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Kaempferol and isonicotinamide co-crystal and preparation method and pharmaceutical composition and use thereof

A technology of isonicotinamide and kaempferol, applied in the fields of kaempferol and isonicotinamide co-crystals and preparations, as well as pharmaceutical compositions and uses thereof, can solve the problem of not finding patents or literature reports of kaempferol and isonicotinamide co-crystals, etc. problem, to achieve the effect of good safety drug advantage

Active Publication Date: 2021-12-07
INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] After domestic and foreign patent and literature searches, no patents or literature reports on the co-crystal of kaempferol and isonicotinamide were found

Method used

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  • Kaempferol and isonicotinamide co-crystal and preparation method and pharmaceutical composition and use thereof
  • Kaempferol and isonicotinamide co-crystal and preparation method and pharmaceutical composition and use thereof
  • Kaempferol and isonicotinamide co-crystal and preparation method and pharmaceutical composition and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Kaempferol and isonicotinamide co-crystal sample preparation method 1:

[0064] As shown in the table below, take an appropriate amount of kaempferol and isonicotinamide and put it into a mortar according to the molar ratio of 1:2, add an appropriate amount of organic solvent, grind it manually for a suitable time, and conduct powder X-ray diffraction analysis on it. image 3 Consistent, indicating that the obtained sample is a co-crystal of kaempferol and isonicotinamide.

[0065] Table 4 Specific examples of preparation method 1 of kaempferol and isonicotinamide cocrystal

[0066]

[0067] Kaempferol and isonicotinamide co-crystal sample preparation method 2:

[0068] According to the table below, take an appropriate amount of kaempferol and isonicotinamide and put it into a ball mill tank according to the molar ratio of 1:2, add an appropriate amount of organic solvent, select an appropriate ball-to-material ratio, set an appropriate speed, and grind for an appro...

Embodiment 2

[0077] Solubility characteristics of kaempferol and isonicotinamide cocrystal:

[0078] With 0.5% SDS aqueous solution as solvent, investigate the solubility difference of kaempferol and isonicotinamide cocrystal and kaempferol, the results show that the solubility of kaempferol and isonicotinamide cocrystal is obviously better than kaempferol, see Figure 8 .

[0079]Since kaempferol is a poorly soluble drug, the dissolution rates of different crystal forms are not clearly distinguished in water or aqueous solutions with different pH values, so an aqueous solution containing 0.5% SDS co-solvent is used for experiments. The dissolution rates of the amide co-crystal and kaempferol have good discrimination. Refer to the solubility determination method ("Technical Guidelines for Dissolution Test of Ordinary Oral Solid Preparations (Draft)", 2012.10 Drug Evaluation Center) for determination. Using the high performance liquid phase method, the mass percentage of sample dissolutio...

Embodiment 3

[0084] The preparation method 1 (tablet) of combination pharmaceutical preparation:

[0085] A preparation method of a combination medicine tablet is characterized in that kaempferol and isonicotinamide co-crystal is used, and several excipients are used as auxiliary material components for preparing the combination medicine tablet, and each tablet contains Tablet 8 shows the tablet formula ratio for the tablet samples with eutectic in the range of 10-500 mg:

[0086] Table 8 Preparation formula of kaempferol and isonicotinamide cocrystal combination drug tablet

[0087]

[0088] The method of preparing kaempferol and isonicotinamide co-crystals as raw materials into tablet preparations is: mixing several excipients and raw materials evenly, and directly compressing tablets; or mixing excipients with dry granulation and then mixing with raw materials evenly After compression, it is ready.

[0089] The preparation method 2 (tablet) of combination pharmaceutical preparation...

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Abstract

The invention discloses a co-crystal of kaempferol and isonicotinamide, a preparation method, a composition and an application thereof. Specifically, the present invention discloses a new kaempferol and isonicotinamide co-crystal with kaempferol (such as formula a) as the active ingredient of medicine and isonicotinamide (such as formula b) as the eutectic ligand; kaempferol The preparation method of the co-crystal with isonicotinamide; the application of the co-crystal of kaempferol and isonicotinamide as active ingredients in the preparation of anti-cancer, anti-cancer, anti-inflammatory, anti-oxidation, antibacterial or antiviral drugs.

Description

technical field [0001] The invention discloses a co-crystal of kaempferol and isonicotinamide, a preparation method, a composition and an application thereof. Specifically, the present invention discloses a co-crystal of kaempferol and isonicotinamide; a method for preparing a co-crystal of kaempferol and isonicotinamide; a co-crystal of kaempferol and isonicotinamide is used as an active ingredient in the preparation of Application in anticancer, anticancer, anti-inflammatory, antioxidant, antibacterial or antiviral drugs. Background technique [0002] Drug co-crystal refers to the crystal formed by the intermolecular non-covalent interaction force between the active drug molecule and the co-crystal ligand in a certain ratio. By forming co-crystals, drugs can improve their physical and chemical properties and improve clinical therapeutic effects on the one hand, and on the other hand, co-crystals can enrich their crystalline forms. For innovative drugs, the solubility and...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D213/81C07D311/30A61K31/352A61P35/00A61P29/00A61P39/06A61P31/04A61P31/12
CPCC07D213/81C07D311/30
Inventor 吕扬杜冠华王英龚宁波杨世颖
Owner INST OF MATERIA MEDICA CHINESE ACAD OF MEDICAL SCI
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