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Galantamine hydrobromide powder, The molecular formula is C17H22BrO3, CAS 1953-04-4, and the molecular weight is 368.27. White to off white powder, odorless or slightly with a distinctive odor. Easily soluble in water (with the highest solubility at pH 5.2), 0.1N hydrochloric acid, and 0.1N sodium hydroxide solution, slightly soluble in ethanol, and almost insoluble in ether or chloroform. It is an alkaloid isolated from plants of the Allium genus. It is a reversible acetylcholinesterase (AChE) inhibitor that easily enters brain tissue through the blood-brain barrier and has a strong effect on the central nervous system. Compared with coumarin, neostigmine, and pyridostigmine, it has a wide therapeutic range, low toxicity, and weak and short-lived toxic masking effect. Easy for patients to tolerate and with few adverse reactions. AChE inhibitors can improve learning and memory function in animals and humans through a cholinergic mechanism. As an anticholinesterase drug, it can improve the transmission between nerves and muscles, and is used for myasthenia gravis, progressive muscular dystrophy, sequelae of poliomyelitis, childhood paralysis, sensory or motor disorders caused by neurological disorders, multiple neuritis, etc.
Additional information of chemical compound:
| Product Name | Galantamine Hydrobromide Powder | Galantamine Hydrobromide Tablets |
| Product Type | Powder | Tablet |
| Product Purity | ≥99% | ≥99% |
| Product Specifications | Customizable | Customizable |
| Product Package | Customizable | Customizable |
Galantamine Hydrobromide +. COA
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Certificate of Analysis |
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Compound name |
Galantamine Hydrobromide | |
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CAS No. |
1953-04-4 | |
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Grade |
Pharmaceutical grade | |
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Quantity |
Customized | |
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Packaging standard |
Customized | |
| Manufacturer | Shaanxi BLOOM TECH Co., Ltd | |
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Lot No. |
20250109001 |
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MFG |
Jan 12th 2025 |
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EXP |
Jan 8th 2029 |
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Structure |
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| TEST STANDARD | GB/T24768-2009 Industry. Stnndard | |
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Item |
Enterprise standard |
Analysis result |
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Appearance |
White or almost white powder |
Conformed |
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Water content |
≤4.5% |
0.30% |
| Loss on drying |
≤1.0% |
0.15% |
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Heavy Metals |
Pb≤0.5ppm |
N.D. |
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As≤0.5ppm |
N.D. | |
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Hg≤0.5ppm |
N.D. | |
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Cd≤0.5ppm |
N.D. | |
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Purity (HPLC) |
≥99.0% |
99.5% |
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Single impurity |
<0.8% |
0.48% |
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Residue on ignition |
<0.20% |
0.064% |
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Total microbial count |
≤750cfu/g |
80 |
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E. Coli |
≤2MPN/g |
N.D. |
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Salmonella |
N.D. | N.D. |
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Ethanol (by GC) |
≤5000ppm |
400ppm |
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Storage |
Store in a sealed, dark and dry place at-20 degrees |
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Galantamine hydrobromide powder is a reversible acetylcholinesterase inhibitor that can increase acetylcholine concentration by inhibiting acetylcholinesterase activity, thereby improving nerve conduction function. Its clinical applications are extensive, covering multiple fields such as neurodegenerative diseases, neuromuscular diseases, central nervous system diseases, and prevention and treatment of postoperative complications. The specific uses and mechanisms of action are as follows:
Alzheimer's disease
As a core indication, galantamine hydrobromide improves cognitive function by inhibiting acetylcholinesterase activity, reducing acetylcholine degradation, and increasing synaptic acetylcholine concentration. Clinical studies have shown that it can significantly improve patients' abilities in directional memory, associative learning, image recall, and delay the progression of dementia.
Medication characteristics: Short half-life, requiring multiple daily doses (such as tablets taken four times a day); Some formulations use sustained-release technology and can be administered once a day.
Relief of symptoms related to Parkinson's disease
Parkinson's disease patients have dysfunction of the cholinergic system in the striatum, leading to symptoms such as bradykinesia and muscle stiffness. Galantamine hydrobromide alleviates the above symptoms by increasing acetylcholine levels and improving striatal neurotransmitter balance.
Mechanism of action: Regulate the function of presynaptic membrane acetylcholine receptors and enhance the efficiency of information transmission between neurons.
Myasthenia gravis:
Myasthenia gravis is an autoimmune disease caused by dysfunction of the neuromuscular junction, characterized by symptoms such as eyelid ptosis, diplopia, and chewing weakness. Galantamine hydrobromide, as a competitive and reversible acetylcholinesterase inhibitor, can enhance the action of acetylcholine at the neuromuscular junction and restore obstructed neuromuscular conduction.
Clinical effect: significantly improve muscle weakness symptoms and enhance patients' quality of life.
