Goldenseal (Hydrastis canadensis) 43525850
A clinical study of transporter-mediated goldenseal drug interactions CSV JSON

Effects of the goldenseal product on the efflux transporter breast cancer resistance protein (BCRP) and uptake transporters organic anion transporting polypeptide (OATP) 1B1/3, as well as organic anion transporters (OATs), organic cation transporters (OCTs), multidrug and toxin extrusion proteins (MATEs), and CYP3A, were next evaluated in 16 healthy volunteers using a cocktail approach.

1 . clinical goldenseal - midazolam experiment (id=NPDI-DboNmw)

In Vivo Interaction Study

Increased systemic exposure was detected.

midazolam 708298

  • CYP3A4 4306811

Results

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Probe cocktail study
Fixed-sequence

Population

Healthy volunteers

16

8 male and 8 female (non-lactating women )

Pharmacokinetic (PK) Sampling Information

24, 48, 72, and 96 hours after cocktail administration

Drug or Natural Product Administration

Object Administration — midazolam

Oral

Furosemide (10 mg/mL solution; West-ward Pharmaceuticals Corp., Eatontown, NJ), metformin (500 mg/5 mL solution; Ranbaxy Pharmaceuticals, Inc., Jacksonville, FL), rosuvastatin (10 mg tablet; Camber Pharmaceuticals Inc., Piscataway, NJ), and midazolam (2 mg/mL syrup; West-ward Pharmaceuticals Corp.)

1 mg furosemide, 50 mg metformin, 10 mg rosuvastatin, and 2.5 mg midazolam

single dose

once

Precipitant Administration — goldenseal root extract

Oral

capsule

3 g

1 g every 4 hours

3 times

Natural Product Characteristics

Now Foods, Bloomingdale, IL

2019

2 . clinical goldenseal - furosemide experiment (id=NPDI-bcNEPw)

In Vivo Interaction Study

No Effect (based on bioequivalence limits) was detected.

furosemide 956874

  • OAT1 (SLC22A6)
  • OAT3 (SLC22A8)

Results

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Probe cocktail study
Fixed-sequence

Population

Healthy volunteers

16

8 male and 8 female (non-lactating women )

Pharmacokinetic (PK) Sampling Information

24, 48, 72, and 96 hours after cocktail administration

Drug or Natural Product Administration

Object Administration — furosemide

Oral

Furosemide (10 mg/mL solution; West-ward Pharmaceuticals Corp., Eatontown, NJ), metformin (500 mg/5 mL solution; Ranbaxy Pharmaceuticals, Inc., Jacksonville, FL), rosuvastatin (10 mg tablet; Camber Pharmaceuticals Inc., Piscataway, NJ), and midazolam (2 mg/mL syrup; West-ward Pharmaceuticals Corp.)

1 mg furosemide, 50 mg metformin, 10 mg rosuvastatin, and 2.5 mg midazolam

single dose

once

Precipitant Administration — goldenseal root extract

Oral

capsule

3 g

1 g every 4 hours

3 times

Natural Product Characteristics

Now Foods, Bloomingdale, IL

2019

3 . clinical goldenseal - rosuvastatin acid experiment (id=NPDI-8KuZrA)

In Vivo Interaction Study

No Effect (based on bioequivalence limits) was detected.

rosuvastatin 1510813

  • BCRP (ABCG2)
  • OATP1B1 (SLCO1B1)
  • OATP1B3 (SLCO1B3)

Results

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Probe cocktail study
Fixed-sequence

Population

Healthy volunteers

16

8 male and 8 female (non-lactating women )

Pharmacokinetic (PK) Sampling Information

24, 48, 72, and 96 hours after cocktail administration

Drug or Natural Product Administration

Object Administration — rosuvastatin

Oral

Furosemide (10 mg/mL solution; West-ward Pharmaceuticals Corp., Eatontown, NJ), metformin (500 mg/5 mL solution; Ranbaxy Pharmaceuticals, Inc., Jacksonville, FL), rosuvastatin (10 mg tablet; Camber Pharmaceuticals Inc., Piscataway, NJ), and midazolam (2 mg/mL syrup; West-ward Pharmaceuticals Corp.)

1 mg furosemide, 50 mg metformin, 10 mg rosuvastatin, and 2.5 mg midazolam

single dose

once

Precipitant Administration — goldenseal root extract

Oral

capsule

3 g

1 g every 4 hours

3 times

Natural Product Characteristics

Now Foods, Bloomingdale, IL

2019

4 . clinical goldenseal - rosuvastatin lactone experiment (id=NPDI-M015vQ)

In Vivo Interaction Study

No Effect (based on bioequivalence limits) was detected.

rosuvastatin lactone

  • OATP1B1 (SLCO1B1)
  • OATP1B3 (SLCO1B3)

Results

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Probe cocktail study
Fixed-sequence

Population

Healthy volunteers

16

8 male and 8 female (non-lactating women )

Pharmacokinetic (PK) Sampling Information

24, 48, 72, and 96 hours after cocktail administration

Drug or Natural Product Administration

Object Administration — rosuvastatin lactone

Oral

Furosemide (10 mg/mL solution; West-ward Pharmaceuticals Corp., Eatontown, NJ), metformin (500 mg/5 mL solution; Ranbaxy Pharmaceuticals, Inc., Jacksonville, FL), rosuvastatin (10 mg tablet; Camber Pharmaceuticals Inc., Piscataway, NJ), and midazolam (2 mg/mL syrup; West-ward Pharmaceuticals Corp.)

1 mg furosemide, 50 mg metformin, 10 mg rosuvastatin, and 2.5 mg midazolam

single dose

once

Precipitant Administration — goldenseal root extract

Oral

capsule

3 g

1 g every 4 hours

3 times

Natural Product Characteristics

Now Foods, Bloomingdale, IL

2019

5 . clinical goldenseal - metformin study (id=NPDI-_zSDOQ)

In Vivo Interaction Study

Decreased systemic exposure was detected.

metformin 1503297

  • MATE1 (SLC47A1)
  • MATE2-K (SLC47A2)
  • OCT1 (SLC22A1)
  • OCT2 (SLC22A2)

Results

Sample Compound measured Value Measurement Study sequence Additional information N replicates

Experimental Conditions

Probe cocktail study
Fixed-sequence

Population

Healthy volunteers

16

8 male and 8 female (non-lactating women )

Pharmacokinetic (PK) Sampling Information

24, 48, 72, and 96 hours after cocktail administration

Drug or Natural Product Administration

Object Administration — metformin

Oral

Furosemide (10 mg/mL solution; West-ward Pharmaceuticals Corp., Eatontown, NJ), metformin (500 mg/5 mL solution; Ranbaxy Pharmaceuticals, Inc., Jacksonville, FL), rosuvastatin (10 mg tablet; Camber Pharmaceuticals Inc., Piscataway, NJ), and midazolam (2 mg/mL syrup; West-ward Pharmaceuticals Corp.)

1 mg furosemide, 50 mg metformin, 10 mg rosuvastatin, and 2.5 mg midazolam

single dose

once

Precipitant Administration — goldenseal root extract

Oral

capsule

3 g

1 g every 4 hours

3 times

Natural Product Characteristics

Now Foods, Bloomingdale, IL

2019