Modified release of coated sugar spheres using drug-containing polymeric dispersions.
A drug-containing polymeric dispersion was applied onto nonpareil sugar spheres (18/20 mesh) using a fluid-bed spray coater. Eudragit RS30D was selected as the polymeric coating material. Melatonin secreted by the pineal gland in a circadian rhythm was used as a model drug. The release behaviors of the coated sugar spheres were investigated in gastric fluid (pH 1.4) for 2 h, and then continuously in intestinal fluid (pH 7.4) for 14 h. The release rate of the coated sugar spheres decreased with increasing coating levels. The solvent (ethanol) in the coating dispersions significantly decreased the release of the drug due to the good dispersion of the low solubility melatonin in the polymeric films. The polymer (polyvinylpyrrolidone, PVP) and drug contents in the coating dispersions did not affect the release rate. Most of all, the release profiles were drastically changed according to the type and concentration of plasticizers used. The current coating methods that use drug-containing polymeric dispersions could be useful for simultaneous drug loadings and their modified release. The solubilization and controlled release of poorly water-soluble drugs can be achieved as both the solubilizers and drugs are present in the drug-containing polymeric dispersions.
Kim
Tae-Wan
TW
National Research Laboratory for Bioavailability Control, College of Pharmacy, Kangwon National University, Chuncheon 200-701, Korea.
Ji
Chang-Won
CW
Shim
Sang-Young
SY
Lee
Beom-Jin
BJ
D000180:Acrylic Resins / Q000737:chemistry*; D002241:Carbohydrates / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D004339:Drug Compounding; D000431:Ethanol / Q000737:chemistry; D005079:Excipients / Q000737:chemistry*; D006863:Hydrogen-Ion Concentration; D008550:Melatonin / Q000737:chemistry; D010968:Plasticizers / Q000737:chemistry; D011205:Povidone / Q000737:chemistry; D012995:Solubility; D012997:Solvents / Q000737:chemistry; D013678:Technology, Pharmaceutical / Q000379:methods*; D013997:Time Factors
D000180:Acrylic Resins; D002241:Carbohydrates; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005079:Excipients; D010968:Plasticizers; D012997:Solvents; C050528:Eudragit RS; D000431:Ethanol; D011205:Povidone; D008550:Melatonin