OBJECTIVE: To measure the release profile of metronidazole from controlled release strip in different time phases in vivo and vitro. METHOD: Tritium labelled metronidazole (specific activity=5.44×104Bq·mmol-1, purification ≥95%) was prepared for metronidazole controlled release strip [weight (19.0±0.1)mg, containing metronidazole (5.59±0.03)mg] according to original art. The release was measured by inserting into the periodontal site of guinea pig and 100 μl normal saline in microplate. RESULTS: The results turned out that it can decrease the superhigh peak and delay the previous peak. It can constantly release effective level about 200 μg·ml-1 metronidazole in gingival crevicular fluid within 48 h. CONCLUSION:3H labelled metronidazole could release β redial which could be traced the amount and location of the drug in vivo from time to time. This is a good method for development and application in pharmacokinetics and drug tracer.