Preparation and physicochemical characterization of 5 niclosamide solvates and 1 hemisolvate |
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Authors: | Elsa C van Tonder Mabatane D Mahlatji Sarel F Malan Wilna Liebenberg Mino R Caira Mingna Song Melgardt M de Villiers |
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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 purpose of the study was to characterize the physicochemical, structural, and spectral properties of the 1∶1 niclosamide
and methanol, diethyl ether, dimethyl sulfoxide, N,N' dimethylformamide, and tetrahydrofuran solvates and the 2∶1 niclosamide
and tetraethylene glycol hemisolvate prepared by recrystallization from these organic solvents. Structural, spectral, and
thermal analysis results confirmed the presence of the solvents and differences in the structural properties of these solvates.
In addition, differences in the activation energy of desolvation, batch solution calorimetry, and the aqueous solubility at
25°C, 24 hours, showed the stability of the solvates to be in the order: anhydrate > diethyl ether solvate > tetraethylene
glycol hemisolvate > methanol solvate > dimethyl sulfoxide solvate > N,N' dimethylformamide solvate. The intrinsic and powder
dissolution rates of the solvates were in the order: anhydrate > diethyl ether solvate > tetraethylene glycol hemisolvate
> N,N' dimethylformamide solvate > methanol solvate > dimethyl sulfoxide solvate. Although these nonaqueous solvates had higher
solubility and dissolution rates than the monohydrous forms, they were unstable in aqueous media and rapidly transformed to
one of the monohydrous forms. |
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Keywords: | niclosamide solvates solubility physical stability |
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