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Development and preliminary characterization of levofloxacin pharmaceutical cocrystals for dissolution rate enhancement

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Abstract

The current investigation aimed to enhance the dissolution rate and mask the bitter taste of levofloxacin by developing pharmaceutical cocrystals using stearic acid and saccharin sodium as coformers. The developed cocrystals were characterized by Fourier transform infrared spectroscopy, which showed the formation of a regular carboxylic acid homosynthon in 1:1 ratio of levofloxacin-stearic acid and carboxylic acid- imide heterosynthon in 2:1 ratio of levofloxacin-saccharin sodium. The existence of the drug in a new crystalline form in the developed cocrystals was confirmed by solid state characterization. The dissolution studies of the developed cocrystals in simulated gastric fluid (pH 1.2) showed significant improvement of the drug dissolution rate (%min−1) from L-ST1 (7.8 ± 0.1) and L-SA2 (7.2 ± 0.4) cocrystals compared to supplied levofloxacin (4.4 ± 0.3). The taste masking ability of L-ST1 and L-SA2 was determined by conducting dissolution studies at salivary pH 6.6 and the results showed a very low drug release of 6.6 ± 0.6% from L-ST1 compared to supplied levofloxacin (64.5 ± 1.5%) and L-SA2 (55.1 ± 1.5%) in 5 min. This study demonstrates that pharmaceutical cocrystals of levofloxacin with stearic acid at 1:1 ratio enhanced the dissolution rate and masked the bitter taste of levofloxacin whereas saccharin sodium has showed only improved dissolution.

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Acknowledgements

The corresponding author acknowledges the financial support from Science & Engineering Research Board (File No. SB/YS/LS-119/2013), Department of Science and Technology, New Delhi, India. The authors are grateful to Dr. Reddy’s laboratories (Hyderabad, India) for the gift sample of levofloxacin. The authors thank Mrs. Rajani Nanam, Mrs. Sri Ramya and Mr. Narla Sagar for suggestions in chemical structure analysis. The authors also thank Mr. T. Jayapal Reddy, Chairman, St. Peter’s Institute of Pharmaceutical Sciences, Hanamkonda for providing the necessary facilities. The authors report no conflicts of interest. This article does not contain any studies with human and animal subjects performed by any of the authors. The authors report no conflicts of interest.

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Authors and Affiliations

  1. Department of Pharmaceutics and Industrial Pharmacy, St. Peter’s Institute of Pharmaceutical Sciences, Vidyanagar, Hanamkonda, Warangal, 506001, Telangana, India

    Suresh Bandari, Venkateshwara Rao Dronam & Basanth Babu Eedara

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  1. Suresh Bandari
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  2. Venkateshwara Rao Dronam
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  3. Basanth Babu Eedara
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Correspondence to Suresh Bandari.

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Bandari, S., Dronam, V.R. & Eedara, B.B. Development and preliminary characterization of levofloxacin pharmaceutical cocrystals for dissolution rate enhancement. Journal of Pharmaceutical Investigation 47, 583–591 (2017). https://doi.org/10.1007/s40005-016-0302-8

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  • DOI: https://doi.org/10.1007/s40005-016-0302-8

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