Leaching of 2,4-D from a soil in the presence of beta-cyclodextrin: laboratory columns experiments.

This study reports on the effect of the presence of beta-cyclodextrin (beta-CD) on the adsorption and mobility of the pesticide 2,4-dichlorophenoxyacetic acid (2,4-D) through soil columns. The previous application of beta-CD to the soil produced a retarded leaching of 2,4-D through the soil column, due probably to herbicide adsorption on the soil through beta-CD adsorbed. However, the application of beta-CD solution to the soil column where 2,4-D had been previously adsorbed, led to the complete desorption of the herbicide, due to the formation of water-soluble 1:1 inclusion complexes between 2,4-D and beta-CD. Beta-CD can be viewed as a microscopic organic-phase extractant. It can be an advantage to remove from soil pesticides which are able to form inclusion complexes with cyclodextrins, making them possible candidates for use in in situ remediation efforts.

Ethyl cellulose polymer microspheres for controlled release of norfluazon.

The pesticide norfluazon has been microencapsulated using ethyl cellulose to develop controlled-release formulations that decrease its mobility through the soil and protect it from photodegradation. Ethyl cellulose microspheres loaded with norfluazon were prepared by the solvent-evaporation method. To obtain the microspheres, certain conditions (pesticide/polymer ratio, percentage of emulsifying agent and solvent) were varied. The shape and size of the microspheres obtained were studied by scanning electron microscopy. Other parameters, such as solids recovery, encapsulation efficiency and pesticide loading, were also studied. The release rate of norfluazon from the different microspheres was slower than that of pure norfluazon. In particular, microspheres obtained with o-xylene, which provided the largest diameter, retarded the initial release of the pesticide relative to microspheres obtained with chloroform, or to pure norfluazon. Moreover, the studies showed that the pesticide/polymer ratio controlled the release of norfluazon, which was slower when this ratio was low. Release rates conformed to a generalised kinetic equation for a diffusion-controlled release mechanism, and the time taken for 50% of the active ingredient to be released into water, t50, was calculated.

Channeling agent and drug release from a central core matrix tablet.

A new oral dosage form for controlled and complete release of drug after a predetermined lag time is described. The system, designed to exploit the relatively constant small intestine transit time, consists of a drug-containing core coated with a polymeric matrix formed by a channeling agent (NaCl, mannitol, and Emdex) and an inert polymer (Eudragit RS100). The lag time was found to be dependent on type and particle size of the channeling substances used. Also, rheological properties of the binary mixtures (channeling substance--polymer) can affect the lag time periods. On the other hand, the release kinetics were found to be influenced significantly by excipient type and particle size. Results obtained from in vitro dissolution testing demonstrated that this device potentially could be used to deliver drugs orally for up to once-a-day dosing at controllable rates.

Effects of the host cavity size and the preparation method on the physicochemical properties of ibuproxam-cyclodextrin systems.

The effect of cyclodextrin (Cd) complexation on ibuproxam (IBUX) dissolution properties was studied by evaluating both the influence of Cd cavity size and the preparation method used for obtaining solid inclusion complexes. Binary systems of IBUX with natural Cds, prepared using different techniques (kneading, sealed-heating, spray-drying), were studied by differential scanning calorimetry (DSC), hot-stage microscopy (HSM), Fourier transform infrared (FTIR) spectroscopy, scanning electron microscopy (SEM), and their dissolution behavior was evaluated according to the dispersed amount method. The nature and the dissolution performance of the end product appeared to be related to both steric factors of host molecule and preparation method of the solid system. The alpha Cd cavity size was less suitable for accommodating the IBUX molecule, whereas spray-drying and sealed-heating methods led to a true inclusion complex of IBUX in the beta Cd and gamma Cd cavity. In contrast, the kneading method did not lead in any case to a real inclusion complex. Spray-dried systems with beta Cd and gamma Cd were the most effective in achieving the enhancement of the IBUX dissolution rate.

Nuclear magnetic resonance investigations of the inclusion complexation of gliclazide with beta-cyclodextrin.

The formation of the gliclazide-beta-cyclodextrin (GL-beta-CD) inclusion compound has been studied in the liquid state by phase solubility techniques and by 1H and 13C NMR spectroscopy. From the initial straight portion of the solubility curve (Bs type), the value of the apparent stability constant (Kc) was calculated as 1094 M(-1). The nuclear magnetic resonance studies confirm that GL yields a complex with beta-CD in aqueous medium, which is mainly due to the penetration of the azabicyclooctyl group of GL into the cavity of beta-CD. The study of the monodimensional nuclear Overhauser effect (NOE) of the H3 proton of CD has shown that the tolyl group also interacts with CD, but to a lesser extent than the azabicyclooctyl moiety. Finally, the application of the continous variation technique confirmed the 1:2 drug:CD stoichiometry of the complex.