4.6 Article

Development of novel ibuprofen-loaded solid dispersion with enhanced bioavailability using cycloamylose

期刊

ARCHIVES OF PHARMACAL RESEARCH
卷 35, 期 4, 页码 683-689

出版社

PHARMACEUTICAL SOC KOREA
DOI: 10.1007/s12272-012-0412-4

关键词

Bioavailability; Cycloamylose; Ibuprofen; Solid dispersion

资金

  1. Rural Development Administration, Republic of Korea
  2. Ministry for Health, Welfare and Family Affairs, Republic of Korea [A092018]

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To develop a novel ibuprofen-loaded solid dispersion with enhanced bioavailability using cycloamylose, it was prepared using spray-drying techniques with cycloamylose at a weight ratio of 1:1. The effect of cycloamylose on aqueous solubility of ibuprofen was investigated. The physicochemical properties of solid dispersions were investigated using scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction. The dissolution and bioavailability in rats were evaluated compared with ibuprofen powder. This ibuprofen-loaded solid dispersion improved about 14-fold drug solubility. Ibuprofen was present in an unchanged crystalline state, and cycloamylose played the simple role of a solubilizing agent in this solid dispersion. Moreover, the dispersion gave 2-fold higher AUC (area under the drug concentration-time curve) value compared with a ibuprofen powder, indicating that it improved the oral bioavailability of ibuprofen in rats. Thus, the solid dispersion may be useful to deliver ibuprofen with enhanced bioavailability without crystalline change.

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