Disclosed in the present invention are a bulleyaconitine D crystal and a preparation method therefor. FIG. 1 shows an X-ray powder diffraction spectrum of the crystal according to the present invention, the spectrum being measured with Cu—K alpha ray. The bulleyaconitine D crystal is prepared by an anti-solvent process with isopropanol, anisole, 1,4-dioxane or methylbenzene acting as a positive solvent and n-heptane as a negative solvent. The preparation process is simple, and the prepared crystal has a high purity. Upon characterization via XRD, DSC, TGA and 1HNMR, the crystal is determined as D crystal type. Stability test shows that the prepared bulleyaconitine crystal is well stable to light, damp and heat.
Provided is a crystal form E of bulleyaconitine A and a preparation method for the crystal form E of bulleyaconitine A. An X-ray powder diffraction spectrum of the crystal form measured by Cu-Kα-ray is as shown in FIG. 1. The crystal form E of bulleyaconitine A is prepared by adding a mixed solution of alcohol and water to bulleyaconitine A, stirring to obtain a suspended solid, and centrifugally collecting the solid. The alcohol is methanol, ethanol or n-butanol. The preparation process is simple, and the obtained crystal form has high purity and is characterized by XRD, DSC, TGA, and 1HNMR to be determined as the crystal form E. The obtained bulleyaconitine A crystal is an anhydrous crystal form, and stability test results show that the crystal has good light, humidity and heat stability.
The present disclosure belongs to the field of pharmaceuticals. Disclosed is a use of bulleyaconitine A in treating pruritus or a secondary lesion thereof, especially pruritus induced by histamine and/or chloroquine.
A01N 37/00 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids
A01N 25/00 - Biocides, pest repellants or attractants, or plant growth regulators, characterised by their forms, or by their non-active ingredients or by their methods of application; Substances for reducing the noxious effect of the active ingredients to organisms other than pests
A01N 37/12 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing the group , wherein Cn means a carbon skeleton not containing a ring; Thio-analogues thereof
A01N 37/44 - Biocides, pest repellants or attractants, or plant growth regulators containing organic compounds containing a carbon atom having three bonds to hetero atoms with at the most two bonds to halogen, e.g. carboxylic acids containing at least one carboxylic group or a thio-analogue, or a derivative thereof, and a nitrogen atom attached to the same carbon skeleton by a single or double bond, this nitrogen atom not being a member of a derivative or of a thio-analogue of
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 31/215 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
A61K 31/24 - Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group having an amino or nitro group
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
A61K 47/44 - Oils, fats or waxes according to two or more groups of ; Natural or modified natural oils, fats or waxes, e.g. castor oil, polyethoxylated castor oil, montan wax, lignite, shellac, rosin, beeswax or lanolin
A bulleyaconitine A crystalline form C, and a preparation method therefor. An X-ray powder diffraction spectrum of the crystalline obtained by measurement using a Cu-Kα ray is as shown in fig. 1. The preparation method therefor comprises: using DMF as a solvent and obtaining by means of a gas-solid permeation method. The procedure of the preparation process is simple, and the obtained crystalline form is a solvate crystalline form, has high purity, and has good stability to light, humidity, and heat.
Disclosed in the present invention are a bulleyaconitine D crystal and a preparation method therefor. Figure 1 shows an X-ray powder diffraction spectrum of the crystal according to the present invention, the spectrum being measured with Cu-K alpha ray. The bulleyaconitine D crystal is prepared by an anti-solvent process with isopropanol, anisole, 1,4-dioxane or methylbenzene acting as a positive solvent and n-heptane as a negative solvent. The preparation process is simple, and the prepared crystal has a high purity. Upon characterization via XRD, DSC, TGA and 1HNMR, the crystal is determined as D crystal type. Stability test shows that the prepared bulleyaconitine crystal is well stable to light, damp and heat.
Provided is a crystal form E of bulleyaconitine A and a preparation method for the crystal form E of bulleyaconitine A. An X-ray powder diffraction spectrum of the crystal form measured by Cu-K α-ray is as shown in FIG. 1. The crystal form E of bulleyaconitine A is prepared by adding a mixed solution of alcohol and water to bulleyaconitine A, stirring to obtain a suspended solid, and centrifugally collecting the solid. The alcohol is methanol, ethanol or n-butanol. The preparation process is simple, and the obtained crystal form has high purity and is characterized by XRD, DSC, TGA, and 1HNMR to be determined as the crystal form E. The obtained bulleyaconitine A crystal is an anhydrous crystal form, and stability test results show that the crystal has good light, humidity and heat stability.
Crystal form G of bulleyaconitine A and a preparation method therefor. Crystal form G of bulleyaconitine A was prepared by adding bulleyaconitine A to a mixed solution of methanoic acid and n-heptane and dissolving, stirring at a low temperature, evaporating a solvent at a high temperature, and leaving the resultant to stand at room temperature to obtain a solid. After characterization by XRD, the solid was determined to have crystal form G.
The present invention belongs to the field of pharmaceuticals. Disclosed is a use of bulleyaconitine A in treating pruritus or a secondary lesion thereof, especially pruritus induced by histamine and/or chloroquine.
A61K 31/439 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
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