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

被引：25

作者：

Bandari S. ^{[1
]}

Dronam V.R. ^{[1
]}

Eedara B.B. ^{[1
]}

机构：

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

来源：

Journal of Pharmaceutical Investigation | 2017年 / 47卷 / 6期

关键词：

Dissolution; Levofloxacin; Pharmaceutical cocrystals; Saccharin sodium; Stearic acid;

D O I：

10.1007/s40005-016-0302-8

中图分类号：

学科分类号：

摘要：

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. © 2017, The Korean Society of Pharmaceutical Sciences and Technology.

引用

页码：583 / 591

页数：8

共 29 条

[1]

Aakeroy C.B., Desper J., Salmon D.J., Smith M.M., Cyanophenyloximes: reliable and versatile tools for hydrogen-bond directed supramolecular synthesis of co-crystals, Cryst Growth Des, 6, pp. 1033-1042, (2006)

[2]

Agarwal R., Mittal R., Singh A., Studies of ion-exchange resin complex of chloroquine phosphate, Drug Dev Ind Pharm, 26, pp. 773-776, (2000)

[3]

Ayenew Z., Puri V., Kumar L., Bansal A.K., Trends in pharmaceutical taste masking technologies: a patent review, Recent Pat Drug Deliv Formul, 3, pp. 26-39, (2009)

[4]

Basavoju S., Bostrom D., Velaga S.P., Indomethacin-saccharin cocrystal: design, synthesis and preliminary pharmaceutical characterization, Pharm Res, 25, pp. 530-541, (2008)

[5]

Deng Y., Chen B., Qi Y., Magdalou J., Wang H., Chen L., The effects of levofloxacin on rabbit anterior cruciate ligament cells in vitro, Toxicol Appl Pharmacol, 257, pp. 67-73, (2011)

[6]

Drozak J., Miecznik A., Jarzyna R., Bryla J., The inhibition of gluconeogenesis by gatifloxacin may contribute to its hypoglycaemic action, Eur J Pharmacol, 594, pp. 39-43, (2008)

[7]

Eedara B.B., Bandari S., Lipid-based dispersions of exemestane for improved dissolution rate and intestinal permeability: in vitro and ex vivo characterization, Artif Cells Nanomed Biotechnol, (2016)

[8]

Eedara B.B., Kankane M., Jukanti R., Nagabandi V.K., Bandari S., Enhanced solubility and permeability of exemestane solid dispersion powders for improved oral delivery, J Pharm Investig, 43, pp. 229-242, (2013)

[9]

Eedara B.B., Veerareddy P.R., Jukanti R., Bandari S., Improved oral bioavailability of fexofenadine hydrochloride using lipid surfactants: ex vivo, in situ and in vivo studies, Drug Dev Ind Pharm, 40, pp. 1030-1043, (2014)

[10]

Elder D.P., Holm R., Diego H.L., Use of pharmaceutical salts and cocrystals to address the issue of poor solubility, Int J Pharm, 453, pp. 88-100, (2013)

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