Single‐Dose Pharmacokinetic Properties and Relative Bioavailability of Different Formulations of Posaconazole Oral Suspension in Healthy Volunteers

2018 ◽  
Author(s):  
Lucija Vuletić ◽  
Marina Herceg ◽  
Kristina Ferderber ◽  
Iva Tunjić ◽  
Simona Rizea‐Savu ◽  
...  
Keyword(s):  
Single Dose ◽  
Healthy Volunteers ◽  
Relative Bioavailability ◽  
Oral Suspension ◽  
Pharmacokinetic Properties

scholarly journals Comparative single-dose bioavailability study of two 10 mg Zolpidem tablet formulations in healthy volunteers

2019 ◽  
Vol 65 (01) ◽  
pp. 11-17
Author(s):  
Dimce Zafirov ◽  
Jasmina Trojacanec ◽  
Dragica Zendelovska ◽  
Nikola Kolovcevski ◽  
Bojan Labachevski
Keyword(s):  
Single Dose ◽  
Healthy Volunteers ◽  
Plasma Concentrations ◽  
Bioequivalence Study ◽  
Relative Bioavailability ◽  
Serious Adverse Events ◽  
Test Formulation ◽  
Single Oral Administration ◽  
Hypnotic Agent ◽  
Bioavailability Study

Zolpidem is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, pyrrolopyrazines, pyrazolopyrimidines or other drugs with known hypnotic properties. Zolpidem as conventional tablets is used as a hypnotic agent in the short-term management of insomnia, generally for periods not exceeding 7–10 days in duration. The objective of this study was to evaluate and compare the relative bioavailability, and therefore the bioequivalence of Zolpidem 10 mg test formulation versus a reference Zolpidem 10 mg formulation, following a single dose administration under fasting conditions The study was a single center, open, single dose, randomized, two - way crossover study in healthy male volunteers with a wash - out period of one week between study periods. Twenty-eight male healthy volunteers, aged 20-49 years were included into study. Blood samples for determination of zolpidem plasma concentrations were withdraw at 0 (pre-drug administration), 0.33, 0.66, 1, 1.33, 1.66, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 10, 12, 16 and 24 hours post-drug. The zolpidem concentrations in plasma were determined with HPLC, using fluorescence detection. The test formulation of zolpidem, dosed at 10 mg is bioequivalent for primary zolpidem parameters (Cmax, AUC0-t and AUC0-∞) to the reference formulation after a single oral administration of 10 mg zolpidem. Both medications are well tolerated with no serious adverse events. Thus, in view of the clinical use, both formulations are exchangeable without restrictions. Keywords: Zolpidem, bioavailability, bioequivalence study, single-dose

scholarly journals Single-dose pharmacokinetics of amphetamine extended-release tablets compared with amphetamine extended-release oral suspension

CNS Spectrums ◽  
2020 ◽  
Vol 25 (6) ◽  
pp. 774-781
Author(s):  
Antonio Pardo ◽  
Judith C. Kando ◽  
Thomas R. King ◽  
Eman Rafla ◽  
Barry K. Herman
Keyword(s):  
Single Dose ◽  
Adverse Events ◽  
Extended Release ◽  
Food Effect ◽  
Relative Bioavailability ◽  
Oral Suspension ◽  
Plasma Samples ◽  
Serious Adverse Events ◽  
Time Points ◽  
Extended Release Tablet

