Design, Formulation Development and Evaluation of Matrix Tablet Containing Labetalol HCL
Abstract
The objective of present work was to design and develop sustained release matrix tablets of anti-hypertensive drug Labetalol hydrochloride. Hydroxypropyl methyl cellulose K15, Sodium CMC, Xanthan gum and Tamarind seed polysaccharide used as a rate retarding polymer. Whereas Polyvinyl Pyrrolidone and Microcrystalline cellulose are used as granulating agent and diluent. The influence of variable concentration of polymers on the release rate of drug was investigated. The results of the present work point out that the rate of Labetalol hydrochloride release from polymers like Hydroxypropyl methyl cellulose K15, Sodium CMC, Xanthan gum and Tamarind seed polysaccharide are mainly controlled by the drug–polymer ratio. The prepared sustained release matrix tablets were evaluated for various parameters like hardness, friability, uniformity of weight, uniformity of drug content and in vitro drug release studies
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Introduction
Sustained release system includes any drug delivery system that “achieves slow release of drug over an extended period of time.” The term sustained release has become associated with those systems from which therapeutic agent may be automatically delivered over a long period of time. A simple dosing scheme with a once or twice daily administration of the antihypertensive agent is known to increase patient compliance. For this reason, the pharmaceutical industry is intensively searching for longer-acting antihypertensive drugs, either by the development of novel agents with a longer elimination half life, or by the improvement of the dosage form of existing shorter acting compounds, so that plasma concentrations compatible with a blood pressure lowering activity are maintained during the whole day. Sustained drug delivery has been introduced to overcome the drawback of fluctuating drug level associated with conventional dosage form [1-3].
The goal in designing oral sustained or controlled delivery is to reduce the frequency of the dosing or to increase effectiveness of the drug by localizing at the site of action, reducing the dose required or provide uniform drug delivery, thereby also improving patient compliance. Controlled or sustained release dosage forms provide a better control drug levels, less dosage frequency, less than effects, increased efficiency and constant delivery [4].
In order to overcome the drawbacks of conventional drug delivery systems, several technical advancements have led to the development of sustained release drug delivery system like application of different polymers to achieve sustained delivery that could revolutionize method of medication and provide a number of therapeutic benefits. To fabricate matrix tablet of Labetalol HCl using polymers like Hydroxypropylmethylcellulose (HPMC), Sodium CMC, Xanthan gum and Tamarind seed polysaccharide (carried out the Isolation and Extraction of Tamarind seeds polysaccharide from tamarind husk kernels).
Conclusion
From the present study, The sustained release matrix tablet of Labetalol HCl using polymers such as HPMC K 15, Sodium CMC, Xanthan gum and Tamarind seed polysaccharide, prepared by wet granulation method were found to be good without chipping, capping and sticking. The drug content was uniform in all the formulations of tablets prepared. The low values of standard deviation indicate uniform distribution of drug within the matrices.IR and DSC studies indicated that the drug and polymers are in the pure form and compatible with each other. The drug-polymer ratio was found to influence the release of drug from the formulations. As the polymer concentration is increased, the drug release rates were found to be decreased. Formulation F3 and F12 with drug-polymer ratio 1:1 containing PVP K30 and MCC as binder and diluents respectively have shown promising results as per USP Test-I requirements. Sustained release matrix tablets of Labetalol hydrochloride can be prepared using HPMC K 15 and Tamarind seed polysaccharide achieve a desired drug release rates over a period of 12 hours, which can help to reduce the dose and frequency. Among the various formulations prepared, F3 and F12 appear suitable for further pharmacodynamic and pharmacokinetic evaluation in a suitable animal model.