Preparation and Characterization of Beclomethasone Dipropionate Solvates

Cordula Weiss, Peter McLoughlin, Panagiotis Manesiotis, Wynette Redington, Helen Cathcart

Research output: Contribution to journalArticle

Abstract

Active pharmaceutical ingredients in dry powder inhaler (DPI) formulations need to have well-defined material properties. These can be influenced by the choice of processing parameters. The impact of methanol, ethanol, 1-propanol, 2-propanol, 1-butanol, 1-pentanol, and acetone on the crystallization of beclomethasone dipropionate (BDP), an anti-inflammatory agent, was studied using X-ray powder diffraction, thermal analysis, gas chromatography with mass spectrometry, scanning electron microscopy, and atomic force microscopy. Crystallization from methanol, 1-butanol, and 1-pentanol resulted in particulate BDP with a predominantly anhydrous character. In contrast, BDP solvates were formed using ethanol, 1-propanol, 2-propanol, or acetone. The solvates had different crystalline structures depending on the solvent used. Distinct thermal properties confirmed the inclusion of ethanol, 1-propanol, 2-propanol, and acetone within the crystalline BDP host. Furthermore, the size, shape, and surface characteristics of the crystalline particles were found to be influenced by the choice of solvent in a reproducible way. These properties were also found to translate to the anhydrous products prepared from the solvates through controlled desolvation. Such information is of value to the pharmaceutical industry, where knowledge of how specific factors affect the crystalline product would potentially allow one to tailor BDP to have specific material properties. Knowledge of how to control these properties by controlling specific processing parameters and to adjust them as desired would be of great benefit to DPI formulations, where surface properties are crucial to the efficacy of the treatment.
Original languageEnglish
Pages (from-to)5832-5844
Number of pages13
JournalCrystal Growth and Design
Volume18
Issue number10
DOIs
Publication statusPublished - 28 Aug 2018

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