Evaluation of the deformation behavior of binary systems of methacrylic acid copolymers and hydroxypropyl methylcellulose using a compaction simulator.
Methacrylic acid copolymers have been shown to enhance release of weakly basic drugs from rate controlling polymer matrices through the mechanism of microenvironmental pH modulation. Since these matrices are typically formed through a compaction process, an understanding of the deformation behavior of these polymers in there neat form and in combination with rate controlling polymers such as HPMC is critical to their successful formulation. Binary mixes of two methacrylic acid copolymers, Eudragit L100 and L100-55 in combination with HPMC K4M were subjected to compaction studies on a compaction simulator. The deformation behavior of the powder mixes was analyzed based on pressure-porosity relationships, strain rate sensitivity (SRS), residual die wall force data and work of compaction. Methacrylic acid copolymers, L100-55 and L-100 and the hydrophilic polymer, HPMC K4M exhibited Heckel plots representative of plastic deformation although L-100 exhibited significantly greater resistance to densification as evident from the high yield pressure values ( approximately 120MPa). The yield pressures for the binary mixes were linearly related to the weight fractions of the components. All powder mixes exhibited significant speed sensitivity with SRS values ranging from 21.7% to 42.4%. The residual die-wall pressures indicated that at slow speeds (1mm/s) and at lower pressures (<150MPa), HPMC possesses significant elastic behavior. However, the good compacts formed at this punch speed indicate significant plastic deformation and bond formation which is able to predominate over the elastic recovery component. The apparent mean yield pressure values, the residual die-wall forces and the net work of compaction exhibited a linear relationship with mixture composition, thereby indicating predictability of these parameters based on the behavior of the neat materials.
Tatavarti
Aditya S
AS
Department of Pharmaceutical Sciences, School of Pharmacy, University of Maryland, Baltimore, MD 21201, USA.
Muller
Francis X
FX
Hoag
Stephen W
SW
D000180:Acrylic Resins / Q000737:chemistry*; D004548:Elasticity; D065347:Hypromellose Derivatives; D019563:Mechanics; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry; D008853:Microscopy; D014677:Pharmaceutical Vehicles / Q000737:chemistry; D011109:Polymethacrylic Acids / Q000737:chemistry*; D011208:Powders / Q000737:chemistry*; D011312:Pressure; D013314:Stress, Mechanical; D013607:Tablets / Q000737:chemistry
D000180:Acrylic Resins; C446821:Eudragit L100-55; D014677:Pharmaceutical Vehicles; D011109:Polymethacrylic Acids; D011208:Powders; D013607:Tablets; C038300:methylmethacrylate-methacrylic acid copolymer; D065347:Hypromellose Derivatives; D008747:Methylcellulose