Fibrauretine-terephthalic acid medicine eutectic crystal and preparation method thereof
A technology of terephthalic acid and palmatine, applied in the direction of carboxylate preparation, organic chemical methods, antibacterial drugs, etc. Problems such as lumps can be solved, and the effect of improving moisture absorption stability and antibacterial ability can be improved
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Embodiment 1
[0029] A kind of palmatine-terephthalic acid pharmaceutical co-crystal, with palmatine as the active ingredient of the medicine, terephthalic acid as the co-crystal ligand, and the single crystal structure of the palmetine-terephthalic acid pharmaceutical co-crystal The symmetric unit contains a palmatine cation and a terephthalate anion, and the molecular formula is C 21 h 22 NO 4 ·C 8 h 5 o 4 , the relative molecular weight is 517.53, and the single crystal X-ray diffraction structure analysis shows that the single crystal of palmatine-terephthalic acid drug cocrystal is an orthorhombic crystal system, and the space group is P nna , its axial length Shaft angle α=90°, β=90°, γ=90°, Z=4, its structural formula is as follows:
[0030]
[0031] A drug co-crystal of palmetine-terephthalic acid, the characteristic peaks of the XRD spectrum of the drug co-crystal appear at: 6.81-7.22°, 7.93-8.34°, 9.24-9.48°, 13.88-14.26°, 14.48- 14.69°, 16.68-17.08°, 15.70-16.30°...
Embodiment 2
[0037] A kind of preparation method of palmatine-terephthalic acid pharmaceutical co-crystal, 0.07mmol of palmatine hydrochloride and 0.07mmol of terephthalic acid are added to the water of 10mL in molar ratio 1:1, obtain after fully reacting and filtering After the precipitate was dried at 70°C for 3 hours, it was dissolved in a mixed solution of ethanol (5mL) and methanol (5mL). After being dissolved, the resulting mixed solution was slowly volatilized at room temperature to obtain Diformic acid drug cocrystal.
Embodiment 3
[0039] A kind of preparation method of palmatine-terephthalic acid drug co-crystal, 0.07mmol of palmetine hydrochloride and 0.07mmol of terephthalic acid are added into 10mL water in molar ratio of 1:1, fully react and obtain after filtering After the precipitate was dried at 70°C for 4 hours, it was dissolved in a mixed solution of isopropanol (5mL) and ethyl acetate (5mL). After being dissolved, the resulting mixed solution was slowly evaporated at room temperature to obtain a yellow Phalaenol-terephthalic acid drug cocrystal.
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