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Enhanced Solubility and Dissolution of Drug-drug Cocrystals of Lopinavir-Ritonavir

1, 1, 2, 2, 3

  1. 1Department of Pharmaceutical Chemistry, Institute of Pharmacy, Nirma University, Ahmedabad, Gujarat, INDIA.
  2. 2Emcure Pharmaceuticals, Mehsana, Gujarat, INDIA.
  3. 3Department of Quality Assurance, Smt. N. M. Padalia Pharmacy College, Ahmedabad, Gujarat, INDIA.

CORRESPONDENCE

Dr. Jignasa K Savjani

Department of Pharmaceutical Chemistry, Institute of Pharmacy, Nirma University, Sarkhej-Gandhinagar Road, Ahmedabad-38248, Gujarat, INDIA.

jignasa.savjani@nirmauni.ac.in

Received: 09-11-2022; Accepted: 20-02-2023.

Volume 57, Issue 2s (Supplement) · pp. s292-s300 · 2023 · DOI: 10.5530/ijper.57.2s.33

ABSTRACT

Introduction: Drug-drug cocrystals of Lopinavir and Ritonavir were designed and characterized. In view of literature, Ritonavir increases the oral bioavailability of Lopinavir in low dosage.Aim: The present research aimed to improve the solubility, dissolution, and oral bioavailability of Lopinavir through a cocrystallization approach using Ritonavir as a coformer.Materials and Methods: Cocrystallization was carried out using wet grinding and solvent evaporation methods. Prepared Cocrystals were examined and evaluated using characterization methods such as DSC, PXRD, FTIR, Polarized light microscopy, % Drug content, FE-SEM, Micromeritics properties, Solubility, Dissolution, and Stability studies as per ICH guidelines.Results: Developed cocrystals were showed superior solubility and dissolution as compared to pure drug. After 48 hr, aqueous solubility of Lopinavir and Ritonavir co-amorphous formulation (LRCWG) was increased 3.7-fold in the wet grinding method, while Lopinavir and Ritonavir Cocrystals Prepared by Solvent Evaporation Method (LRCSE) indicated 5.9-fold increase compared to pure drug. The co-amorphous formulation was developed using wet grinding showed 86% drug release at 60 min, and cocrystals synthesized through solvent evaporation method showed 94% of drug release.Conclusion: Cocrystals produced using solvent evaporation approach were stable and showed excellent physico-chemical characteristics. The study concluded that the cocrystallization approach would prove to be a successful method to improve physico-chemical and mechanical properties.

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    Chaudhari, K. R., Savjani, J. K., Savjani, K. T., Dahiya, S., & Bhangale, J. O. (2023). Enhanced Solubility and Dissolution of Drug-drug Cocrystals of Lopinavir-Ritonavir. Indian Journal of Pharmaceutical Education and Research, 57(2s), s292-s300. https://doi.org/10.5530/ijper.57.2s.33

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    © 2023 Author(s)

    This is an open access article distributed under the terms of the Creative Commons Attribution 4.0 License, which permits unrestricted use, distribution and reproduction in any medium, provided the original author and source are credited. CC BY 4.0