4TH International Congress on Technology - Engineering & SCIENCE - Kuala Lumpur - Malaysia (2017-08-05)

Characteristics Of Agomelatine Cocrystals Prepared By Spray Drying Process

It has been extensively demonstrated that the pharmaceutical properties including the solubility, dissolution rate, and ultimately bioavailability of BCS classⅡ insoluble drugs such as agomelatine can be substantially moderated by the co-crystal approach. In regard to the importance of pharmaceutical cocrystals, US FDA issued a draft guidance for industry in 2013 and updated it in 2016. As a consequence, pharmaceutical cocrystals are classified as a special case of solvates in which the second component is nonvolatile. In this study, cocrystals of agomelatine with the hydroquinone and resorcinol as coformer were produced employing the spray-drying process. Several solvents including cosolvents were examined to find out the ethyl acetate as optimal solvent in terms of powder’s physicochemical properties. Agomelatine co-crystals prepared by the spray drying method have a rather uniform particle size distribution. The average size was dependent upon process parameters such as spray rate. Powder sizes ranging 200~250 microns are expected to fit well for solid formulations such as tablets and capsules. The cocrystal powders were characterized powder x-ray diffraction (PXRD), differential scanning calorimetry (DSC) and others. Experimental procedure and data will be presented in detail in the poster session for scientific discussion.
MinYong Cho, Paul Kim, GuangJin Choi