Abstract: Aim ：To study the effects of borneol-β-cyclodextrin inclusion complex on mice plasma and brain concentrations of tetramethylpyrazine phosphate. Methods ：Tetramethylpyrazine phosphate plasma and brain concentrations in mice after oral administration of tetramethylpyrazine phosphate with borneol-β-cyclodextrin inclusion complex at selected intervals were determined by GC-FID.The pharmacokinetic parameters were estimated by the program 3P97. Results ：Both tetramethylpyrazine phosphate plasma and brain concentration-time courses in mice were best fitted to open two-compartment model with first-order absorption.No changes to in vivo behavior of tetramethylpyrazine phosphate in the presence of borneol-β-cyclodextrin inclusion complex.Furthermore，borneol-β-cyclodextrin inclusion complex resulted in less enhancement in the oral absorption of tetramethylpyrazine phosphate and tetramethylpyrazine phosphate levels in brain tissue than did borneol alone. Conclusion ：Borneol material or other borneol dosages rather than β-cyclodextrin inclusion complex is more fitted to the Chinese medicines containing borneol.