Preparation Of Tablets Containing Sustained-release Lovastatin Pellets

Objective:The solid dispersion of Lovastatin was prepared for elevate the speed of dissolution and water-solubility. To enhance the bioavailability of lovastatin , the extrusion and spheronization technology was used to study the pellets containing the solid dispersion of Lovastatin. Then the sustained-release pellets of lovastatin were prepared by the fluidized bed coating technology for reduce times of medication,gain stable plasma-drug concentration,reduce side effects, elevate complaisance and safety. Finally, to resolve the indivisibility of sustained-release tablet the tablet containing sustained-release Lovastatin Pellets were made. And the release characteristics and the micromentics were investigated.Method:1,To establish a method for determination of the content and release of Lovastatin tablets containing sustained-release pellets.2,To study the physico-chemical property of Lovastatin including solubility and oil-water partition coefficientthe .3,To prepare the solid dispersion of Lovastatin for elevate the speed of dissolution.4,To prepare pellets containing Lovastatin with extrusion and spheronization technology.5,The sustained-release pellets were prepared in the fluid bed with Eudragit NE 30D.6,To prepare tablets containing sustained-release Lovastatin Pellets with sustained- release pellets and cushioning pellets mixture. Results:1,Adjuvant will interfere the determination of Lovastatin with ultraviolet spectrophotometry but not high efficiency liquid chromatography.2,It was acquired from preformulation study that Lovastatin is water-insoluble but slightly soluble in methanol, ethanol, 0.1mol/L HCl and pH6.8 phosphate buffer,and SDS can enhance the water-solubility of Lovastatin.3,It was revealed from differential scanning calorimeter, that Lovastatin was amorphism, and Lovastatin solid dispersion was prepare successfully.4,Pellets containing Lovastatin were prepared by extrusion and sphironization technology with optimized parameter. The drug release profile of the pellets coating with Eudragit NE 30D was 12 hour sustained–release.5,The curve of cumulative drug release was accord with the Higuchi equation,and the drug release profile did not change after sheeting.Conclusion:1,The HPLC for determination of drug release and content was simple and reliable.2,The dissolution speed of Lovastatin was enhanced greatly by Solid dispersion, which provihes basis for.3,The drug release from sustained-release could last 12h, which was reproducible.4,The drug release profile did not change after sheeting, which revealed that mixed with cushioning pellets can protect sustained-release pellets.