AbstractObjectiveEvaluate the relative bioavailability of single-dose amphetamine extended-release tablet (AMPH ER TAB) 20 mg, swallowed whole or chewed, and amphetamine extended-release oral suspension (AMPH EROS) 2.5 mg/mL; evaluate food effect on AMPH ER TAB.MethodsHealthy volunteers (18–55 years) were randomized to 1 dose of AMPH ER TAB 20 mg swallowed (fasted), chewed (fed/fasted), or 20 mg AMPH EROS (fasted). A crossover study design was used. Plasma samples were collected each period predose and at time points to 60 hours postdose. d- and l-amphetamine were measured and pharmacokinetic (PK) was calculated (90% confidence intervals of the ratios of the plasma levels) for AUC0-t, AUC0-∞, and Cmax. Comparative relative bioavailability between formulations was determined when ratios were within 80% and 125%. Safety was also assessed.ResultsThirty-two subjects completed the study. AMPH ER TAB swallowed versus AMPH EROS (fasted): for d- and l-amphetamine, the total and peak exposure was similar: d: AUC0-t: 100.68% to 108.08%, AUC0-∞: 101.47% to 109.52%, Cmax: 98.10% to 103.17%; l: AUC0-t: 100.31% to 108.57%, AUC0-∞: 101.27% to 111.09%, Cmax: 98.2% to 103.37%. For d- and l-amphetamine when the tablet is swallowed whole, Tmax was 5.00 hours (with a range of 2.00–9.00 hours). AMPH ER TAB chewed versus AMPH EROS (fasted): for d- and l-amphetamine, the total and peak exposure was similar: d: AUC0-t: 99.23% to 106.62%, AUC0-∞: 99.58% to 107.59%, Cmax: 99.91% to 105.14%; l: AUC0-t: 98.16% to 106.35%, AUC0-∞: 98.44% to 108.11%, Cmax: 99.53% to 104.75%. For d- and l-amphetamine when the tablet has been chewed, Tmax was 5.00 hours (with a range of 3.00-7.00 hours). PK results were similar for patients in the fasted and fed groups, indicative of no presence of food effect. No serious adverse events (AEs) were reported, overall AE profiles between the tablet and oral suspension were comparable without any unanticipated safety concerns.ConclusionsSingle doses of AMPH ER TAB for both d- and l-amphetamine demonstrated comparable bioavailability to a 20 mg dose of AMPH EROS, 2.5 mg/mL under fasted conditions when chewed and swallowed whole, and demonstrated equivalent peak and overall exposure without apparent food effect. AMPH ER TAB was well-tolerated and consistent with adverse events noted in other amphetamine formulations.

scholarly journals Bioavailability of Lumefantrine Is Significantly Enhanced with a Novel Formulation Approach, an Outcome from a Randomized, Open-Label Pharmacokinetic Study in Healthy Volunteers

2017 ◽  
Vol 61 (9) ◽  
Author(s):  
Jay Prakash Jain ◽  
F. Joel Leong ◽  
Lan Chen ◽  
Sampath Kalluri ◽  
Vishal Koradia ◽  
...  
Keyword(s):  
Single Dose ◽  
Healthy Volunteers ◽  
Solid Dispersion ◽  
Vital Signs ◽  
Study Drug ◽  
Relative Bioavailability ◽  
Open Label ◽  
Significant Treatment ◽  
Conventional Formulation ◽  
Clinically Significant

ABSTRACT The artemether-lumefantrine combination requires food intake for the optimal absorption of lumefantrine. In an attempt to enhance the bioavailability of lumefantrine, new solid dispersion formulations (SDF) were developed, and the pharmacokinetics of two SDF variants were assessed in a randomized, open-label, sequential two-part study in healthy volunteers. In part 1, the relative bioavailability of the two SDF variants was compared with that of the conventional formulation after administration of a single dose of 480 mg under fasted conditions in three parallel cohorts. In part 2, the pharmacokinetics of lumefantrine from both SDF variants were evaluated after a single dose of 480 mg under fed conditions and a single dose of 960 mg under fasted conditions. The bioavailability of lumefantrine from SDF variant 1 and variant 2 increased up to ∼48-fold and ∼24-fold, respectively, relative to that of the conventional formulation. Both variants demonstrated a positive food effect and a less than proportional increase in exposure between the 480-mg and 960-mg doses. Most adverse events (AEs) were mild to moderate in severity and not suspected to be related to the study drug. All five drug-related AEs occurred in subjects taking SDF variant 2. No clinically significant treatment-emergent changes in vital signs, electrocardiograms, or laboratory blood assessments were noted. The solid dispersion formulation enhances the lumefantrine bioavailability to a significant extent, and SDF variant 1 is superior to SDF variant 2.

scholarly journals Comparative single-dose bioavailability study of two 500 mg clarithromycin tablet formulations in healthy volunteers under fasting condition

