Berberine nanocomposite and preparation method

A nano-composite, berberine technology, applied in the field of medicine and health, can solve the problems of affecting absorption, protein adsorption, limiting the use of berberine, etc.

Active Publication Date: 2016-06-15
175TH HOSPITAL OF PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] However, berberine has not been widely used clinically at present. Current research shows that berberine belongs to the quaternary ammonium isoquinoline alkaloid, which is strongly alkaline and positively charged. Due to its low solubility and poor biofilm permeability, Oral absorption is not good, and

Method used

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  • Berberine nanocomposite and preparation method

Examples

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Example Embodiment

[0036] Example 1

[0037] A berberine nanocomposite, its preparation method is as follows:

[0038] At room temperature, dissolve 2g of styrene-maleic anhydride alternating copolymer with a molecular weight of 20,000 in 10ml of N,N-dimethylformamide and 1ml of triethylamine, and then add 500mg of berberine hydrochloride or sulfuric acid. Salt, stir overnight; add 5 ml of saturated aqueous solution of sodium bicarbonate to remove acid anhydride, and stir again for 1 h; use a dialysis bag with a molecular weight cut-off of 3500 kD to remove substances with a molecular weight below 3500 kD, freeze-dry or vacuum dry, and dissolve the dried solid. A solution of 10 mg / ml was prepared in water, and ultrasonically treated for 40 minutes to promote the formation of particles by self-assembly, to obtain the berberine nanocomposite, which is a microbeam structure.

Example Embodiment

[0039] Example 2

[0040] The difference between the berberine nanocomposite in this example and Example 1 is that rhodamine dRB is added as a marker, which is convenient for subsequent detection, but the addition of rhodamine dRB affects the formation and The structure has no effect, and the specific preparation method is as follows:

[0041]At room temperature, 2g of styrene-maleic anhydride alternating copolymer with a molecular weight of 20,000 was dissolved in 10ml of N,N-dimethylformamide and 1ml of triethylamine, and 1ml of 500mg / ml was added dropwise to it. ml of dRB solution in N,N-dimethylformamide, stirred for 2 h; added 500 mg of berberine hydrochloride, stirred overnight; added 5 ml of saturated aqueous sodium bicarbonate solution to remove the acid anhydride, stirred again for 1 h; After removing substances with a molecular weight below 3500kD for a 3500kD dialysis bag, freeze-drying or vacuum drying, dissolving the dried solid in water to make a 10mg / ml solutio...

Example Embodiment

[0044] Experimental Example 1 UV Characterization

[0045] The solutions of berberine hydrochloride, dRBP-Berb obtained in Example 2, and dRBP obtained in Comparative Example 1 were prepared with PBS with a concentration of 100 μg / mL; between UV absorption. The characteristic absorption peak of berberine is at λ=425 nm, and the characteristic absorption peak of dRB is at λ=575 nm.

[0046] The result is as Figure 4 As shown, the berberine solution has a maximum absorption peak at λ=425 nm, the dRBP solution of Comparative Example 1 has a maximum absorption peak at λ=575 nm; while the dRBP-Berb solution of Example 2 has a maximum absorption peak at λ=425 nm and λ= There are absorption peaks at 575 nm, indicating that the dRBP-Berb of Example 2 contains both berberine and dRB, that is, the dRBP-Berb of Example 2 was successfully prepared.

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Abstract

The invention discloses a berberine nanocomposite and a preparation method. A styrene-maleic anhydride alternating copolymer is dissolved in N,N-dimethylformamide and triethylamine, and berberine is added with overnight stirring; a saturated aqueous solution of sodium bicarbonate is added; after drying, solid is redissolved in water, ultrasonic treatment is carried out, and the berberine nanocomposite is obtained; Berberine and the styrene-maleic anhydride alternating copolymer form the high-molecular nanocomposite, so that biomembrane permeability of berberine is improved, bioavailability of berberine is enhanced, and the nanocomposite has a wide application prospect.

Description

technical field [0001] The invention belongs to the field of medicine and health, and relates to a new dosage form of berberine, in particular to a berberine nanocomposite and a preparation method thereof. Background technique [0002] Berberine (berberine, BBR, Berb) is one of the active ingredients of various Chinese herbal medicines such as Coptis chinensis and Scutellaria baicalensis. It is clinically used to treat acute and chronic gastroenteritis and other gastrointestinal diseases, with a long history and definite curative effect. Studies in recent years have shown that berberine has anti-tumor, anti-arrhythmia, lowering blood fat, lowering blood sugar, improving insulin resistance, preventing vascular stenosis, and treating Alzheimer's disease. It has a wide range of applications, and berberine is currently a traditional Chinese medicine. It is one of the few small molecular compounds that can be synthesized artificially. [0003] However, berberine has not been wi...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/4375A61K47/34A61P1/00A61P5/00A61P9/00A61P9/10A61P35/00
CPCA61K9/1075A61K31/4375A61K47/34
Inventor 唐庆林赖敏灵郭以和费燕陈钟苏军凯张鸣青
Owner 175TH HOSPITAL OF PEOPLES LIBERATION ARMY
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