Drug-polymer mixed coating: a new approach for controlling drug release rates in pellets.
A new approach to developing a drug-polymer mixed coat for highly water-soluble diltiazem pellets was investigated at different coating levels. Drug layering and the coating procedures were performed using a bottom spray fluidized bed coater. Drug pellets were coated with Eudragit NE40 (NE40) alone and in combination with diltiazem and hydrophilic cellulose derivatives. Dissolution studies revealed that incorporation of hydrophilic substances such as methylcellulose (MC), hydroxypropyl methylcellulose (HPMC), and the drug itself considerably increased the release rates. The release from mixed polymer coatings was fast compared to pellets coated with NE40 only. The major portion of the drug was released in about 2 hours in case of MC and NE40 mixed coat compared to hours from coated pellets containing HPMC or diltiazem. Incorporation of 15% to 25% drug with respect to the polymer coat helped to achieve a drug-release profile at a desirable rate over a 12 hour period. Moreover, the test formulation comprising 25% diltiazem with respect to 7% NE40 had a dissolution profile that matched the commercial product, Herbesser SR capsules. The release of diltiazem from the coated pellets was slightly affected by the pH of dissolution media.
Nisar ur Rahman
Department of Pharmacy, Islamia University, Bahawalpur, Pakistan. Nisar60@yahoo.com
Yuen
K H
KH
Khan
Nurzalina A K
NA
Wong
Jia Woei
JW
D000465:Algorithms; D003627:Data Interpretation, Statistical; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004110:Diltiazem / Q000008:administration & dosage / Q000737:chemistry; D004339:Drug Compounding; D004356:Drug Storage; D005079:Excipients; D006863:Hydrogen-Ion Concentration; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives; D008855:Microscopy, Electron, Scanning; D004364:Pharmaceutical Preparations / Q000008:administration & dosage* / Q000737:chemistry*; D011108:Polymers; D012995:Solubility
D003692:Delayed-Action Preparations; D005079:Excipients; D004364:Pharmaceutical Preparations; D011108:Polymers; D065347:Hypromellose Derivatives; D008747:Methylcellulose; D004110:Diltiazem