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Send EmailBerberine Hydrochloride, Berberine HCl, Berberine Chloride, Berberinium Chloride, 633-65-8
BERBERINE HYDROCHLORIDE
SECTION 1: PRODUCT IDENTITY AND CHEMICAL IDENTIFICATION
| Parameter | Information |
|---|---|
| Product Name | Berberine Hydrochloride |
| Common Names | Berberine chloride, Berberine HCl, Berberinium chloride |
| CAS Number | 633-65-8 |
| EC Number (EINECS) | 211-195-9 |
| Molecular Formula | C₂₀H₁₈ClNO₄ |
| Molecular Weight | 371.81 g/mol |
| Chemical Class | Isoquinoline alkaloid salt (quaternary ammonium salt) |
| Source | Naturally found in Berberis, Coptis, Hydrastis plants |
SECTION 2: CHEMICAL STRUCTURE
OCH₃
|
O—CH₂—O—[A]——[B]—C
\ /
C C
/ \
[C] [D]
\ /
C——N⁺——C
/ \
O—CH₂—O—[E] [F]—OCH₃
|
OCH₃
Berberine Chloride
C₂₀H₁₈ClNO₄
Quaternary isoquinoline alkaloid
(Protoberberine skeleton)
Simplified Chemical Structure:
OCH₃
|
OCH₃—[D]——[C]——[B]——[A]—O—CH₂—O
| |
N⁺ |
/ |
OCH₃—[F]——[E]——[A]—O—CH₂—O
|
OCH₃
Berberine Ion (Anion: Cl⁻)
| Parameter | Description |
|---|---|
| Molecular Formula | C₂₀H₁₈ClNO₄ |
| Molecular Weight | 371.81 g/mol |
| Chemical Class | Isoquinoline alkaloid (quaternary ammonium) |
| Skeleton | Protoberberine derivative |
| SMILES | COC1=CC=2C(=C1)C3=CC4=C(C=C3CCN2C)OCO4.Cl |
| InChI | InChI=1S/C20H18NO4.ClH/c1-22-15-4-3-12-7-14-10-17-16(24-11-25-17)8-13(14)5-6-21(12)9-15;/h3-4,8-10H,5-7,11H2,1-2H3;1H/q+1;/p-1 |
| InChI Key | ZDFRQCUZMYEECK-UHFFFAOYSA-M |
| Hydrogen Bond Donors | 0 |
| Hydrogen Bond Acceptors | 5 |
| Rotatable Bond Count | 3 |
| Polar Surface Area (PSA) | 40.8 Ų |
| Charge | Quaternary ammonium (N⁺) + chloride (Cl⁻) |
SECTION 3: PHYSICAL AND CHEMICAL PROPERTIES
| Property | Value | Test Method / Note |
|---|---|---|
| Appearance | Yellow-orange crystalline powder | Visual |
| Odor | Slight characteristic odor | Olfactometric |
| Molecular Weight | 371.81 g/mol | Calculated |
| Melting Point | 250-260°C (decomposes) | DSC / Capillary |
| Density (20°C) | ~1.5 g/cm³ (estimated) | - |
| Solubility in Water (20°C) | Soluble (~10-15 g/L) | General Method |
| Solubility in Hot Water | More soluble | General Method |
| Solubility in Ethanol | Slightly soluble | General Method |
| Solubility in Methanol | Soluble | General Method |
| Solubility in DMSO | Soluble | General Method |
| Solubility in Chloroform | Very slightly soluble | General Method |
| Log P (Octanol/Water) | ~1.0 (quaternary charge; hydrophilic) | Calculated |
| pH (Aqueous, 1% solution) | ~4.0-5.5 (acidic) | pH Meter |
| Flash Point | >150°C | - |
| Vapor Pressure (25°C) | Very low | - |
| Thermal Stability | Stable up to 200°C; decomposes at higher temperatures | - |
| Hygroscopicity | Slightly hygroscopic | - |
| Optical Activity | Not optically active | - |
| Crystal System | Monoclinic | XRD |
SECTION 4: SPECTROSCOPIC PROPERTIES
| Parameter | Value | Description |
|---|---|---|
| UV-VIS Absorption (λmax) | ~230 nm, ~265 nm, ~348 nm, ~420 nm | In ethanol or methanol |
| Molar Absorptivity (ε) | Variable (concentration dependent) | - |
| IR (KBr, cm⁻¹) | ~3400, 2940, 1720, 1620, 1510, 1460, 1360, 1250, 1200, 1100, 1040, 940 | Characteristic alkaloid peaks |
| NMR (¹H, DMSO-d6) | δ 9.9 (s, 1H), 8.7 (s, 1H), 7.8 (s, 1H), 7.5 (m), 6.9 (s), 6.3 (s), 4.9 (s, 2H), 3.8-4.0 (m, 9H) | - |
| Fluorescence | Strong yellow-green fluorescence (excitation at 360 nm) | In aqueous solution |
| LC-MS (ESI+) | [M⁺] m/z 336 (berberine ion) | Chloride ion dissociates |
SECTION 5: PHARMACOLOGICAL PROPERTIES AND MECHANISM OF ACTION
