Baclofen Raw Material Baclofen Powder

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Baclofen Powder Usage and Synthesis .

Baclofen Powder is a type of non-steroidal Anti-inflammatory drug (NSAIDs) commonly used to relieve mild to moderate pain, reduce fever, and reduce It inhibits prostaglandin production in the body, which reduces pain and fever symptoms. Baclofen Raw Materials are absorbed when taken orally. Baclofen Raw Materials are absorbed when taken orally, reaching peak concentrations in about 1-2 hours, and are usually metabolized by the liver within 4-6 hours and subsequently excreted through the kidneys .

Baclofen, also known as Becomfen, Baclofen, and Liruxin, is a derivative of gamma-aminobutyric acid, an antispasmodic drug that acts as a skeletal muscle relaxant and sedative in the brain and spinal cord of the central nervous system. It inhibits the release of excitatory amino acids such as glutamate and menadione by stimulating the receptors, thereby inhibiting the transmission of monosynaptic and polysynaptic reflexes in the brain and spinal cord of the central nervous system, thus acting as an antispasmodic agent.

Application/Function of Baclofen Powder.

Baclofen has been used clinically as a racemic agent for the treatment of muscle spasticity since the mid-1960s. Recent studies have also found that it can significantly reduce gastroesophageal reflux and improve its symptoms, effectively alleviate the symptoms of dystonia in children, and treat urinary dysfunction after central intractable spinal cord injury.

In addition, the clinical application of intrathecal injection therapy can further improve the clinical efficacy and adjust the drug dosage at any time to stabilize the therapeutic effect. In the past 10 years, the clinical application of baclofen, a central muscle relaxant, has made great progress, especially in the treatment of neurorehabilitation for reducing muscle tone and pain relief, and has gained much experience.

Mechanism of action of Baclofen Powder:

GABA is the main inhibitory transmitter in the brain and spinal cord of the central nervous system, but it cannot cross the blood-brain barrier. GABA is the main inhibitory transmitter in the brain and spinal cord of the central nervous system, but it cannot cross the blood-brain barrier, and can cross the blood-brain barrier by changing from a hydrophilic substance to a lipophilic one through the attachment of the carbon atom to the para-chlorophenyl group, which is baclofen.

The main effect of GABA is to agonize the receptors of GABA, inhibit the release of excitatory amino acids such as aspartate and glutamate through synapses, and cause the outflow of K+ and Ga+2 ions from neurons, resulting in hyperpolarization, reducing the transmission of monosynaptic and polysynaptic reflexes, promoting the normal activity of intermediate neurons and reducing the activity of motor neurons, thus relieving the skeletal muscle spasm caused by damage to the pyramidal fasciculus, reducing muscle tone, and promoting motor activity. This can alleviate the skeletal muscle spasm caused by the damage of the pyramidal bundle, reduce the muscle tone and promote the recovery of motor function.

Preparation process of Baclofen Powder.

Ethyl p-chlorobenzylidene-bis-acetoacetate is formed by the condensation of p-chlorobenzaldehyde with ethyl acetoacetate. Hydrolyzed by heat to yield p-chlorophenylglutaric acid. Dehydration and cyclization with ethyl anhydride to produce p-chlorophenyl glutaric anhydride. Then amination with concentrated ammonia to form p-chlorophenyl glutaric acid amide, and finally ring opening and degradation to obtain.

This product is an antispasmodic agent. It inhibits monosynaptic and polysynaptic spinal transmission by agonizing GABA-receptors and inhibiting the release of the excitatory amino acids glutamate and menadione. Thus, it can reduce the increased muscle tone of limbs caused by spinal cord lesions, multiple sclerosis, and spinal cord injury. It is used for muscle spasm caused by spinal cord and brain diseases or injuries.

Chemical properties white powder. Melting point 206-208℃. Soluble in hot water, its aqueous solution is neutral, almost insoluble in ethanol, ether, acetone and other organic solvents, easily soluble in acidic and alkaline aqueous solutions. The melting point of chlorphenamine tyrosine hydrochloride is 179-181℃. UsesThe product is a skeletal muscle relaxant and antispasmodic agent that acts on the spine. It is used in spasm of skeletal femur of multiple sclerosis; spinal cord infection, degenerative muscle spasm; spinal cord traumatic, redundant muscle spasm.

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