Design and Evaluation of Microwave Induced Solid Dispersion of Tinidazole and Molecular Modelling with beta-cyclodextrin

作者：Jagdale Swati^*; Kulkarni Anish; Chabukswar Anuruddha; Kuchekar Bhanudas

来源：Letters in Drug Design and Discovery, 2016, 13(8): 781-792.

DOI：10.2174/1570180813999160429113650

• Solubility
• microwave
• solid dispersion
• molecular modelling
• tinidazole

The Objective of the present work was to enhance the solubility and dissolution profile of poorly water soluble BCS class II drug Tinidazole (TNZ). Microwave energy was utilized to prepare solvent free solid dispersions of TNZ and combination of TNZ with hydrophilic carriers as urea, gum acacia, beta cyclodextrin (beta CD), polyethylene glycol 6000 and polyvinyl pyrolidone Formulated solid dispersions were characterized by FTIR, solubility, microscopy, melting point and physical characterization by DSC and PXRD. Results revealed principal peak values in FTIR spectra of the drug remain unchanged in microwave-induced solid dispersions indicating no chemical interaction. Enhancement of solubility in microwave irradiated TNZ ranged from 7.52% to 55.02%, while for MSD TNZ: Urea it enhances from 9.70% to 86.82%. This may be due to conversion of crystalline to amorphous form, which was confirmed by differential scanning calorimetry and powder X-ray diffraction. Dissolution profile of the microwave irradiated TNZ enhanced by 22% and that of MSD TNZ: Urea by 25%. TNZ was interacted with beta-CD and the docking enrgy was found to be -9.4558 kcal/mol. Binding energies of complex (TNZ: beta-CD) has shown favourable electrostatic interaction. It was found that binding energies decrease after docking indicating stability of beta-CD-TNZ complex.

• 出版日期2016