Thermal analysis, structure, spectroscopy and DFT calculations of a pharmaceutical cocrystal of salicylic acid and salicylamide

2019 ◽  
Vol 138 (2) ◽  
pp. 1207-1220
Author(s):  
Hirihattaya Phetmung ◽  
Kanlayanee Musikapong ◽  
Teerapol Srichana
Author(s):  
HIRIHATTAYA PHETMUNG ◽  
SOMCHAI SAWATDEE

Objective: The objective of this present work was to develop the chemical peeling cream containing the synthesized active ingredient pharmaceutical cocrystal of salicylic acid and phenylalanine. Methods: The salicylic acid and phenylalanine cocrystal (H2Sal·Phe) was synthesized by the solvent evaporation method and characterized by various techniques such as single-crystal X-ray diffraction and Fourier transform infrared spectroscopy. The five formulas of cocrystal cream were prepared. All formulas were then examined and observed for appearance, spreadability, viscosity, pH, homogeneity, SPF test, microbial limit test and stability test. Results: The (H2Sal·Phe) consists of no zwitterion phenylalanine for the first time. X-ray crystal structure of cocrystal consists of double H2Sal and Phe molecules with stabilized by inter-, intra-molecular and π-π interactions. By using this cocrystal as an active ingredient for cosmetic development, the chemical peeling cream was produced along with the pharmaceutical examinations. The (H2Sal·Phe) formulations were prepared 0-1% and excipients included of jojoba oil, isopropyl myristate, castor oil, glyceryl monostearate cetostearyl alcohol, cyclomethicone (and) dimethicone crosspolymer, vitamin E, white bee's wax, glycerin, PEG 400, xanthan gum, Span 80 and Tween 60. We finally found that the F4 (1% H2Sal·Phe) was the best formulation with suitable physical properties of cream and chemical stable after storage. The results of cell viability show H2Sal·Phe is non-toxic with cell. Conclusion: The chemical peeling cream containing (H2Sal·Phe) has shown the promising results which are both safe and efficacious peeling agent. Cocrystal (H2Sal·Phe) cream can be used as an alternative choice in whitening skin.


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