Increasing Bioavailability of Simvastatin Using New Drug Formulation

Simvastatin (SMV) is a cholesterol lowering drug. It is currently given independently to patients with hypercholesterolemia or in combination with other drugs when hyperlipidemia is a comorbidity. The drug itself is considered a BCS Class II drug because of its high permeability but low solubility properties. Currently, it is created as a prodrug, which means it needs to be converted by liver enzymes to work. This results in a high hepatic extraction with low bioavailability. Because of its low solubility and low bioavailability after high hepatic extraction, the amount of simvastatin being processed into tablets is not enough to effectively treat hypercholesterolemia. Therefore, a Simvastatin granule (SMV combined with other substances) was created to increase the solubility of the drug, which would increase its bioavailability in the body without causing adverse effects that are dose related. To test bioavailability is increased in the granule formulation, a UV spectrophotometer and two-step dissolution method were used to compare the granule to the Simvastatin powder by itself. The two-step dissolution method allows one to compare the concentration of the granule to that of the powder after certain time intervals, and the UV spectrophotometer was used to determine these concentrations throughout this study. From the two-step dissolution study conducted, it was shown that the granule consistently had higher bioavailability compared to the powder counterpart at the same time interval. Therefore, this indicates that the granule formulation has potential to increase Simvastatin’s solubility and bioavailability, which can change the way the drug is packaged into tablets and given as a medication in the future.