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Orphenadrine Citrate Powder is the core component of Orfenadine and is a white or almost white crystalline powder. Chemical formula C18H23NO · C6H8O7, CAS 4682-36-4, molecular weight approximately 461.5 g/mol. It usually exists in the form of citrate and is an odorless compound.
Due to its hydrochloride nature, it has high solubility and stability. It has a high solubility in water and is easily soluble in water at room temperature. It can also be soluble in various organic solvents such as ethanol, methanol, and chloroform. Citrate of ortho toluidine is a derivative of ethanolamine, which has certain antihistamine effects, local anesthesia, antiemetic and anticholinergic effects.
It is a component of skeletal muscle relaxation medication that acts on the central nervous system, producing muscle relaxation effects. It is a drug with analgesic and anticholinergic effects, commonly used to relieve muscle spasms and related pain. As a nervous system drug, it has broad application value in the medical field. It is mainly used to relieve local muscle spasmodic pain, treat diseases such as arteriosclerosis and Parkinson's disease.
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Chemical Formula |
C24H31NO8 |
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Exact Mass |
461 |
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Molecular Weight |
462 |
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m/z |
461 (100.0%), 462(26.0%), 463(2.7%), 463 |
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Elemental Analysis |
C, 80.26; H, 8.61; N, 5.20; O, 5.94 |
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Morphological |
neat |
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Color |
powder |
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Melting point |
132-1340 ° C |
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Boiling point |
360 ° C |
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Storage conditions |
sealed in dry, 2-8 ° C |
Solubility sparingly soluble in water, slightly soluble in ethanol (96 per cent), Morphological neat, InChIKeyASDBZPGDZBFZAH-UHFFFAOYSA-N, Hazard symbol (GHS), GHS07,GHS08, Warning word, Hazard description h302-h351, Precautions p280-p301 + p312 + p330-p281, Dangerous goods signs xn, Xi, Hazard category code 22-40-20 / 21 / 22, Safety instructions 22-36-62-38-36 / 37 / 39-28-26-24 / 25, Dangerous goods transport No. 3249, WGK Germany 3, HazardClass 6.1(b), PackingGroup III
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Orphenadrine Citrate Powder, also known as Orphenadrine Citrate or o-Methyldiphenhydramine Citrate, is a medication with central muscle relaxation effects, as well as antihistamines, anticholinergic and neuroprotective properties. Its chemical structure is an ethanolamine derivative, which exerts multiple pharmacological effects by acting on the central nervous system and neurotransmitter system.
Clinical Application: Muscle Relaxation and Pain Management
1. Adjuvant treatment for acute muscle spasms
The core use of Fennarin citrate is to relieve acute muscle spasmodic pain caused by trauma, strain, or degenerative osteoarthritis. Its mechanism of action involves regulating the motor center of the central nervous system, reducing muscle tone and relieving pain by inhibiting the dopamine, serotonin, and norepinephrine pathways.
In clinical practice, this drug is often used in combination with nonsteroidal anti-inflammatory drugs (NSAIDs) to enhance analgesic effects. For example, in the short-term management of acute low back pain or neck and shoulder syndrome, Fennarin citrate can be used as a second-line muscle relaxant, especially for patients who are intolerant to benzodiazepines.
2. Adjuvant treatment for Parkinson's disease and movement disorders
In early research, Fenneryl citrate was used to alleviate muscle stiffness symptoms associated with Parkinson's disease. Its non competitive NMDA receptor antagonistic effect (Ki=6.0 μ M) can regulate glutamatergic neurotransmission, alleviate typical symptoms such as bradykinesia and muscle rigidity.
Although this indication has gradually been marginalized with the popularity of more efficient drugs such as levodopa, in some developing countries or resource limited areas, Fennercept citrate remains an economically effective adjuvant treatment option. In addition, its relieving effect on drug-induced extrapyramidal reactions (such as tremors caused by antipsychotic drugs) has also been clinically validated.
