Co-crystals and eutectic compound of Nevirapine

COSTA, ROGERIA; REVIGLIO, ANA LUCÍA; GUIMARÃES, RENATA; SIEDLER, SANA; GARRO LINCK, YAMILA; MONTI, GUSTAVO; JACKSON, ANTÕNIO LAMOUNIER CAMARGO; ROCHA, HELVÉTICO VINÍCIUS ANTUNES; CUFFINI, SILVIA

Limerick

Conferencia; 2018 Annual Conference of Britich Assosiation of Crystal Growth (BACG); 2018

Britich Assosiation of Crystal Growth (BACG)

Nevirapine (NVP) is an anti-HIV drug approved for the treatment of human immunodeficiency virus type 1 infection (HIV-1) [1]. Co-crystals and eutectics are among all possible crystalline modifications; moreover both co-crystals and eutectics have been used to improve the physicochemical and pharmaceutical properties of drugs. 2,3 Hence, the aim of this work is the screening using different coformers in order to determine the possible compounds of NVP with the structural and  physicochemical characterization. Five different co-formers were used, namely: salicylic acid (SA), saccharin (SAC), caffeine (CAF), theophylline (THEO) and urea (URE). Samples were characterized by X-ray diffraction pattern (XRPD) conventional and synchrotron radiation, differential scanning calorimetry (DSC) and nuclear magnetic resonance spectroscopy (NMR). Caira and co-workers reported the crystal structure and solid-state properties of several NVP co-crystals, 4 including NVP-SA and NVP-SAC. These data were used as reference to characterize NVP-SAC and NVP-SA. However, differences were observed in NVP-SA co-crystal and, also, a phase transition between room temperature and 100K. In the case of NVP-CAF, NVP-THEO and NVP-URE, the eutectic compounds were characterized for the CAF and THEO and a solid mixture for URE.