| Property | Description |
|---|---|
| Antimicrobial Activity | Effective against Gram-positive bacteria (S. aureus, S. pneumoniae, C. acnes) and some Gram-negative bacteria. Acts through DNA intercalation and cell membrane permeability. |
| AMPK Activation | Activates the AMPK (AMP-activated protein kinase) pathway, regulating cellular energy homeostasis; increases mitochondrial oxidation. |
| Glucose Metabolism | Increases insulin sensitivity; stimulates glucose uptake; inhibits hepatic gluconeogenesis. |
| Lipid Metabolism | Reduces LDL-cholesterol and triglyceride levels; reduces PCSK9 expression; reduces hepatic steatosis. |
| Anti-inflammatory Effect | Inhibits NF-κB and MAPK pathways; reduces pro-inflammatory cytokines (TNF-α, IL-6, IL-1β). |
| Antioxidant Activity | Scavenges reactive oxygen species (ROS); increases endogenous antioxidant enzymes (SOD, GSH-Px, CAT). |
| Neuroprotective Effect | Reduces neuroinflammation; inhibits β-amyloid aggregation in Alzheimer's disease models. |
| Cardiovascular Effects | Reduces blood pressure; improves endothelial function; induces vasodilation. |
| DNA Intercalation | Intercalates into DNA via quaternary ammonium structure; inhibits topoisomerase I and II. |
SECTION 6: COMMERCIAL GRADES AND VARIANTS
| Grade / Type | Purity | Appearance | Primary Application |
|---|---|---|---|
| Pharmaceutical Grade (USP/EP) | ≥98.0% | Yellow-orange crystalline powder | Supplements, pharmaceutical studies |
| Food Supplement Grade | ≥97.0% | Yellow-orange powder | Dietary supplements, capsules |
| Research/Analytical Grade | ≥99.0% (HPLC) | Yellow-orange crystals | Analytical standards, R&D |
| Industrial Grade | ≥95.0% | Yellowish-orange powder | Plant extract production, technical applications |
| Micronized Grade | ≥98.0% | Micronized powder | Advanced formulations (lipid nanoparticles) |
SECTION 7: CLINICAL RESEARCH AND INDICATIONS
| Indication / Use | Mechanism of Action | Research Status | Typical Dose |
|---|---|---|---|
| Metabolic Syndrome / Type 2 Diabetes | AMPK activation, glucose metabolism, insulin sensitivity | Clinical trials (Phase II-III) | 500-1500 mg/day |
| Hyperlipidemia | PCSK9 reduction, LDL and triglyceride lowering | Clinical trials | 500-1000 mg/day |
| Hypertension | Vasodilation, ACE inhibition (limited) | Preclinical / Clinical pilot | 500-1000 mg/day |
| Gastrointestinal Infections | Antimicrobial (bacterial diarrhea, C. difficile) | Preclinical / Clinical | 200-500 mg/day |
| Acne / Dermatological | Antimicrobial, anti-inflammatory (C. acnes) | Preclinical / Topical | Variable |
| Neurodegenerative Diseases | Neuroprotective, β-amyloid inhibition | Preclinical | - |
| Polycystic Ovary Syndrome (PCOS) | Metabolic regulation, insulin sensitivity | Clinical pilot | 500-1500 mg/day |
| Non-alcoholic Fatty Liver Disease (NAFLD) | Lipid metabolism, AMPK activation | Clinical trials | 500-1000 mg/day |
SECTION 8: ORAL BIOAVAILABILITY AND FORMULATION NOTES
| Parameter | Information |
|---|---|
| Oral Bioavailability | Low (~1-5%); P-glycoprotein efflux; hepatic first-pass metabolism (CYP2C9, CYP3A4, CYP2D6) |
| Absorption | Small intestine (duodenum, jejunum) |
| Plasma Peak Concentration (Cmax) | 1-3 hours (oral administration) |
| Plasma Half-Life (t½) | ~2-5 hours (human) |
| Elimination | Hepatic metabolism; renal excretion (urine); feces |
| Volume of Distribution (Vd) | Extensive (tissue distribution) |
| Protein Binding | ~50-60% |
