Co-amorphous compound of donepezil and valsartan, preparation method, composition and use thereof
A kind of donepezil, amorphous technology, applied in the direction of drug combination, active ingredients of heterocyclic compounds, organic chemistry, etc., can solve the problems such as no co-crystal or co-amorphous compound formed between donepezil and valsartan, no research content, etc. , to achieve the improvement of pharmacokinetic parameters, high blood drug concentration, and the effect of being beneficial to treatment and prevention
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Embodiment 1
[0078] Donepezil-valsartan co-amorphous solid substance preparation method 1
[0079] Take an appropriate amount of donepezil and valsartan, the molar ratio of the two is 1:1, completely dissolve the sample in the listed solvent at room temperature, heat to reflux, quickly remove the solvent under vacuum, and dry the sample in vacuum. Powder X-ray diffraction analysis is carried out to the obtained sample, and its diffraction pattern is consistent with figure 1 Consistent, indicating that the obtained sample is a co-amorphous compound of donepezil and valsartan. See Table 2 for specific examples.
[0080] Table 2 Donepezil-valsartan co-amorphous solid substance preparation method 1 specific example
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[0083] Donepezil-valsartan co-amorphous solid substance preparation method 2
[0084] Take an appropriate amount of donepezil and valsartan, the molar ratio of the two is 1:1, completely dissolve the sample in the solvent listed in the following table at...
Embodiment 2
[0093] The preparation method 1 (tablet) of combination pharmaceutical preparation:
[0094] A preparation method of a combination drug tablet, characterized in that the pure product of donepezil and valsartan co-amorphous compound, or the mixed solid substance containing donepezil and valsartan co-amorphous compound in any proportion is used as the raw material of the combination drug Medicine, use several kinds of excipients as the adjuvant components for preparing the combination drug tablet, and make a tablet sample with a drug content of 10-500 mg per tablet according to a certain ratio. Table 5 gives the tablet formula ratio:
[0095] Table 5 The preparation formula of donepezil and valsartan co-amorphous compound combination drug tablet
[0096]
[0097] The method for preparing tablet preparations from the pure substance of donepezil and valsartan co-amorphous compound or the mixed solid substance raw material containing donepezil and valsartan co-amorphous compound...
Embodiment 3
[0109] Dosage 1 (tablet) of the combination drug of donepezil and valsartan co-amorphous compound:
[0110] A pharmaceutical composition developed by using samples of co-amorphous compound of donepezil and valsartan as the active ingredient of the drug, characterized in that the co-amorphous compound of donepezil and valsartan is used as the active ingredient of the drug, and the daily dosage is 300 mg , which can be prepared as a 100mg ordinary tablet 3 times a day / each time, or a 300mg tablet 1 time a day / each time.
[0111] Dosage 2 (capsule) of the combination drug of donepezil and valsartan co-amorphous compound:
[0112] The pharmaceutical composition developed by using the co-amorphous compound of donepezil and valsartan as the active ingredient of the drug is prepared and developed, which is characterized in that the co-amorphous compound of donepezil and valsartan is used as the active component of the drug, and the daily dosage is 500mg , which can be prepared as 2 ...
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