Scientific Coformer Screening, Preparation and Evaluation of Fenofibrate Tartaric Acid Cocrystal

  • Mangesh Bhalekar Department of pharmaceutics, AISSMS College of pharmacy, Savitribai Phule Pune University, Pune, Maharashtra, India
  • Sumedh Bandu Pradhan AISSMS COP
DOI https://doi.org/10.22270/jddt.v9i4.3199

Abstract

Objective: This present study aims to screen pharmaceutical cocrystal of Fenofibrate and coformers. Further the preparation and evaluation of  fenofibrate-coformer cocrystal and In-Vitro drug release and Ex-Vivo Permeation study was done. Material and Methods: The coformers for Fenofibrate were screened using molecular docking. The cocrystals produced were characterized using Differential Scanning Calorimetry (DSC), X-ray diffraction (XRPD) study and Infrared spectroscopy. Results: Cocrystal of Fenofibrate with tartaric acid was successfully prepared. The cocrystals displayed enhanced dissolution rate by 2.36 fold, similarly the ex-vivo drug uptake through everted chicken intestine model was improved by 4.38 fold. The formation of cocrystals of fenofibrate with tartaric acid was evaluated by DSC, IR and XRPD.


Conclusion: The fenofibrate - tartaric acid cocrystal exhibited increased % drug release and permeation compared to fenofibrate. This study confirms that selection of proper coformer is very vital step in preparation of stable, superior cocrystal. Based upon above study and results it revealed that cocrystallization offers a valuable way to improve the physicochemical properties of the API.


Keywords: Pharmaceutical Cocrystal, Fenofibrate , Coformer, Molecular docking.

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Author Biography

Mangesh Bhalekar, Department of pharmaceutics, AISSMS College of pharmacy, Savitribai Phule Pune University, Pune, Maharashtra, India

Department of pharmaceutics, AISSMS College of pharmacy, Savitribai Phule Pune University, Pune, Maharashtra, India

References

1) Fukte SR, Wagh MP, Rawat S. Coformer selection: An important tool in cocrystal formation review article. Int J Pharm Pharm Sci 2014; 6:9-14.
2) McNamara D, Childs S, Giordano J, Iarriccio A, Cassidy J, Shet M et al. Use of a Glutaric Acid Cocrystal to Improve Oral Bioavailability of a Low Solubility API. Pharmaceutical Research. 2006; 23(8):1888-1897.
3) Karagianni A, Malamatari M, Kachrimanis K. Pharmaceutical Cocrystals: New Solid Phase Modification Approaches for the Formulation of APIs. Pharmaceutics. 2018; 10(1):18.
4) Vogt M, Kunath K, Dressman J. Dissolution enhancement of fenofibrate by micronization, cogrinding and spray-drying: Comparison with commercial preparations. European Journal of Pharmaceutics and Biopharmaceutics. 2008; 68(2):283-288.
5) Li, X., Gu, L., Xu, Y. and Wang, Y. (2009). Preparation of fenofibrate nanosuspension and study of its pharmacokinetic behavior in rats. Drug Development and Industrial Pharmacy, 35(7), pp.827-833.
6) Choudhary D, Gangal S, Puri D. Solubility enhancement of fenofibrate by modified locust bean gum using solid dispersion techniques. Asian Pacific Journal of Health Sciences. 2018; 5(2):224-230.
7) Khadka, P., Ro, J., Kim, H., Kim, I., Kim, J., Kim, H., Cho, J., Yun, G. and Lee, J. (2014). Pharmaceutical particle technologies: An approach to improve drug solubility, dissolution and bioavailability. Asian Journal of Pharmaceutical Sciences, 9(6), pp.304-316.
8) LigPrep, version 2.3. Schrödinger, LLC: New York; 2009.
9) Maestro, version 9.0 Schrödinger LLC: New York; 2008.
10) ConfGen, version 2.2. Schrödinger, LLC: New York; 2011.
11) Liu Y, Sun C, Hao Y, Jiang T, Zheng L, Wang S. Mechanism of Dissolution Enhancement and Bioavailability of Poorly Water Soluble Celecoxib by Preparing Stable Amorphous Nanoparticles. Journal of Pharmacy & Pharmaceutical Sciences. 2010; 13(4):589.
12) Bhalekar M, Kadam N, Patil N; Gawale N, Madgulkar A, Novel ion exchange resin-based combination drug-delivery system for treatment of gastro esophageal reflux diseases. Brazilian journal of pharmaceutical sciences, 2010; 46: 336-342.
13) Swamy K, Gupta M, Rao P . New validated spectrophotometric method for the estimation of fenofibrate in bulk and dosage forms. International Journal of Biological & Pharmaceutical Research, 2010; 1(2):131-136.
14) Siswandi S, Rusdiana T, Levita J. Virtual screening of co-formers for ketoprofen co-crystallization and the molecular properties of the co-crystal. Journal of Applied Pharmaceutical Science. 2015; 078-082.
15) Panzade P, Shendarkar G, Shaikh S, Balmukund Rathi P. Pharmaceutical Cocrystal of Piroxicam: Design, Formulation and Evaluation. Advanced Pharmaceutical Bulletin. 2017; 7(3):399-408.
16) Panzade P, Shendarkar G. Pharmaceutical Cocrystal: An Antique and Multifaceted Approach. Current Drug Delivery. 2017; 14(8).
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How to Cite
1.
Bhalekar M, Pradhan S. Scientific Coformer Screening, Preparation and Evaluation of Fenofibrate Tartaric Acid Cocrystal. JDDT [Internet]. 15Jul.2019 [cited 1Dec.2023];9(4):406-10. Available from: https://www.jddtonline.info/index.php/jddt/article/view/3199
Issue
Vol 9 No 4 (2019): Volume 9, Issue 4, July-August 2019
Section
Research
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