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Application of 2-phenylphenol and derivatives thereof to medicine for treating epilepsia
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A technology of biphenol and derivatives, applied in the field of medicine, to achieve the effects of strong affinity, excitotoxicity protection, and brain protection
Active Publication Date: 2012-04-11
XIAN LIBANG PHARMA
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Problems solved by technology
Although epilepsy continues to be studied intensively, the pathogenesis of epilepsy is still poorly understood, and current medications provide only partial relief in patients with epilepsy [3][4] , the effective rate for patients with developing grand mal seizures is only 60% to 70%.
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Embodiment 1
[0027] The effect of 2,2',6,6'-tetraisopropyl-4,4'-biphenol on the cortical EEG of pentylenetetrazol epilepsy model rats during the onset period. Material: male SD rats, body weight 250~ 300g, purchased from the Experimental Animal Center of the Fourth Military Medical University. Pentylenetetrazol (Sigma, USA).
[0028] Main instruments: multi-channel physiological recorder, special electrode, dental bench drill, general electroencephalogram.
[0029] Method:
[0030] (1) Preparation of pentylenetetrazol epilepsy model
[0031] 35mg / kg pentylenetetrazol was injected intraperitoneally to induce seizures.
[0032] (2) Pentylenetetrazol epilepsy model rat cortical EEG recording during seizure
[0033] First, the rats are anesthetized with isopentobarbital. Cut the scalp to expose the skull, drill a small hole on the left and right with a dental electric drill 3mm next to the junction of the coronal suture and the sagittal suture, implant electrodes, fix the electrodes and suture the sca...
Embodiment 2
[0042] The other diphenols or derivatives thereof according to the present invention also have the same therapeutic effect as the 2,2',6,6'-tetraisopropyl-4,4'-diphenols described in Example 1.
Embodiment 3
[0043] Example 3: Pharmaceutical composition
[0044] 2,2',6,6'-Tetraisopropyl-4,4'-Biphenol is passed through a 100 mesh sieve for later use; 2,2',6,6'-Tetraisopropyl-4,4'- Diphenol 80.0g, microcrystallinecellulose 45.0g, croscarmellose sodium 5.0g, mixed uniformly, made of soft material with aqueous solution as wetting agent, granulated by 30 mesh screen, ventilated and dried at 55℃, Granules, ready for use; add 0.5 g of micro-powdersilica gel, 1.0 g of magnesiumstearate and mix well, and press to obtain about 1000 round tablets to obtain compressed tablets.
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Abstract
The invention belongs to the technical field of medicines and mainly relates to application of 2-phenylphenol and derivatives thereof to a medicine for treating epilepsia. The structural formula of the 2-phenylphenol derivatives is shown in the specification of the invetion, wherein R1 and R2 can be hydroxide groups, sulfhydryl groups at the same time or one is hydroxide radical and the other is sulfhydryl group; and R1 and R2 can be alkyls of C1-C6, alkenyls of C2-C6, alkyls and aryls of C2-C6 or acyls or alkenyls of C2-C6 and at least one of R1 and R2 is hydroxide group.
Description
Technical field [0001] The invention belongs to the field of medical technology, and mainly relates to the application of diphenol and its derivatives in drugs for treating epilepsy. Background technique [0002] Epilepsy is a chronic disease caused by sudden abnormal discharge of brain neurons, leading to transient brain dysfunction [1][2] . The epileptic seizure refers to the clinical phenomenon caused by abnormal and excessive supersynchronized discharge of brain neurons. It is characterized by sudden and transient symptoms, which have a variety of manifestations due to the different locations of abnormally firing neurons in the brain. Clinically, it can be divided into generalized tonic-clonic seizures (grand seizures), absence seizures (minor seizures), simple partial seizures, complex partial seizures (psychomotor seizures), and autonomic seizures (intermittent seizures). ). [0003] Due to the increasing prevalence of epilepsy at home and abroad, it has become a health is...
Claims
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