Green Tea (Camellia sinensis) 19124972
Phase I pharmacokinetic study of tea polyphenols following single-dose administration of epigallocatechin gallate and polyphenon E. CSV JSON

Phase I pharmacokinetic study of tea polyphenols following single-dose administration of epigallocatechin gallate and polyphenon E. There are a total of 8 experiments, 1 each for EGCG capsules at 4 dose levels, and 1 each for Polyphenon E capsules at 4 dose levels.

The PK results for the EGCG compound is recorded for the four experiments that used EGCG capsules but not the 4 experiments using Polyphenon E capsules because the there were not significant differences at any of the dose levels. This is true for both unconjugated and total EGCG.

The EGC and EC results were only available for the 4 Polyphenon E experiments and these are recorded.

PMID:11205489

11205489

1 . In vivo PK of tea polyphenols 800 mg Polyphenon E capsules (id=NPDI-IkNjmw)

In Vivo Pharmacokinetics Study

Results

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Randomized crossover
Multiple dosing

Population

Healthy volunteers

20

5 subjects per dose level, biased toward females at every dose level

Pharmacokinetic (PK) Sampling Information

0.5, 1, 2, 4, 6, 8, and 24 h after drug administration

Drug or Natural Product Administration

Natural Product Administration

Oral

capsule

800

Fed

All study participants were required to refrain from the ingestion of tea or tea products for 7 days before the dose administration. The day before the pharmacokinetic study, study partici- pants were instructed to fast after midnight except for drinking water. On the pharmacokinetic study day, study subjects skipped breakfast and took no over the counter medications, vitamins, or health food products. Study participants came to the clinic in the early morning (6 – 8 a.m.) and were provided with one to two bagels for breakfast.

single dose

1 day

Natural Product Characteristics

Food Research Laboratories, Mitsui Norin Co., Ltd., (Fujieda City, Japan) and Chemoprevention Agent Development Re- search Group, National Cancer Institute

2000

This experiment used capsules containing 200 mg of EGCG, 37 mg of EGC, and 31 mg of EC in the Polyphenon E formulation.

Source year is an assumption based on publication date

Pharmacodynamics (PD) & Adverse Events

General disorders and administration site conditions 35800000

Mild headache and fatigue

2 . In vivo PK of tea polyphenols 600 mg Polyphenon E capsules (id=NPDI-MopEIQ)

In Vivo Pharmacokinetics Study

Results

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Randomized crossover
Multiple dosing

Population

Healthy volunteers

20

5 subjects per dose level, biased toward females at every dose level

Pharmacokinetic (PK) Sampling Information

0.5, 1, 2, 4, 6, 8, and 24 h after drug administration

Drug or Natural Product Administration

Natural Product Administration

Oral

capsule

600

Fed

All study participants were required to refrain from the ingestion of tea or tea products for 7 days before the dose administration. The day before the pharmacokinetic study, study partici- pants were instructed to fast after midnight except for drinking water. On the pharmacokinetic study day, study subjects skipped breakfast and took no over the counter medications, vitamins, or health food products. Study participants came to the clinic in the early morning (6 – 8 a.m.) and were provided with one to two bagels for breakfast.

single dose

1 day

Natural Product Characteristics

Food Research Laboratories, Mitsui Norin Co., Ltd., (Fujieda City, Japan) and Chemoprevention Agent Development Re- search Group, National Cancer Institute

2000

This experiment used capsules containing 200 mg of EGCG, 37 mg of EGC, and 31 mg of EC in the Polyphenon E formulation.

Source year is an assumption based on publication date

Pharmacodynamics (PD) & Adverse Events

General disorders and administration site conditions 35800000

Mild headache and fatigue

3 . In vivo PK of tea polyphenols 400 mg Polyphenon E capsules (id=NPDI-_7AWMw)

In Vivo Pharmacokinetics Study

Results

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Randomized crossover
Multiple dosing

Population

Healthy volunteers

20

5 subjects per dose level, biased toward females at every dose level

Pharmacokinetic (PK) Sampling Information

0.5, 1, 2, 4, 6, 8, and 24 h after drug administration

Drug or Natural Product Administration

Natural Product Administration

Oral

capsule

400

Fed

All study participants were required to refrain from the ingestion of tea or tea products for 7 days before the dose administration. The day before the pharmacokinetic study, study partici- pants were instructed to fast after midnight except for drinking water. On the pharmacokinetic study day, study subjects skipped breakfast and took no over the counter medications, vitamins, or health food products. Study participants came to the clinic in the early morning (6 – 8 a.m.) and were provided with one to two bagels for breakfast.

single dose

1 day

Natural Product Characteristics

Food Research Laboratories, Mitsui Norin Co., Ltd., (Fujieda City, Japan) and Chemoprevention Agent Development Re- search Group, National Cancer Institute

2000

This experiment used capsules containing 200 mg of EGCG, 37 mg of EGC, and 31 mg of EC in the Polyphenon E formulation.

