安徽医科大学国际教育学院教案与讲稿 Bioavailability evaluation methodl 3min (1)Pharmacokinetics method (2)Pharmacological effect method: To evaluate bioavailability by using some pharmacological index(such as body temperature, blood pressure,etc.),and the index are graded or quantitated. Generally,pharmacokinetics method is more sensitive than pharmacological effect method. [The test design of single dose of human bioavailability] 4min (1)To choose healthy adult volunteers (2)Double cross test design(two-way cross over) (3)Drug plan (4)The length of time of sampling:3 to 5 times of a half-life,if the half-life of drug is unknown, to sample the blood need to continue after 1/10~1/20 of the peak value of the drug concentration. (5)The frequency of taking blood samples:to sample 2 ~3 times in absorption phase and distribution,sampling 4~10 times in eliminate phase. (6)Washout period shall be the length of time that active drugs or metabolism product is eliminated for more than five times as much as half-life at least. [Many times for bioequivalence test] 4min (1)The absorption degree of two agents have no significant difference,but the absorption rate is rather different. (2)Single dose bioavailability have significant differences between individuals (3)The concentrations of active drug or metabolite in blood were too low after single dose medicine (4)The drug is controlled release formulation. (5)The drug has the nonlinear dynamic behavior. [Discussion and homeworks] 5 min 7安徽医科大学国际教育学院教案与讲稿 7 [Bioavailability evaluation method] 3min (1) Pharmacokinetics method (2) Pharmacological effect method: To evaluate bioavailability by using some pharmacological index (such as body temperature, blood pressure, etc.), and the index are graded or quantitated. Generally, pharmacokinetics method is more sensitive than pharmacological effect method. [The test design of single dose of human bioavailability] 4min (1) To choose healthy adult volunteers (2) Double cross test design (two-way cross over) (3) Drug plan (4) The length of time of sampling : 3 to 5 times of a half-life, if the half-life of drug is unknown, to sample the blood need to continue after 1/10 ~ 1/20 of the peak value of the drug concentration. (5) The frequency of taking blood samples: to sample 2 ~ 3 times in absorption phase and distribution, sampling 4 ~ 10 times in eliminate phase. (6) Washout period shall be the length of time that active drugs or metabolism product is eliminated for more than five times as much as half-life at least. [Many times for bioequivalence test] 4min (1)The absorption degree of two agents have no significant difference, but the absorption rate is rather different. (2) Single dose bioavailability have significant differences between individuals. (3) The concentrations of active drug or metabolite in blood were too low after single dose medicine. (4) The drug is controlled release formulation. (5) The drug has the nonlinear dynamic behavior. [Discussion and homeworks] 5 min