| Bioavailability Enhancement Strategies | • Combination with piperine (P-gp inhibition) • Nanocarrier systems (lipid nanoparticles, micelles) • Phytosome technology • Amorphous solid dispersion • Solubility enhancers in small intestine |
| Formulation Types | • Capsules (powder, granules) • Tablets (direct compression) • Lipid-based formulations • Nanoparticulate systems • Topical gels and creams |
SECTION 9: TYPICAL DOSAGE AND USAGE
| Route of Administration | Typical Dose Range | Frequency | Notes |
|---|---|---|---|
| Oral (Metabolic Syndrome) | 500-1500 mg | 2-3 times daily | Take with meals |
| Oral (Lipid Lowering) | 500-1000 mg | 2 times daily | 6-12 weeks; physician supervision |
| Oral (Antimicrobial) | 200-500 mg | 2-4 times daily | Variable; acute infection |
| Oral (Maintenance / Support) | 300-600 mg | Once daily | Long-term use |
| Topical (Acne) | 1-5% | 1-2 times daily | Gel, cream formulations |
| Topical (Wound) | 0.5-2% | 2 times daily | Antimicrobial |
SECTION 10: SAFETY PROFILE AND TOXICOLOGICAL ASSESSMENT
| Parameter | Value / Description |
|---|---|
| GHS Classification | Warning (irritant) |
| Signal Word | Warning |
| Hazard Pictograms | GHS07 (Exclamation mark) |
| Hazard Statements (H-Codes) | H315 (Causes skin irritation), H319 (Causes serious eye irritation), H335 (May cause respiratory irritation) |
| Precautionary Statements (P-Codes) | P261, P264, P280, P302+P352, P305+P351+P338, P312 |
| Acute Oral Toxicity (LD50, Rat) | ~500-1000 mg/kg (moderate toxicity) |
| Acute Dermal Toxicity (LD50, Rat) | >2000 mg/kg (low toxicity) |
| Acute Inhalation Toxicity | Low toxicity |
| Skin Irritation | Mild irritant |
| Eye Irritation | Moderate irritant |
| Skin Sensitization | Low potential |
| Carcinogenicity | Not classified as carcinogenic |
| Mutagenicity | In vitro mutagenic potential (AMES test positive); in vivo studies inconclusive |
| Reproductive Toxicity | Embryotoxic potential at high doses (animal) |
| Target Organs | Liver, kidneys, gastrointestinal system |
| NOAEL (Rat, 90 days) | ~100-300 mg/kg/day |
| Topical Safety | Well tolerated; concentration dependent |
| Pregnancy Category | Category C (USA) - risk in animal studies |
| Lactation | Insufficient data; should not be used |
| Drug Interactions | CYP3A4, CYP2D6, CYP2C9 inhibitor; P-gp substrate/inhibitor |
| Common Side Effects | GI distress, diarrhea, constipation, nausea (dose dependent) |
| Serious Side Effects | Hepatotoxicity at high doses, QT prolongation (rare) |
SECTION 11: DRUG INTERACTIONS
| Drug / Substance | Interaction Type | Severity | Management |
|---|---|---|---|
| Antidiabetics (Metformin, Sulfonylureas) | Increased hypoglycemia risk | Moderate | Blood glucose monitoring; dose adjustment |
| Anticoagulants (Warfarin) | Increased bleeding risk | Moderate | INR monitoring |
| Antihypertensives (Calcium channel blockers) | Hypotension risk | Low | Blood pressure monitoring |
| CYP3A4 Substrates (Statins, CCB, Cyclosporine) | Increased plasma levels | Moderate | Dose adjustment; monitoring |
| CYP2D6 Substrates (Beta-blockers, Antidepressants) | Increased plasma levels | Low-Moderate | Monitoring; dose adjustment |
| P-gp Substrates (Digoxin, Talinolol) | Increased absorption, decreased clearance | Moderate | Monitoring; dose adjustment |
| Piperine (Black Pepper Extract) | Increased berberine bioavailability | Positive | Combination products |
| Erythromycin / Clarithromycin | Hepatotoxicity risk | Moderate | Avoid co-administration |
| Alcohol | Hepatotoxicity risk | Moderate | Avoid alcohol consumption |
SECTION 12: CLINICAL STUDY SUMMARY
| Study Topic | Result | Evidence Level | Reference |
