Physical solid-state properties and dissolution of sustained-release matrices of polyvinylacetate.
Solid-state compatibility and in vitro dissolution of direct-compressed sustained-release matrices of polyvinylacetate (PVAc) and polyvinylpyrrolidone (PVP) containing ibuprofen as a model drug were studied. Polyvinylalcohol (PVA) was used as an alternative water-soluble polymer to PVP. Differential scanning calorimetry (DSC) and powder X-ray diffractometry (PXRD) were used for characterizing solid-state polymer-polymer and drug-polymer interactions. The mechanical treatment for preparing physical mixtures of polyvinyl polymers and the drug (i.e. simple blending or stressed cogrinding) was shown not to affect the physical state of the drug and the polymers. With the drug-polymer mixtures the endothermic effect due to drug melting was always evident, but a considerable modification of the melting point of the drug in physical binary mixtures (drug:PVP) was observed, suggesting some interaction between the two. On the other hand, the lack of a significant shift of the melting endothermic peak of the drug in physical tertiary drug-polymer mixtures revealed no evidence of solid-state interaction between the drug and the present polymers. Sustained-release dissolution profiles were achieved from the direct-compressed matrices made from powder mixtures of the drug and PVAc combined with PVP, and the proportion of PVAc in the mixture clearly altered the drug release profiles in vitro. The drug release from the present matrix systems is controlled by both diffusion of the drug through the hydrate matrix and the erosion of the matrix itself.
Gonzalez Novoa
Gelsys Ananay
GA
Institute of Pharmacy and Food, University of Havana, Havana, Cuba.
Heinämäki
Jyrki
J
Mirza
Sabir
S
Antikainen
Osmo
O
Colarte
Antonio Iraizoz
AI
Paz
Alberto Suzarte
AS
Yliruusi
Jouko
J
D002152:Calorimetry, Differential Scanning; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D003692:Delayed-Action Preparations / Q000032:analysis / Q000737:chemistry / Q000493:pharmacokinetics; D007700:Kinetics; D008956:Models, Chemical; D011145:Polyvinyls / Q000032:analysis / Q000737:chemistry* / Q000493:pharmacokinetics*; D033362:Powder Diffraction; D012995:Solubility; D014961:X-Ray Diffraction
D003692:Delayed-Action Preparations; D011145:Polyvinyls; C013215:polyvinyl acetate