DESIGN, DEVELOPMENT & EVALUATION OF SELF EMULSIFYING DRUG DELIVERY SYSTEM OF AMLODIPINE

Jograna M.B.*, Bhosale A.V. and Kakade S.S.

ABSTRACT

Amlodipine (3-ethyl-5-methyl-2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-1, 4-dihydro-6-methyl-3,5-pyridinedicarboxylate) is used to treat high blood pressure and chest pain (angina). Amlodipine is given orally (5mg or 10mg daily) with peak plasma concentration occurring after 6-12 hrs, and has oral bioavailability of 60-65% only due to extensive hepatic metabolism. Amlodipine belonging to the 1, 4-dihydropyridine class are photosensitive since light catalyzes their oxidation to pyridine derivatives, lacking any therapeutic effect. From a pharmaceutical point of view, dry emulsions are attractive because they are physically and microbiologically stable formulations, which are easy to administer in the form of powders as capsules and tablets. Hence a novel a solid form of lipid-based self- emulsifying drug delivery system (SEDDS) is formulated by spray drying liquid SEDDS with an inert solid carrier to improve the photostability and oral bioavailability of poorly water-soluble drug amlodipine. Solid self-emulsifying drug delivery systems of amlodipine were prepared by using different oils, surfactants and co-surfactants and evaluated for its in vitro performance. Optimized, Solid amlodipine SEDD composed of amlodipine (5 mg), Labrafil M1944 CS (30%), Smix (70%) and Maltodextrin (10 gm). The globule size distribution of this formulation was within appropriate range (0.600–0.900 μm). In vitro release in 0.1 N HCl revealed a prompt release within 5 minute up to 90%. SEDDS of amlodipine showed a significant increase in photostability and oral bioavaibility of amlodipine.

Keywords: Amlodipine, Solid self-emulsifying drug delivery system (SEDDS), Bioavailability, Photostability.