STUDIES ON THE PREPARATION, CHARACTERIZATION AND SOLUBILITY OF Β-CYCLODEXTRIN-NELFINAVIR INCLUSION COMPLEXES

Nelfinavir is a poor water-soluble antiretroviral drug with relatively low bioavailability. The effect of β-cyclodextrin on the aqueous solubility and dissolution rate of nelfinavir was investigated. Phase solubility studies indicated that the solubility of nelfinavir was significantly enhanced by complexing it with β- cyclodextrin. It was classified as Bs type indicating the 1:2 stoichiometric inclusion complexes. The various solid complexes prepared by physical mixture, Kneading, coprecipitation & common solvent methods were characterized by DSC, X-RD & FT-IR. Dissolution study showed that the solubility and dissolution rate of nelfinavir was significantly improved by complexation with β-cyclodextrin

Design and Optimization of Floating Drug Delivery System of Acyclovir

The purpose of the present work was to design and optimize floating drug delivery systems of acyclovir using psyllium husk and hydroxypropylmethylcellulose K4M as the polymers and sodium bicarbonate as a gas generating agent. The tablets were prepared by wet granulation method. A 32 full factorial design was used for optimization of drug release profile. The amount of psyllium husk (X1) and hydroxypropylmethylcellulose K4M (X2) were selected as independent variables. The times required for 50% (t50%) and 70% (t70%) drug dissolution were selected as dependent variables. All the designed nine batches of formulations were evaluated for hardness, friability, weight variation, drug content uniformity, swelling index, in vitro buoyancy, and in vitro drug release profile. All formulations had floating lag time below 3 min and constantly floated on dissolution medium for more than 24 h. Validity of the developed polynomial equation was verified by designing two check point formulations (C1 and C2). The closeness of predicted and observed values for t50% and t70% indicates validity of derived equations for the dependent variables. These studies indicated that the proper balance between psyllium husk and hydroxypropylmethylcellulose K4M can produce a drug dissolution profile similar to the predicted dissolution profile. The optimized formulations followed Higuchi's kinetics while the drug release mechanism was found to be anomalous type, controlled by diffusion through the swollen matrix