preparation and invitro characterization of cholestrol loweringdrug incorated captisol® inclusion complex

Abstract: in present study, a novel formulation was developed to enhance solubility, stability, and bioavailability ofatorvastatin. atorvastatin as an anti-cholesterol drug has poorr water solubility of 14% which reduces its therapeutic benefit [1] the ability of captisol®(sulphobutylether-b-cyclodextrin, sbe-b-cd), to from inclusion complexes, both in solution and in thesolidstate, haz been tested in order to improve some unfavorable chemical-physical characteristics [2] the aim of present study was to explore the impacy of atorvastatin (atr) sulfobutylether beta-cyclodextrin complex (atr-sbe-b-cd) on atr dissollotion rate and oral bioavailability. preliminary comparative phase solubility study indicated atr exhibited maximum solubility in sbe-β-cd solution.the job ʼs method performed to illustrate the atr was intended to from a 1:1 complex with captisol. solid state of complex was obtained through freeze drying and assessed by the formation of inclusion complex was charactenrized by fourier transform spectroscopy (ftir) , ultraviolet –visible (uv-vis) and nuclear magnetic resonance (nmr) spectrscopies [3].the phase solubility study conducted in distilled water was carried out to acquire the stability constant. the estimated apparent stability constant (k1:1) according to the higuchi and connors method. the results of this study confirm. the formation of inclusion complex in solution and suggest that the complexes formation between atr and sbe-β-cds could improve the bioavailability of the drug due to the enhancing absorption expected from increased drug solubility. furthermore, the antioxidant activity of atr and sbe-β-cds inclusion complexes were determined by the 1,1-diphenyl-2-picrylhydrazyl (dpph) method. the experimental results confirmed the forming of atr complexes with sbe-β-cds also these indicated that the atr/sbe-β-cds inclusion complexes were the most reactive than its free from into antioxidant activity [4].