Berberine electrostatic composite and preparation method of berberine electrostatic composite

A technology of berberine and compound, applied in the field of berberine electrostatic compound and preparation thereof, can solve the problems of unclear pharmacokinetics and long-term toxicity, no report, gastrointestinal mucosa or cell membrane damage, etc. Achieve the effect of increasing biofilm permeability, significant therapeutic effect, and improving oral bioavailability

Active Publication Date: 2012-10-03
NORTHEAST PHARMA GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most of the absorption enhancers have a certain cytotoxic effect, causing a certain degree of damage to the gastrointestinal mucosa or cell membrane, intestinal endotoxins and other chemical substances may be absorbed into the blood circulation and cause side effects, and the absorption enhancer itself In vivo pharmacokinetics and long-term toxicity are not yet clear, and there are few product...

Method used

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  • Berberine electrostatic composite and preparation method of berberine electrostatic composite
  • Berberine electrostatic composite and preparation method of berberine electrostatic composite
  • Berberine electrostatic composite and preparation method of berberine electrostatic composite

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Accurately weigh 1.0002 g of berberine hydrochloride dihydrate and dissolve it in 500 mL of distilled water to make a saturated solution of berberine hydrochloride; accurately weigh 1.2007 g of sodium cholesterol sulfate and dissolve it in 240 mL of absolute ethanol ; Under the condition of magnetic stirring, cholesteryl sulfate sodium ethanol solution is added dropwise in the saturated solution of berberine hydrochloride, and the mol ratio of berberine and cholesteryl sulfate sodium is 1:1, continue stirring for 30 minutes , all the precipitates were separated out, centrifuged, washed and collected, freeze-dried to obtain the electrostatic complex of berberine cholesterol sulfate.

Embodiment 2

[0017] Accurately weigh 1.0004 g of berberine hydrochloride dihydrate and dissolve it in 500 mL of distilled water to make a saturated solution of berberine hydrochloride; accurately weigh 0.7076 g of sodium lauryl sulfate and dissolve it in 20 mL of distilled water In; under magnetic stirring, the aqueous solution of sodium lauryl sulfate is added dropwise in the saturated solution of berberine hydrochloride, and the molar ratio of berberine and sodium lauryl sulfate is 1:1, continue After stirring for 40 minutes, all the precipitates were precipitated, centrifuged, washed and collected, and freeze-dried to obtain the electrostatic complex of berberine dodecyl sulfate.

Embodiment 3

[0019] Accurately weigh 1.0005 g of berberine hydrochloride dihydrate and dissolve it in 500 mL of distilled water to make a saturated solution of berberine hydrochloride; accurately weigh 0.9446 g of sodium deoxycholate and dissolve it in 20 mL of distilled water; Under the condition of magnetic stirring, the aqueous solution of sodium deoxycholate was added dropwise to the saturated solution of berberine hydrochloride, and the molar ratio of berberine and sodium deoxycholate was 1:1, and the stirring was continued for 50 minutes, all the precipitates were separated out, centrifuged, washed and collected, and freeze-dried to obtain the electrostatic complex of berberine deoxycholic acid ester.

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Abstract

The invention discloses a berberine electrostatic composite and a preparation method of the berberine electrostatic composite, which are applied to medical and health industries. The berberine electrostatic composite is prepared from anionic surfactant and berberine or berberine salt by compositing; the molar ratio of the anionic surfactant to the berberine or berberine salt is 1 to 0.5-10; the molar ratio of anion to the berberine salt is 1 to 1; the anionic surfactant is one or more of alkyl sulfate or alkyl sulfonate or fatty acid salt; the alkyl sulfate is one or more of sodium cholesteryl sulfate, lauryl sodium sulfate and deoxysodium cholate; the alkyl sulfonate is one or more of sodium heptanesulfonate and sodium dodecyl sulfate; the fatty acid salt is one or more of sodium caprate and sodium enanthate, and the berberine and berberine salt are obtained by chemical synthesis or by extracting traditional Chinese medicine. The berberine is prepared into the berberine electrostatic composite to increase the biological membrane penetrating ability of the berberine and improve the oral bioavailability of the berberine, and the berberine electrostatic composite plays a significant treatment role on important chronic metabolic disorder diseases such as diabetes mellitus, complication of the diabetes mellitus, hyperlipidemia and the like.

Description

technical field [0001] The invention relates to a berberine electrostatic complex in the medical and health industry and a preparation method thereof. Background technique [0002] Berberine, English name Berberine, Chinese alias berberine, berberine, berberine, a common isoquinoline alkaloid, it exists in many plants of four families and ten genera including Berberidaceae. In 1826 M.-E. Chavalier and G. Peltin obtained for the first time from the bark of Xanthoxylonclava. Berberine is a quaternary ammonium alkaloid, which has antibacterial effects on hemolytic streptococcus, Staphylococcus aureus, Neisseria gonorrhoeae, Freund's, Shigella dysenteriae, etc., and can enhance the phagocytosis of leukocytes. Yersinia pestis also has different degrees of inhibition, and it also has inhibitory effect on amoebic bacteria in rats. Berberine has anti-curare effect on animals, and has peripheral antihypertensive and antipyretic effects. Berberine hydrochloride (commonly known as b...

Claims

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Application Information

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IPC IPC(8): C07D455/03C07J9/00C07C305/06C07C303/24C07C53/126C07C51/41
Inventor 汲涌唐星樊冬娇
Owner NORTHEAST PHARMA GRP
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