3. Postoperative Rehabilitation and Sports Medicine
In the postoperative rehabilitation of orthopedics, Fennarizine citrate promotes muscle relaxation, reduces the frequency of spasms, and accelerates patient functional recovery. For example, after knee replacement surgery, patients who use this medication experience a reduction in joint range of motion improvement time by approximately 30%.
In the field of sports medicine, it is used to treat local pain caused by sports injuries such as muscle strains and ligament sprains. It is usually administered twice daily with 100mg tablets for a treatment period of no more than 7 days.
Neuroscience Research: Neuroprotection and Disease Models
1. Research on pain mechanisms
As an NMDA receptor antagonist, Orphenadrine Citrate Powder is used to explore the central sensitization mechanism of pain. For example, in the formalin induced persistent pain model, the drug can dose dependently inhibit abnormal firing of spinal dorsal horn neurons, providing a theoretical basis for the treatment of chronic pain.
2. Research on neurodegenerative disease models
Fennarizine citrate is widely used in neuroscience research to construct models of neurodegenerative diseases. Its neuroprotective effect is achieved through the following mechanisms:
Antioxidant stress: In the cerebellar granule cell toxicity model induced by 3-nitropropionic acid (3-NPA), treatment with 12 μ M fenadine citrate for 24.5 hours significantly inhibited cell aggregation, volume reduction, and neuronal fragmentation, with a 40% increase in cell survival rate.
Anti apoptotic effect: Animal experiments have shown that intraperitoneal injection at a dose of 30mg/kg can reduce 3-NPA induced mortality in rats (from 80% to 10-40%) and restore weight loss. The mechanism is related to the inhibition of the expression of mitochondrial apoptosis pathway related proteins (such as HSP27).
Neurotransmitter regulation: By blocking HERG potassium ion channels, fenadine citrate can regulate neuronal excitability and improve cognitive function in Alzheimer's disease models.
Special purpose and exploratory applications
1. Treatment for motion sickness
The anticholinergic effect of Fennarin citrate makes it have certain potential in the treatment of motion sickness (such as motion sickness and seasickness). It alleviates symptoms such as nausea and vomiting by inhibiting excessive excitation of the vestibular nucleus. Clinical small sample studies have shown that a dose of 50mg orally takes effect within 30 minutes and the therapeutic effect lasts for about 6 hours.
2. Adjuvant treatment for drug addiction and withdrawal
In the treatment of opioid withdrawal, fentanyl citrate can alleviate withdrawal symptoms such as anxiety and muscle spasms by regulating central nervous system excitability. Preliminary studies have shown that its combination with clozapine can increase the completion rate of withdrawal by 25%.
3. Application in the field of veterinary medicine
In animal medicine, Fennarin citrate is used to treat muscle spasms in dogs and cats. For example, in hind limb paralysis caused by intervertebral disc disease, intramuscular injection at a dose of 0.5mg/kg can significantly improve motor function and is safer than traditional benzodiazepines.
The preparation of fenadryl citrate has been reported in the patent US2567351. According to the example provided by US2567351, the following process can be installed for the experiment:
(1) Add N, N-dimethylethanolamine into xylene, protect it with nitrogen, keep it at a certain temperature, slowly add 2 - methyldiphenyl chloromethane, and stir for reaction. After the reaction is completed, it is cooled, and there are solids at the bottom of the reactor. Take out the upper clear liquid, remove the solvent xylene under vacuum conditions, and obtain o-toluidine crude product;
(2) The crude product of o-toluidine is added to the isopropyl alcohol solution of oxalic acid to generate o-toluidine oxalate, filtered, and vacuum dried;
(3) The o-toluidine oxalate is treated with KOH solution to obtain o-toluidine, and then extracted with anhydrous ether, washed with water, dried, and drained with ether to obtain pure o-toluidine. The experimental process is complicated, the requirements for conditions are high, and the yield of o-toluidine is relatively low, which is not suitable for industrial production.
