[Optimization of preparation procedures of tanshinone-ⅡA /β-cyclodextrin inclusion complex and dissolution study of tanshinone-ⅡA in vitro]

Zhongguo Zhong Yao Za Zhi. 2017 Dec;42(23):4611-4617. doi: 10.19540/j.cnki.cjcmm.20171023.005.
[Article in Chinese]

Abstract

In this paper, tanshinone-ⅡA (Tan-IIA)/β-cyclodextrin (β-CD) inclusion complexes were prepared by saturated aqueous solution method. Based on the single factor experiment, Box-Benhnken design and response surface method were utilized to optimize the preparation procedures of tanshinone-ⅡA/β-cyclodextrin inclusion complexes. The ratio of β-CD to Tan-ⅡA, experimental temperature and time were defined as independent variables, while the yield of the inclusion complexes, encapsulation efficiency and the generalized "normalized value" were set as the response value. In addition, the inclusion complexes were characterized by infrared spectroscopy (IR) and nuclear magnetic resonance (NMR). The results showed that optimum preparation conditions for Tan-ⅡA/β-CD inclusion complex were as follows: Tan-ⅡA/β-CD ratio of 1:7, the temperature of 48 ℃ and the time of 3 h. Under the optimized conditions, the encapsulation efficiency of Tan-ⅡA/β-CD inclusion complex was 84.75%. The Tan-IIA and β-CD inclusion complex can significantly improve the dissolution of Tan-ⅡA.

Keywords: Tan-ⅡA; box-benhnkendesign and response surface method; dissolution in vitro; inclusion process; β-CD.

MeSH terms

  • Abietanes / chemistry*
  • Nuclear Magnetic Resonance, Biomolecular
  • Solubility
  • Spectrum Analysis
  • beta-Cyclodextrins / chemistry*

Substances

  • Abietanes
  • beta-Cyclodextrins
  • tanshinone