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Ionic Liquid Forms of Carvedilol: Preparation, Characterization, and Solubility Studies

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Abstract

Purpose

Pharmaceutically active compounds (API) in solid form have several disadvantages which may include polymorphism, poor solubility, and low bioavailability. To overcome these issues, API-based ionic liquids have been proposed to solve this problem.

Methods

Solvent evaporation method was selected to prepare ionic liquid forms of CVD. A binary mixture of CVD with citric acid, tartaric acid, and saccharin in 1:1 M ratio was dissolved in 5 ml of methanol then they left 4 days for solvent evaporation. The solubility of CVD and prepared ionic liquids were measured in different media.

Results

A viscous yellow liquid in all cases was obtained. More than three-unit differences between pKa of CVD and studied compounds and characterization by different instrumental analysis methods confirmed the formation of an ionic liquid form of CVD and the prepared ionic liquids could significantly change the solubility of CVD.

Conclusion

Overall, ionic liquids of CVD could be used for overcoming the disadvantages of its solid form and increasing CVD solubility. However, pH, type, and concentration of dissolution medium and the solubility of counter-ions are critical issues which they should be considered in evaluating solubility of CVD and its ionic liquid forms.

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Acknowledgments

This article is a part of the results of S.S’s Pharm.D thesis No. 3965 registered at Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran. The authors would like to give special thanks to East Azarbaijan Sciences and Technology Park for providing DSC thermograms. We appreciate the editor and reviewers of this manuscript for editing and their valuable comments.

Funding

A.S. thanks the Ministry of Health and Medical Education (grant for young assistant professors), Tehran, Iran, for financial support.

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Authors and Affiliations

  1. Drug Applied Research Center, Tabriz University of Medical Sciences, Tabriz, Iran

    Shadi Shayanfar

  2. Student Research Committee and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran

    Shadi Shayanfar

  3. Pharmaceutical Analysis Research Center and Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, 51664, Iran

    Ali Shayanfar

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  1. Shadi Shayanfar
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Correspondence to Ali Shayanfar.

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Shayanfar, S., Shayanfar, A. Ionic Liquid Forms of Carvedilol: Preparation, Characterization, and Solubility Studies. J Pharm Innov 14, 382–390 (2019). https://doi.org/10.1007/s12247-018-9361-x

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