In vitro evaluation of pectin-HPMC compression coated 5-aminosalicylic acid tablets for colonic delivery.
In this study, we report pectin-HPMC compression coated core tablets of 5-aminosalicylic acid (5-ASA) for colonic delivery. Each 100 mg core tablet contained 5-ASA and was compression coated at 20 kN or 30 kN using 100% pectin, 80% pectin-20% HPMC, or 60% pectin-40% HPMC, at two different coat weights as 400 or 500 mg. Drug dissolution/system erosion/degradation studies were carried out in pH 1.2 and 6.8 buffers using a pectinolytic enzyme. The system was designed based on the gastrointestinal transit time concept, under the assumption of colon arrival times of 6 h. It was found that pectin alone was not sufficient to protect the core tablets and HPMC addition was required to control the solubility of pectin. The optimum HPMC concentration was 20% and such system would protect the cores up to 6 h that corresponded to 25-35% erosion and after that under the influence of pectinase the system would degrade faster and delivering 5-ASA to the colon. The pectin-HPMC envelope was found to be a promising drug delivery system for those drugs to be delivered to the colon.
Turkoglu
Murat
M
Marmara University, Faculty of Pharmacy, 81010 Haydarpaşa, Istanbul, Turkey. turkoglu@marun.edu.tr
Ugurlu
Timucin
T
D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000493:pharmacokinetics*; D000930:Antidiarrheals / Q000008:administration & dosage / Q000493:pharmacokinetics; D003106:Colon / Q000187:drug effects / Q000378:metabolism*; D019245:Compressive Strength; D016503:Drug Delivery Systems / Q000379:methods*; D004353:Drug Evaluation, Preclinical / Q000379:methods / Q000706:statistics & numerical data; D007785:Lactose / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D019804:Mesalamine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D008747:Methylcellulose / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics*; D010078:Oxazines; D010368:Pectins / Q000008:administration & dosage / Q000493:pharmacokinetics*; D012995:Solubility; D013608:Tablets, Enteric-Coated
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000930:Antidiarrheals; D010078:Oxazines; D013608:Tablets, Enteric-Coated; D019804:Mesalamine; D010368:Pectins; D008747:Methylcellulose; C071191:MK 458; D007785:Lactose