Release profiles of indometacin in beta-cyclodextrin complexes from HPMC capsules

• Type: Article in International Scientific Journal
• Date: 2013

Authors

salustio, pj (Author) Other; pinto, jf (Author) Other; costa, pc (Author) FFUP; cabral-marques, hm (Author) Other

Journal

Title: Journal of Inclusion Phenomena and Molecular Recognition in Chemistry

Vol. 75

Pages: 101-109

ISSN: 0923-0750

Publisher: Kluwer Academic Publishers

Indexing

ISI Web of Knowledge - 1 Citation

Scopus - 2 Citations

Other information

Authenticus ID: P-002-0R9

DOI: 10.1007/s10847-012-0151-7

Abstract (EN): Powders containing indometacin complexed with beta-cyclodextrin (1:1 ratio) obtained by two complexation methods (suspension/solution [with water removed by air stream, spray- and freeze-drying] and kneading techniques) were compared between them to observe the increase on the drug solubility and yield of the complexation process. The tests used for this comparison included the determination of the moisture content, true and bulk densities, angle of repose, Carr's index and in vitro drug release (at pH 1.0) from HPMC capsules. In the dissolution tests the drug release was analyzed considering different parameters (similarity factor (f (2)), dissolution efficiency (DE) and the amounts released (M (t)) at certain times (30, 60 and 180 min) by statistic analysis (alpha = 0.05)). The results obtained showed poor pharmaceutical properties for all mixtures and that the indometacin released from capsules containing inclusion complexes presented an increase on solubility when compared with reference formulation (lactose and microcrystalline cellulose instead of beta-cyclodextrin). The release of indometacin showed no dependency on the amount of water used in the formation of the complexes being the differences observed mostly due to the characteristics of the particles, which were dependent on the complexation method. However the low yield of the complexation that occurred can be explained by the difference between the size of the drug molecule, the guest (diameter-7.5 , length-14.2 ) and the size of the beta-cyclodextrin cavity, the host (diameter-6.0-6.5 angstrom).

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 9