FORMULATION AND EVALUATION OF CONTROLLED RELEASE OSMOTIC TABLET OF CARVEDILOL PHOSPHATE

Carvedilol Phosphate Osmotic Tablets were prepared using a Direct Compression approach. A mixture of osmogens i.e. NaCl and Mannitol was used to achieve a desired osmotic pressure in the tablets which were then coated with Cellulose Acetate polymer with PEG as a plasticizer and Povidone K30 as a pore former. Early screening batches showed drastic effect of osmogens and pore former, as well as % weight gain on drug release of the tablets. The prepared tablets were evaluated for Weight variation, Thickness, Hardness, Dissolution, and the final optimized formulation was exposed to Accelerated Stability Study. A full factorial statistical optimization was carried out on the best optimized formulation to establish the design space for selected factors i.e., NaCl and Povidone K30 against Response Dissolution. A significant effect of both factors was found on Dissolution rate, which justifies the use and rationale of the excipients Key Words: Carvedilol Phosphate, Osmotic Tablets, Direct Compression, NaCl, Mannitol, Cellulose Acetate.

EFFICACY OF CARVEDILOL COMBINED WITH ENDOSCOPIC VARICEAL LIGATION IN THE PREVENTION OF RECURRENT VARICEAL BLEEDING IN PATIENTS OF CIRRHOSIS

Background: The recurrent variceal bleeding is still very high with a very poor prognosis. The combination of a non-selective beta-blocker and endoscopic variceal ligation (EVL) is still a standard therapy for the prevention, but many patients showed no response to propranolol. Carvedilol is a new, non-selective beta-blocker having intrinsic alpha-blocker activity, but the data about the efficacy and safety of carvedilol is still very limited. This study is aimed at assessing the efficacy and safety of carvedilol combined with EVL in the prevention of recurrent variceal bleeding. Patients and methods: 33 patients having variceal bleeding were enrolled. All patients received carvedilol and were performed the EVL until variceal eradication. All the patients were followed after 9 months. Results: rate of variceal eradication of oesophageal varices was 87.88%; the recurrence rate of variceal bleeding was 12.12% after 9 months. The side effects of carvedilol were rare and not severe, including vertiges, headache, and orthostatic hypertension. Conclusion: Carvedilol combined with EVL appeared as a relatively safe and effective in the prevention of recurrent variceal bleeding in patients of cirrhosis. Key words: carvedilol, variceal bleeding, EVL

Drug Complexation and Formulation of a Buccal Tablet

In the present work use of Beta-Cyclodextrin for inclusion of Carvedilol, an antihypertensive drug with poor solubility and high first pass metabolism was studied, in order to improve its dissolution rate. The complex prepared by kneading method was characterized by Differential Scanning Calorimetry, Fourier Transformation Infra Red Spectroscopy and X-Ray Diffractometry along with the plain drug and physical mixture. The drug so complexed was incorporated into a buccal dosage form to by pass first pass metabolism to improve its bioavailability. The buccal tablets containing complex showed reasonable mucoadhesive strength. The dissolution and permeability across pig buccal mucosa were improved in case of tablets containing the complex as compared to plain drug tablet. Key words: Carvedilol; Beta-Cyclodextrin; Complexation; Dissolution; Characterization; Permeation. DOI: 10.3329/bjsir.v45i2.5709Bangladesh J. Sci. Ind. Res. 45(2), 123-128, 2010