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Abstract

Fenofibrate-Nicotinamide Cocrystals: Molecular Docking Studies and Evaluation in Tablet Dosage Form

Author(s): A. S. Shete*, V. V. Shah, P. A. Bhosale and R. C. Doijad
Department of Pharmaceutics, 1Department of Pharmaceutical Chemistry, Krishna Institute of Pharmacy of Krishna Institute of Medical Sciences Deemed To Be University, Karad, Maharashtra 415539, 2Research Group Department of Pharmaceutics and Quality Assurance, Shree Santkrupa College of Pharmacy, Ghogaon, Karad, Maharashtra 415111, India

Correspondence Address:
A. S. Shete, Department of Pharmaceutics, Krishna Institute of Pharmacy of Krishna Institute of Medical Sciences Deemed To Be University, Karad, Maharashtra 415539, India, E-mail: [email protected]


The objectives of present investigation were to evaluate prepared cocrystals of fenofibrate and nicotinamide for pre-compression characteristics, docking studies for target peroxisome proliferator-activated receptor alpha, evaluate performance of cocrystals in tablet dosage form and to carry out in vivo antihyperlipidemic activity. The cocrystals were prepared by antisolvent addition method. Docking studies of cocrystals and pure fenofibrate against of target peroxisome proliferator-activated receptor alpha were carried out by using PyRx (version 0.8) docking tool, AutoDock Vina as docking program. The prepared cocrystals were evaluated for pre-compression properties like angle of repose, bulk density and Carr’s index. Cocrystals were formulated in tablet dosage form and evaluated for official and unofficial quality control tests. The antihyperlipidemic activity carried out in rats by using Triton X-100 induced hyperlipidemia model. Cocrystals binds with peroxisome proliferator-activated receptor alpha with more binding affinity as compared with fenofibrate. Cocrystal shows binding energy of -9.3 kcal/mol while fenofibrate shows -8.5 kcal/mol. The pre-compression properties were within the limits of United States Pharmacopeia guidelines. The pure fenofibrate tablet showed 24.7 % drug release at the end of 90 min and cocrystal based tablet showed 100 % at 45 min. There was no statistically significant difference in values for all biochemical parameters in case of in vivo activity for cocrystals in comparison with pure fenofibrate. From the docking studies we can conclude that cocrystals showed stronger more substantial formed stable complexes with target peroxisome proliferator-activated receptor alpha, but no statistically significant difference in pharmacodynamic studies.

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