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  • Research Paper The Effect of Superdisintegrants on the Dissolution of Promethazine. HCl Fast Dissolving Tablets

    Ganesh kumar Gudas*, B. Manasa, K. Senthil Kumaran, V.V. Rajesham, S. Kiran Kumar, J. Prasanna Kumari and V. Malla Reddy Srikrupa Institute of Pharmaceutical Sciences, Velkalla Siddipet, Medak, India.

    ABSTRACT: Promethazine.HCl is a potent anti-emetic. The central antimuscarinic actions of antihistamines are probably responsible for their anti-emetic effects. Promethazine is also believed to inhibit the medullary chemoreceptor trigger zone, and antagonize apomorphine -induced vomiting. Fast dissolving tablets of Promethazine.HCl were prepared using five superdisintegrants viz; sodium starch glycolate, crospovidone, croscarmellose, L-HPC and pregelatinised starch. The precompression blend was tested for angle of repose, bulk density, tapped density, compressibility index and Hausners ratio. The tablets were evaluated for weight variation, hardness, friability, disintegration time (1 min), dissolution rate, content uniformity, and were found to be within standard limit. It was concluded that the fast dissolving tablets with proper hardness, rapidly disintegrating with enhanced dissolution can be made using selected superdisintegrants. Among the different formulations of Promethazine.HCl was prepared and studied and the formulation S2 containing crospovidone, mannitol and microcrystalline cellulose combination was found to be the fast dissolving formulation. In the present study an attempt has been made to prepare fast dissolving tablets of Promethazine.HCl, by using different superdisintegrants with enhanced disintegration and dissolution rate.

    KEYWORDS: Fast dissolving tablets; Promethazine.HCl; Superdisintegrant

    Introduction The concept of Fast dissolving drug delivery system (FDDDS) emerged from the desire to provide patients with conventional means of taking their medication. Difficulty in swallowing (dysphasia) is a common problem of geriatrics and pediatrics, because of physiological changes associated with these groups of patients. Since the average life span is goingup considerably in this modern era, the number of geriatric patients is increasing and hence will have significant impact on development of drug delivery systems. Fast dissolving tablet is one of such example, for the reason of rapid disintegration or dissolution in mouth with little amount of water or even with saliva. Significance of this drug delivery system includes administration without water, accuracy of dosage, ease of portability, alternative to liquid dosage forms, ideal for pediatric and geriatric patients and rapid onset of action (Vandana B et al., 2005) Superdisintegrants act by swelling and due to swelling pressure exerted in the outer direction or radial direction which causes the tablet to burst or the accelerated absorption of water leading to promote disintegration. Proposed mechanism for the action of disintegrants include water uptake through wicking, swelling, deformation recovery and particle repulsion. (Abu-lazza et al., 2004).

    Promethazine.HCl is chemically (RS) dimethyl (1-metyl-2-(phenothiazine-10-yl) ethyl) - amine hydrochloride. The central antimuscarinic actions of antihistamines probably are responsible for their anti-emetic effects, promethazine also is believed to inhibit the medullary chemoreceptor trigger zone, and antagonize apomorphine- induced vomiting. In the present study, an attempt had been made to prepare fast dissolving (in the oral cavity) tablets of Promethazine.HCl with enhanced dissolution rate and hence improved patient compliance. (Sweetman et al., 2002)

    Materials and Methods Materials Promethazine.HCl, sodium starch glycolate, crosscarmellose sodium, crospovidone, microcrystalline cellulose, L-HPC and pregelatinised starch were obtained as gift samples from Alembic Ltd, Vadodara and all other chemicals/ solvents used were of analytical grade.

    Method Preparation of Mixed Blend of Drug and Excipients All the Ingredients were passed through mesh # 60. Required quantity of each ingredient was taken for each specified formulation (depicted in Table 1) and all the ingredients were co- grind in a mortar and pestle. The powder blend was evaluated for flow properties such as

    International Journal of Pharmaceutical Sciences and Nanotechnology

    Volume 3 Issue 1 April June 2010

    * For correspondence: Ganesh Kumar Gudas, E-mail:


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