Medicine for treating Parkinson's disease and preparation method thereof
A technology for Parkinson's disease and drugs, applied in the field of drugs and the preparation of said drugs, can solve the problems of undisclosed compound A, etc., and achieve the effect of improving behavioral abnormalities
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Embodiment 1
[0023] The synthesis of embodiment 1 compound A
[0024] Referring to the method of Preparation Example 122 of WO2013 / 151832A1, N-[(4aR,7aR)-7a-(5-cyanothiophen-2-yl)-4,4a,5,6,7,7a-hexahydropyrrole And[3,4-d][1,3]thiazin-2-yl]benzamide, diisopropylethylamine and 2-(2-chloro-5-fluoropyrimidin-4-yl)propane-2 -alcohol as the main raw material to prepare light yellow compound A.
Embodiment 2
[0025] Example 2 tablet
[0026] 【Prescription Composition】
[0027]
[0028] 【Preparation】
[0029] (1) After heating and melting povidone k25, disperse compound A in it while hot, pulverize after quenching, and pass through a 20-mesh sieve to obtain a matrix mixture of compound A;
[0030] (2) Grind calcium phosphate, sodium carboxymethyl starch and hydroxypropyl methylcellulose respectively, pass through an 80-mesh sieve, and then mix calcium phosphate, sodium carboxymethyl starch and hydroxypropyl methylcellulose accounting for 1 / 2 of the total amount Mix base cellulose evenly, use a 50% ethanol solution of an appropriate amount of poloxamer (prepared by dissolving poloxamer in an appropriate amount of 50% ethanol as a wetting agent) to make a soft material, use 8 mesh and 14 mesh successively Screen granulation and dry at 50°C;
[0031] (3) Mix the matrix mixture obtained in step (1), the dry granules obtained in step (2) and the remaining amount of hydroxypropyl me...
Embodiment 3
[0032] Embodiment 3 pharmacodynamic experiment
[0033] 1. Purpose of the experiment
[0034] The purpose of this experiment is to investigate the therapeutic effect of compound A on the Parkinson's disease rat model established by unilateral striatal microinjection of 6-hydroxydopamine, and to provide a preliminary experimental basis for the clinical development of compound A.
[0035] 2. Experimental animals
[0036] The experimental animals used in this experiment were male Wistar rats (purchased from Beijing Weitong Lihua Experimental Animal Technology Co., Ltd.) with a body weight of 200±10 g. Before the start of the experiment, the rats were put into a clean experimental animal room (indoor temperature was about 22° C., relative humidity was 50-55%, light / dark switching every 12 hours) to adapt to the environment for 2 days. Rats had free access to clean food and drinking water.
[0037] 3. Experimental method
[0038] a. Establishment of Parkinson's disease rat model ...
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