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Berberine-chrysin pharmaceutical eutectic crystal and preparation method thereof
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A technology of chrysin and berberine, applied in the field of berberine-chrysin drug co-crystal and its preparation, achieving the effect of simple and easy preparation method and clear crystal structure
Active Publication Date: 2018-09-25
MINJIANG UNIV
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At present, there is no public report on the drug co-crystal formed by berberine and chrysin
Method used
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Embodiment 1
[0027] Dissolve 0.371 g of berberine hydrochloride, 0.254 g of chrysin and 0.04 g of sodiumhydroxide in 20 mL of absolute ethanol respectively, mix and stir for 1 hour, add 0.254 g of chrysin in batches, and continue stirring for 2 hours to obtain a large amount of yellow precipitate , suction filtration, the obtained precipitate was washed with absolute ethanol, and dried in the air; the obtained powder was recrystallized in absolute ethanol to obtain a berberine-chrysin drug cocrystal.
[0028] figure 1 It is the XRD figure of the berberine-chrysin drug cocrystal crystal prepared in the present embodiment. Depend on figure 1 It can be seen that the prepared crystals, with a diffraction angle of 2 θ ° ± 0.1 is expressed as: 8.2°, 8.9°, 9.8°, 11.3°, 11.8,° 12.8°,13.7°, 14.5°, 14.8°, 15.5°, 16.3°, 16.5°, 17.3°, 17.6°, 18.0° , 18.4°, 18.7°, 19.3°, 19.5°, 19.8°, 20.1°, 20.5°, 21.5°, 22.0°, 22.4°, 22.9°, 23.4°, 23.6°, 24.3°, 24.7°, 25.0°, 26.0 °, 26.6 °, 27.4 °, 28.1 °, 28...
Embodiment 2
[0033] Pharmacokinetic parameters of berberine-chrysin co-crystal in rats:
[0034] SD male rats with a body weight of 190-210 g were reared under conventional feeding conditions, free to drink water, and after fasting for 12 hours, press
[0035] 24 mg / kg (chrysin dosage) was administered orally, and blood was collected from the retroocular venous plexus at 0.10, 0.25, 0.25, 0.75, 1, 2, 3, 6, 8, 10, and 12 h before and after administration About 0.5 ml, centrifuge at 4000 rpm for 10 min. Take 200 μl of plasma, add 400 μl of methanol, vortex for 2 minutes, centrifuge at 10,000 rpm for 10 minutes, take the supernatant, and blow dry with nitrogen. Add 100 μl of mobile phase (methanol:water=50:50), vortex for 1 min, centrifuge at 10,000 rpm for 1 min, and take 40 μl of the supernatant for HPLC-MS detection. The HPLC-MS detection system is Aligent 1260 LC-6410 MS high-performance liquid chromatographysystem, and the chromatographic column is Ultimate XB-C 18 (2.1×50 mm, 3.5 μm),...
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Abstract
The invention discloses a berberine-chrysin pharmaceutical eutectic crystal and a preparation method thereof and belongs to the technical field of pharmaceutical crystallization. The berberine-chrysinpharmaceutical eutectic crystal is prepared by dissolving berberinehydrochloride, chrysin and sodiumhydroxide in ethanol according the ratio; a eutectic crystal structure unit comprises berberine cations, chrysin anions and chrysin molecules at the mol ratio of 1 to 1 to 2 and a molecular formula is [C20H18N O4]+[C15H9O4]-2[C15 H10 O4]. The preparation method disclosed by the invention has theadvantages of simplicity and feasibility, low cost and high crystal yield; the relative bioavailability of the chrysin of the prepared pharmaceutical eutectic crystal in rats is remarkably improved relative to the relative bioavailability of the pure chrysin, and the relative bioavailability is 1.7 times as much as the relative bioavailability of the pure chrysin.
Description
technical field [0001] The invention belongs to the technical field of drugcrystallization, and in particular relates to a berberine-chrysin drug co-crystal and a preparation method thereof. Background technique [0002] The crystalline form of drug molecules is the core constraint factor for the efficacy of solid drugs. For a specific drug, different crystalline forms such as polymorphs, salt forms, and co-crystals determine different pharmaceutical effects, and one crystalline form may be better than another. Drug co-crystals do not change the chemical structure of drug molecules, but can effectively improve the druggability of drug molecules through intermolecular hydrogen bonding, and thus become a highly valued drug crystal form. In July 2015, the US FDA approved Novartis Pharmaceuticals' new anti-heart failure drug Entresto (sacubitrilvalsartansodium tablets), which further set off an upsurge in drug co-crystal research[ Chem.Commun ., 2016, 52, 640-655]. Valsart...
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