scholarly journals Relative bioavailability, food effect, and safety of the single-dose pharmacokinetics of omecamtiv mecarbil following administration of different modified-release formulations in healthy subjects

2016 ◽  
Vol 54 (03) ◽  
pp. 217-227 ◽  
Author(s):  
Rameshraja Palaparthy ◽  
Christopher Banfield ◽  
Paco Alvarez ◽  
Lucy Yan ◽  
Brian Smith ◽  
...  
Keyword(s):  
Single Dose ◽  
Healthy Subjects ◽  
Food Effect ◽  
Relative Bioavailability ◽  
Modified Release ◽  
Omecamtiv Mecarbil

scholarly journals Single-dose FTY720 pharmacokinetics, food effect, and pharmacological responses in healthy subjects

2004 ◽  
Vol 57 (5) ◽  
pp. 586-591 ◽  
Author(s):  
John M. Kovarik ◽  
Robert Schmouder ◽  
Denise Barilla ◽  
Yibin Wang ◽  
Gerolf Kraus
Keyword(s):  
Single Dose ◽  
Healthy Subjects ◽  
Food Effect

scholarly journals 0745 The Pharmacokinetics of FT218, Once Nightly Sodium Oxybate: Food Effect and Bioavailability Compared to Twice Nightly Sodium Oxybate

SLEEP ◽  
2020 ◽  
Vol 43 (Supplement_1) ◽  
pp. A283-A283
Author(s):  
M Thorpy ◽  
D Seiden ◽  
J Grassot ◽  
D Monteith ◽  
J Dubow ◽  
...  
Keyword(s):  
Single Dose ◽  
Controlled Release ◽  
Food Effect ◽  
Relative Bioavailability ◽  
Sodium Oxybate ◽  
Pharmacokinetic Studies ◽  
Release Formulation ◽  
Fed State ◽  
Fasted State ◽  
Bioavailability Study

Abstract Introduction Sodium oxybate is an effective treatment for excessive daytime sleepiness and cataplexy in patients with narcolepsy. The FDA approved formulation requires twice-nightly dosing; at bedtime and 2.5 - 4 hours later. FT218 is a controlled-release formulation of sodium oxybate intended for once-nightly dosing, using Avadel’s proprietary Micropump™ technology. The objective of this study was to evaluate the relative bioavailability of investigational once-nightly sodium oxybate, FT218, 6 g, compared to commercially available twice-nightly sodium oxybate and the food effect of FT218. Methods Two crossover, single-dose pharmacokinetic studies were conducted in healthy volunteers. The first, a relative bioavailability study (n=28) was completed comparing FT218 6 g to twice-nightly sodium oxybate 6 g (in two divided doses of 3 g). The second, evaluated the food effect (n=16) of FT218 6g in the Fed vs. Fasted state. Results FT218 had a lower overall Cmax than twice-nightly sodium oxybate, while AUC was equivalent. C8h level and variability was comparable between FT218 and twice-nightly sodium oxybate. In the Fed, compared to the Fasted state, FT218 had a longer Tmax, lower Cmax and decreased AUC (Cmax 67%, AUC 86%, Tmax 1-hour slower than Fasted values). Adverse Events with FT218 were mostly mild or moderate in severity, non-serious and known AEs associated with sodium oxybate. The safety profiles of FT218 and twice-nightly sodium oxybate at 6 g appeared similar. Conclusion Once-nightly FT218 at 6 g demonstrated a lower overall Cmax and similar exposure to twice-nightly sodium oxybate, with similar C8h plasma levels and C8h variability. In the Fed state, AUC and Cmax of FT218 was lower than in the Fasted State. FT218 was generally safe and well tolerated and the safety profile appeared comparable to twice-nightly sodium oxybate. Support This work was supported by Avadel Pharmaceuticals.

scholarly journals Single‐dose pharmacokinetics, safety, and tolerability of modified‐release formulations of lersivirine in healthy subjects

2014 ◽  
Vol 3 (6) ◽  
pp. 472-476
Author(s):  
Manoli Vourvahis ◽  
Ronnie Wang ◽  
Laure Mendes da Costa ◽  
Cunshan Wang ◽  
Barry Weatherley ◽  
...  
Keyword(s):  
Single Dose ◽  
Healthy Subjects ◽  
Modified Release

scholarly journals Apixaban, an oral, direct factor X a inhibitor: single dose safety, pharmacokinetics, pharmacodynamics and food effect in healthy subjects

2013 ◽  
Vol 75 (2) ◽  
pp. 476-487 ◽  
Author(s):  
Charles Frost ◽  
Jessie Wang ◽  
Sunil Nepal ◽  
Alan Schuster ◽  
Yu Chen Barrett ◽  
...  
Keyword(s):  
Single Dose ◽  
Healthy Subjects ◽  
Food Effect ◽  
Factor X ◽  
Direct Factor

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 Relative Bioavailability of a Single Dose of Belimumab Administered Subcutaneously by Prefilled Syringe or Autoinjector in Healthy Subjects

2015 ◽  
Vol 5 (3) ◽  
pp. 208-215 ◽  
Author(s):  
Herbert Struemper ◽  
Thomas Murtaugh ◽  
Jane Gilbert ◽  
Matthew E. Barton ◽  
Joseph Fire ◽  
...  
Keyword(s):  
Single Dose ◽  
Healthy Subjects ◽  
Relative Bioavailability ◽  
Prefilled Syringe
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