Aliphatic organic acid salt of berberine type alkaloid and preparation method and usage thereof

A technology of organic acid salts and alkaloids, which is applied in the field of pharmacy, can solve problems such as drug accumulation, and achieve the effects of improved bioavailability, good therapeutic effect, and high bioavailability

Inactive Publication Date: 2008-01-30
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, the oral dosage of berberine for antibacterial use is 0.3-0.9g / day, and the dosage range for antiarrhythmia is 1.2-3g / day. Such long-term use may excessively inhibit the intestinal flora and affect the intestinal environment; new Most of the indications are chronic diseases with long-term medication. According to the literature, the average residence time of berberine in the human body is 33 hours. Long-term large-dose administration will cause drug accumulation.

Method used

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  • Aliphatic organic acid salt of berberine type alkaloid and preparation method and usage thereof
  • Aliphatic organic acid salt of berberine type alkaloid and preparation method and usage thereof
  • Aliphatic organic acid salt of berberine type alkaloid and preparation method and usage thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 Preparation of berberine laurate

[0038] Dissolve equivalent amounts of berberine sulfate and sodium laurate in 20 times the amount of 80℃ hot water, mix, continue stirring at 80℃ for 4 hours, let cool to room temperature, add the equivalent reactant (with berberine sulfate The reaction product was extracted three times with dichloromethane in an amount of 30 times the mass based on alkali and sodium laurate. The dichloromethane layer was separated and concentrated under reduced pressure. In the concentrated solution, 10 times the amount of petroleum ether was added to the filtrate to precipitate and filter. Take the precipitate, dry, and get it.

Embodiment 2

[0039] Example 2 Preparation of santengin stearate

[0040] Dissolve equivalent amounts of yellow rattan hydrochloride and sodium stearate in 10 times the amount of 90℃ hot water, mix, continue stirring at 90℃ for 4 hours, let cool to room temperature, add 20 times the amount of the reactant n-butyl The reaction product was extracted with alcohol three times, the n-butanol layer was separated, an appropriate amount of anhydrous sodium sulfate was added, shaken and stood still, filtered, the filtrate was taken and concentrated under reduced pressure, and 20 times the amount of petroleum ether was added to the concentrate to precipitate Precipitate, filter the precipitate, dry, and get it.

Embodiment 3

[0041] Example 3 Oral relative bioavailability of palmatine stearate.

[0042] Take the yellow rattan stearate prepared in Example 2 to make a solution with PEG 400, and give it to rats at a dose of 15 mg / kg. The same dose of yellow rattan hydrochloride PEG 400 solution was used as a control for comparison. Their pharmacokinetic curve characteristics and relative bioavailability. The pharmacokinetic curve shows that it has the advantages of good absorption and high bioavailability.

[0043] The classic two-compartment model after oral administration of yellow rattan stearate, the time lag is about 0.5h, the peak blood concentration is reached at 4-6h, and the elimination half-life is about 5.11h. Compared with santengin hydrochloride, the relative bioavailability of santengin stearate is 1855%, which does have the advantages of good absorption and high bioavailability.

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PUM

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Abstract

The invention relates to preparation method and application of berberine fatty group organic acid salt, pertaining to pharmacy field. The chemical general formula of barberine type alkaline of the invention is shown as a formula (I), wherein, X represents organic acid group, and the berberine type alkaline is berberin, palmatine, jaterohitine or coptisine. The invention relates berberine alkaline fatty group organic acid, which is of good oral taking absorption, can be used for preparing medical components, greatly improves the bio-availability of the alkaline type, and play comparatively better effect to the therapies of such diseases as bacterial infection, heart rate abnormity, platelet aggregation, hyperlipidemia, diabetes, hypertension, cardiac failure, etc.

Description

Technical field [0001] The invention belongs to the field of pharmacy, and relates to aliphatic organic acid salts of berberine alkaloids, and a preparation method, medicinal composition and application thereof. Background technique [0002] Berberines (berberines) alkaloids include berberine (berberine), palmatine (palmatine), jatrorrhizine (jatrorrhizine) and coptisine (coptisine). Berberine alkaloids have long been used clinically as antibacterial drugs, mainly for the treatment of diseases such as gastroenteritis and bacillary dysentery. In recent years, the new pharmacological effects of this type of alkaloids have been gradually discovered, which has attracted the attention of researchers again. The most extensive and in-depth research is its representative alkaloid-berberine. There are many reports on the pharmacological research of berberine in domestic and foreign journals, including the lipid-lowering effect and mechanism reported by Chinese scholars in Nature Medicine....

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D455/03A61K31/4375A61K9/00A61P31/04A61P9/06A61P9/04A61P3/06A61P3/10A61P9/12
Inventor 翁伟宇黄建明仇缀百沈腾张建芳徐惠南郭济贤
Owner FUDAN UNIV
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