Application of fingolimod and analogue thereof in preparing medicines for treating cerebral infarction
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A technology with a similar structure to fingolimod hydrochloride, applied in the field of fingolimod and its structural analogs, can solve the problems of no cerebral infarction and achieve the effect of expanding clinical indications, significant curative effect, and highlighting the promotion prospect
Inactive Publication Date: 2014-11-19
施福东 +10
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[0004] In the prior art, fingolimod is only used to treat multiple sclerosis, and there is no application of this drug in the treatment of cerebral infarction
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Embodiment 1
[0027] 1. Preparation of drugs
[0028] Take 50g of fingolimod and 2450g of starch, mix 950g of starch with water to make a thin slurry, then gradually add the remaining starch and all of fingolimod to the slurry under stirring, stir all the ingredients evenly, make granules, and then Sieve, dry, and pack into capsules.
[0029] 2. Selection of experimental objects
[0030] From March 2013 to December 2013, 11 patients with onset time of more than 4.5 hours but less than 72 hours had the first episode of anterior circulation, the infarct volume was more than 5ml, and the National Institutes of Health stroke score was more than 5 points. Patients with lacunar infarction, without arrhythmia, macular edema, tumors and immunosuppressants were used as experimental subjects, and 11 matched controls with clinical and imaging characteristics.
[0031] 3. Experimental method
[0032] Patients were divided into fingolimod treatment group and control group, the control group received ...
Embodiment 2
[0048] Take 50g of fingolimod and 2450g of starch, mix 950g of starch with water to make a thin slurry, then gradually add the remaining starch and all of fingolimod to the slurry under stirring, stir all the ingredients evenly, make granules, and then Sieve and dry to form granules.
Embodiment 3
[0050]Take 50g of fingolimod, 2300g of starch, and 150g of magnesium stearate, mix 950g of starch and water to make a thin slurry, and then gradually add the remaining starch, all of fingolimod and all of the stearin to the slurry while stirring Magnesium acid, all stirred evenly, dried and compressed into tablets, film-coated to form tablets.
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Abstract
The invention provides a new application of fingolimod and an analogue thereof in preparing medicines for treating cerebral infarction and further shows the mechanism of treatment, effective dose, suitable dosage form and the specific compound of the analogue. Experiments confirm that the fingolimod and the analogue thereof can relieve lymphocyte infiltration caused by cerebral infarction, the relieving effect can be taken as a new target for treating cerebral infraction, furthermore, based on the new properties of the fingolimod and the analogue thereof, the new application of the fingolimod and the analogue thereof in preparing medicines for treating cerebral infraction is confirmed. The clinical applicability of the fingolimod and the analogue thereof is enlarged, the fact that the immune cells involve in cerebral infarction pathological lesion is disclosed, and the medicine prepared by the fingolilmod and the analogue thereof has a remarkable curative effect on cerebral infraction injure, and has prosperous generalization prospect.
Description
technical field [0001] The present invention relates to a new application of fingolimod and its structural analogues, in particular to an application of fingolimod and its structural analogues in the preparation of drugs for treating cerebral infarction. Background technique [0002] Cerebral infarction is a common clinical disease with high morbidity and mortality rates. Except for 4.5 hours of thrombolytic therapy, there is currently no effective drug for treatment. [0003] Fingolimod is an immunomodulator, mainly used in the treatment of multiple sclerosis, which was approved by the FDA in 2010. It is originally an immunosuppressant synthesized by chemically modifying the antibiotic component myriocin (ISP-I) extracted from the culture fluid of Cordyceps sinensis (Ascomycete subphylum Chiromycin) and is a structural analog of sphingosine, which is phosphorylated in vivo After that, it binds to the S1P receptor on the lymphocytes, thereby inhibiting the migration of lymp...
Claims
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