Influence of beta-cyclodextrin on the Properties of Norfloxacin Form A

Author(s)

Chierentin, Lucas ^[1] ; Garnero, Claudia ^{[2, 3]} ; Karina Chattah, Ana ^{[4, 5]} ; Delvadia, Poonam ^[6] ; Karnes, Thomas ^[6] ; Raquel Longhi, Marcela ^{[2, 3]} ; Nunes Salgado, Herida Regina ^[1]

Affiliation

^[1] Univ Estadual Paulista, Fac Ciencias Farmaceut, BR-14801902 Sao Paulo - Brazil

^[2] Univ Nacl Cordoba, Fac Ciencias Quim, Dept Farm, RA-5000 Cordoba - Argentina

^[3] Univ Nacl Cordoba, UNITEFA, CONICET, RA-5000 Cordoba - Argentina

^[4] Univ Nacl Cordoba, Fac Matemat Astron & Fis, RA-5000 Cordoba - Argentina

^[5] Univ Nacl Cordoba, IFEG, CONICET, RA-5000 Cordoba - Argentina

^[6] Virginia Commonwealth Univ, Sch Pharm, Dept Pharmaceut, Richmond, VA 23298 - USA

• Document type: Journal article
• Source: AAPS PHARMSCITECH; v. 16, n. 3, p. 683-691, JUN 2015.
• Web of Science Citations: 6

Abstract

Cyclodextrins are able to form host-guest complexes with hydrophobic molecules to result in the formation of inclusion complexes. The complex formation between norfloxacin form A and beta-cyclodextrin was studied by exploring its structure affinity relationship in an aqueous solution and in the solid state. Kneading, freeze-drying, and physical mixture methods were employed to prepare solid complexes of norfloxacin and beta-cyclodextrin. The solubility of norfloxacin significantly increased upon complexation with beta-cyclodextrin as demonstrated by a solubility isotherm of the AL type along with the results of an intrinsic dissolution study. The complexes were also characterized in the solid stated by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), Fourier-transform infrared (FT-IR) spectroscopy, X-ray diffractometry, scanning electron microscopy (SEM), and solid-state nuclear magnetic resonance (ssNMR) spectrometry. The thermal analysis showed that the thermal stability of the drug is enhanced in the presence of beta-cyclodextrin. Finally, the microbiological studies showed that the complexes have better potency when compared with pure drug. (AU)

• FAPESP's process: 10/13335-2 - Validation of analytical methods for quantification of norfloxacin in tablets and stability studies
• Grantee: Lucas Chierentin
• Support Opportunities: Scholarships in Brazil - Master