Solubility and Dissolution Enhancement of Atorvastatin Calcium using Solid Dispersion Adsorbate Technique

[摘要] Atorvastatin (ATR) is a poorly soluble anti-hyperlipidemic drug. The drug belongs to the class II group according to the biopharmaceutical classification system (BCS) with low bioavailability due to its low solubility. Solid dispersions adsorbate is an effective technique for enhancing the solubility and dissolution of poorly soluble drugs. The present study aims to enhance the solubility and dissolution rate of ATR using solid dispersion adsorbate technique in comparison with ordinary solid dispersion. polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000), Poloxamer188 and Poloxamer 407were used as hydrophilic carriers besides Aerosil 200, Aerosil 300 and magnesium aluminium silicate (MAS) as adsorbents. All solid dispersion adsorbate (SDA) formulas were prepared in ratios of 1:1:1 (drug: carrier: adsorbent) and evaluated for their water solubility, percentage yield, drug content, , dissolution, crystal lattice using X-ray powder diffraction (XRD) and Differential Scanning Calorimetry (DSC) studies and Fourier Transform Infrared Spectroscopy (FTIR) for determination the drug-carrier- adsorbate interaction. The prepared (SDA) showed improvement of drug solubility in all prepared formula. The best result was obtained with formula SDA12 (ATR: Poloxamer407: MAS 1:1:1) that showed 8.07 and 5.38 fold increase in solubility compared to solubility of pure ATR and solid dispersion(SD4) (Atorvastatin: Poloxamer 407 1:1) respectively due to increased wettability and reduced crystallinity of the drug which leads to improving drug solubility and dissolution.

[学科分类] 计算机网络和通讯

[关键词] Atorvastatin;Solid dispersions adsorbate;PEG4000 and 6000;Aerosil 300;Magnesium aluminium silicate