A Scintigraphy and Pharmacokinetic Study to Evaluate the Absorption and Distribution of Buspirone Hydrochloride from a Triple-Pulse, Timed-Release Tablet.

Abstract: Purpose: To obtain data for development of a precision-timed release buspirone hydrochloride tablet (CTx-2103) that will provide a once-daily, anxiety treatment. This study elucidated the bioavailability, absorption of buspirone within the GI tract and evaluated the pharmacokinetics of four different release profiles. Methods: Multi-layered oral tablets formulated utilizing Cingulate’s Precision Timed Release ™ (PTR) platform and BDD’s patented OralogiK™ technology evaluated three timed-release profiles and one IR profile of buspirone. This four-arm, open-label study was conducted in healthy male volunteers. Dosing was separated by a minimum of 7 days. For the scintigraphy, timed-released doses were radiolabelled with 4 MBq technetium-99m. Abdominal images and blood sampling were evaluated at defined intervals. Results: Scintigraphic imaging visualized transit of the tablets through the gastrointestinal tract, confirming both the site and onset of release. Mean onset of radio-label release was 3.87±0.48 hrs., 9.40±1.10 hrs., and 10.1±1.52 hrs for the 4 hr, 8 hr and for the triple-pulse radio-labelled tablets, respectively. Pharmacokinetic data will be correlated with scintigraphic onset times to establish the full release profile of the tablets. Conclusions: Scintigraphic imaging demonstrated successful timed release of buspirone in the GI tract and pharmacokinetic data will determine bioavailability. Together, this data will inform the precise formulation and release profile of CTx-2103.Short Description: Cingulate has embarked on a program to develop CTx-2103 (buspirone), to expand the PTR platform into the anxiety therapeutic category. A four-arm, open-label study was conducted in healthy male volunteers dosed as follows: one timed-released 10 mg tablet (4-hr delay), one-timed released 10 mg tablet (8-hr delay), one triple-release 30 mg tablet (10 mg released at 0, 4, and 8 hrs.), and one IR 10 mg tablet. Scintigraphic imaging and pharmacokinetic data will be presented.Name of Sponsoring Organization(s): Cingulate