Preparation and characterization of a new naproxen salt and its hydrates

ANTONIO, MARINA; MAGGIO, RUBÉN M.

Virtual

Congreso; VI Reunión Internacional de Ciencias Farmacéuticas (RICIFA 2020+1); 2021

RICIFA

Naproxen (NAP) is a nonsteroidal anti-inflammatory drug indicated in the treatment of muscle pain, dysmenorrhea, rheumatoid arthritis and osteoarthritis. Due to its poor solubility, its generally administered orally as the sodium salt (NS) but is contraindicated in patients with hypertension. In the present work a new salt of potassium (NP) was obtained by direc recritalization and two hydrates, monohydrate (MH) and dihydrate (DH), were prepared under controles tempertures and humidity conditions, as suitable soluble and sodium less altenatives to NS. The full characterization of new forms was carried out by powder X-ray diffraction, differential scanning calorimetry, thermogravimetry, raman, middle- and near-infrared spectroscopies. These studies revealed that the crystalline structure of NP, MH and DH are different from that of the NAP and NS. The purity degree was determined by determining free naproxen (USP). Functional characterization of new forms by intrinsic dissolution rate showed a significant increase in the solubility of NP with respect to NS, as aditional advante of the new salt. In conclusions, it was possible to obtain a NP salt and its hydrates by a simple and efficient crystallization procedure, which can be considered as a suitable alternative to improve the solubility characteristics of NAP, without sodioum intake.