Solvated Crystalline Forms of Nevirapine: Thermoanalytical and Spectroscopic Studies |
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Authors: | Renu Chadha Poonam Arora Anupam Saini Dharamvir Singh Jain |
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Institution: | (1) University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh, 160014, India;(2) Department of Chemistry, Panjab University, Chandigarh, 160014, India |
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Abstract: | The study is aimed at exploring the utility of thermoanalytical methods in the solid-state characterization of various crystalline
forms of nevirapine. The different forms obtained by recrystallization of nevirapine from various solvents were identified
using differential scanning calorimetry and thermogravimetric analysis (TGA). The appearance of desolvation peak accompanied
by weight loss in TGA indicated the formation of solvates: hemi-ethanolate (Form I), hemi-acetonitrilate (Form II), hemi-chloroformate
(Form III), hemi-THF solvate (Form IV), mixed hemi-ethanolate hemi-hydrate (Form V), and hemi-toluenate (Form VI). The higher
desolvation temperatures of all the solvates except toluenate than their respective boiling point indicate tighter binding
of solvent. Emphasis has been laid on the determination of heat capacity and heat of solution utilizing microreaction calorimeter
to further distinguish the various forms. The enthalpy of solution (ΔH
sol), an indirect measure of the lattice energy of a solid, was well correlated with the crystallinity of all the solid forms
obtained. The magnitude of ΔH
sol was found to be −14.14 kJ/mol for Form I and −2.83 kJ/mol for Form V in phosphate buffer of pH 2, exhibiting maximum ease
of molecular release from the lattice in Form I. The heat capacity for solvation (ΔC
p) was found to be positive, providing information about the state of solvent molecules in the host lattice. The solubility
and dissolution rate of the forms were also found to be in agreement with their enthalpy of solution. Form (I), being the
most exothermic, was found to be the most soluble of all the forms. |
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