Source year is an assumption based on publication date

Pharmacodynamics (PD) & Adverse Events

General disorders and administration site conditions 35800000

Mild headache and fatigue

4 . In vivo PK of tea polyphenols 800 mg EGCG capsules (id=NPDI-iisBhQ)

In Vivo Pharmacokinetics Study

Results

The authors report a CL/F value but they don't have or mention administration of any IV formulation to use for calculating oral bioavailability (assuming F = (AUC_{po}XDose_{iv})/(AUC_{iv}XDose_{po}). So, I think that the they are really just reporting Cl from Dose/AUC. A similar comment applies to volume of distribution. These two values have not been entered into the repository.

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Randomized crossover
Multiple dosing

Population

Healthy volunteers

20

5 subjects per dose level, biased toward females at every dose level

Pharmacokinetic (PK) Sampling Information

0.5, 1, 2, 4, 6, 8, and 24 h after drug administration

Drug or Natural Product Administration

Natural Product Administration

Oral

capsule

800

Fed

All study participants were required to refrain from the ingestion of tea or tea products for 7 days before the dose administration. The day before the pharmacokinetic study, study partici- pants were instructed to fast after midnight except for drinking water. On the pharmacokinetic study day, study subjects skipped breakfast and took no over the counter medications, vitamins, or health food products. Study participants came to the clinic in the early morning (6 – 8 a.m.) and were provided with one to two bagels for breakfast.

single dose

1 day

Natural Product Characteristics

Food Research Laboratories, Mitsui Norin Co., Ltd., (Fujieda City, Japan)

2000

This experiment used capsules containing only 200 mg of EGCG.

Source year is an assumption based on publication date

Pharmacodynamics (PD) & Adverse Events

General disorders and administration site conditions 35800000

Mild headache and fatigue

5 . In vivo PK of tea polyphenols 600 mg EGCG capsules (id=NPDI-aYDjxA)

In Vivo Pharmacokinetics Study

Results

The authors report a CL/F value but they don't have or mention administration of any IV formulation to use for calculating oral bioavailability (assuming F = (AUC_{po}XDose_{iv})/(AUC_{iv}XDose_{po}). So, I think that the they are really just reporting Cl from Dose/AUC. A similar comment applies to volume of distribution. These two values have not been entered into the repository.

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Randomized crossover
Multiple dosing

Population

Healthy volunteers

20

5 subjects per dose level, biased toward females at every dose level

Pharmacokinetic (PK) Sampling Information

0.5, 1, 2, 4, 6, 8, and 24 h after drug administration

Drug or Natural Product Administration

Natural Product Administration

Oral

capsule

600

Fed

All study participants were required to refrain from the ingestion of tea or tea products for 7 days before the dose administration. The day before the pharmacokinetic study, study partici- pants were instructed to fast after midnight except for drinking water. On the pharmacokinetic study day, study subjects skipped breakfast and took no over the counter medications, vitamins, or health food products. Study participants came to the clinic in the early morning (6 – 8 a.m.) and were provided with one to two bagels for breakfast.

single dose

1 day

Natural Product Characteristics

Food Research Laboratories, Mitsui Norin Co., Ltd., (Fujieda City, Japan)

2000

This experiment used capsules containing only 200 mg of EGCG.

Source year is an assumption based on publication date

Pharmacodynamics (PD) & Adverse Events

General disorders and administration site conditions 35800000

Mild headache and fatigue

6 . In vivo PK of tea polyphenols 400 mg EGCG capsules (id=NPDI-UhMAjQ)

In Vivo Pharmacokinetics Study

Results

The authors report a CL/F value but they don't have or mention administration of any IV formulation to use for calculating oral bioavailability (assuming F = (AUC_{po}XDose_{iv})/(AUC_{iv}XDose_{po}). So, I think that the they are really just reporting Cl from Dose/AUC. A similar comment applies to volume of distribution. These two values have not been entered into the repository.

