Preparation of natural borneol/2-hydroxypropyl-β-cyclodextrin inclusion complex and its effect on the absorption of tetramethylpyrazine phosphate in mouse.

Jianyu Su, Jianping Chen, Lin Li, Bing Li, Lei Shi, Hongmei Zhang, Xiong Ding

Index: Chem. Pharm. Bull. 60(6) , 736-42, (2012)

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Abstract

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 A(L)-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.