Preparation and Optimization of Atorvastatin-Loaded Eudragit L100 Polymeric Microbeads by Ionotropic Gelation Method

Download PDF

Atorvastatin is used with a proper diet to lower cholesterol and triglyceride (fats) levels in the blood. It may be given orally. It is given as tablets of doses like 10-80 mg once daily for oral administration. It falls under the Class II category of Biopharmaceutical Classification System (BCS) i.e., having low solubility and high permeability. Problems regarding atorvastatin are that after administering in tablet formulation, high first-pass metabolism as well as the bioavailability of this drug varies due to instability in the acidic environment of stomach. Hence the patient becomes susceptible to a high chance of adverse effects of the drug which are nausea, vomiting and diarrhoea. To resolve such problems the drug should be incorporated in the microspheres for sustained release action using a suitable polymer. In the present research work atorvastatin drug was prepared into microspheres with sodium alginate, Eudragit L100 to be made as a controlled release formulations using calcium chloride and glutaraldehyde as cross-linking agents. Atorvastatin could be incorporated effectively into a combination of Eudragit and Sodium alginate microbeads by ionotropic gelation method. Several formulation variables were studied to establish the optimum condition for preparing almost spherical Eudrajit microspheres with high atorvastatin entrapment. The processing variables affected the properties of the microspheres in different ways. In most cases, the drug release from the microspheres was found to be controlled by Non Fickian diffusion mechanism. No incompatibility was found between drug and polymer as reported after evaluation study.