Sequela of poliomyelitis:
Poliovirus damages the anterior horn motor neurons of the spinal cord, leading to sequelae such as flaccid paralysis and muscle atrophy. Galantamine hydrobromide improves motor function by promoting the recovery of neuromuscular conduction.
Progressive muscular dystrophy:
Progressive muscular dystrophy is a hereditary muscular degenerative disease characterized by muscle weakness, atrophy, and eye movement disorders. Galantamine hydrobromide improves neuromuscular conduction and delays disease progression.
Medication principle: Long term regular medication is required, and the efficacy and safety should be evaluated regularly.
Polyneuritis
Multiple neuritis is caused by factors such as heavy metals, drugs, or infections, and is characterized by symptoms such as pain, numbness, and decreased sensation. Galantamine hydrobromide promotes nerve function repair by improving peripheral neuromuscular disorders.
Combination therapy: often used in combination with drugs such as vitamin B and glucocorticoids to enhance therapeutic efficacy.
Neurasthenia and menopausal syndrome
Patients with neurasthenia exhibit symptoms such as mental excitability, nervousness, and sleep disorders; Patients with menopausal syndrome may experience symptoms such as hot flashes, emotional instability, insomnia, and forgetfulness. Galantamine hydrobromide alleviates the above symptoms through its sedative and sedative effects.
Medication precautions: Other organic diseases should be excluded and medication should be taken under the guidance of a doctor.
Prevention and treatment of postoperative complications
Antagonistic effect of non depolarizing muscle relaxants
Non depolarizing muscle relaxants such as chlorpromazine can block neuromuscular conduction, leading to postoperative respiratory depression. Galantamine hydrobromide rapidly reverses muscle relaxation by competitively inhibiting the binding of muscle relaxants to N2 cholinergic receptors.
Medication timing: Usually administered 30 minutes before the end of surgery to avoid residual effects of muscle relaxation.
Rehabilitation of sequelae of cerebrovascular disease
Patients with cerebral hemorrhage or stroke often experience symptoms such as dizziness, headache, and limb numbness during the recovery period. Galantamine hydrobromide promotes the repair of damaged nerve function and reduces sequelae.
Comprehensive treatment: It is necessary to combine rehabilitation training, physical therapy, and other methods to improve the rehabilitation effect.
Pharmacokinetic characteristics
1. Absorption and distribution
Oral bioavailability: 88.5%, food can slow down absorption rate but does not affect total absorption.
Peak time: 1-2 hours, peak blood drug concentration is 56.81 ± 10.40 ng/mL.
Penetration of blood-brain barrier: The concentration of drugs in the brain is three times that of plasma, ensuring effective action on the central nervous system.
Organizational distribution: The concentration of drugs is highest in the kidneys, liver, and brain, in order of kidney>liver>brain>lungs>heart>muscle.
2. Metabolism and excretion
Metabolic pathway: Mainly metabolized by CYP2D6 and CYP3A4 enzymes, generating various inactive metabolites.
Excretion: Approximately 75% is excreted through the kidneys (of which 20% is the prototype drug), and 20% is excreted through feces.
Half life: The final half-life is 7-8 hours, supporting a 2-4 time daily dosing regimen.
The synthesis of galantamine hydrobromide powder involves multiple organic reactions, with the core being the construction of its unique phenanthridine alkaloid skeleton (containing a benzofuran benzodiazepine structure). According to existing literature and patents, their synthesis methods can be divided into two categories: fully synthetic routes and semi synthetic routes. The following analysis will be conducted from the perspectives of reaction principles, key steps, and process optimization.
Total synthesis route: from simple raw materials to complex skeleton construction
The fully synthetic route starts with commercially available organic compounds and gradually constructs the core skeleton of Galantamine through multiple reactions. The key issues that need to be addressed by such methods include stereoselective control (formation of multiple chiral centers), regioselective functional group introduction (such as localization of hydroxyl and methoxy groups), and ring fusion reactions (closure of benzofuran and benzodiazepine rings).
1. Route based on Isovanilin (Trost 2005)
This route uses Isovanillin as the starting material and achieves skeleton construction through the following key steps:
Isocoumarin (1) undergoes electrophilic aromatic substitution under bromine/acetic acid conditions, producing brominated products (2); Subsequently, selective demethylation was carried out using sulfuric acid catalysis to obtain phenolic hydroxyl compound (3).
Compound (3) undergoes reductive amination with Tyramine (4) under sodium borohydride conditions, resulting in the formation of amine intermediate (5); Further react with ethyl formate/formic acid in dioxane to introduce formyl groups, resulting in compound (6).