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Randomized crossover
Multiple dosing

Population

Healthy volunteers

20

5 subjects per dose level, biased toward females at every dose level

Pharmacokinetic (PK) Sampling Information

0.5, 1, 2, 4, 6, 8, and 24 h after drug administration

Drug or Natural Product Administration

Natural Product Administration

Oral

capsule

400

Fed

All study participants were required to refrain from the ingestion of tea or tea products for 7 days before the dose administration. The day before the pharmacokinetic study, study partici- pants were instructed to fast after midnight except for drinking water. On the pharmacokinetic study day, study subjects skipped breakfast and took no over the counter medications, vitamins, or health food products. Study participants came to the clinic in the early morning (6 – 8 a.m.) and were provided with one to two bagels for breakfast.

single dose

1 day

Natural Product Characteristics

Food Research Laboratories, Mitsui Norin Co., Ltd., (Fujieda City, Japan)

2000

This experiment used capsules containing only 200 mg of EGCG.

Source year is an assumption based on publication date

Pharmacodynamics (PD) & Adverse Events

General disorders and administration site conditions 35800000

Mild headache and fatigue

7 . In vivo PK of tea polyphenols 200 mg Polyphenon E capsules (id=NPDI-EVjSRA)

In Vivo Pharmacokinetics Study

Results

All of these results are the sum of unchanged and conjugated forms reported in Table 3

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Randomized crossover
Multiple dosing

Population

Healthy volunteers

20

5 subjects per dose level, biased toward females at every dose level

Pharmacokinetic (PK) Sampling Information

0.5, 1, 2, 4, 6, 8, and 24 h after drug administration

Drug or Natural Product Administration

Natural Product Administration

Oral

capsule

200

Fed

All study participants were required to refrain from the ingestion of tea or tea products for 7 days before the dose administration. The day before the pharmacokinetic study, study partici- pants were instructed to fast after midnight except for drinking water. On the pharmacokinetic study day, study subjects skipped breakfast and took no over the counter medications, vitamins, or health food products. Study participants came to the clinic in the early morning (6 – 8 a.m.) and were provided with one to two bagels for breakfast.

single dose

1 day

Natural Product Characteristics

Food Research Laboratories, Mitsui Norin Co., Ltd., (Fujieda City, Japan) and Chemoprevention Agent Development Re- search Group, National Cancer Institute

2000

This experiment used capsules containing 200 mg of EGCG, 37 mg of EGC, and 31 mg of EC in the Polyphenon E formulation.

Source year is an assumption based on publication date

Pharmacodynamics (PD) & Adverse Events

General disorders and administration site conditions 35800000

Mild headache and fatigue

8 . In vivo PK of tea polyphenols 200 mg EGCG capsules (id=NPDI-fXRM8w)

In Vivo Pharmacokinetics Study

Results

The authors report a CL/F value but they don't have or mention administration of any IV formulation to use for calculating oral bioavailability (assuming F = (AUC_{po}XDose_{iv})/(AUC_{iv}XDose_{po}). So, I think that the they are really just reporting Cl from Dose/AUC. A similar comment applies to volume of distribution. These two values have not been entered into the repository.

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Randomized crossover
Multiple dosing

Population

Healthy volunteers

5

Pharmacokinetic (PK) Sampling Information

Blood samples were collected before administration of the medication administration and 0.5, 1, 2, 4, 6, 8, and 24 h after drug administration. Study subjects self-collected urine before dosing and at three intervals during the 24 h period after dosing (0-4, 4-8, and 8-24 h)

Drug or Natural Product Administration

Natural Product Administration

Oral

capsule

200 mg

Fed

All study participants were required to refrain from the ingestion of tea or tea products for 7 days before the dose administration. The day before the pharmacokinetic study, study partici- pants were instructed to fast after midnight except for drinking water. On the pharmacokinetic study day, study subjects skipped breakfast and took no over the counter medications, vitamins, or health food products. Study participants came to the clinic in the early morning (6 – 8 a.m.) and were provided with one to two bagels for breakfast.

single dose

Natural Product Characteristics

Food Research Laboratories, Mitsui Norin Co., Ltd., (Fujieda City, Japan)

Each EGCG capsule contained 200 mg EGCG

not available

Pharmacodynamics (PD) & Adverse Events

General disorders and administration site conditions 35800000

Mild headache and fatigue