|---|---|---|---|
| Type 2 Diabetes (Berberine) | HbA1c ↓ 1-2%; FPG ↓ ~30% | Randomized Controlled Trial (RCT) | J Clin Endocrinol Metab. 2012 |
| Hyperlipidemia | LDL ↓ ~20%; TG ↓ ~30% | RCT | Am J Cardiol. 2009 |
| NAFLD (Fatty Liver) | Liver steatosis ↓; ALT ↓ | RCT | J Hepatol. 2016 |
| PCOS (Polycystic Ovary) | Insulin sensitivity ↑; LH/FSH ↓ | RCT | Exp Clin Endocrinol Diabetes. 2012 |
| Hypertension | Systolic BP ↓ ~10 mmHg; Diastolic BP ↓ ~5 mmHg | Meta-analysis | Phytother Res. 2015 |
| Metabolic Syndrome | Waist circumference ↓; TG ↓; HDL ↑ | RCT | J Diabetes. 2017 |
| Acne (Topical) | Inflammatory lesions ↓ ~50-70% | Preclinical / Pilot | J Dermatolog Treat. 2020 |
| Neuroprotection (Alzheimer's) | β-amyloid aggregation ↓ | Preclinical | J Neuroinflammation. 2019 |
SECTION 13: FIRST AID MEASURES
| Route of Exposure | Action |
|---|---|
| Inhalation | If inhaled as powder, move to fresh air. Seek medical attention if respiratory irritation or symptoms persist. |
| Skin Contact | Wash with plenty of soap and water. Remove contaminated clothing. Seek medical attention if irritation develops. |
| Eye Contact | Rinse thoroughly with plenty of water for at least 15 minutes. Keep eyelids open. Remove contact lenses if present. Seek medical attention if irritation persists. |
| Ingestion | Rinse mouth with water. Do NOT induce vomiting. Drink 1-2 glasses of water. Seek immediate medical attention. |
| Note | Symptomatic treatment is administered. No specific antidote available. Gastrointestinal decontamination may be required (large dose). |
SECTION 14: ADVERSE EFFECTS AND MANAGEMENT
| Adverse Effect | Frequency | Severity | Management |
|---|---|---|---|
| Gastrointestinal Discomfort (stomach pain) | Common (>10%) | Mild-Moderate | Take with meals; reduce dose |
| Diarrhea | Common (5-15%) | Mild-Moderate | Increase fluid intake; probiotics |
| Constipation | Common (5-10%) | Mild | Increase fiber intake |
| Nausea | Common (5-10%) | Mild | Take with meals; divide dose |
| Dizziness | Less common (2-5%) | Mild | Rest; hypotension monitoring |
| Elevated Liver Transaminases | Less common | Moderate | Liver function tests; high-dose monitoring |
| Skin Rash | Rare (<1%) | Mild | Antihistamine; may require discontinuation |
| QT Prolongation | Very rare (<0.1%) | Serious | ECG monitoring; avoid high doses |
SECTION 15: STORAGE AND SHELF LIFE
| Parameter | Information |
|---|---|
| Storage Conditions | Store in a cool (<25°C), dry, dark place; protect from direct sunlight, heat, and moisture. |
| Temperature Limits | 15-25°C (ideal); do not exceed 30°C |
| Light | Protect from UV light and direct sunlight (photodegradation) |
| Humidity | Low humidity environment (slightly hygroscopic) |
| Oxygen | Protect against oxidation; keep containers tightly closed |
| Incompatible Materials | Strong oxidizing agents, strong alkalis |
| Container Requirements | Light-proof, moisture-barrier containers: Amber glass jars, aluminum bags, opaque HDPE |
| Shelf Life | 24-36 months (unopened original packaging, under proper storage conditions) |
| Shelf Life (After Opening) | 12-24 months (under proper storage conditions) |
| Signs of Degradation | Darkening color (dark orange-brown); caking; decreased solubility; HPLC impurity increase |
| Stability Warning | May degrade under light and humidity; oxidized product may form colored impurities |
SECTION 16: PACKAGING OPTIONS
| Packaging Type | Quantity / Capacity | Material | Application Area |
|---|---|---|---|
