Development of L-lysine Amino Acid-based Cocrystal of Telmisartan Using Crystal Engineering Approach to Improve Solubility, Dissolution, and Micrometric Properties

(E-pub Ahead of Print)

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

Journal Name: Current Drug Delivery

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Aim: To develop cocrytsal of telmisartan for enhancing its solubility in water.

Background: Intermolecular interaction happens in crystal packing; it utilizes and helps us to understand the design of new solid with their respective chemical and physical properties called that 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 solubility if 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: A dry grinding technique, solvent evaporation & cooling crystallization, the results revealed a generation of cocrystals with enhanced solubility by liquid drop grinding method. Hence, this process was further explored to investigate various formulation and process parameters that could significantly affect the crystal solubility, dissolution, and micrometric properties.

Results: The solubility of TEL cocrystals was enhanced by L-lysine. Further, the optimized batch was subjected to its micrometric evaluation & 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 cocrystal tablets than TEL tablets formulation.

Conclusion: Cocrystals 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

(E-pub Ahead of Print)
DOI: 10.2174/1567201817666200902151528
Price: $95

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