Autor(es):
Salústio, Paulo
; Feio, Gabriel
; Figueirinhas, João
; Pinto, João
; Marques, Helena Cabral
Data: 2008
Identificador Persistente: http://hdl.handle.net/10451/3805
Origem: Repositório da Universidade de Lisboa
Assunto(s): Ibuprofen; Indomethacin; Cyclodextrin; Freeze-drying; Spray-drying; Physical mixture; Kneading; NMR; X-ray; Optical microscopy; FT-IR spectroscopy; UV spectroscopy; DSC
Descrição
NOTICE: this is the author’s version of a work that was accepted for publication in European Journal of Pharmaceutics and Biopharmaceutics. Changes resulting from the publishing process, such as peer review, editing, corrections, structural formatting, and other quality control mechanisms may not be reflected in this document. Changes may have been made to this work since it was submitted for publication. A definitive version was subsequently published in Eur J Pharm Biopharm. 2009 Feb;71(2):377-386. Epub 2008 Oct 17. The work aims to prove the complexation of two model drugs (ibuprofen, IB and indomethacin, IN) by bcyclodextrin
(bCD), and the effect of water in such a process, and makes a comparison of their complexation
yields. Two methods were considered: kneading of a binary mixture of the drug, bCD, and inclusion
of either IB or IN in aqueous solutions of bCD. In the latter method water was removed by air stream,
spray-drying and freeze-drying. To prove the formation of complexes in final products, optical microscopy,
UV spectroscopy, IR spectroscopy, DSC, X-ray and NMR were considered. Each powder was added
to an acidic solution (pH = 2) to quantify the concentration of the drug inside bCD cavity. Other media
(pH = 5 and 7) were used to prove the existence of drug not complexed in each powder, as the drugs solubility
increases with the pH. It was observed that complexation occurred in all powders, and that the
fraction of drug inside the bCD did not depend neither on the method of complexation nor on the
processes of drying considered.