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A kind of berberine nanocomposite and preparation method thereof

A nanocomposite, berberine technology, applied in the field of medicine and health, can solve the problems of low bioavailability, difficult effective concentration, poor oral absorption, etc.

Active Publication Date: 2018-08-10
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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  • A kind of berberine nanocomposite and preparation method thereof
  • A kind of berberine nanocomposite and preparation method thereof
  • A kind of berberine nanocomposite and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0038] At room temperature, dissolve 2g of styrene-maleic anhydride alternating copolymer with a molecular weight of 20000 in 10ml of N,N-dimethylformamide and 1ml of triethylamine, and then add 500mg of berberine hydrochloride or sulfuric acid Add 5ml of a saturated aqueous solution of sodium bicarbonate to remove the 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 A solution of 10 mg / ml is made in water, and ultrasonic treatment is performed for 40 minutes to promote self-assembly to form particles, and the berberine nanocomposite is obtained with a microbeam 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 to facilitate subsequent detection, but the addition of rhodamine dRB affects the formation of the berberine nanocomposite. The structure has no effect, the specific preparation method is as follows:

[0041] At room temperature, dissolve 2g of styrene-maleic anhydride alternating copolymer with a molecular weight of 20000 in 10ml of N,N-dimethylformamide and 1ml of triethylamine, and drop 1ml into it with a concentration of 500mg / ml of dRB N,N-dimethylformamide solution, stir for 2h; add 500mg of berberine hydrochloride, stir overnight; add 5ml of saturated aqueous sodium bicarbonate to remove acid anhydride, stir again for 1h; adopt molecular weight cutoff After removing substances with a molecular weight below 3500kD for a 3500kD dialysis bag, freeze-dry or vacuum dry, dissolve the dried solid in water to make a 10mg / ml solution, and ultrasonicall...

experiment example 1

[0044] Experimental example 1 UV characterization

[0045] The solutions of berberine hydrochloride with a concentration of 100μg / mL, dRB@P-Berb obtained in Example 2 and dRB@P obtained in Comparative Example 1 were prepared with PBS; the above three solutions were detected by a microplate reader Ultraviolet absorption between 350nm and 600nm. λ=425nm is the characteristic absorption peak of berberine, and λ=575nm is the characteristic absorption peak of dRB.

[0046] The result is Figure 4 As shown, the berberine solution has a maximum absorption peak at λ=425nm, the dRB@P solution of Comparative Example 1 has a maximum absorption peak at λ=575nm; while the dRB@P-Berb solution of Example 2 has a maximum absorption peak at λ=425nm There are absorption peaks at and λ=575nm, indicating that the dRB@P-Berb of Example 2 contains both berberine and dRB, that is, the dRB@P-Berb of Example 2 is 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 (BBR, Berb) is one of the effective ingredients of many Chinese herbal medicines such as Coptis and Scutellaria. It is clinically used to treat gastrointestinal diseases such as acute and chronic gastroenteritis, with a long history and definite curative effect. Recent studies have shown that berberine has anti-tumor, anti-arrhythmia, lowering blood lipids, lowering blood sugar, improving insulin resistance, preventing vascular stenosis, treating Alzheimer's disease, etc., and has a wide range of applications, and berberine is the current Chinese medicine Among the few small molecule compounds that can be synthesized artificially. [0003] However, berberine is still not widely used in clinical practice. Current studies have shown that be...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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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