Development of Metronidazole Controlled Release Pellets in the Rotary Fluid-bed Spray GranulatorJuan C. Menéndez and Adel Sakr Industrial Pharmacy Program, College of Pharmacy, University of Cincinnati, Cincinnati, Ohio (USA) Metronidazole (CAS 443-48-1) pellets with a concentration of 88 % were prepared in the rotary fluid-bed spray granulator GPCG-1 using Kollidon 30. The effect of Eudragit L 3 0 D-55 (enteric-coating) and/or Eudragit NE 30 D was, individually and as consecutive layers, evaluated on the release of metronidazole up to 30 % of weight gain of dry polymer. These pellets were tested in the USP XXV apparatus 1 (baskets) for 2 h in acidic medium (0.1 N HCl) followed by phosphate buffer pH 6.8 up to 24 h. More than 10 % of weight gain of enteric-coating is required to block effectively drug release in acidic medium. Pellets coated with Eudragit NE 30 D showed bi-phase dissolution with the higher release rate in acidic medium and sustained release for the remaining 22 h in phosphate buffer pH 6.8. The pellets prepared by layering of the two film-coatings showed intermediate properties with delayed release in the acidic stage and sustained release thereafter. Key words CAS 443-48-1 · Eudragit L 3 0 D-55 · Eudragit NE 30 D · Granulation, layering Pellets · Rotary fluid-bed spray granulator
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pharmind 2003, Nr. 5, Seite 448
