Romanian Society of Pharmaceutical Sciences

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DEVELOPMENT OF A PH AND TIME CONTROLLED RELEASE COLON DELIVERY SYSTEM OBTAINED BY COMPRESSIONCOATING AND FILM-COATING

DANA HALES, RAREȘ IULIU IOVANOV, MARCELA ACHIM, SORIN E. LEUCUȚA, DANAMARIA MUNTEAN*, LAURIAN VLASE, IOAN TOMUȚĂ

“Iuliu Haţieganu” University of Medicine and Pharmacy Cluj-Napoca, Faculty of Pharmacy, Department of Pharmaceutical Technology and Biopharmacy, 41 Victor Babeș, 400012, Cluj-Napoca, România

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The purpose of this study was to develop a colonic delivery system with pH and time-dependent release. Ketoprofen cores, mini-tablet type, were prepared; then, they were coated by compression with different powder mixtures containing 25% - 35% hydroxypropylmethylcellulose (HPMC) K4M and K100M, and embedded by film coating with two types of polymers with pH-dependent solubility (Eudragit® FS 30D and Eudragit® L 30D-55). In vitro release studies were carried out in pH gradient: 1.2, 6.8, and 7.4. The polymers with pH-dependent solubility, located in the outer film layer, prevented the drug release in the gastric environment: Eudragit® L 30D-55 and Eudragit® FS 30D dissolved in the simulated intestinal fluid, at pH 6.8 and at pH 7.4, respectively. The polymer with time-dependent solubility, HPMC, situated in the subsequent layer of the film coating, allowed water penetration and subsequent swelling of the tablet core that gradually released the active drug. The obtained results showed that the ratio and properties of the two types of Eudragit polymers are capable to initiate the delivery of the active drug at the alkaline pH (after more than 5 h), the type and percentage of the HPMC polymer prolonging by swelling this process (until about 8 h). This study proved that compression-coated tablets, coated with enteric polymers are a promising technology for colon specific delivery of drugs.