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Baclofen Powder is an antispasmodic drug that inhibits monosynaptic and polysynaptic spinal transmission by agonising GABA-receptors and inhibiting the release of the excitatory amino acids glutamate and aspartate. Thus, it can reduce the increase of limb muscle tension caused by spinal cord lesions, multiple sclerosis and spinal cord injury. It is used for muscle spasms caused by spinal cord and brain diseases or injuries.
Uses and functions of Baclofen Powder.
Baclofen Powder is a spinal muscle relaxant and antispasmodic. It is indicated for spasticity of the skeletal muscles in multiple sclerosis; spasticity of the spinal cord in infections and degeneration of the spinal cord; spasticity of the spinal cord in traumatic, redundant muscle spasms.
Baclofen Powder is the most effective muscle relaxant available with the fewest side effects.
Baclofen Powder is used as a skeletal muscle relaxant and sedative for the spinal cord.
Pharmacological Effects of Baclofen Raw Powder.
Baclofen Powder is a muscle relaxant that acts on the spinal cord. Baclofen inhibits monosynaptic and polysynaptic reflexes in the spinal cord by stimulating GABAB receptors, thereby inhibiting the release of the excitatory amino acids glutamate and aspartate.
Baclofen Powder has no effect on the transmission of impulses between neuromuscles and is analgesic. In neurological disorders associated with skeletal muscle spasms, the clinical effects of Baclofen are characterised by relief of reflex muscle spasms and significant relief of painful spasms, automatisms and clonus. Baclofen is effective in improving mobility, facilitating activities of daily living, catheter insertion and physiotherapy. Indirect effects of baclofen administration also include the prevention and promotion of healing of bedsores, improvement of sleep (due to the elimination of painful muscle spasms), and improvement of bladder and anal sphincter function. This can significantly improve the quality of life of patients.
Production method of Baclofen.
Baclofen Powder condenses p-chlorobenzaldehyde with ethyl acetoacetate to form p-chlorophenylmethylene-bis-acetoacetate. Hydrolysis with heated water gives p-chlorophenylglutaric acid. Dehydration and cyclisation with ethyl anhydride to form p-chlorophenylglutaric anhydride. Then aminated with concentrated ammonia to produce p-chlorophenyl glutaric acid imide, and finally ring-opened and degraded to p-chlorophenyl aminotyrosic acid.
The final ring-opening and degradation was carried out as follows: 42.25 g of β-(p-chlorophenyl)glutaric acid imide was added to 200 ml of an aqueous solution containing 8.32Chemicalbookg of sodium hydroxide under stirring. The mixture was heated at 50 °C for 10 min, cooled to 10-15 °C, and 200 ml of aqueous solution containing 40.9 g of sodium hydroxide was added dropwise, and after 20 min, 38.8 g of bromine was added, and stirred at 20-25 °C for 8 h. The pH of the reaction solution was carefully adjusted to 7 with concentrated hydrochloric acid, after which fine crystals of β-(p-chlorophenyl)-γ-amino-butanoic acid were precipitated, and then recrystallised from water, melting point 206-208 °C.
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