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Clin Pharmacol. 2016 Oct 12;8:155-162. eCollection 2016.

Bioavailability study of dronabinol oral solution versus dronabinol capsules in healthy volunteers.

Author information

1
INSYS Therapeutics, Inc., Chandler, AZ, USA.
2
Kramer Consulting LLC, North Potomac, MD, USA.

Abstract

BACKGROUND:

Dronabinol, a pharmaceutical Δ-9-tetrahydrocannabinol, was originally developed as an oral capsule. This study evaluated the bioavailability of a new formulation, dronabinol oral solution, versus a dronabinol capsule formulation.

METHODS:

In an open-label, four-period, single-dose, crossover study, healthy volunteers were randomly assigned to one of two treatment sequences (T-R-T-R and R-T-R-T; T = dronabinol 4.25 mg oral solution and R = dronabinol 5 mg capsule) under fasted conditions, with a minimum 7-day washout period between doses. Analyses were performed on venous blood samples drawn 15 minutes to 48 hours postdose, and dronabinol concentrations were assayed by liquid chromatography-tandem mass spectrometry.

RESULTS:

Fifty-one of 52 individuals had pharmacokinetic data for analysis. The 90% confidence interval of the geometric mean ratio (oral solution/capsule) for dronabinol was within the 80%-125% bioequivalence range for area under the plasma concentration-time curve (AUC) from time zero to last measurable concentration (AUC0-t) and AUC from time zero to infinity (AUC0-∞). Maximum plasma concentration was also bioequivalent for the two dronabinol formulations. Intraindividual variability in AUC0-∞ was >60% lower for dronabinol oral solution 4.25 mg versus dronabinol capsule 5 mg. Plasma dronabinol concentrations were detected within 15 minutes postdose in 100% of patients when receiving oral solution and in <25% of patients when receiving capsules.

CONCLUSION:

Single-dose dronabinol oral solution 4.25 mg was bioequivalent to dronabinol capsule 5 mg under fasted conditions. Dronabinol oral solution formulation may provide an easy-to-swallow administration option with lower intraindividual variability as well as more rapid absorption versus dronabinol capsules.

KEYWORDS:

pharmacokinetics; safety; variability; Δ-9-tetrahydrocannabinol

Conflict of interest statement

NP, VK, CCS, and SV are full-time employees of INSYS Therapeutics, Inc. WGK is a paid consultant to INSYS Therapeutics, Inc. The authors report no other conflicts of interest in this work.

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