Affiliation:
1. Research Directorate, Gedeon Richter Plc, Budapest,
Hungary
Abstract
Abstract
IntroductionCariprazine is an atypical dopamine receptor partial agonist
antipsychotic available in the form of capsules. Although capsules are one of
the most desirable routes of administration, there are certain situations
(e. g., in an acute psychiatric setting, or when swallowing difficulties, or
liquid shortages are present) when they cannot be administered. Therefore,
alternative solutions like orodispersible tablets are needed. This study aimed
to investigate the bioequivalence of a newly developed orodispersible tablet to
the commercially available hard gelatine capsule of cariprazine 1.5 mg.
MethodsThis was a phase I, open-label, randomized, single-dose
bioequivalence study. It had a 2-period, 2-sequence, cross-over design, where
each subject received one test and one reference product in a randomized
sequence, separated by a wash-out period of 55 days. Blood sampling was
performed over 72 h after dosing. Cariprazine concentrations were analyzed by a
validated HPLC-MS/MS method. Standard bioequivalence statistics was applied to
PK parameters calculated by non-compartmental analysis. Safety measures were
analyzed descriptively.
ResultPharmacokinetic data of 43 healthy volunteers and safety data of 54
subjects was analyzed. Cariprazine AUC0–72h and Cmax
geometric mean ratios were 117.76% and 100.88%, respectively. The 90% confidence
intervals were within the pre-defined bioequivalence acceptance limits of 80.00%
– 125.00%. Safety data was in line with the Summary of Product Characteristics
of Cariprazine.
Discussion The result of this clinical trial proved the bioequivalence of
the new orodispersible tablet formulation when compared to hard gelatine
capsules, enabling an alternative option for treatment of those suffering from
schizophrenia.