Vignesh, E (2019) Formulation and Evaluation of Colon Targated Prednisolone Compression Coated Tablet. Masters thesis, C.L.Baid Metha College of Pharmacy, Chennai..
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Abstract
Colonic delivery refers to targeted delivery of drugs into the lower GI tract, which occurs primarily in the large intestine (i.e. colon). These delayed mechanisms are designed to improve the efficacy of the drug by concentrating the drug molecules where they are needed most, and also minimize the potential side effects and drug instability issues associated with premature release of drug in the upper parts of the GIT, namely stomach and small intestine. The drugs used in the treatment of Irritable bowel syndrome, ulcerative colitis, diarrhea, and colon cancer are ideal candidates for local colon delivery. The selection of carrier for particular drugs depends on the physiochemical nature of the drug as well as the disease for which the system is to be used. Factors such as chemical nature, stability and partition coefficient of the drug and type of absorption enhancer chosen influence the carrier selection. Compression coating has gained increased interest in the recent years for creating modified released products. It involves the compaction of granular materials around a preformed tablet core using specially designed tableting equipment. Compression coating is a dry process. This type of tablet (compression coated tablet) has two parts, internal core and surrounding coat. The core is a small porous tablet and prepared on one turret. For preparing the final tablet, a bigger die cavity in another turret is used in which first the coat material is filled to half and then core tablet is mechanically transferred, again the remaining space is filled with coat material and finally compression force is applied. Inflammatory bowel disease (IBD) is an umbrella term used to describe disorders that involve chronic inflammation of your digestive tract. Types of IBD include: Ulcerative colitis. This condition causes long-lasting inflammation and sores (ulcers) in the innermost lining of your large intestine (colon) and rectum. Crohn's disease. This type of IBD is characterized by inflammation of the lining of your digestive tract, which often spreads deep into affected tissues. Both ulcerative colitis and crohn's disease usually involve severe diarrhea, abdominal pain, fatigue and weight loss. IBD can be debilitating and sometimes leads to life-threatening complications. For the past 30 years, corticosteroids have been the mainstay of therapy in patients with moderate to severe active inflammatory bowel disease. Initial treatment is prednisone, 40 to 60 mg per day. In severely ill hospitalized patients, reasonable initial therapy is hydrocortisone, 100 mg administered intravenously every eight hours. Intravenous therapy generally produces rapid improvement of symptoms, with maximal benefit occurring when the corticosteroid has been administered for six to eight days. Once improvement has occurred, prednisone is tapered by 5 to 10 mg per week until the dosage is 15 to 20 mg per day. This dosage is then tapered by 2.5 to 5 mg per week until the drug is discontinued The objective of this study was to design compression coated tablets of Prednisolone for an effective and safe therapy of ulcerative colitis and inflammatory bowel disease using pectin and xanthan gum and HPMC as carriers. The core tablets of Prednisolone coated with pectin: HPMC in the ratio 1:1 and 1:2 and xanthan gum: HPMC in the ratio 1:1 and 1:2 . Pectin: HPMC coated pellets offer a greater degree of protection from premature drug release in the upper GI tract than pectin alone. The pectin is still available for enzymatic degradation, which allows greater drug release under conditions that may be expected to pertain in the colon. It is possible by careful formulation of the compression coated tablet to have different drug release profiles, whereby an increase in the amount of drug released can be induced by the action of pectinolytic enzymes. By changing the other variables such as the pectin and HPMC ratio or the molecular weight of the polymers, it may be possible to produce a system with a release profile, which is tailored to meet the particular requirements of any individual drug. From the results it can be concluded that pectin: HPMC coated tablets could be used to treat the inflammatory conditions of the colon. Natural polysaccharides such as xanthan gum, are not digested in the human stomach or small intestine, but are degraded in the colon by resident bacteria. HPMC delayed the drug release in the small intestine, but was degraded by colonic bacterial enzymes thereby releasing the drug. Xanthan gum is a high molecular weight extracellular polysaccharide. The molecule consists of a backbone identical to that of cellulose, with side chains attached to alternate glucose residues. It is a hydrophilic polymer, which until recently had been limited for use in thickening, suspending and emulsifying water based systems. It appears to be gaining appreciation for fabrication of matrices, as it not only retards drug release, but also provides time- independent release kinetics with added advantages of biocompatibility and inertness. Based on drug release in the colon compressed coated tablets with mixture of pectin was more successful to produce a drug targeting to the colon with minimum amount released in the other parts of gastro intestinal tract.
| Item Type: | Thesis (Masters) |
|---|---|
| Additional Information: | 261710013 |
| Uncontrolled Keywords: | Formulation, Evaluation, Colon Targated Prednisolone, Coated Tablet |
| Subjects: | PHARMACY > Pharmaceutics |
| Depositing User: | Ramakrishnan J |
| Date Deposited: | 04 Dec 2021 06:06 |
| Last Modified: | 22 Mar 2022 08:52 |
| URI: | http://repository-tnmgrmu.ac.in/id/eprint/18811 |
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