Co-crystal of pyrazinamide and quercetin and preparation method of co-crystal
A technology of pyrazinamide and quercetin, which is applied in the field of pharmaceutical co-crystals of pyrazinamide and quercetin and its preparation, can solve the problems of limited clinical application and low bioavailability, and achieve high yield and purity, The effect of low cost and simple process
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[0021] Specific embodiment 1: The structural formula of the pyrazinamide-quercetin co-crystal of this embodiment is [C 5 H 5 N 3 O·C 15 H 10 O 7 ·H 2 O], a basic structural unit is formed by a pyrazinamide molecule, a quercetin molecule, and a water molecule. The pyrazinamide-quercetin co-crystal is a monoclinic crystal system, and the space group is P 2 1 / n, the unit cell parameters are: a = 8.759 Å, b = 23.793 Å, c = 10.012 Å, α = 90°, β = 114.56°, γ = 90°. The PXRD characteristic diffraction peaks appear at 7.422°, 11.702°, 13.362°, 15.901°, 17.799°, 21.183°, 23.042°, 23.402°, 26.703°, 26.978°.
[0022] The pyrazinamide-quercetin co-crystal described in this embodiment is composed of a pyrazinamide molecule, a quercetin molecule, and a water molecule combined together through supramolecular effects such as hydrogen bonds. Such as figure 2 As shown, the pyrazinamide molecules in the co-crystal form hydrogen bond dimers through amide-amide synthons; four quercetin molecules an...
Example Embodiment
[0023] Specific embodiment 2: The preparation method of the pyrazinamide-quercetin co-crystal of this embodiment is implemented in the following steps:
[0024] Mix the pyrazinamide crude drug and quercetin at a molar ratio of 1:1, add them to the ethanol solution at 60 ℃, stir for 1 to 2 hours and then filter while hot. After the filtrate is allowed to stand and cool to room temperature, a solid phase will precipitate. The pyrazinamide-quercetin co-crystal was obtained.
Example Embodiment
[0025] Specific embodiment three: This embodiment is different from the specific embodiment two in that the solid-to-liquid ratio of the mixture powder and ethanol in the system is 100 mg: (10-15) mL. Other steps and parameters are the same as in the second embodiment.
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