title: Development and validation of dissolution test for lopinavir, a poorly water-soluble drug, in soft gel capsules, based on in vivo data.
abstract: The objective of the present study was to develop and validate a dissolution test for lopinavir soft gel capsules (Kaletra), using a simulated absorption profile based on in vivo data. Different conditions such as surfactant concentration, apparatus and rotation speed were evaluated. In vivo release profiles were obtained from the literature. The fraction (and percentage) of dose absorbed (FA) was calculated by using Wagner-Nelson method. The best in vitro dissolution profile was obtained using Apparatus 2 (paddle) at 25 rpm, 1000 ml of medium with 2.3% of sodium lauryl sulfate and pH 6.0. Under these conditions a level-A in vitro-in vivo correlation (IVIVC) was obtained (r = 0.997). The in vitro dissolution samples were analyzed using a HPLC method and the validation was performed according to USP protocol. The method showed accuracy, precision, linearity and specificity within the acceptable range. Both the HPLC method and the in vitro dissolution method were validated and could be used to evaluate the release profile of lopinavir soft gel capsules.
authors.affiliation: Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul., Av. Ipiranga 2752, 90610-000 Porto Alegre, RS, Brazil.
authors.forename: Eliane Maria
authors.initials: EM
authors.lastname: Donato
authors.forename: Laura Alegria
authors.initials: LA
authors.lastname: Martins
authors.forename: Pedro Eduardo
authors.initials: PE
authors.lastname: Fröehlich
authors.forename: Ana Maria
authors.initials: AM
authors.lastname: Bergold
mesh_terms: D002214:Capsules; D002851:Chromatography, High Pressure Liquid; D006801:Humans; D016014:Linear Models; D061466:Lopinavir; D011744:Pyrimidinones / Q000008:administration & dosage / Q000737:chemistry*; D012995:Solubility
chemical_list: D002214:Capsules; D011744:Pyrimidinones; D061466:Lopinavir