A synthesis method of orfenadine citrate powder, comprising the following steps:
Step (1): Synthesis of intermediate o-toluidine
Mix N, N-dimethylethanolamine (usually used as a base or catalyst in organic synthesis) with 2-methyldiphenyl chloromethane (which may refer to the chloride of 2-methyldiphenylamine, but the standard name does not include the term "2-methyldiphenyl chloromethane").
Stir the mixture and raise the temperature to the reaction temperature for reaction. This step may be to replace the chlorine atom with the nitrogen atom of N, N-dimethylethanolamine through nucleophilic substitution reaction, thereby generating a derivative of o-toluidine. However, it should be noted that N, N-dimethylethanolamine is usually not directly used for such reactions and may require other more suitable bases or catalysts.
After the reaction is completed, cool the mixture and extract the upper solution with a solvent (possibly to remove unreacted raw materials and by-products). Then, wash the extraction solution with detergent and dry it with a desiccant. Finally, the solvent is evaporated to obtain the intermediate o-toluidine (or its derivatives).
Step (2): Synthesize o-toluidine citrate salt
(1) Dissolve citric acid:
Dissolve citric acid in a crystalline solvent. The selection of crystallization solvents should be based on the difference in solubility between citric acid and ortho toluidine for subsequent crystallization.
(2) Add intermediate:
Slowly add the intermediate o-toluidine (or its derivatives) obtained in step (1) and stir for 0.5h-1h.
(3) Crystallization and washing:
As the reaction proceeds, white crystals will precipitate, which are salts formed by o-toluidine and citric acid. Wash the crystals with a washing solvent to remove unreacted raw materials and by-products.
(4) Drying:
Dry the washed crystals to obtain ortho toluidine citrate.
matters needing attention
Optimization of reaction conditions:
Further optimization of reaction temperature and time may be needed to achieve higher yields and purity.
Raw material purity:
Raw material purity: The purity of raw materials has a significant impact on the quality and yield of the final product, therefore high-purity raw materials should be used.
Safe operation:
During the operation process, attention should be paid to the safety of chemicals and relevant safety operating procedures should be followed.
Product identification:
The final product should be identified through appropriate analytical methods to ensure that its structure and purity meet the requirements.
Compared with the prior art, the method has the following beneficial effects:
The synthesis method of the invention does not use toxic solvent, thus reducing environmental pollution and cost;
The purification process of intermediates in the synthesis process is simplified, simplifying the operation process, making the actual production easier, increasing the product yield and reducing the pollution;
The commonly used solvent is used in the process of crystallization and salification, and the operation process is simple, which is conducive to industrial Orphenadrine citrate powder.
Frequently Asked Questions
What is orphenadrine citrate used for?
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Norflex Tablet 100mg (Orphenadrine) x20 | MedeCifyOrphenadrine citrate is a prescription skeletal muscle relaxant used alongside rest and physical therapy to relieve acute pain, spasms, and stiffness from muscle injuries. It works by acting on the central nervous system (CNS) and providing anticholinergic effects. Common side effects include dry mouth, dizziness, and sedation.
Is orphenadrine citrate safe to take?
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Orphenadrine citrate is generally safe for short-term use in treating acute muscle pain when taken as prescribed, though it can cause common side effects like drowsiness, dizziness, and dry mouth. It is not recommended for long-term use, especially in older adults, and carries risks of serious allergic reactions, cardiac issues, or dependency.
Is orphenadrine used for anxiety?
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Diazepam is a benzodiazepine that treats anxiety, alcohol withdrawal, muscle spasms, and seizures. It works by increasing gamma-aminobutyric acid (GABA) levels in the brain. Orphenadrine, on the other hand, is a muscle relaxant used specifically for relieving muscle pain and discomfort.
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