title: Studies of phase transitions in the aripiprazole solid dosage form.
abstract: Studies of the phase transitions in an active substance contained in a solid dosage form are very complicated but essential, especially if an active substance is classified as a BCS Class IV drug. The purpose of this work was the development of sensitive methods for the detection of the phase transitions in the aripiprazole tablets containing initially its form III. Aripiprazole exhibits polymorphism and pseudopolymorphism. Powder diffraction, Raman spectroscopy and differential scanning calorimetry methods were developed for the detection of the polymorphic transition between forms III and I as well as the phase transition of form III into aripiprazole monohydrate in tablets. The study involved the initial 10 mg and 30 mg tablets, as well as those stored in Al/Al blisters, a triplex blister pack and HDPE bottles (with and without desiccant) under accelerated and long term conditions. The polymorphic transition was not observed in the initial and stored tablets but it was visible on the DSC curve of the Abilify(®) 10 mg reference tablets. The formation of the monohydrate was observed in the diffractograms and Raman spectra in the tablets stored under accelerated conditions. The monohydrate phase was not detected in the tablets stored in the Al/Al blisters under long term conditions. The results showed that the Al/Al blisters can be recommended as the packaging of the aripiprazole tablets containing form III.
authors.affiliation: Pharmaceutical Research Institute, 8 Rydygiera Street, Warsaw 01-793, Poland.
authors.forename: Marta
authors.initials: M
authors.lastname: Łaszcz
authors.affiliation: Pharmaceutical Research Institute, 8 Rydygiera Street, Warsaw 01-793, Poland. Electronic address: m.laszcz@ifarm.eu.
authors.forename: Anna
authors.initials: A
authors.lastname: Witkowska
mesh_terms: D014150:Antipsychotic Agents / Q000032:analysis* / Q000737:chemistry*; D000068180:Aripiprazole / Q000032:analysis* / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods; D004304:Dosage Forms; D044367:Phase Transition; D033362:Powder Diffraction / Q000379:methods; D013607:Tablets; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D014150:Antipsychotic Agents; D004304:Dosage Forms; D013607:Tablets; D000068180:Aripiprazole
keywords: Active substance; Aripiprazole; Phase transitions; Solid dosage form