Preparation and characterization of a new naproxen salt and its hydrates

ANTONIO, MARINA; MAGGIO, RUBÉN M.

Córdoba

Congreso; 6ta Reunión Internacional de Ciencias Farmacéuticas (RICiFa); 2021

Universidad Nacional de Córdoba

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 direct recrytallization and two hydrates, monohydrate (MH) and dihydrate (DH), were prepared under controlled temperturesand humidity conditions, as suitable soluble alternatives 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 demonstrated by determining free naproxen (USP 38-NF 33). Functional characterization of new forms by intrinsic dissolution rate showed a significant increase in the solubility of NP with respect to NS, as additional advantage 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 sodium intake.