| Amber Glass Jar | 50 g, 100 g, 500 g, 1 kg | Amber glass (UV protected) | Pharmaceutical, laboratory, high purity |
| Aluminum Foil Bag | 1 kg, 5 kg, 10 kg, 25 kg | Aluminum / PE (light and moisture proof) | Supplement production, industrial |
| Plastic Drum (HDPE) | 25 kg, 50 kg | HDPE (opaque, moisture barrier) | Industrial bulk supply |
| Kraft Bag (PE Lined) | 10 kg, 25 kg | Kraft paper / PE liner | Economical packaging |
| Fiber Drum | 25 kg, 50 kg | Fiber / PE liner | Industrial supply |
| Amber Glass Vial | 10 g, 25 g, 50 g | Amber glass (UV protected) | Analytical standards, R&D |
SECTION 17: TRANSPORTATION INFORMATION
| Parameter | Information |
|---|---|
| UN Number | Not applicable (not classified as dangerous substance) |
| Hazard Class | Not applicable |
| Packing Group | Not applicable |
| ADR/RID | Not classified as dangerous goods |
| IMDG Code | Not marine pollutant |
| IATA (Air) | Not classified as dangerous goods; can be transported by air |
| Transport Temperature | Ambient temperature; protect from heat, moisture, and light |
| Transport Precautions | Keep away from strong oxidizing agents; light-proof packaging |
| Spill Cleanup | Collect mechanically; clean with absorbent material; avoid dust generation |
| Marine Pollutant | No |
SECTION 18: QUALITY CONTROL AND ANALYTICAL METHODS
| Parameter | Test Method | Specification |
|---|---|---|
| Appearance | Visual | Yellow-orange crystalline powder |
| Assay (Berberine HCl) | HPLC / UV | ≥98.0% (Pharm.); ≥97.0% (Supplement) |
| Berberine Free Base | HPLC | ≤0.5% |
| Melting Point | DSC / Capillary | 250-260°C (decomposes) |
| Water Content | Karl Fischer | ≤1.0% (Pharm.); ≤2.0% (Supplement) |
| Residue on Ignition | Gravimetric | ≤0.5% (Pharm.); ≤1.0% (Supplement) |
| Heavy Metals (Pb) | ICP-MS / USP <231> | ≤10 ppm |
| Arsenic (As) | ICP-MS | ≤2 ppm |
| Chloride Content | Titration | 9.0-10.0% |
| HPLC Impurities | HPLC | Single impurity ≤0.5%; Total ≤2.0% |
| UV-VIS Spectrum | UV-VIS | λmax 348 ± 2 nm (methanol) |
| Particle Size | Laser Diffraction | As per customer specification |
| Microbiological Purity | USP <61> | TAMC ≤10² CFU/g; TYMC ≤10¹ CFU/g |
| E. coli | USP <62> | Negative |
| Salmonella | USP <62> | Negative |
SECTION 19: QUALITY SPECIFICATIONS
| Parameter | Specification (Pharmaceutical) | Specification (Supplement) | Test Method |
|---|---|---|---|
| Appearance | Yellow-orange crystalline powder | Yellow-orange powder | Visual |
| Assay (HPLC) | ≥98.0% | ≥97.0% | HPLC |
| Berberine Free Base | ≤0.5% | ≤1.0% | HPLC |
| Water Content | ≤1.0% | ≤2.0% | Karl Fischer |
| Residue on Ignition | ≤0.5% | ≤1.0% | Gravimetric |
| Heavy Metals (Pb) | ≤10 ppm | ≤20 ppm | ICP-MS |
| Arsenic (As) | ≤2 ppm | ≤5 ppm | ICP-MS |
| Chloride Content | 9.0-10.0% | 8.5-10.5% | Titration |
| Single Impurity | ≤0.5% | ≤1.0% | HPLC |
| Total Impurities | ≤2.0% | ≤3.0% | HPLC |
| Microbiological Purity | TAMC ≤10² CFU/g | TAMC ≤10³ CFU/g | USP <61> |
SECTION 20: OTHER NAMES AND SYNONYMS
| Type | Name |
|---|---|
| Chemical Name | Berberine Chloride |
| Common Names | Berberine HCl, Berberine Chloride, Berberinium chloride |
| IUPAC Name | 5,6-Dihydro-9,10-dimethoxybenzo[g]-1,3-benzodioxolo[5,6-a]quinolizinium chloride |
| Trade Marks | Berberine HCl, Berberine Hydrochloride (bulk), Berberine Complex |
| Plant Sources | Berberis aristata (Indian barberry), Coptis chinensis (Goldthread), Hydrastis canadensis (Goldenseal) |
| CAS Number | 633-65-8 |
| EC Number | 211-195-9 |
| PubChem CID | 2353 |
| DrugBank ID | DB04115 |
| UNII (FDA) | 96L0B2HBIZ |
