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.
Highlights
Carvedilol phosphate is the drug of choice in the treatment of hypertension and congestive heart failure
This study suggested that as the quantity of hydroxypropyl methylcellulose (HPMC) increased in the formulation, lag time and total floating time of tablet increased
The Higuchi plots has shown good linearity, indicating that the drug release was proportional to the square root of time and the drug was released at a slower rate. Both immediate release and controlled release tablets of carvedilol phosphate were formulated by designing compression coating floating drug delivery system
Summary
Carvedilol phosphate is the drug of choice in the treatment of hypertension and congestive heart failure. Carvedilol phosphate is a class II drug which has low solubility and high permeability, practically insoluble in water, have a slow onset of action and poor bioavailability [1]. This research is designed with a dual approach such as compression coating technique, where the core would be a gastroretentive floating tablet and the coating material is to provide a quick onset of action. Hurdles in such formulation were identified as the low solubility, high permeability of carvedilol phosphate, which caused the poor oral bioavailability. To improve bioavailability and to reduce dosing frequency, a suitable formulation was required with a controlled rate towards the treatment of hypertension and congestive heart failure
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