Inclusion complexes of nicardipine-HCL for oral administration

Inclusion complexes of nicardipine HCl [NIC] with beta-cyclodextrin [beta-CD] and hydroxypropyl-beta-cyclodextrin [HP-beta-CD] were prepared using different methods: co-evaporation, kneading and co-precipitation. Inclusion complexation in aqueous solution and in solid state was studied by the solubility method, Fourier transform-infrared spectroscopy [FTIR], Differential scanning calorimetry [DSC] and X-ray diffractometry [XRD]. The solubility of [NIC] increased as a function of cyclodextrin concentration, showing B s and AL type diagrams for [beta-CD] and [HP-beta-CD], respectively. The dissolution rate of [NIC] / cyclodextrin complexes were investigated and compared with those of the physical mixtures and pure drug. The dissolution efficiency of [NIC] increased by complexation with cyclodextrins to 2.8-2.9 fold than [NIC] alone. Oral bioavailability in rabbits increased to 6 fold by complexation with [beta-CD]

Formulation and evaluation of a transdermal drug delivery system for nicardipine hydrochloride: in vitro and in vivo studies

In the present investigation, nicardipine HCl was formulated in different traditional transdermal formulations that are used topically on the skin for systemic action. These formulations were an ointment, an o/w emulsion, a gel, an emulgel and a cellulose acetate butyrate film. Enhancers; namely, dimethyl sulfoxide [DMSO], Tween 80, urea, cetrimide and sodium lauryl sulfate [SLS], were added in different concentrations to the selected pharmaceutical formulations. In vitro studies were carried out on an isolated abdominal rabbit skin using diffusion cell. The correlation coefficient [r], the steady-state flux [J] and permeability coefficient [kp] were calculated. The results revealed that the permeation of the drug trough the skin was mainly dependent on the composition of each base and the type of the added enhancer and its concentration

Adsorption-desorption characteristics of azapropazone

The aim of the present study was to illustrate the interaction of various adjuncts of common use in pharmaceutical formulations with azapropazone. This was tackled via the study of adsorption and desorption properties of the drug. The results revealed that azapropazone was adsorbed on the surface of adjuncts to varying degrees, depending on the nature of these adjuncts. The adsorbents can be arranged according to their efficiency to absorb azapropazone in the following order: Beegum > bentonite > magnesium trisilicate > kaolin > aluminum hydroxide > agar. The adsorption data were found to follow the Freunidch adsorption isotherm. The presence of either polyhydroxy compounds, polymers or non-ionic surfactants decreased the amount of drug adsorbed. No effect was observed on the adsorption of drug in the presence of ethyl alcohol. Concerning the effect of electrolytes, it was found that magnesium chloride decreased the amount of drug adsorbed; while sodium chloride did not affect the adsorption. Elution study revealed that both vegum and agar exhibited low desorption, indicating that azapropazone is strongly bound to the surface of these two adsorbents. On the other h and, aluminum hydroxide exhibited the highest desorption of azapropazone, indicating that attraction forces occurring between the drug and the adsorbent are different