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Binary and ternary complexes of norfloxacin with hydroxypropyl ß cyclodextrin and amino acids to improve the solubility of the pharmaceutical active ingredient

Article

Authorship
Date
2019
Publishing House and Editing Place
Future Science Ltd
Magazine
Therapeutic Delivery, vol. 9 (pp. 639-652) - ISSN 2041-5990
Future Science Ltd
ISSN
2041-5990
Summary Information provided by the agent in SIGEVA
Aim: Binary and ternary complexes with hydroxypropyl-β-cyclodextrin (HPβCD), using glutamic acid (GA),proline or lysine as the third component, were developed to increase the solubility and the dissolutionrate of norfloxacin (NOR). Methods/results: Complexation was evaluated by phase solubility studies, obtaining the highest NOR solubility with GA and HPβCD. Thermal analysis suggested that different kindsof interactions occur among NOR, HPβCD and each amino acid, and wh... Aim: Binary and ternary complexes with hydroxypropyl-β-cyclodextrin (HPβCD), using glutamic acid (GA),proline or lysine as the third component, were developed to increase the solubility and the dissolutionrate of norfloxacin (NOR). Methods/results: Complexation was evaluated by phase solubility studies, obtaining the highest NOR solubility with GA and HPβCD. Thermal analysis suggested that different kindsof interactions occur among NOR, HPβCD and each amino acid, and when the systems were prepared bykneading or by means of freeze-drying technique. Dissolution studies, performed on simulated gastricfluid and subsequent simulated intestinal fluid, showed the highest rate of NOR from NOR?HPβCD?GA.Conclusion: NOR:HPβCD:GA was the best approach for improving the bioavailability of NOR.
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Key Words
GLUTAMIC ACIDPROLINETHERMAL ANALYSISFT-IR SPECTROSCOPYNORFLOXACINTERNARY COMPLEXESLYSINESOLUBILITYHYDROXIPROPYL-B-CYCLODEXTRINRELEASE