Multiparticulate systems containing 5-aminosalicylic acid for the treatment of inflammatory bowel disease

In recent years, many achievements have been realized in the therapy of inflammatory bowel disease (IBD) although its etiology remains unknown. Thus IBD treatment is symptomatic and targets general inflammatory mechanisms. Oral formulations containing 5-aminosalicylic acid (5-ASA) have become the standard therapy for mild-to-moderate IBD

The diuretic effect of cornflower water extract

The objective of this study was to evaluate and compare the effect of cornflower water extract and hydrochlorothiazide on diuresis, Na+ and K+ excretion, and the changes in the prostaglandin E2 and kinins levels in the blood plasma.Material and methods. Male Wistar rats were used in all experiments. Animals were divided into nine groups. Diuretic activity was investigated according to the technique proposed by E. B. Berchin; urinary electrolyte contents were analyzed by flame photometry. Prostaglandin E2 content was measured by radioimmunoassay using 3H isotopes, kinins – by enzymatic methods. Results. It has been established that in male rats, receiving hydrochlorothiazide, the volume of urine excreted two and four hours after the administration of the drug was by 18% and 17%, respectively, higher as compared to the rats that were given cornflower water extract (P<0.05). The diuretic effect of cornflower water extract was noted in the animal group receiving this extract as compared to the control group: after two hours, the volume of urine excreted increased from 2.03±0.03 mL to 2.44±0.04 mL and after four hours – from 3.88±0.07 mL to 5.35±0.1 mL. Administration of hydrochlorothiazide under the load of salts and water resulted in a higher excretion of sodium and potassium as compared to the effect of cornflower water extract. The highest prostaglandin levels were found in the blood plasma of the animals receiving hydrochlorothiazide. Under the load of salts and water, a 13% and 15% increase, respectively, in the amount of prostaglandins was observed in the animals that were given cornflower water extract compared to the control animals (P<0.05). The greatest increase in the amount of kinins was found in the groups of animals that were given hydrochlorothiazide under the load of salts and water (14% and 22%, respectively). Kinin levels did not differ statistically significantly between the control group and the groups receiving cornflower water extract. Conclusion. Cornflower water extract possesses diuretic activity, but its effect was lower than that of hydrochlorothiazide

Bioadhesive pellets increase local 5-aminosalicylic acid concentration in experimental colitis

Topical delivery of 5-aminosalicylic acid (5-ASA) to the colonic mucosa is important in order to achieve effective drug concentration in the site of inflammation and to minimize its systemic availability. 5-ASA loaded pellets were prepared by an extrusion/spheronization method. Mucoadhesive biopolymer chitosan was incorporated into the pellets, and drug delivery to the colon was controlled by the pH-sensitive polymer Eudragit® FS. Dissolution profiles of coated pellets revealed no drug release at pH 1.2 within 2h and release as intended in the simulated distal ileum and colon. In vivo, chitosan-core drug loaded pellets (AMCh) showed 2.5-fold higher drug metabolite concentration than after chitosan free pellets (AM) administration in the inflamed colonic tissue. Additionally, AMCh demonstrated decreased in AUC in colitis group (1507 ± 400 ng h/ml) compared with AM (1907 ± 122 ng h/ml). In terms of therapeutic efficiency, administration of pellets markedly decreased the colon/body weight ratio (colitis: 0.0355 ± 0.0028; AM 0.0092 ± 0.0033; AMCh 0.0086 ± 0.0022) and myeloperoxidase activity (colitis: 3212 ± 294 U/g tissue; AM 796 ± 211 U/g; AMCh 552 ± 319 U/g). Bioadhesive chitosan pellets showed additional beneficial properties for colonic 5-ASA delivery in the treatment of inflammatory bowel disease by increasing the drug concentration locally

Coated chitosan pellets containing rutin intended for the treatment of inflammatory bowel disease: in vitro characteristics and in vivo evaluation

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

Pellets for oral administration of low-molecular-weight heparin

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