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Berberine-phthalic acid drug salt single crystal and preparation method thereof

A technology of phthalic acid and potassium hydrogen phthalate, which is applied in the field of berberine-phthalic acid pharmaceutical salt single crystal and its preparation, can solve the effects, uniformity and Stability is difficult to guarantee, deliquescence or mildew and other problems, to achieve the effect of improving clinical medicinal value, improving moisture absorption stability, and increasing antibacterial activity

Active Publication Date: 2021-02-09
JIAMUSI UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, berberine hydrochloride has poor hygroscopic stability, and it is prone to agglomeration, deliquescence or mildew after absorbing moisture in the air, and may even bring unforeseen medication risks, thereby affecting its transportation, storage and clinical medicinal effects.
Therefore, in the clinical medicinal research and development of berberine hydrochloride, the poor hygroscopic stability of berberine hydrochloride is an important factor restricting its industrial production and development
At present, there are mainly methods such as chemical structure modification and adding pharmaceutical excipients to improve the hygroscopic stability of berberine hydrochloride. However, these traditional methods all have some shortcomings or shortcomings, such as the original drug may become a new compound after chemical structure modification, making Its biological activity or toxic and side effects produce unpredictable changes; after berberine hydrochloride is physically mixed with pharmaceutical excipients, its uniformity and stability are difficult to guarantee

Method used

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  • Berberine-phthalic acid drug salt single crystal and preparation method thereof
  • Berberine-phthalic acid drug salt single crystal and preparation method thereof
  • Berberine-phthalic acid drug salt single crystal and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0029] A preparation method of berberine-phthalic acid pharmaceutical salt single crystal, adding 0.1mmol of berberine hydrochloride and 0.1mmol of potassium hydrogen phthalate to 10mL of water at a molar ratio of 1:1, under the condition of 60°C water bath After stirring for 4 hours, the obtained precipitate was dried at 70°C for 3 hours, dissolved in a mixed solution of ethanol (3mL) and ethyl acetate (7mL), and after being fully reacted, the resulting mixed solution was placed in Slowly volatilize at room temperature, and obtain berberine-phthalic acid drug salt single crystal after about 1-30 days.

Embodiment 2

[0031] A preparation method of berberine-phthalic acid pharmaceutical salt single crystal, adding 0.1mmol of berberine hydrochloride and 0.2mmol of potassium hydrogen phthalate to 10mL of water at a molar ratio of 1:2, under the condition of 60°C water bath After stirring for 3 hours, the obtained precipitate was dried at 70°C for 3 hours, dissolved in a mixed solution of ethanol (4mL) and ethyl acetate (6mL), and after fully reacting, the resulting mixed solution was placed in Slowly volatilize at room temperature, and obtain berberine-phthalic acid drug salt single crystal after about 1-30 days.

Embodiment 3

[0033] A preparation method of berberine-phthalic acid pharmaceutical salt single crystal, adding 0.1mmol of berberine hydrochloride and 0.1mmol of potassium hydrogen phthalate to 10mL of water at a molar ratio of 1:1, under the condition of 60°C water bath Stir for 3 hours, filter and dry the precipitate at 70°C for 4 hours, dissolve in a single solvent of ethanol (10 mL), and after fully reacting, place the resulting mixed solution at room temperature to slowly volatilize, about 1 -A single crystal of berberine-phthalic acid drug salt was obtained after 30 days.

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Abstract

Berberine-phthalic acid drug salt single crystal and preparation method thereof, the present invention provides a method for preparing berberine drug salt single crystal, the invention prepares berberine-phthalic acid drug salt single crystal, its chemical formula for C 20 h 18 NO 4 ·C 8 h 5 o 4 , the crystal structure belongs to the triclinic system, the space group is P, a =7.3443(6)Å, b =11.1081(9)Å, c =14.3643(11)Å, α =90°, β =99°, gamma =97°, V =1144.18(16)Å 3 , Z =2. The berberine-phthalic acid pharmaceutical salt single crystal prepared by the present invention can effectively improve the hygroscopic stability of berberine and its anti-Escherichia coli and gold The antibacterial activity of Staphylococcus aureus has important academic significance and clinical application value for improving the physicochemical properties and biological activities of berberine.

Description

technical field [0001] The invention provides a single crystal of berberine-phthalic acid medicinal salt and a preparation method thereof. Background technique [0002] Berberine hydrochloride, C 20 h 18 NO 4 Cl, its chemical structure is as follows: [0003] [0004] Berberine, also known as berberine, is an isoquinoline alkaloid, mainly found in the root bark and stem bark of many plants in multiple families such as Berberidaceae, Poppyaceae, Ranunculaceae and Rutaceae. Berberine has good antibacterial, anti-dysentery and anti-tumor and other pharmacological activities. It mainly exists in nature in the form of ions, and berberine hydrochloride is commonly used in clinical practice. However, berberine hydrochloride has poor hygroscopic stability, and it is prone to agglomeration, deliquescence or mildew after absorbing moisture in the air, and may even bring unforeseen medication risks, thereby affecting its transportation, storage and clinical medicinal effects. ....

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D455/03A61K31/4375C07C63/20C07C51/41A61P31/04
CPCA61P31/04C07B2200/13C07C63/20C07D455/03Y02A50/30
Inventor 张羽男刘盈利刘立新
Owner JIAMUSI UNIVERSITY
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