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KMID : 0043320090320111629
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Archives of Pharmacal Research
2009 Volume.32 No. 11 p.1629 ~ p.1635
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Solubilized Formulation of Olmesartan Medoxomil for Enhancing Oral Bioavailability
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Choi Young-Wook
Choi Woo-Sik
Choi Yoon-Bae
Kim Hyung-Soo
Lee Sang-Kil
Lee Jae-Hwi
Lee Bong-Sang
Kang Myung-Joo
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Abstract
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Olmesartan medoxomil (OLM) is an antihypertensive angiotensin II receptor blocker. OLM has a low bioavailability (BA), approximately 26% in humans, due to its low water solubility and efflux by drug resistance pumps in the gastrointestinal tract. Self-microemulsifying drug delivery system (SMEDDS), which is easily emulsified in aqueous media under gentle agitation and digestive motility, was formulated to increase the oral BA of OLM. Among the surfactants and oils studied, Capryol 90, Tween 20, and Tetraglycol were chosen and combined at a volume ratio of 1:6:3 on the basis of equilibrium solubility and phase diagram experiments. The mean droplet size of SMEDDS was 15 nm. In an oral absorption study in rats, SMEDDS formulation brought faster absorption compared to suspension, showing a Tmax value of 0.2 hr. The Cmax and AUC values of SMEDDS formulation were significantly higher than those of suspension, revealing a relative BA of about 170%. Our study demonstrated the potential usefulness of SMEDDS for the oral delivery of poorly absorbable compounds, including OLM.
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KEYWORD
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Olmesartan medoxomil, SMEDDS, Solubilization, Bioavailability, Oral delivery
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