methylcellulose and Stomach-Ulcer

Recently, great attention has been paid to nanocapsules. The interest of these structures is due to their promising applications as drug delivery systems. The objective of this study was to develop novel enteric coating technique based on instantaneous encapsulation of the acid-labile drug, omeprazole in innovative enteric nanocapsules. Omeprazole enteric nanocapsules were formulated by varying the type and amount of the enteric polymer. The particle size (PS), polydispersity index (PDI), zeta potential (ZP) and encapsulation efficiency (EE) values of the prepared enteric nanocapsules were determined. A full 2(1)×3(1) factorial design was used for planning and analysis of the experimental trials to select the optimized formulation. The highest desirability value was 0.7463 for formula E3 (containing 200mg hydroxypropyl methylcellulose phthalate (HPMCP)). The stability of omeprazole was reflected by the absence of the exothermal peak when the drug was encapsulated as detected by differential scanning calorimetry (DSC) thermograms. In vitro drug release study confirmed the USP specifications required to meet the key formulation characteristics of gastro-resistance. In vivo pharmacological assessment showed that the optimized nanocapsules were able to protect rat stomach against ulcer formation compared to the aqueous suspension of the drug which showed less significant protection.

Topics: Animals; Anti-Ulcer Agents; Calorimetry, Differential Scanning; Chemistry, Pharmaceutical; Disease Models, Animal; Ethanol; Kinetics; Male; Methylcellulose; Microscopy, Electron, Transmission; Nanocapsules; Nanotechnology; Omeprazole; Proton Pump Inhibitors; Rats, Wistar; Solubility; Stomach Ulcer; Technology, Pharmaceutical; Thermography

Usual treatment for Helicobacter pylori-induced peptic ulcer includes a 'triple therapy' consisting of two antibiotics (amoxicillin and clarithromycin) and a proton pump inhibitor (omeprazole). The objective of this project work was defined with a view to retain the drug in stomach for better antiulcer activity and substituting one of the synthetic drugs in this therapy with a herbal alternative. Hence, aim of the present work was to design and develop a bilayer floating tablet of amoxicillin and Aloe vera gel powder for the treatment of peptic ulcer. A. vera gel powder is used for its cytoprotective action. Bilayer floating tablets were prepared by applying direct compression technique. The proportion of sodium bicarbonate and citric acid was adjusted to get the least possible lag time with good matrix integrity and total floating time. Polymer concentration was adjusted to get the maximum release in 8 h. The formulation was developed using hydroxypropyl methyl cellulose (HPMC) K4M and HPMC K100M in a ratio of 85:15 along with 1:4 ratio of effervescent agents was found to give floating lag time of less than 1 min with total floating time of more than 8 h and 97.0% drug release in 8 h. In vivo study in rats meets the requirement of antiulcer activity for bilayer tablet in comparison to single amoxicillin as standard.

Topics: Aloe; Amoxicillin; Animals; Chemistry, Pharmaceutical; Citric Acid; Drug Compounding; Gels; Hypromellose Derivatives; Male; Methylcellulose; Polymers; Powders; Rats; Rats, Wistar; Sodium Bicarbonate; Stomach Ulcer; Tablets

Pantoprazole is used in the treatment of acid related disorders and Helicobacter pylori infections. It is activated inside gastric parietal cells binding irreversibly to the H+/K(+)-ATPase. In this way, pantoprazole must be absorbed intact in gastro-intestinal tract, indicating that enteric delivery systems are required. The purpose of this study was to prepare pantoprazole-loaded microparticles by spray-drying using a blend of Eudragit S100 and HPMC, which can provide gastro-resistance and controlled release. Microparticles presented acceptable drug loading (120.4 mgg(-1)), encapsulation efficiency (92.3%), surface area (49.0 m2g(-1)), and particle size (11.3 microm). DSC analyses showed that the drug is molecularly dispersed in the microparticles, and in vivo anti-ulcer evaluation demonstrated that microparticles were effective in protecting stomach against ulceration. Microparticles were successfully tabletted using magnesium stearate. In vitro gastro-resistance study showed that microparticles stabilized pantoprazole in 62.0% and tablets in 97.5% and provided a controlled release of the drug.

Topics: 2-Pyridinylmethylsulfinylbenzimidazoles; Acrylic Resins; Animals; Anti-Ulcer Agents; Calorimetry, Differential Scanning; Chemistry, Pharmaceutical; Chromatography, High Pressure Liquid; Delayed-Action Preparations; Desiccation; Drug Compounding; Ethanol; Excipients; Hypromellose Derivatives; Methylcellulose; Microscopy, Electron, Scanning; Nanoparticles; Pantoprazole; Particle Size; Porosity; Rats; Solvents; Stomach Ulcer; Surface Properties

The effects of solid non-nutritive diet on pylorus-ligation ulcers were tested. An experimental group of 16 rats received a bulky mixture of silica and methylcellulose during 48 hr prior to ligation. Control rats were food deprived for the same period of time. A multivariate analysis of variance was applied to nine measures of the study. It was found that rumenal ulceration and total acidity were lower in experimental animals than in controls. This finding confirms a previous observation indicating that the physical property of diet has antiulcerogenic effects.

Topics: Animals; Body Weight; Diet; Dietary Fiber; Female; Gastric Juice; Ligation; Male; Methylcellulose; Pylorus; Rats; Silicon Dioxide; Stomach; Stomach Ulcer

Topics: Animal Nutritional Physiological Phenomena; Animals; Diet; Female; Food; Food Deprivation; Gastric Juice; Male; Methylcellulose; Rats; Rumen; Silicon Dioxide; Stomach Ulcer; Stress, Physiological; Sucrose

Topics: Carboxylic Acids; Carboxymethylcellulose Sodium; Methylcellulose; Parasympatholytics; Peptic Ulcer; Stomach Ulcer