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KMID : 0369820170470060583
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Jorunal of Korean Pharmaceutical Sciences
2017 Volume.47 No. 6 p.583 ~ p.591
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Development and preliminary characterization of levofloxacin pharmaceutical cocrystals for dissolution rate enhancement
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Bandari Suresh
Dronam Venkateshwara Rao
Eedara Basanth Babu
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Abstract
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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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KEYWORD
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Dissolution, Levofloxacin, Pharmaceutical cocrystals, Saccharin sodium, Stearic acid
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