Romanian Society of Pharmaceutical Sciences

« Back to Farmacia Journal 1/2019

DEVELOPMENT OF MELOXICAM ORAL LYOPHILISATES: ROLE OF THERMAL ANALYSIS AND COMPLEMENTARY TECHNIQUES

LUCIA MARIA RUS 1#, SONIA IURIAN 2#, IRINA KACSO 3, GHEORGHE BORODI 3, SEBASTIAN PORAV 3, SIMONA CODRUŢA HEGHEŞ 1, CRISTINA ADELA IUGA 1,4*, IOAN TOMUŢĂ 2

1.“Iuliu Hațieganu” University of Medicine and Pharmacy Cluj-Napoca, Faculty of Pharmacy, Department of Drug Analysis, 6 Louis Pasteur Street, 400349 Cluj-Napoca, Romania
2.“Iuliu Hațieganu” University of Medicine and Pharmacy Cluj-Napoca, Faculty of Pharmacy, Department of Pharmaceutical Technology and Biopharmaceutics, 41 Victor Babeș Street, 400012 Cluj-Napoca, Romania
3.National Institute of Research and Development for Isotopic and Molecular Technologies, 67-103 Donat Street, 400293 Cluj-Napoca, Romania
4.“Iuliu Hațieganu” University of Medicine and Pharmacy, Department of Proteomics and Metabolomics, MedFuture - Research Centre for Advanced Medicine, 8 Victor Babeș Street, 400000 Cluj-Napoca, Romania

Download Full Article PDF

The purpose of this study was to highlight the way in which thermoanalytical and complementary techniques can guide the development of meloxicam oral lyophilisates both in the preformulation and formulation stages, as well as for the final products characterization. Thermoanalytical methods (differential scanning calorimetry – DSC, thermogravimetry – TGA) and complementary methods (Fourier transform infrared – FTIR, X-Ray powder diffraction – XRPD, scanning electron microscopy – SEM) were applied in order to obtain a complete set of data. In the preformulation stage, the compatibility between meloxicam and excipients was assessed. DSC results showed the compatibility between meloxicam and excipients. Tg’ measurement in the frozen state led to the addition of an annealing step at -25°C into the freezing stage, to facilitate complete crystallization and end-product integrity. The designed lyophilization cycle yielded good cake appearance. The DSC, XRPD analysis as well as SEM morphology studies, performed in the final stage, evidenced that the meloxicam freeze-dried products were partially crystalline. By the TGA analysis the moisture content was evaluated in accordance or close to the recommended limits. In conclusion, thermoanalytical techniques are well suited for the design of freeze-drying process, in order to obtain good quality oral lyophilisates.