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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

AI Technical Summary

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 it is easily absorbed by the protein in the gastrointestinal tract, which affects the absorption, making it difficult to reach the effective concentration for exerting pharmacological effects, and the bioavailability is extremely low, which seriously limits the application of berberine in major clinical diseases

Method used

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  • Berberine nanocomposite and preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

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

Embodiment 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 has an effect on the formation of berberine nanocomposite and The structure has no effect, and the specific preparation method is as follows:

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

experiment example 1

[0044] Experimental example 1 UV characterization

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

[0046] The result is as Figure 4 Shown, berberine solution has maximum absorption peak at λ=425nm place, and the dRBP solution of comparative example 1 has maximum absorption peak at λ=575nm place; And the dRBP-Berb solution of embodiment 2 has maximum absorption peak at λ=425nm place and λ= There are absorption peaks at 575nm, 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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