations available in the Brazilian market (product A as reference formulation and product B as test formulation). Dissolution efficiency (DE%) was calculated for both formulations to evaluate their <italic>in vitro</italic>biopharmaceutical features. The oral bioequivalence study was performed in twenty-four healthy volunteers in a crossover design. Single oral dose (tablet containing 500 mg of cephalexin) of each product was administered with two weeks of washout period. Urinary concentrations of cephalexin were measured by high-performance liquid chromatography (HPLC) method and pharmacokinetics parameters were estimated by urinary excretion data. The bioequivalence was determined by the following parameters: the cumulative amount of cephalexin excreted in the urine, the total amount of cephalexin excreted in the urine and the maximum urinary excretion rate of cephalexin. DE values of immediate-release cephalexin tablets (500 mg) were 68.69±4.18% for product A and 71.03±6.63% for product B. Regarding the dissolution test of the two brands (A and B) analysed, both were in compliance with the official pharmacopeial specifications, since the dissolution of both formulations was superior to 80% of the amount declared in the label after 45 minutes of test (A=92.09%±1.84; B=92.84%±1.08). The results obtained indicated that the products A and B are pharmaceutical equivalents. Confidence intervals for the pharmacokinetic parameters were in compliance with the international standards, indicating that products A and B can be considered bioequivalents and, therefore, interchangeable.</p>

scholarly journals Bioequivalence Study of Donepezil Hydrochloride Tablets in Healthy Male Volunteers

2012 ◽  
Vol 2012 ◽  
pp. 1-4
Author(s):  
Noppamas Rojanasthien ◽  
Siriluk Aunmuang ◽  
Nutthiya Hanprasertpong ◽  
Sukit Roongapinun ◽  
Supanimit Teekachunhatean
Keyword(s):  
High Performance ◽  
Reference Product ◽  
Bioequivalence Study ◽  
Pharmacokinetic Parameters ◽  
Two Phase ◽  
Test Product ◽  
Male Volunteers ◽  
Bioequivalence Range ◽  
The Mean ◽  
The Difference

The objective of this study was to investigate the bioequivalence of two formulations of 5 mg donepezil HCL tablets: Tonizep as the test and Aricept as the reference. The two products were administered as a single oral dose according to a randomized two-phase crossover with a 3-week washout period in 20 healthy Thai Male volunteers. After drug administration, serial blood samples were collected over a period of 216 hours. Plasma donepezil concentrations were measured by high performance liquid chromatography with UV detection. Pharmacokinetic parameters were analyzed based on noncompartmental analysis. The logarithmically transformed data of AUC0–∞ and were analyzed for 90% confidence intervals (CI) using ANOVA. The mean (90% CI) values for the ratio of AUC0–∞ and values of the test product over those of the reference product were 1.08 (1.02–1.14) and 1.08 (0.99–1.17), respectively (within the bioequivalence range of 0.8–1.25). The median for the test product was similar to that of the reference product (2.0 hr), and the 90% CI for the difference between the two preparations was –0.19 to 0.29 hr and within the bioequivalence range of ± 20% of the of the reference formulation. Our study demonstrated the bioequivalence of the two preparations.

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 Pharmacokinetics of Pentanedioic Acid Imidazolyl Ethanamide in Healthy Volunteers

2021 ◽  
Vol 66 (1-2) ◽  
pp. 19-25
Author(s):  
I. G. Gordeev ◽  
V. I. Kazey ◽  
A. V. Kapashin ◽  
E. Е. Luchinkina ◽  
A. A. Globenko ◽  
...  
Keyword(s):  
Healthy Volunteers ◽  
High Performance ◽  
Antiviral Agent ◽  
Systemic Circulation ◽  
Medical Intervention ◽  
Intraindividual Variability ◽  
Pharmacokinetic Parameters ◽  
Plasma And Urine Samples ◽  
Long Time ◽  
Pentanedioic Acid

Relevance. Pentanedioic acid imidazolyl ethanamide (PAIE) has been used clinically as an antiviral agent for a long time, however, there is no information in the available literature concerning the dependence of PAIE pharmacokinetics on isoenzymes polymorphism of the cytochrome P450 system (CYP), as well as on the variability of pharmacokinetic parameters in humans. The aim of the study is to determine the main pharmacokinetic parameters of PAIE in healthy volunteers and to assess the contribution of polymorphism of CYP P450 isoenzymes to the variability of pharmacokinetic parameters.Material and methods. The study included 12 healthy volunteers (5 men and 7 women) of the Caucasian race, who took In[1]gavirin® at a dose of 180 mg (2 capsules of 90 mg) on an empty stomach during two dosing periods, separated by a 7-day washout period. Determination of PAIE concentration in blood plasma and urine samples was carried out by high-performance liquid chromatography–mass spectrometry. Polymorphism of CYP genes was analyzed using the polymerase chain re[1]action method in order to analyze the pharmacogenetic features of PAIE metabolism in volunteers during the study.Results. After oral administration, PAIE quickly reached the systemic circulation: the maximum concentration of 578.88±145.21 ng/ml was observed after about 2 hours. Pharmacokinetic parameters of PAIE did not show high intraindividual variability and did not depend on polymorphism of isoenzymes CYP1A1, CYP2C9, and CYP2D6. Within 48 hours after the administration of the studied drug, about half of the taken dose of PAIE was excreted in the urine unchanged, which indicates a significant contribution of the kidneys to the elimination of PAIE. The only adverse event registered in 1 volunteer was a clinically insignificant decrease in the level of leukocytes, which did not require medical intervention and was resolved without consequences.Conclusion. PAIE is characterized by predictable pharmacokinetics, low intraindividual variability of pharmacokinetic parameters, and a favorable safety profile.

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