title: A novel beads-based dissolution method for the in vitro evaluation of extended release HPMC matrix tablets and the correlation with the in vivo data.
abstract: The aim of this work was to establish alternative in vitro dissolution method with good discrimination and in vivo predictability for the evaluation of HPMC extended release matrix tablets. For this purpose, two different HPMC matrix tablet formulations were first evaluated by a range of conventional dissolution testing methods using apparatus 1, apparatus 2, and apparatus 3 according to US Pharmacopoeia. Obtained results showed low discrimination between the tested samples. Afterward, a novel dissolution testing method which combines plastic beads and apparatus 3 was developed with the aim to better mimic the mechanical forces that occur in vivo. Results showed that sufficiently large mechanical stress with high dips per minute program setting (apparatus 3) was needed to obtain in vitro discriminative results, which are in accordance with the in vivo data. The in vivo relevance of the method was confirmed with the establishment of the level A in vitro-in vivo correlation.
authors.affiliation: Lek Pharmaceuticals d.d., Verovškova 57, 1526, Ljubljana, Slovenia.
authors.forename: Uroš
authors.initials: U
authors.lastname: Klančar
authors.forename: Boštjan
authors.initials: B
authors.lastname: Markun
authors.forename: Saša
authors.initials: S
authors.lastname: Baumgartner
authors.forename: Igor
authors.initials: I
authors.lastname: Legen
mesh_terms: D002626:Chemistry, Pharmaceutical; D018592:Cross-Over Studies; D003692:Delayed-Action Preparations; D006801:Humans; D007785:Lactose / Q000031:analogs & derivatives* / Q000737:chemistry; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D012995:Solubility; D013607:Tablets
chemical_list: D003692:Delayed-Action Preparations; D013607:Tablets; C509290:hydroxypropylmethylcellulose-lactose matrix; D008747:Methylcellulose; D007785:Lactose