Optimization of salting-out taste-masking system for micro-beads containing drugs with high solubility.
The salting-out taste-masking system is a multiparticulate system consisting of a drug core, a salting-out layer containing salts and water-soluble polymers, and a water-penetration control layer containing water-insoluble materials. The system generates a long lag time (time when released drug is less than 1%) for numbness masking, and a subsequent immediate drug release for high bioavailability. Aiming to contain the system and drugs that cause numbness in oral disintegrating tablets, the system was optimized to reduce the particle size and contain drugs with high water solubility in this study. The amount of coating on the layers, the coating solvent, and the positioning of the components were also optimized. The findings in this study will lead to the provision of numbness-masked oral disintegrating tablets to patients.
Yoshida
Takayuki
T
Drug Delivery, Pharmaceutical Research and Development Labs, Astellas Pharma Inc, Japan. takayuki.yoshida@jp.astellas.com
Tasaki
Hiroaki
H
Maeda
Atsushi
A
Katsuma
Masataka
M
Sako
Kazuhiro
K
Uchida
Takahiro
T
D000082:Acetaminophen / Q000737:chemistry; D002254:Carbonates / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D016503:Drug Delivery Systems; D065347:Hypromellose Derivatives; D007099:Imipramine / Q000737:chemistry; D008747:Methylcellulose / Q000031:analogs & derivatives; D008863:Microspheres; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D013607:Tablets; D013649:Taste
D002254:Carbonates; D004364:Pharmaceutical Preparations; D013607:Tablets; D000082:Acetaminophen; D065347:Hypromellose Derivatives; C005686:sodium carbonate; D008747:Methylcellulose; D011205:Povidone; D007099:Imipramine