Preparation of Natural Borneol/2-Hydroxypropyl-β-cyclodextrin Inclusion Complex and Its Effect on the Absorption of Tetramethylpyrazine Phosphate in Mouse
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概要
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Natural borneol (NB)/2-hydroxypropyl-β-cyclodextrin (HP-β-CD) inclusion complex has been prepared, and characterized by differential scanning calorimetry (DSC), X-ray diffractometry (XRD) and Fourier transform infrared spectroscopy (FT-IR). The phase solubility and release of NB, and its effect on the absorption of tetramethylpyrazine phosphate (TMPP) in mice were also measured. The results demonstrated that NB could be efficiently loaded into HP-β-CD to form an inclusion complex at a mass ratio of 1 : 6, and the inclusion complex had different physicochemical characteristics from free NB. The profile of phase solubility displayed a typical AL-type, indicating the formation of 1 : 1 stoichiometric inclusion complex. Additionally, the stability of the inclusion complex was greatly improved compared with that of NB. The results of absorption of TMPP in mouse indicated that NB/HP-β-CD enhanced the absorption of TMPP and the concentration of TMPP in brain tissue, especially in the early period. Both TMPP plasma and brain concentration–time courses in mice were fitted to open two-compartment model with first-order absorption after oral administration of TMPP with NB/HP-β-CD. However, the use of NB/HP-β-CD did not change the in vivo behavior of TMPP. Our results suggest the application potential of NB/HP-β-CD inclusion in pharmaceutics.
著者
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Shi Lei
College of Light Industry and Food Sciences, South China University of Technology
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Su Jianyu
College Of Food And Biological Engineering South China University Of Technology
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Zhang Hongmei
Department Of Clinical Oncology Xi Jing Hospital The Fourth Military Medical University
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Li Lin
College Of Light Industry And Food Sciences South China University Of Technology
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Li Bing
College Of Horticulture Northwest A&f University
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Chen Jianping
College of Light Industry and Food Sciences, South China University of Technology
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Ding Xiong
College of Light Industry and Food Sciences, South China University of Technology
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Zhang Hongmei
Department of Food and Biology Technology, Guangdong University of Technology
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ZHANG Hongmei
Department of Applied Chemistry, Fushun Petroleum Institute
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Li Bing
College of Light Industry and Food Sciences, South China University of Technology
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Su Jianyu
College of Light Industry and Food Sciences, South China University of Technology
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LI Lin
College of Biological Science and Technology, Beijing Forestry University
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