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서지반출
Solubilized Formulation of Olmesartan Medoxomil for Enhancing Oral Bioavailability
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  • Solubilized Formulation of Olmesartan Medoxomil for Enhancing Oral Bioavailability
  • Solubilized Formulation of Olmesartan Medoxomil for Enhancing Oral Bioavailability
저자명
Lee. Bong-Sang,Kang. Myung-Joo,Choi. Woo-Sik,Choi. Yoon-Bae,Kim. Hyung-Soo,Lee. Sang-Kil,Lee. Jae-Hwi,Choi. Young-Wook
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2009년|32권 11호|pp.1629-1635 (7 pages)
발행정보
대한약학회
파일정보
정기간행물|ENG|
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기타
이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

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 $T_{max}$ value of 0.2 hr. The $C_{max}$ 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.