Exploring Co-Amorphous Formulations Of Nevirapine: Insights From Computational, Thermal, And Solubility Analyses.

Autor: Dos Santos KA; Quality Control Core of Medicines and Correlates - NCQMC, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife, PE, Brazil., Chaves LL; Quality Control Core of Medicines and Correlates - NCQMC, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife, PE, Brazil.; Postgraduate Program in Pharmaceutical Sciences, Pharmaceutical Sciences Institute, Federal University of Alagoas, Maceió, Alagoas, Brazil., Nadvorny D; Postgraduate Program in Pharmaceutical Sciences, Pharmaceutical Sciences Institute, Federal University of Alagoas, Maceió, Alagoas, Brazil., de La Roca Soares MF; Quality Control Core of Medicines and Correlates - NCQMC, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife, PE, Brazil.; Postgraduate Program in Pharmaceutical Sciences, Pharmaceutical Sciences Institute, Federal University of Alagoas, Maceió, Alagoas, Brazil., Sobrinho JLS; Quality Control Core of Medicines and Correlates - NCQMC, Department of Pharmaceutical Sciences, Federal University of Pernambuco, Recife, PE, Brazil. joselamartine@hotmail.com.
Jazyk: angličtina
Zdroj: AAPS PharmSciTech [AAPS PharmSciTech] 2024 Sep 12; Vol. 25 (7), pp. 214. Date of Electronic Publication: 2024 Sep 12.
DOI: 10.1208/s12249-024-02932-5
Abstrakt: This study aimed to assess the formation of nevirapine (NVP) co-amorphs systems (CAM) with different co-formers (lamivudine-3TC, citric acid-CAc, and urea) through combined screening techniques as computational and thermal studies, solubility studies; in addition to develop and characterize suitable NVP-CAM. NVP-CAM were obtained using the quench-cooling method, and characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD), Fourier Transform Infrared Spectroscopy (FTIR), and polarized light microscopy (PLM), in addition to in vitro dissolution in pH 6.8. The screening results indicated intermolecular interactions occurring between NVP and 3TC; NVP and CAc, where shifts in the melting temperature of NVP were verified. The presence of CAc impacted the NVP equilibrium solubility, due to hydrogen bonds. DSC thermograms evidenced the reduction and shifting of the endothermic peaks of NVP in the presence of its co-formers, suggesting partial miscibility of the compounds. Amorphization was proven by XRD and PLM assays. In vitro dissolution study exhibited a significant increase in solubility and dissolution efficiency of NVP-CAM compared to free NVP. Combined use of screening studies was useful for the development of stable and amorphous NVP-CAM, with increased NVP solubility, making CAM promising systems for combined antiretroviral therapy.
(© 2024. The Author(s), under exclusive licence to American Association of Pharmaceutical Scientists.)
Databáze: MEDLINE
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