carriers

Solubility is the phenomenon of dissolution of solid in liquid phase to give a homogenous system. Solubility is one of the important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown. Poorly water soluble drugs often require high doses in order to reach therapeutic plasma concentrations after oral administration. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities. Any drug to be absorbed must be present in the form of an aqueous solution at the site of absorption. The ability to increase aqueous solubility can thus be a valuable aid to increasing efficiency and/or reducing side effects for certain drugs. This is true for parenterally, topically and orally administered solutions. The solubility of drugs is defined according to (bio-pharmaceutical classification system) BCS classification system which divides drugs to different class according to its solubility. Solid dispersion is defined as dispersion of one or more active ingredients in an inert carrier or matrix known as solid dispersion. Solid dispersion reduces the particle size and changes the micro environment of the drug particle, increases the rate of dissolution and absorption and thus changes the biopharmaceutical properties of poorly water soluble drugs. The solid dispersion method, by which a drug is dispersed in a carrier to make it amorphous, is one of the pharmaceutical approaches most commonly employed to enhance bioavailability of poorly water soluble drugs. Various pharmaceutical approaches for the preparation of SDs, including co-precipitation, lyophilization, spray drying, solvent evaporation, fusion and powder mixing methods, have been reported. It’s a new and efficient technique to improve the solubility of poorly soluble drugs.

  The objective of present study is to improve the dissolution rate of Acyclovir a poorly water soluble drug by solid dispersion technique using a water soluble carrier, PEG-6000, urea, mannitol. The solid dispersions are prepared by physical method, co-grinding method and solvent evaporation method. The prepared solid dispersions showed an enhancement in dissolution rate and solubility compared to plain drug. In vitro release profiles of all SDs were comparatively evaluated and also studied against pure acyclovir. Faster dissolution was exhibited by solid dispersion containing 1:4 ratio of drug: PEG-6000. The increase in dissolution rate of the drug may be due to increase in wettability, hydrophilic nature of the carrier and due to reduction in drug crystallinity. The prepared solid dispersion was subjected for % practical yield, drug content, infrared (IR) spectroscopic, differential scanning calorimetry (DSC). FT‐IR spectra revealed no chemical incompatibility between drug and PEG-6000.Drug– polymer interaction was investigated using differential scanning calorimetry (DSC) studies. Key words: Solid dispersions, carriers, solubility enhancement, poorly soluble drugs, bioavailability