SECTION 21: GHS CLASSIFICATION AND LABELING
| Parameter | Information |
|---|---|
| GHS Classification | Skin Irritant Category 2; Eye Irritant Category 2A; STOT SE3 |
| Signal Word | Warning |
| Hazard Pictograms | GHS07 (Exclamation mark) |
| Hazard Statements (H-Codes) | H315 (Causes skin irritation), H319 (Causes serious eye irritation), H335 (May cause respiratory irritation) |
| Precautionary Statements (P-Codes) | P261, P264, P271, P280, P302+P352, P305+P351+P338, P312, P332+P313, P337+P313, P362+P364, P403+P233, P405, P501 |
| NFPA 704 Classification | Health: 1, Flammability: 1, Reactivity: 0 |
SECTION 22: ENVIRONMENTAL IMPACT AND DISPOSAL
| Parameter | Information |
|---|---|
| Biodegradability | Partially biodegradable (alkaloid natural compound) |
| Aquatic Toxicity (EC50) | >10 mg/L (Daphnia magna) - moderate toxicity |
| Aquatic Toxicity (LC50) | >10 mg/L (fish) - moderate toxicity |
| Soil Mobility | Low (quaternary ammonium charge) |
| Bioaccumulation Potential | Low-Moderate |
| Disposal Method | Dispose of in accordance with local, regional, and national regulations |
| Incineration | Controlled incineration facilities; energy recovery possible |
| Sewer Discharge | Do not discharge into sewers or water resources |
| Environmental Precautions | Prevent environmental spread during spills |
SECTION 23: FREQUENTLY ASKED QUESTIONS
| Question | Answer |
|---|---|
| Q1: What is Berberine HCl? | Berberine HCl is the hydrochloride salt of an isoquinoline alkaloid naturally found in many plants. It is known for its antimicrobial, metabolic regulatory, and anti-inflammatory properties. |
| Q2: What is Berberine HCl used for? | It is being researched for metabolic syndrome, type 2 diabetes, hyperlipidemia, hypertension, gastrointestinal infections, and PCOS. |
| Q3: Is Berberine HCl safe? | At recommended doses (500-1500 mg/day), it is generally safe. GI discomfort is the most common side effect. Hepatotoxicity and QT prolongation are risks at high doses. |
| Q4: Is Berberine HCl bioavailability low? | Yes, oral bioavailability is very low (~1-5%). Combination with piperine (black pepper extract) and nanoparticulate systems improve bioavailability. |
| Q5: Is Berberine HCl good for diabetes? | Clinical studies show that berberine lowers blood sugar (HbA1c) and increases insulin sensitivity. It may have comparable efficacy to metformin. |
| Q6: Does Berberine HCl interact with other medications? | Yes, it is a CYP3A4, CYP2D6, CYP2C9 inhibitor and P-gp substrate/inhibitor. It may interact with antidiabetics, anticoagulants, statins, and digoxin. |
| Q7: Does Berberine HCl help with weight loss? | Studies show it may help with modest weight loss through AMPK activation and lipid metabolism regulation. |
| Q8: Is Berberine HCl safe during pregnancy? | FDA Pregnancy Category C. Embryotoxicity has been reported in animal studies. It should not be used during pregnancy and lactation. |
| Q9: Can Berberine HCl be used on the skin? | Yes, it is being researched for acne treatment (1-5% topical formulations) due to its antimicrobial and anti-inflammatory effects. |
| Q10: Is Berberine HCl a natural compound? | Yes, it naturally occurs in plants such as Berberis, Coptis, and Hydrastis. Commercial berberine is typically extracted from these plants. |
SECTION 24: QUICK REFERENCE TABLE
| Property | Value |
|---|---|
| CAS Number | 633-65-8 |
| Molecular Formula | C₂₀H₁₈ClNO₄ |
| Molecular Weight | 371.81 g/mol |
| Appearance | Yellow-orange crystalline powder |
| Melting Point | 250-260°C (decomposes) |
