methylcellulose and Colitis

The purpose of this study is to increase the lag time and prevent release of budesonide, a corticosteroid drug used in Crohn's disease for the first 5 h and efficiently deliver it to the colon. Eudragit S100 spray-coated capsules and pulsatile systems using tablet plugs of cellulose acetate butyrate (CAB), HPMC K4M, guar gum, and pectin were prepared. Eudragit S100-coated capsules released 80.62% after 5 h. In pulsatile systems, decreasing the ratio of the polymer significantly increased the rate and extent of drug release. Spray-coating with EUD S100 decreased the extent of drug release to 48.41%, 69.94%, 80.58%, and 45.23% in CAB, HPMC K4M, pectin, and guar gum, respectively; however, the entire amount was released in the target area. In the presence of bacterial enzymes, selected formulas showed nearly 100% release. X-ray imaging performed to monitor the capsules throughout the GIT in human volunteers of the capsules and spray-coated pulsatile systems with 25% guar gum in the plug showed bursting in the transverse and ascending colon, respectively. Both formulations showed marked reduction in induced rabbit colitis model.

Topics: Administration, Oral; Adult; Animals; Biological Availability; Budesonide; Capsules; Cellulose; Chemistry, Pharmaceutical; Colitis; Colon; Colon, Transverse; Delayed-Action Preparations; Galactans; Gastric Mucosa; Humans; Hydrogen-Ion Concentration; Hypromellose Derivatives; Ileum; Lactose; Male; Mannans; Mannosidases; Methylcellulose; Pectins; Peroxidase; Plant Gums; Polygalacturonase; Polymethacrylic Acids; Rabbits; Radiography; Rectum; Stomach; Tablets; Trinitrobenzenesulfonic Acid; Young Adult

Preparation of coated pellets intended for rutin colon delivery, their evaluation in vitro and in vivo in experimental colitis in rats was the purpose of this study. Pellets were obtained using extrusion/spheronization and coated with three types of coatings (caffeic acid/hypromellose/alginic acid; sodium alginate/hypromellose/zinc acetate; sodium alginate/chitosan). Dissolution using buffers of pH values, β-glucosidase and times corresponding to gastrointestinal tract (GIT) was provided. Pellets coated with alginate/chitosan showed low rutin dissolution (12-14%) in upper GIT conditions and fast release (87-89%) under colon conditions; that is a good presumption of intended rutin release. After colitis induction and development, the rats were treated with pellets and rutin solution administered orally, solution also rectally. Colon/body weight ratio, myeloperoxidase activity and histological evaluation were performed. Rutin was able to promote colonic healing at the dose of 10mg/kg: colon/body weight ratio decreased and myeloperoxidase activity was significantly suppressed. Pellets coated with alginate/chitosan applied orally and rutin solution administered rectally showed the best efficacy. The combination of rutin as natural product, mucoadhesive chitosan degraded in the colon and sodium alginate as the main coating substance in the form of pellets create a promising preparation for therapy of this severe illness.

Topics: Administration, Oral; Alginates; Animals; Anti-Inflammatory Agents; Buffers; Caffeic Acids; Chemistry, Pharmaceutical; Chitosan; Colitis; Colon; Disease Models, Animal; Drug Compounding; Drug Implants; Drug Stability; Gastrointestinal Agents; Glucuronic Acid; Hexuronic Acids; Hydrogen-Ion Concentration; Hypromellose Derivatives; Male; Methylcellulose; Rats; Rats, Wistar; Rutin; Solubility; Technology, Pharmaceutical; Time Factors; Trinitrobenzenesulfonic Acid; Zinc Acetate

The purpose of this study was to formulate budesonide (BUD) compression-coated tablets for colonic specific delivery. Pectin and guar gum were used as enzyme-dependent polymers. For comparison purposes, both pH- and time-dependent polymers were also tried. In vitro release studies were carried out at different pH (1.2, 6.8, and 7.4). Therapeutic efficacy of the prepared tablets compared to commercially available capsules and enema were evaluated in trinitrobenzenesulfonic acid-induced rabbit colitis model. In pH-dependent polymers, Eudragit (EUD) S100/EUD L100 (1:1) released 45.58% in the target area (colon). For time-dependent polymers, decreasing cellulose acetate butyrate (CAB) ratio increased the release in both pH 6.8 and 7.4 till it reached 40.58% and 93.65%, respectively, for 25% CAB. In enzyme-dependent polymers, increasing pectin ratio to 75% retarded the release (4.59% in pH 6.8 and 54.45% in pH 7.4) which was significantly enhanced to 99.31% using pectinolytic enzyme. Formula F14 coated with 75% pectin significantly reduced the inflammatory cells in the connective tissue core of the colon of the treated group and significantly decreased myeloperoxidase activity (3.90 U/g tissue weight). This study proved that BUD compression-coated with 75% pectin may be beneficial in the treatment of inflammatory bowel disease.

Topics: Administration, Oral; Animals; Anti-Inflammatory Agents; Budesonide; Calorimetry, Differential Scanning; Cellulose; Chemistry, Pharmaceutical; Colitis; Colon; Delayed-Action Preparations; Disease Models, Animal; Drug Carriers; Drug Compounding; Galactans; Gastrointestinal Agents; Hydrogen-Ion Concentration; Hypromellose Derivatives; Kinetics; Male; Mannans; Methylcellulose; Pectins; Plant Gums; Polymethacrylic Acids; Rabbits; Rheology; Solubility; Tablets, Enteric-Coated; Technology, Pharmaceutical; Trinitrobenzenesulfonic Acid

This project aims to investigate the anti-inflammatory properties of mastic [(Pistacia lentiscus var. Chia (Anacardiaceae)] extracted from the Chios mastic plant to help reduce intestinal inflammation in inflammatory bowel disease patients. Mastic and mastic resin were obtained from the Chios Mastiha Growers Association (www.mastihashop.com). The resin was ground into a fine powder using a pestle and mortar and formulated in factorial design manner. Evaluation of the efficacy of specific anti-inflammatory/antioxidant compounds in mitigating the clinical colitis parameters in a mouse model of colitis were performed with mastic itself and combination of tocopherol compounds. Colonic drug delivery system was developed consisting of two compartment model and its release profile was also investigated.

Topics: alpha-Tocopherol; Animals; Anti-Inflammatory Agents; Antioxidants; Chemistry, Pharmaceutical; Colitis; Dextran Sulfate; Disease Models, Animal; Dosage Forms; Drug Carriers; Drug Therapy, Combination; Gastrointestinal Agents; Hydrogen-Ion Concentration; Hypromellose Derivatives; Kinetics; Male; Methylcellulose; Mice; Mice, Inbred C57BL; Pectins; Pistacia; Resins, Plant; Solubility

Coloscopic small bowel enema, a new diagnostic method, permits small and large intestinal investigation in one session. A coloscope is required equipped with a circular mounted balloon at the distal end. The endoscope is placed into coecum using the conventional technique (coloscopy). After intubation of the ileocoecal valve the balloon is inflated in the terminal ileum. This prevents reflux of the contrast medium and methyl-cellulose solution which are instilled into the small bowel through the endoscope instrumentation bore. Double-contrast investigation of the small bowel is particularly suitable for diagnosis of inflammatory diseases (e.g. Crohn's disease), Meckel's diverticulum and polypoid lesions such as carcinoid tumours.

Topics: Adult; Barium Sulfate; Colitis; Colonoscopy; Crohn Disease; Female; Humans; Intestine, Small; Male; Methylcellulose; Middle Aged; Radiography