The main purpose of this study was to illustrate the effect of synthetical borneol (SB) on the plasma and brain concentration profile of tetramethylpyrazine phosphate (TMPP) in mice after oral administration of TMPP without or with different amounts of SB. The concentrations of TMPP on the plasma and brain in mice were determined by GC-FID. The pharmacokinetic parameters were computed by software program 3p97. Our data showed that after oral administration of 15, 30, 90 mg kg(-1) of SB, oral bioavailability of TMPP in plasma was 1.52, 2.21, 2.95 times increase, respectively, than that without SB, and 1.12, 1.62, 1.93 times increase, respectively, in brain tissue. The pharmacokinetic data were simulated by non-linear least squares. The results showed that both open two-compartment model and one-order absorption were fitted to TMPP plasma and brain concentration-time course in vivo in mice. The MRT of TMPP showed same results under the conditions without or with SB. SB did enhance the oral absorption of TMPP and the concentration of TMPP in brain tissue, especially in the early period. But the use of SB did not change the behavior in vivo of TMPP.