Development of L-Lysine Amino Acid-Based Co-Crystal of Telmisartan Using Crystal Engineering Approach to Improve Solubility, Dissolution, and Micrometric Properties

Author(s): Nitin Kumar Bhatt, Jamshed Haneef, Manish Vyas, Gopal L. Khatik*

Journal Name: Current Drug Delivery

Volume 18 , Issue 5 , 2021

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Graphical Abstract:


Aim: To develop a co-crytsal of Telmisartan for enhancing its solubility in water.

Background: Intermolecular interaction happens in crystal packing; it utilizes and helps to understand the design of new solid with their respective chemical and physical properties called crystal engineering. It is a blueprint of molecular solids with specific chemical and physical properties through an understanding and handling of intermolecular interaction for increasing the solubility, in case of poor water-soluble drugs.

Objectives: The study was taken under consideration with an aim to generate and synthesize a cocrystal form of Telmisartan (TEL) with L-lysine to improve its water solubility, dissolution, and micrometric properties.

Methods: Using dry grinding technique, solvent evaporation and cooling crystallization, the results revealed a generation of co-crystals with enhanced solubility by liquid drop grinding method. Hence, this process was further explored to investigate various formulations and process parameters that could significantly affect the crystal solubility, dissolution, and micrometric properties.

Results: The solubility of TEL co-crystals was enhanced by L-lysine. Further, the optimized batch was subjected to its micrometric evaluation and physiochemical characterization like FT-IR, NMR, PXRD. The result of the micrometric evaluation showed better results as compared to standards. The dissolution studies also showed a better dissolution rate for TEL co-crystal tablets than TEL tablets formulation.

Conclusion: Co-crystals of TEL with L-lysine showed better solubility and dissolution rate.

Keywords: Cocrystal, telmisartan, L-lysine, solubility, dissolution, conformer.

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Article Details

Year: 2021
Published on: 02 September, 2020
Page: [596 - 606]
Pages: 11
DOI: 10.2174/1567201817666200902151528
Price: $65

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PDF: 151