S. K. Prajapati

Clotrimazole (CLTZ) is a local imidazolic antifungal agent. A major problem associated with the successful formulation of effective dosage forms containing CLTZ is its poor aqueous solubility, which presents a hindrance for the local availability of CLTZ and limits the effective antifungal therapy. In the present study, the effects of various concentrations of poly(amidoamine) (PAMAM) dendrimers generation 3.5 (G3.5) and generation 4 (G4) with carboxylate (DCC), amine (DCN) and hydroxyl surface groups (DCO) on aqueous solubility, in vitro drug release studies, and for stability studies of CLTZ drug. The obtained results showed that all tested PAMAM dendrimers improved the solubility of CLTZ and the more potent were (DCC) dendrimers. The increase in solubility of CLTZ was highest at dendrimer concentration of 10 mg/ml. These observations indicate that PAMAM dendrimers enhance the solubility of CLTZ, The drug dendrimers complexes displayed the controlled release action during in vitro release studies. Formulation with amine and carboxylate were subjected to accelerated stability studies. Key words: poly(amidoamine) dendrimers; clotrimazole; aqueous solubility; surface groups

  Fast dissolving, fast melting, chewable and orally dissolving or disintegrating tablets are solid dosage forms that disintegrate rapidly and dissolve in the mouth withoutwater. The principle challenge with orally disintegrating tablets (ODTs) is to develop tablet formulations for standard direct compression processes that deliver rapid disintegration, pleasant mouth feel and high breaking force for tablet robustness. Superdisintegrant affect a range of formulation parameters, including the rate of disintegration, tablet breaking force, and mouth feel. The emphasis on the availability of drug highlights the importance of the relatively rapid disintegration of a tablet as a criterion for ensuring uninhibited drug dissolution behavior. Number of factors affects the disintegration behavior of tablets. The development of fast dissolving or disintegrating tablets provides an opportunity to take an account of tablet disintegrants. Superdisintegrants are generally used at a low level in the solid dosage form, typically 1 – 10 % by weight relative to the total weight of the dosage unit. Key words: Tablet Disintegrants, Superdisintegrants, Kyron T-314.