title: Acetylation enhances the tabletting properties of starch.
abstract: The aim of this study was the evaluation of starch acetate (SA) powders used as tablet excipients. Deformation during powder volume reduction, strain-rate sensitivity, intrinsic elasticity of the materials, and tensile strength of the tablets were examined. Results showed that SA with the lowest degree of substitution (ds) still possessed characteristics of native starch granules. Due to dissolution in synthesis, the properties of higher ds SAs depended on precipitation and drying processes. The acetate moiety, perhaps in combination with existing hydroxyl groups, was a very effective bond-forming substituent. The formation of strong molecular bonds increased, leading to a very firm and intact tablet structure. Small changes existed in compression-induced deformation due to acetylation. Some fragmentation was induced due to the slightly harder and more irregular shape of high-substituted SA particles. The plastic flow under compression was enhanced. Acetylated material was slightly less sensitive to fast elastic recovery in-die, but somewhat more elastic out-of-die. In spite of their superior bonding, SAs under compression behaved similarly to native starches. It was concluded that deformation properties were more the consequence of the molecular chain structure properties of the starch polymer than the effect of the acetate moiety itself. In contrast, the opposite seemed to be the case with the extensive improvement in bond-forming properties.
authors.affiliation: University of Kuopio, Department of Pharmaceutics, Finland. praatika@messi.uku.fi
authors.forename: Pasi
authors.initials: P
authors.lastname: Raatikainen
authors.forename: Ossi
authors.initials: O
authors.lastname: Korhonen
authors.forename: Soili
authors.initials: S
authors.lastname: Peltonen
authors.forename: Petteri
authors.initials: P
authors.lastname: Parone
mesh_terms: D000107:Acetylation; D002626:Chemistry, Pharmaceutical / Q000379:methods; D005079:Excipients / Q000737:chemistry*; D011208:Powders; D013213:Starch / Q000031:analogs & derivatives* / Q000737:chemistry*; D013314:Stress, Mechanical; D013607:Tablets
chemical_list: D005079:Excipients; D011208:Powders; D013607:Tablets; D013213:Starch; C050766:starch acetate