title: Development and validation of a dissolution test for lutein tablets and evaluation of intestinal permeability.
abstract: Lutein is a carotenoid with antioxidant activity that is present in various dosage forms. The bioavailability of carotenoid from oral dosage formulations depends on their release, dissolution and its permeability through the gastrointestinal tract. Here, a dissolution test was developed for evaluating formulations and the bioavailability was assessed. The test utilized a USP-apparatus II with rotations of 50, 75 and 100rpm in water with P80 at 1, 2 and 5% (w/v). A non-everted rat intestinal sac model was used in conjunction to assess the intestinal permeability. The most discriminative conditions were 100rpm in water with 2% polysorbate 80, which showed profile differences between two formulations. The intestinal permeation studies showed a lag-time and apparent permeability coefficient that were characteristic of highly permeable drugs. We suggest that a dissolution test can be an essential quality control tool for formulations containing compounds as lutein, although not mandatory by the regulation agencies.
authors.affiliation: Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.
authors.forename: Carina de Souza
authors.initials: Cde S
authors.lastname: Anselmo
authors.affiliation: Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.
authors.forename: Thamara de Carvalho
authors.initials: Tde C
authors.lastname: Mendes
authors.affiliation: Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.
authors.forename: Thiago da Silva
authors.initials: Tda S
authors.lastname: Honorio
authors.affiliation: Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.
authors.forename: Flávia Almada
authors.initials: FA
authors.lastname: do Carmo
authors.affiliation: Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil.
authors.forename: Lucio Mendes
authors.initials: LM
authors.lastname: Cabral
authors.affiliation: Department of Drugs and Pharmaceutics, Faculty of Pharmacy, Federal University of Rio de Janeiro, Rio de Janeiro, Brazil. Electronic address: valeria@pharma.ufrj.br.
authors.forename: Valeria Pereira
authors.initials: VP
authors.lastname: de Sousa
mesh_terms: D000818:Animals; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D007413:Intestinal Mucosa / Q000378:metabolism*; D014975:Lutein / Q000494:pharmacology; D008297:Male; D010539:Permeability / Q000187:drug effects; D051381:Rats; D012995:Solubility; D013607:Tablets
chemical_list: D013607:Tablets; D014975:Lutein
keywords: Carotenoid; Dissolution test; Drug release; Food regulation; Intestinal permeation; Non-everted rat intestinal sac model; USP apparatus II