Formulation, Development and Evaluation of Fixed Dose Combination of Antihyperlipidemic Agents

Abstract

The oral route of drug administration is the predominant and the most preferred route out of all the routes of drug administration. Amongst all the solid oral dosage forms, tablets are the widely used dosage forms. Hyperlipidemia is a condition in which there occur abnormally elevated levels of LDL-C. Literature claimed that single drug therapy of AHL 2 which is an HMG-CoA reductase inhibitor did not decrease the LDL levels. Also the side effects were observed. Therefore AHL 2 in a dose of 40 mg was used in combination with AHL 1 (Cholesterol absorption inhibitor) in a dose of 10 mg which could reduce the levels of LDLC by 12-15%, with minimum side effects. As both of these drugs were BCS-II, they were the suitable moieties for the preparation of IR tablets (10+40) mg once a day. The issue of emergence of impurities when two drugs were used together was solved by carrying out two separate granulations of both the parts. Systematic optimization of selected binder (HPMC 3 cps), disintegrant (Croscarmellose sodium), and all the process parameters was carried out by trial and error method. The dissolution profile of the optimized batch was found similar to that of innovator product, which was confirmed with help of similarity factor (>50). The QbD approach was proposed at the end of the investigation, in order to understand the flaws with that of trial and error method.