Abstract
The physical and chemical characterization of the solid-state properties of drugs and excipients is fundamental for planning new formulations and developing new strategies for the treatment of diseases. Techniques such as differential scanning calorimetry, thermogravimetry, X-ray powder diffraction, Fourier transform infrared spectroscopy, and scanning electron microscopy are among the most commonly used techniques for these purposes. Penciclovir and lysine are individually used to treat the herpes virus. As such, the development of a formulation containing both drugs may have therapeutic potential. Solid-state characterization showed that both penciclovir and lysine were crystalline materials with melting points at 278.27 °C and 260.91 °C, respectively. Compatibility studies of penciclovir and lysine indicated a possible interaction between these substances, as evidenced by a single melting point at 253.10 °C. The compatibility of several excipients, including ethylenediaminetetraacetic acid, cetostearyl alcohol, sodium lauryl sulphate, di-tert-butyl methyl phenol, liquid petrolatum, methylparaben, nonionic wax, paraffin, propylene glycol, and propylparaben, was evaluated in ternary (penciclovir-lysine-excipient) mixtures (1:1:1, w/w/w) to determine the optimal formulation. The developed formulation was stable under accelerated and ambient conditions, which demonstrated that the interaction between penciclovir and lysine was suitable for the development of a formulation containing both drugs.
Highlights
Penciclovir (PCV, 9-[4-hydroxy-3-(hydroxymethyl)butyl]guanine, Figure 1), a synthetic acyclic guanine derivative, is a potent antiviral drug with activity against herpes simplex virus, varicella zoster virus, Epstein–Barr virus, hepatitis virus, and cytomegalovirus [1,2,3]
The differential scanning calorimetry (DSC) curve of LYS (Figure 2) showed an endothermic peak at 261 ◦ C, which corresponded to its melting temperature and degradation, which agreed with a previous study [32]
LYS (Figure 2) showed an endothermic event at 253 ◦ C. This was the result of a reduction in the melting point of the LYS when combined with the PCV, which agreed with a previous study [33]
Summary
Penciclovir (PCV, 9-[4-hydroxy-3-(hydroxymethyl)butyl]guanine, Figure 1), a synthetic acyclic guanine derivative, is a potent antiviral drug with activity against herpes simplex virus, varicella zoster virus, Epstein–Barr virus, hepatitis virus, and cytomegalovirus [1,2,3]. PCV is widely indicated for the treatment of recurrent cold sores caused by the herpes virus [5]. PCV is more stable, resulting in greater in vitro antiviral activity and a longer half-life in vivo [6,7]. PCV can be formulated in topical preparations [8,9,10,11] but is absorbed poorly via the oral route. Its prodrug (famciclovir) is used for oral administration
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