title: Preparation of acetaminophen capsules containing beads prepared by hot-melt direct blend coating.
abstract: Twelve hydrophobic coating agents were assessed for their effects on drug release after coating sugar cores by a flexible hot-melt coating method using direct blending. Drug-containing pellets were also produced and used as cores. The cores were coated with single or double wax layers containing acetaminophen (APAP). The harder the wax, the slower the resultant drug releases from single-coated beads. Wax coating can be deposited on cores up to 28% of the beads final weight and reaching 58% with wax and drug. Carnauba-coated beads dissolved in approximately 6 h releasing 80% of the loaded drug. Applying another wax layer extended drug release over 20 h, while still delivering 80% of the loaded drug. When drug-containing pellets (33-58% drug loading) were used as cores, double wax-coated pellets exhibited a near zero-order drug release for 16 h, releasing 80% of the loaded drug delivering 18 mg/h. The simple process of hot-melt coating by direct blending of pellet-containing drug-coated formulations provides excellent options for immediate and sustained release formulations when higher lipid coating or drug loading is warranted. Predicted plasma drug concentration time profiles using convolution and in vitro drug release properties of the beads were performed for optimal formulations.
authors: Camargo Pharmaceutical Services , Cincinnati, OH , USA and.
authors: Loan
authors: L
authors: Pham
authors: John M
authors: JM
authors: Christensen
mesh_terms: D000082:Acetaminophen / Q000008:administration & dosage* / Q000737:chemistry; D018712:Analgesics, Non-Narcotic / Q000008:administration & dosage* / Q000737:chemistry; D002214:Capsules; D002626:Chemistry, Pharmaceutical; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry; D012995:Solubility; D014885:Waxes / Q000737:chemistry
chemical_list: D018712:Analgesics, Non-Narcotic; D002214:Capsules; D003692:Delayed-Action Preparations; D005079:Excipients; D014885:Waxes; D000082:Acetaminophen