Solid dispersions of MELOXICAM-POLOXAMER 188. solid state properties

CALCAGNO A.J; PALMA S.D.; GARCÍA M.S. ; CABRERA F.; RAMÍREZ RIGO M.V. ; PIÑA J.

Rosario

Congreso; Reunión Internacional de Ciencias Farmacéuticas/ RICiFA; 2012

Univ. Nac. de Rosario

Meloxicam (MX) is a non-steroidal anti-inflammatory drug used in the treatment of osteoarthritis and other joint diseases that has low solubility and poor wetting properties (1). These characteristics make MX a good candidate for the development of solid dispersions (SDs, dispersions of one or more drugs in a solid inert matrix) (2). In order to improve the bioavailability of MX, SDs of the drug with Poloxamer 188 (PX, an amphiphilic copolymer) were prepared by melting (3). In previous studies, the effects of PX on the MX aqueous solubility and on the in vitro drug dissolution were evaluated. PX was found effective to increase both the apparent solubility and dissolution rate of MX (4). Furthermore, FT-Infrared Spectroscopy (FT-IR), Differential Scanning Calorimetry (DSC), Powder X-ray diffractometry (XRD) and Scanning Electron Microscopy (SEM) allowed postulating that the increase in drug dissolution rate was not due to a MX crystalline-to-amorphous transformation. The results also revealed the lack of homogeneity in physical mixtures (PMs). In this work and for the developed solid products, Hot Stage Microscopy (HSM), Particle Size Distribution (PSD) and Powder Rheology tests were performed in order to clarify the thermal behavior of the samples during heating, the changes in PSDs associated to the production processes and the flow properties, respectively.