Formulation and Evaluation of Compression Coating Floating Tablets of Carvedilol Phosphate Once Daily Dose

Abstract

Objective: The rationale for the study was to develop a once-daily dose of immediate as well as a gastro-retentive form of carvedilol phosphate by compression coating floating technique. Methods:In the presented study the core tablet was containing half the quantity of the drug formulated as floating drug delivery using different controlled release polymers blend in various proportions like ethyl cellulose, carbopol, hydroxypropyl methylcellulose (HPMC) K4, K15, and K100 by direct compression method. Outer coat layer was formulated with rest of the drug with the blend of different super disintegrants in various proportions like crospovidone, croscarmellose sodium (CCS), sodium starch glycolate (SSG) for the immediate release of the drug. Both the immediate and controlled formulation was separately formulated from sf1 to sf9 and f1 to f9 respectively. Based on the evaluation parameters finally, formulation F1 to F9 were formulated by applying compression coating floating method. These formulations were characterized for their tablet density, disintegration time, floating lag time, in vitro drug release, drug-excipients interaction and accelerated stability studies etc. Results:The result revealed formulation sf9 containing SSG of 15% was able to 97.2% of drug release within 15 min towards the achievement of immediate release. Similarly, the formulation f9 containing 0.5:0.5:4.5 ratios of ethyl cellulose, carbopol and HPMC K15 was able to 95.3% of drug release within 16h. From compressed coat tablets batches of F1 to F9, based on the dissolution data F9 was considered as an optimized formulation which was able to release 48.6% of drug release within 15 min and cumulatively controlled the release up to 96.4% for 16 h, followed zero-order kinetics and Higuchi pattern. Conclusion:The results obtained in this research work clearly indicated that the compression coating floating tablet of carvedilol phosphate was the best dosage form for the treatment of hypertension. Results of the evaluation of prepared batches indicate that the batch F9 is a promising formulation for both a quick onset of action as well as gastro-retentive dosage form to maintain the constant drug action which would improve the maximum therapeutic efficacy and patient compliance.

The DESIGN AND DEVELOPMENT OF CARVEDILOL GASTRORETENTIVE FLOATING DRUG DELIVERY SYSTEMS USING HYDROPHILIC POLYMERS AND IN VITRO CHARACTERIZATION

“…And so, the microcrystalline cellulose (MCC) was mixed uniformly with the blend, and then magnesium stearate mixed with the tablet mixture as a lubricant [15,17]. The geometric dilution technique was used for the mixing of the contents.…”

“…From each formulation randomly, five tablets selected and each tablet hardness measured by using a Monsanto hardness tester. The unit of hardness is normally in terms of kg/cm 2 [17,21,22].…”

“…pH 1.2 (900 ml) buffer solution used as dissolution fluid. Through a filter (0.45 μm) the 5 ml of dissolution medium was getting back from the flask at various times interims and the same volume of the fresh dissolution medium substituted [15,17,20]. After reasonably diluted with a buffer solution, at 241 nm by utilizing a dual-beam UV-Visible spectrophotometer, the absorbance was estimated [24].…”

“…[16,22]. [15,17]. The weight variation test for all formulated carvedilol phosphate tablets evaluated and every one of the tablets was discovered uniform weight having less standard deviation as compared to the prescribed Indian Pharmacopoeia limits of±7.5%.…”

Formulation and in Vitro Evaluation of Salbutamol Sulphate and Theophylline Extended-Release Tablets Using Modified Polymers

“…The pharmaceutical effect has only seen for the time duration in which the concentration of the drug remains within the therapeutic range that can be best achieved with ER tablets [3]. The significance of administering single-dose extended-release tablet that has discharged over an extended timeframe instead of multiple doses becomes the area of interest for the formulation designing scientists in the Pharmaceutical industry [4]. The oral prolonged discharge dosage form has been prepared for those medications that are comfortably absorbed from the gastrointestinal tract (GIT), have a short half-life and eliminated quickly from the bloodstream [5].…”