| Title | Physicochemical characteristics and oral bioavailability of andrographolide complexed with hydroxypropyl-beta-cyclodextrin. | | Author(s) | Ren K, Zhang Z, Li Y, Liu J, Zhao D, Zhao Y, Gong T | | Institution | Key Laboratory of Drug Targeting, West China School of Pharmacy, Sichuan University. Chengdu, PR China. | | Source | Pharmazie 2009 Aug; 64(8):515-20. | | Abstract | A significant increase in solubility of andrographolide (AND), a slightly water soluble anti-inflammatory and antimicrobial drug, was achieved by inclusion with hydroxypropyl-beta-cyclodextrin (HP-beta-CD). The inclusion complex was prepared by solvent evaporation and characterized by the phase solubility method, X-ray diffractometry and differential scanning calorimetry. The solubility of AND increased linearly as a function of HP-beta-CD concentration, resulting in A(L)-type phase solubility diagram. Molecular modeling calculations were used to foresee the possible orientations of AND inside the HP-beta-CD cavity. The in vitro dissolution profile showed a significant increase in dissolving rate and percent of the inclusion complex compared with uncomplexed drug. In vivo pharmacokinetic study showed that AUC(0-infinity) was 1.6-fold higher than that of AND suspension after oral administration. These results suggest that HP-beta-CD inclusion system might be a promising formulation for the oral delivery of AND. | | Language | eng | | Pub Type(s) | Journal Article
Research Support, Non-U.S. Gov't
| | PubMed ID | 19746840 |
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