Eutectic substance of donepezil and irbesartan as well as preparation method and composition of eutectic substance and applications of eutectic substance and composition
A technology of donepezil and eutectic, applied in the field of eutectic solid state form, can solve the problems of unseen donepezil and irbesartan
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Embodiment 1
[0069] Preparation method 1 of donepezil and irbesartan co-crystal:
[0070] As shown in the table below, take appropriate amounts of donepezil and irbesartan and put them into a mortar with a molar ratio of 1:1, add an appropriate amount of solvent, and manually grind for an appropriate time. It was analyzed by powder X-ray diffraction, and its diffraction pattern was consistent with that in Figure 1, indicating that the obtained sample was a cocrystal of donepezil and irbesartan.
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[0073]Preparation method 2 of donepezil and irbesartan co-crystal:
[0074] As shown in the table below, take appropriate amounts of donepezil and irbesartan and put them into a ball mill jar at a molar ratio of 1:1, add an appropriate amount of organic solvent, select an appropriate ball-to-material ratio, set an appropriate speed, and grind for an appropriate time. Carry out powder X-ray diffraction analysis to it, its diffraction pattern and figure 1 Consistent, indica...
Embodiment 2
[0081] In Vitro Dissolution and Release Characteristics of Cocrystals of Donepezil and Irbesartan
[0082] The solubility characteristics of donepezil-irbesartan co-crystal and irbesartan bulk drug in aqueous solution and 0.5% SDS aqueous solution were investigated. Refer to the "Technical Guidelines for Dissolution Test of Ordinary Oral Solid Preparations" for determination, the model-independent similarity factor (f2) method is used for the comparison of dissolution curves, and the raw materials and physical mixtures and the co-crystals of donepezil and irbesartan are compared through the calculation of f2 values The similarity of the dissolution curves of the samples in the two solvent systems, when the f2 value is higher than 50, the two curves are considered similar, and when the f2 value is lower than 50, the two curves are considered to be different. In the experiment, the irbesartan sample was used as a reference, and the model-independent similarity factor f2 value wa...
Embodiment 3
[0089] Example 3 Donepezil and irbesartan co-crystal absorption characteristics and blood drug concentration characteristics in rats:
[0090] The metabolic characteristics of the donepezil and irbesartan co-crystals involved in the present invention include the following processes:
[0091] Nine SD rats were randomly divided into 3 groups with 3 rats in each group. No food or water was allowed 12 hours before administration. The weight of the rat was weighed, and the physical mixture of donepezil and irbesartan, the raw material of irbesartan, and the cocrystal samples of donepezil and irbesartan were packed according to the irbesartan dosage of 100 mg kg-1. Put the drug powder into the solid applicator directly into the stomach of the rat through the oral cavity. At 5 minutes, 15 minutes, 30 minutes, 45 minutes, 1 hour, 1.5 hours, 2 hours, 3 hours, 4 hours, 6 hours, 9 hours, 12 hours, and 24 hours after administration, blood was collected from the ocular vein plexus and he...
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