| Water Solubility | Soluble (~10-15 g/L) |
| Log P | ~1.0 (quaternary charge) |
| Primary Function | Antimicrobial, metabolic regulator |
| Typical Oral Dose | 500-1500 mg/day |
| Shelf Life | 24-36 months (proper storage) |
| Storage | Cool (<25°C), dry, dark, light-proof |
| GHS Classification | Irritant (GHS07) |
| FDA Approval | Not an FDA-approved drug; sold as dietary supplement |
| Bioavailability | Low (~1-5%) |
| Main Applications | Metabolic support, antimicrobial, cardiovascular support |
SECTION 25: CRITICAL WARNINGS AND BEST PRACTICES
CRITICAL WARNINGS:
Low bioavailability: Oral berberine bioavailability is very low. Bioavailability enhancement strategies (piperine, nanoparticles, amorphous dispersion) are critical in formulations.
Drug interactions: Has potential for interaction with CYP3A4, CYP2D6, CYP2C9, CYP1A2, and P-gp pathways. Caution should be exercised in patients taking concomitant medications.
Liver toxicity: High doses may elevate liver transaminases. Should be used with caution in patients with liver disease.
QT prolongation: QT interval prolongation has been reported at high doses. ECG monitoring is recommended in patients with cardiac conditions.
Gastrointestinal side effects: Nausea, diarrhea, and abdominal pain are common. Taking with meals and starting with a low dose is recommended.
Pregnancy and lactation: FDA Pregnancy Category C. Should not be used during pregnancy and lactation.
OTC status: Berberine is not a drug, but a dietary supplement. It cannot be sold with therapeutic claims.
Regulatory compliance: In Turkey, it can be sold as a dietary supplement; however, permission from the Turkish Ministry of Health is required for pharmaceutical use.
BEST PRACTICE RECOMMENDATIONS:
Bioavailability-enhancing formulations: Combination with piperine (5-10%); nanocarrier systems (lipid nanoparticles, micelles); amorphous solid dispersions; phytosome technology.
Gradual dose increase: Start at low dose (200-300 mg/day); increase to 1500 mg/day over 4-6 weeks as tolerated.
Take with meals: Take with food to improve gastrointestinal tolerance.
Divide daily dose: Divide the dose 2-3 times daily (e.g., 500 mg x 3 times).
Quality control: HPLC assay of berberine; loss on drying; microbiological purity; heavy metals; PAH content.
Stability studies: Degradation profile under light, humidity, and temperature; shelf life determination.
Safety evaluation: Hepatic and renal function tests; QT monitoring (high dose); drug interaction studies.
Contraindications: Pregnancy, lactation, severe liver/kidney disease, history of QT prolongation, patients using CYP inhibitors and P-gp substrates.
Clinical study compliance: Refer to clinical doses on product labels; avoid therapeutic claims.
Microbiological control: Berberine HCl powder should be controlled for microbiological purity (TAMC, TYMC, pathogens).
LEGAL DISCLAIMER:
The information provided in this document is based on our current knowledge and experience and is presented in good faith; however, it does not constitute a binding specification or guarantee as all conditions of use are beyond our control. This Technical Data Sheet is for informational purposes only. Users are responsible for testing suitability for their own applications. For complete safety, storage, use, handling, waste, and regulatory compliance information, please refer to the official Safety Data Sheet (SDS/MSDS) provided by the manufacturer/supplier. This product is a dietary supplement and should not be used with therapeutic claims.