Abstract

COMPATIBILITY STUDIES WITH PHARMACEUTICAL EXCIPIENTS OF SIMVASTATIN FOR THE DEVELOPMENT OF NOVEL DRUG DELIVERY SYSTEMS

Mahmoud Mahyoob Alburyhi*, Abdalwali Ahmed Saif, Maged Alwan Noman and Shada Hassan Yassin

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Abstract

Simvastatin is a lipid lowering drug which is used to lower the risk of cardiovascular disease and manage abnormal lipid levels by inhibiting the endogenous production of cholesterol. Simvastatin is practically insoluble in water and undergoes extensive first-pass metabolism in the liver, thus the oral bioavailability is very low (5%). The main objective of this research is to develop Orodispersible tablets of Simvastatin to overcome the two mentioned problems. The main objective of the present study was to the preformulation studies were performed to know the physico-chemical and mechanical properties of Simvastatin for formulation development of Simvastatin ODTs. The safety, efficacy, quality and stability of a formulation are major concepts of any API development process. In API development process, a detailed characterization of the API and other formulation components is usually carried out during the preformulation stage. The drug-excipient compatibility studies were conducted to characterize the drug Simvastatin present in Orodispersible Tablets Delivery System ODTDS. Preformulation, formulation and evaluation of Simvastatin to avoid problems associated with conventional delivery system such as limited permeation, low dissolution and bioavailability and also to improve bioavailability and for the treatment of hyperlipidemia. In the present study that the compatibility was assessed by, FTIR spectroscopy, and melting point apparatus, precompression parameters and powder flow properties. Results showed that physical mixtures of Simvastatin and various excipients as mannitol, microcrystalline cellulose as diluents, and sodium starch glycolate, croscarmellose sodium, and crospovidone as superdisintegrants and sodium lauryl sulfate as wetting agent were evaluated for preformulation studies parameters. It was concluded that the drug Simvastatin was found to be compatible with various excipients which were selected for the formulation development of the Simvastatin ODTs. Formulation scientist from his experience and knowledge have to significantly in the preformulation study stage and is an important factor in the ADDS (Advanced Drug Delivery Systems) product development process.

Keywords: Simvastatin, Compatibility, Excipients, Development, Preformulation, Formulation.