Objective   To investigate the pharmacokinetics of remote controlled capsule for matrine in the proximal small intestine of healthy volunteers and obtain the standard pharmacokinetic parameters.    Methods   A total of 200 mg matrine was delivered in the proximal small intestine of 12 healthy male volunteers by remote controlled capsule system

which made by our work group. Blood sample of 3 ml for each time was harvested respectively in 0

0.5

1.0

1.5

2.0

4.0

6.0

8.0

12.0

16.0

24.0

30.0 and 36.0 h after the matrine was released when the capsule entered into the proximal small intestine. HPLCUV was used to measure matrine concentrations in the plasma by adding an internal standard (

sophocarpine). Methanol-water-ethylenediamine (70∶30∶0.02) was used as the mobile phase. The main parameters were calculated by 3p87 pharmacokinetic program.    Results   The martine pharmacokinetics conforms to a twocompartment open model after a single delivery of martine at a dose of 200 mg in upper small intestine of healthy volunteers. The main parameters were as follows: C

max

was 10.52 μg/ml

T

max

was 2.08 h

T

1/2α

was 0.90 h

T

1/2β

was 9.02 h

K

12

was 0.21 h

K

21

was 0.53 h

K

10

was 0.12 h

MRT

(0-t)

was 11.56 h and AUC

(0-t)

was 91.90 μg·h/ml.    Conclusion   There is an effective absorption when matrine is site-specific delivered in the proximal small intestine. The process in vivo fits well to two compartment open model.