م.م بسمة مظفر هادي
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Preparation and Characterization of Atorvastatin Calcium Trihydrate-cyclodextrin Inclusion Complex
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Atorvastatin calcium (ATR) is an antihyperlipidemic agent used for lowering blood cholesterol levels. However, it is very slightly soluble in water with poor oral bioavailability, which interferes with its therapeutic action. It is classified as a class II drug according to Biopharmaceutical Classification System (low solubility and high permeability). The present study aimed to enhance the solubility and dissolution rate of ATR by complexation technique using beta-cyclodextrin (β-CD) in comparison with other β-CD derivatives which are hydroxy propyl beta cyclodextrin (HP-β-CD), methyl beta cyclodextrin (M -β-CD) and sulfobutyl ether beta-cyclodextrin ( SBE-β-CD) as binary and ternary complex with Soluplus® using co–grinding, kneading, solvent evaporation and microwave methods. Differential scanning calorimetry (DSC), X-ray diffraction (XRD), Fourier-transform spectroscopy (FT-IR) characterized the resultant complex. The results showed that the ternary complex of ATR/SBE-β-CD/Soluplus )1-mole/ 1-mole/ 10% w/w) prepared by microwave method had the highest solubility, highest percentage yield, and faster release rate, which was greater than 90% (in the first 15–20 minutes). The FT-IR results showed that ATR was partially included in the SBE- β- CD cavity, while the DSC, XRD results confirmed the amorphous nature of the resultant complex.
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