Modifying drug release and tablet properties of starch acetate tablets by dry powder agglomeration.
In this study three model drugs (N-acetyl-D-glucosamine (NAG), anhydrous caffeine, and propranolol hydrochloride) were agglomerated with starch acetate (SA) by mixing the binary powders on a stainless steel (SS) plate. Agglomeration was induced by triboelectrification of the particles during mixing, and it was evaluated as a method to achieve controlled drug release rate. These agglomerates, mixed with different amounts of a disintegrant, were compressed into tablets whose dissolution characteristics were determined. Triboelectric measurements showed that when the drugs were in contact with SS, charges of the opposite polarity were generated to SA (+) and caffeine and NAG (-) promoting adhesion. Instead, propranolol HCl was charged with the same polarity as SA. SEM micrographs showed that smaller caffeine particles, in spite of their larger negative charge, agglomerated less efficiently with SA than larger NAG particles. This emphasizes the importance of particle size in the agglomeration process. Propranolol HCl did not form agglomerates with SA since their particle sizes and charges were identical. As a result, agglomeration of powders prior to tablet compression allows for modification and control of the release rate of the drugs from the SA matrix tablets as well as the tensile strength of the tablets.
Mäki
Riikka
R
Department of Pharmaceutics, University of Kuopio, P.O. Box 1627, FI-70211 Kuopio, Finland. riikka.maki@uku.fi
Suihko
Eero
E
Rost
Susanne
S
Heiskanen
Minna
M
Murtomaa
Matti
M
Lehto
Vesa-Pekka
VP
Ketolainen
Jarkko
J
D000117:Acetylglucosamine / Q000737:chemistry*; D002110:Caffeine / Q000737:chemistry*; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry; D008855:Microscopy, Electron, Scanning; D011205:Povidone / Q000737:chemistry; D011208:Powders; D011433:Propranolol / Q000737:chemistry; D012995:Solubility; D013213:Starch / Q000031:analogs & derivatives* / Q000737:chemistry; D013499:Surface Properties; D013607:Tablets; D013718:Tensile Strength
D005079:Excipients; D011208:Powders; D013607:Tablets; D002110:Caffeine; D013213:Starch; C050766:starch acetate; D011433:Propranolol; D011205:Povidone; D000117:Acetylglucosamine