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ENHANCED ORAL BIOAVAILABILITY OF OLMESARTAN BY USING NOVEL SOLID SELF EMULSIFYING DRUG DELIVERY SYSTEM

Olmesartan Medoxomil (OLM) is an angiotensin II receptor blocker antihypertensive agent. It is a highly lipophilic (log p (octanol/water) 5.55), poorly water soluble drug with absolute bioavailability of 26%. The objectives of the present investigation was to develop a self-microemulsifying drug delivery system (SMEDDS) to enhance the solubility and that may enhance the oral bioavailability of poorly water soluble OLM. The solubility of OLM was determined in various vehicles like oils, surfactants and co-surfactants. Pseudoternary phase diagrams were constructed to identify the efficient self-emulsifying region. Prepared SMEDDS was checked for phase separation, viscosity, droplet size, zeta potential and in vitro dissolution. The optimized SMEDDS formulation contained Tween 20 (45%), Propylene glycol (45%) and Capmul MCM 10 (10%), 20 mg of OLM showing drug release F1 (99.35%), droplet size (36.4 nm), polydispersity (0.186), viscosity (0. 8872 cP) and infinite dilution capability. In vitro drug release of the optimized liquid SMEDDS formulations was highly significant (p <0.05) as compared to marketed conventional tablet and pure drug solution. The optimized liquid SMEDDS was further used for the preparation of Solid SMEDDS (S-SMEDDS) formulations by using adsorption carriers. The optimized formulation of OLM loaded S-SMEDDS exhibited complete in vitro drug release in 60 min as compared pure drug solution The present result confirmed that the potential use of SMEDDS to improve dissolution and oral bioavailability of poorly water -soluble OLM

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