In Situ Intestinal Absorption Behaviors of Tanshinone IIA from Its Inclusion Complex with Hydroxypropyl-.BETA.-cyclodextrin

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  • Ling Wang
    Institution of Clinical Pharmacological, West China Second University Hospital, Sichuan University West China School of Pharmacy, Sichuan University
  • Rui Li Chen
    West China School of Pharmacy, Sichuan University
  • Hua Jiang Xue
    West China School of Pharmacy, Sichuan University

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  • In situ intestinal absorption behaviors of tanshinone 2A from its inclusion complex with hydroxypropyl-β-cyclodextrin
  • In situ intestinal absorption behaviors of tanshinone 2A from its inclusion complex with hydroxypropyl v cyclodextrin

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Abstract

In this paper, the intestinal permeability of the inclusion complex of tanshinone IIA (TS IIA) with 2-hydroxypropyl-β-cyclodextrin (HP-β-CD) was investigated. The corresponding complexation of TS IIA–HP-β-CD was obtained by coevaporation and characterized by differential scanning calorimetry and X-ray diffraction. The recirculation intestinal perfusion technique in rats was used to study the absorption behavior of free and complexed TS IIA. The change of concentration of TS IIA was separately calculated according to Michaelis–Menten and the Fick's equation to investigate its absorption rate-limiting step. Using the mathematical models above, it was concluded that the limit step to absorption of TS IIA was the dissolution process. Different concentrations of complexed TS IIA were administrated to three intestinal segments, with the intestinal permeability ranging from 3.16×10−5 cm·s−1 in the duodenum (50 μg·ml−1) to 4.11×10−5 cm·s−1 in the jejunum (100 μg·ml−1). With the increase of dosage of complex, TS IIA's absorption did not show saturated phenomenon, suggesting its transport mechanism in vivo might primary be passive transport. Besides, the permeability of TS IIA was not apparently influenced by the perfusion section studied, which indicated that there might not exist specific absorption site for TS IIA.

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