2019 ◽  
Vol 65 (01) ◽  
pp. 19-26
Author(s):  
Nikola Labachevski ◽  
Dimche Zafirov ◽  
Jasmina Trojacanec ◽  
Krume Jakjovski ◽  
Emilija Atanasovska ◽  
...  
Keyword(s):  
Single Dose ◽  
Healthy Volunteers ◽  
Drug Administration ◽  
Bioequivalence Study ◽  
Immediate Release ◽  
Relative Bioavailability ◽  
Butyl Ether ◽  
Serious Adverse Events ◽  
Test Formulation

Clarithromycin is a semi-synthetic macrolide antibiotic, chemically 6-0-methylerythromycin, formulated as immediate-release tablets, extended-release tablets, and granules for oral suspension. The objective of this study was to evaluate and compare the relative bioavailability, and therefore the bioequivalence of Clarithromycin 500 mg test formulation versus a reference Klacid® forte 500 mg formulation, following a single dose administration under fasting conditions. The study was a single center, open, single dose, randomized, two-way crossover study in healthy male volunteers, with a wash-out period of one week between study periods. Twenty-four male healthy volunteers, aged 18-49 years were included into study. Blood samples for determination of clarithromycin and 14-OH clarithromycin concentrations were withdrawn at zero (pre-drug administration), 0.33, 0.66, 1, 1.5, 2, 2.5, 3, 3.5, 4, 5, 6, 8, 12, 24 and 36 hours post-drug administration. The determination of clarithromycin and 14-OH clarithromycin concentrations in plasma was performed using validated LC/MS/MS method and internal standardization after liquid/liquid extraction with methyl t-butyl ether. The test formulation of clarithromycin, dosed at 500 mg is bioequivalent for primary clarithromycin and 14-OH clarithromycin parameters (Cmax, AUC0-t and AUC0-∞) to the reference formulation after a single oral administration of 500 mg clarithromycin. Both medications were well tolerated with no serious adverse events. Thus, in view of the clinical use, both formulations are exchangeable without restrictions. Keywords: clarithromycin, 14-OH clarithromycin, bioavailability, bioequivalence study, single-dose

Bioavailability of Three Commercial Preparations of Ibuprofen 600 mg

1988 ◽  
Vol 16 (1) ◽  
pp. 44-49 ◽  
Author(s):  
E. Källström ◽  
M. Heikinheimo ◽  
H. Quiding
Keyword(s):  
Single Dose ◽  
Plasma Concentration ◽  
Crossover Study ◽  
Healthy Volunteers ◽  
Plasma Concentrations ◽  
Analgesic Efficacy ◽  
Relative Bioavailability ◽  
Maximum Plasma ◽  
The Mean ◽  
Extent Of Absorption

The pharmacokinetic variables of ibuprofen 600 mg were investigated after administration of Brufen and compared to administration of Burana and Ibumetin. The investigation was carried out as a randomized single-dose crossover study in 17 healthy volunteers. The mean maximum plasma concentrations of ibuprofen were 58, 45 and 54 μg/ml after administration of Brufen, Burana and Ibumetin, respectively, the time to reach this being 1.4, 2.1 and 1.6 h, respectively, after administration. The differences between Brufen and Burana were significant. The relative bioavailability was very similar between Brufen and Burana but about 8% lower for Ibumetin and this difference between Brufen and Ibumetin was significant. Thus, different brands of ibuprofen may not be pharmacokinetically interchangeable and the results show that Brufen is superior to either Burana or Ibumetin when considering both the rate and extent of absorption. These findings are clinically interesting since a high and early plasma concentration of ibuprofen seems to be related to increased analgesic efficacy.

Effects of Food Intake on the Pharmacokinetic Properties of Dalcetrapib: Findings From Three Phase I, Single-Dose Crossover Studies in Healthy Volunteers

2011 ◽  
Vol 33 (6) ◽  
pp. 754-765 ◽  
Author(s):  
Michael Derks ◽  
Hitoshi Kawamura ◽  
Markus Abt ◽  
Georgina Meneses-Lorente ◽  
Mary Phelan ◽  
...  
Keyword(s):  
Single Dose ◽  
Food Intake ◽  
Phase I ◽  
Healthy Volunteers ◽  
Crossover Studies ◽  
Three Phase ◽  
Pharmacokinetic Properties
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