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Improved pH-Independent Dissolution and Oral Absorption of Valsartan via the Preparation of Solid Dispersion
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  • Improved pH-Independent Dissolution and Oral Absorption of Valsartan via the Preparation of Solid Dispersion
  • Improved pH-Independent Dissolution and Oral Absorption of Valsartan via the Preparation of Solid Dispersion
저자명
Park. Young-Joon,Lee. Hyoung-Kyu,Im. Young-Bin,Lee. Won-Jae,Han. Hyo-Kyung
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2010년|33권 8호|pp.1235-1240 (6 pages)
발행정보
대한약학회
파일정보
정기간행물|ENG|
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기타
이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

This study aimed to improve the pH-independent solubility and dissolution characteristics of valsartan via the preparation of solid dispersions (SD) with poloxamer 407. SDs was prepared by using the solvent method at various drug-polymer ratios and their dissolution characteristics were examined at different pHs. Oral pharmacokinetics of SDs was also evaluated in rats. Compared to the untreated powder, SDs significantly improved the dissolution rate as well as the extent of drug release at low pH. Particularly, SD having the drug-polymer ratio of 1:5 exhibited pH-independent dissolution of valsartan, resulting in the rapid and complete drug release over the pH range of 1.2 to 6.8. The improved dissolution of valsartan via SD formulation appeared to be well correlated with the enhanced oral exposure of valsartan in rats. SDs increased $C_{max}$ and $AUC_{0-24}$ of valsartan by 2-7 folds in rats, implying that SDs should be effective to improve the bioavailability of valsartan. In conclusion, SDs containing poloxamer 407 appeared to be effective to improve the pH-independent dissolution and oral absorption of valsartan.