Formulation and Evaluation of Clopidogrel Bisulfate Immediate Release Tablets

Many patients especially children and elderly have difficulty in swallowing tablets and capsules and consequently unable to take medicine as prescribed. Almost 50% of the population is affected by such problem, resulting in the high incidence of non compliance and ineffective therapy. Most pharmaceutical forms for oral administration are formulated for direct ingestion, or for chewing, or for prior dispersion and/or dissolution in water; some of them are absorbed in the mouth (sublingual or buccal tablets). To obviate the problems associated with conventional dosage forms, orally immediate release tablets have been developed, which combine hardness, dosage uniformity, stability and other parameters, with extremely easy administration, since no water is required for swallowing the tablets and they are thus suitable for geriatric, pediatric and traveling patients. Pharmaceutical products designed for oral delivery and currently available on the prescription and over-the-counter markets are mostly the immediate release type, which are designed for immediate release of drug for rapid absorption. Disintegrating agents are substances routinely included in tablet formulations and in some hard shell capsule formulations to promote moisture penetration and dispersion of the matrix of the dosage form in dissolution fluids. Superdisintegrants improve disintegrant efficiency resulting in decreased use levels when compared to traditional disintegrants. Mechanism of Disintegrants 1) High swellability This investigation is undertaken with an aim to develop pharmaceutically equivalent, stable, cost effective and quality improved formulation of Clopidogrel bisulphate immediate release tablets. The task of developing immediate release tablet is accomplished by using a suitable diluents and super-disintegrants. Faster disintegration of the tablet administrated orally minimizes absorption time and improves its bioavailability in less time. Immediate Release tablet of Anti plate drug is formulated using direct compression using super disintegrant Croscarmellose Sodium and Crospovidone. The current study involves preparation and evaluation of Clopidogrel bisulphate tablets, comparison of dissolution rate of optimized formulation with innovator’s product and estimation of similarity and difference factors. The formulations were further evaluated for pre & post compression parameters and in-vitro dissolution studies. The study reveals that the formulation F8 is found to be the optimized formulation with 99% drug release in 30 minutes in comparison with other super disintegrants. The kinetics study shows that the fast dissolving tablet formulation followed First order kinetic model explaining the diffusion controlled release mechanism. The similarity and dissimilarity factor obtained for Clopidogrel bisulphate was found to be within the standards. The formulation F8 exhibited similar release profile as that of innovators product at each time point. Hence, F8 was considered as the best formulation.