FTIR, dissolution and anti-viral activity of nevirapine co-crystals
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Date
2017
Journal Title
Journal ISSN
Volume Title
Publisher
OMICS International
Abstract
The study uses Fourier Transform Infrared (FTIR) spectroscopy to identify five Nevirapine (NV) co-crystals,
determines the dissolution profile of the co-crystals and the antiviral activity comparative to pure NV.
Hot stage microscopy measured the purity and integrity of each co-crystal. FTIR analysis was used to identify the
co-crystals to make recommendations regarding the future use of the technique to identify the NV co-crystals.
Dissolution studies of the NV co-crystals prepared with maleic acid, salicylic acid and glutaric acid (NVMLE, NVSLI
and NVGLT, respectively) were completed using the rotating basket method. Assays were conducted using High
Performance Liquid Chromatography and compared to pure NV and the five NV: co-former mixtures. The antiviral
activity was tested to determine whether the co-crystals had an improved activity against HIV-1 compared to pure
NV.
All co-crystals, except NVTTA (a NV co-crystal prepared with rac-tartaric acid), were pure and maintained their
integrity for approximately one year. NVGLT, NVMLE and NVTTA, 1:1 molar ratio co-crystals were identified by
FTIR. The C=O stretching frequency of the carboxylic acid groups of NV and GLT were observed at 1638.15 cm-1
and 1719.23 cm-1 in the NVGLT co-crystal which corresponded with spectra of NVMLE and NVTTA. In NVMLE the
C=O stretching frequency of the C=O of NV and MLE were observed at 1640.58 cm-1 and 1694.10 cm-1 and in
NVTTA it was at 1637.25 cm-1 and 1708.50 cm-1, suggesting the presence of both parent molecules in the new
phase for NVGLT, NVMLE and NVTTA.
Dissolution studies suggested that NVGLT was the only co-crystal that yielded better results than both NV and its
physical mixture. The antiviral activity of the NVSC (an NV co-crystal prepared with saccharin) and NVSLI cocrystals
in DMSO was significantly different to pure NV, demonstrating an improvement in anti-viral activity.
Description
Keywords
Co-crystals, Nevirapine, Dissolution rate, Scale-up, Antiviral activity, FTIR, Solubility
Citation
Samsodien, H., et al. (2017). FTIR, dissolution and anti-viral activity of nevirapine cocrystals. Pharmaceautica Analytica Acta, 8(9): 561