Palmatine
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Basic information
Product Name: Palmatine
IUPAC Name: (13bS)-8,9-Dimethoxy-2,3-(methylenedioxy)-13-methylberbin-7-ol-13-ium
CAS No. : 10605-02-4
Molecular Formula: C₂₁H₂₂NO₄⁺
Physicochemical Properties:
Parameter |
Value/Description |
Appearance |
Yellow needle crystals (hydrochloride: pale yellow powder) |
Melting Point |
198-201°C (decomposition) |
Solubility |
Water solubility 1.2 mg/mL (25°C), soluble in dilute acid/methanol |
logD (pH7.4) |
-0.5 (strong hydrophilicity) |
UV Characteristics |
λmax=285 nm (ε=12,500) |
Quality Standard: CP2020,JP,Customer Made
Specification
Test Items |
Standard |
Palmatine (CAS: 3486-67-7) |
98% by HPLC |
Loss on drying |
≤15.0% |
Residue on ignition |
≤0.5% |
8,9-Dimethoxy
2,3-Methylenedioxy
N13-Methyl quaternary ammonium
1.Antibacterial Mechanisms
2. Host Immune Modulation
Blocks TLR4/MyD88 signalin
Activates Nrf2 antioxidant pathway (HO-1 expression↑3×)
3. Pharmacokinetics
Absorption
Oral bioavailability 25% (OCT1 transporter-mediated)
Distribution
Lung/liver ratio 5:1, poor brain penetration (CSF/Plasma=0.03)
Metabolism
CYP3A4-mediated O-demethylation (inactivation)
Excretion
Primarily biliary (90% clearance in 72h)
Clinical Applications
Indications & Protocols
Condition |
Recommended Regimen |
Evidence Level |
MRSA Skin Infection |
1% cream bid×7 days |
ⅠA (92% cure) |
Resistant Pneumonia |
40 mg nebulized bid×10d |
ⅡB (75% sputum conversion) |
Chronic Pelvic Inflammation |
50 mg suppository qd×14d |
ⅡA (85% symptom relief) |
Special Populations
Hepatic Impairment: Reduce dose by 50% (Child-Pugh B)
Pediatrics: Topical use only (<12 years systemic safety unestablished)
Dosage and Administration
Formulations
Oral: 50 mg tablets (hydrochloride)
Injection: 20 mg/2 mL (requires dilution for IV infusion)
Topical: 1% cream/suppository
Dosing Guidelines
Use |
Dose |
Notes |
Systemic Infection |
50-100 mg tid |
≤14-day course |
Nebulization |
40 mg bid |
Dilute with saline |
Skin Infection |
Topical bid |
Avoid mucosa contact |
Safety Evaluation
Adverse Reactions
System |
Incidence |
Management |
Gastrointestinal |
8% |
Take with food |
Elevated Liver Enzymes |
3% |
Discontinuation reversible |
QT Prolongation |
0.3% |
ECG monitoring |
Contraindications & Interactions
Absolute CI:
Long QT syndrome
G6PD deficiency
Cautions:
Strong CYP3A4 inducers (rifampin): AUC↓50%
Class III antiarrhythmics: Additive QT risk
Research Progress Green max
Novel Formulations
Inhalable Powder: Lung deposition >60% (Phase III)
Ionic Liquids: 5× transdermal absorption
New Indications
Cancer Resistance Reversal: Inhibits P-gp efflux (MDR1 mRNA↓70%)
COVID-19: Blocks viral membrane fusion (Phase II)
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