title: Disorder and dissolution enhancement: deposition of ibuprofen on to insoluble polymers.
abstract: Microcrystalline cellulose (MCC) and cross-linked polyvinylpyrrolidone (PVP-CL) were examined as polymeric carriers to support amorphous ibuprofen (IB). Drug/carrier systems were prepared as physical mixes, and drug was loaded onto the polymers by hot mix and solvent deposition methods. The systems were examined using differential scanning calorimetry (DSC), X-ray powder diffractometry (XRD) and by dissolution testing. PVP-CL reduced drug crystallinity more than MCC and, surprisingly, even very simple mixing of ibuprofen with PVP-CL induced disordering of the drug. Increased ibuprofen dissolution rates were achieved with both polymers, in the order of solvent deposition>hot mixes>physical mixes. The increased dissolution rates could be attributed to a combination of faster dissolution from amorphous ibuprofen, microcrystalline drug deposition on carrier surfaces and polymer swelling. However, no clear relationship was observed between ibuprofen dissolution rates (using first order, Higuchi or Hixson-Crowell relationships) and drug crystallinity.
authors.affiliation: Drug Delivery Group, School of Pharmacy, University of Bradford, Bradford BD7 1DP, UK. a.c.williams@reading.ac.uk
authors.forename: Adrian C
authors.initials: AC
authors.lastname: Williams
authors.forename: Peter
authors.initials: P
authors.lastname: Timmins
authors.forename: Mingchu
authors.initials: M
authors.lastname: Lu
authors.forename: Robert T
authors.initials: RT
authors.lastname: Forbes
mesh_terms: D002152:Calorimetry, Differential Scanning; D002482:Cellulose / Q000008:administration & dosage; D003460:Crystallization; D004337:Drug Carriers; D007052:Ibuprofen / Q000008:administration & dosage* / Q000737:chemistry; D011205:Povidone / Q000008:administration & dosage*; D012995:Solubility; D014961:X-Ray Diffraction
chemical_list: D004337:Drug Carriers; D002482:Cellulose; D011205:Povidone; D007052:Ibuprofen