Compound (6) undergoes oxidative coupling under the action of potassium ferrocyanide (K ∝ Fe (CN) ₆) to form the precursor of the benzofuran ring (7); Subsequently, through the Trost asymmetric allyl alkylation (AAA) reaction, side chains were introduced and stereochemistry was controlled to generate the key intermediate (8).
Intermediate (8) undergoes intramolecular Michael addition under alkaline conditions, forming a benzodiazepine ring; The Galantamine skeleton (9) is obtained through the removal and hydrogenation reduction of ketone protecting groups (such as 1,2-propanediol ketone).
Process optimization points:
Using Trost AAA reaction to achieve precise control of chiral centers, avoiding the lengthy separation steps in traditional methods.
In the oxidative coupling step, potassium ferrocyanide acts as a mild oxidant to reduce the generation of by-products.
2. Route based on 3,4-dimethoxybenzaldehyde (Shieh 1994)
This route uses 3,4-dimethoxybenzaldehyde as the raw material and achieves synthesis through the following steps:
3,4-dimethoxybenzaldehyde generates brominated products under bromine/acetic acid conditions, followed by demethylation catalyzed by sulfuric acid to obtain phenolic hydroxyl compounds.
Phenolic hydroxyl compounds undergo Aldol condensation with Glutaraldehyde under alkaline conditions, resulting in the formation of aldehyde intermediates; Introducing allyl side chains through Horner Wadsworth Emmons reaction to form cyclic precursors.
The precursor of cyclization undergoes hydrogenation reduction under palladium catalysis, controlling the stereoconfiguration of the double bond; Finally, Galantamine Hydrobromamide was obtained by introducing methoxy groups and forming salts with hydrobromic acid.
Process optimization points:
Introducing allyl side chains through Horner reaction to enhance regioselectivity.
Palladium catalyzed hydrogenation achieves stereoselective reduction of double bonds, avoiding the use of chiral catalysts in traditional methods.
Semi synthetic route: Extracting intermediates from natural products
The semi synthetic route uses naturally occurring alkaloids (such as Narwedine) as raw materials and chemically modifies them to obtain Galantamine. The key to this type of method lies in the selective reduction of intermediates and the conversion of functional groups.
1. Route using Narwedine as raw material
Narwedine (11 oxide) is an oxidized derivative of Galantamine, and its reduction can directly yield the target product:
Step 1: Selective Reduction
Narwedine undergoes hydrogenation reduction in methanol or ethanol under palladium carbon (Pd/C) catalysis, selectively removing the 11th oxygen atom to generate Galantamine.
Step 2: Salting and Purification
Galantamine free base reacts with hydrobromic acid in ethanol/water mixed solvent to generate hydrobromide salt; Obtain high-purity products through recrystallization or chromatographic purification.
Process optimization points:
Using Pd/C catalyst to achieve mild reduction and avoid excessive reduction leading to skeleton damage.
In the salt formation step of hydrobromic acid, controlling the solvent ratio can adjust the crystal morphology and improve the fluidity of the product.
2. Route using extracts from Alliaceae plants as raw materials
Some studies have extracted alkaloids such as Lycoramine or Narcissine from plants in the Alliaceae family (such as Snow Flower and Red Gate Orchid) and transformed them through the following steps:
Step 1: Structural Modification
Lycoramine undergoes methylation, oxidation, and other reactions to generate Narwedine precursor.
Step 2: Reduction and Salting
Follow the Narwedine route to complete the reduction and hydrobromic acid salt formation steps.
Process limitations:
The process of plant extraction is complex and limited by the supply of raw materials, making it difficult to achieve industrial production.
The fluctuation of the components in the extract may affect the yield of subsequent reactions.
Key points of process optimization and quality control
Galantamine molecule contains four chiral centers (4aS, 6R, 8aS), and its biological activity is highly dependent on its stereoconfiguration. The following strategies should be adopted in synthesis:
Chiral catalysts, such as palladium complexes used in the Trost AAA reaction, can achieve high enantioselectivity.
Crystallization induced splitting: In the salt formation step, the target crystal configuration is preferentially precipitated by selecting a suitable solvent (such as ethanol/water).
Possible impurities introduced during synthesis include:
Unreacted raw materials: such as residual Narwedine or intermediate aldehydes.
Oxidation by-products: such as 11 oxide derivatives of Galantamine.
Regional isomers: such as isomers caused by incorrect closure positions of the benzodiazepine ring.
Control method:
Process monitoring: Use HPLC or TLC to track reaction progress and terminate the reaction in a timely manner.
Purification process: Use recrystallization, column chromatography, or preparative HPLC to remove impurities.
To reduce production costs, galantamine hydrobromide powder is necessary to optimize the recovery process of solvents and catalysts:
Solvent recovery: Recovering organic solvents such as ethanol and acetic acid through distillation or extraction.
Catalyst recycling: Pd/C catalyst can be reused after filtration and washing.
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