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Buxine, buxine hydrochloride, and its preparing method and formulation

A technology of epiphylline hydrochloride and epiphylline, which is applied in pill delivery, pharmaceutical formulations, organic active ingredients, etc., can solve the problems of high cost, and achieve the effects of low cost, clear extraction process route, and clear structure

Inactive Publication Date: 2006-08-09
杭太俊 +6
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] Aiming at the problem of high cost existing in the current monomer raw material of cyclovir buxicine D and the pharmaceutical preparation made from this monomer raw material, the purpose of the present invention is to provide a kind of boxyline, which is easy to extract and low in cost, and has a synergistic effect. Cardiovascular Therapeutic Activity

Method used

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  • Buxine, buxine hydrochloride, and its preparing method and formulation
  • Buxine, buxine hydrochloride, and its preparing method and formulation
  • Buxine, buxine hydrochloride, and its preparing method and formulation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Preparation of boxicine: extract, separate and refine the effective part of alkaloids, boxicine, which contains three main alkaloid components, cycloviric boxwood D, cycloboxyline D and cycloevergreen boxicine C, from boxwood.

[0043] 1.1 Preparation of phylloxine

[0044] Boxwood, crushed into powder, soaked in 10 times the amount of ammonia solution (dilute concentrated ammonia water to 2 times the volume), soaked for 24 hours, added chloroform for extraction three times, combined the chloroform extracts, and recovered the chloroform under reduced pressure to obtain a residue. Add petroleum ether to disperse the residue, add dilute hydrochloric acid solution (3M) to extract four times, combine dilute hydrochloric acid solution, decolorize activated carbon, add concentrated ammonia water to neutralize dilute hydrochloric acid solution to alkaline (pH12), extract three times with chloroform, combine chloroform extract , most of the solvent was evaporated under reduced ...

Embodiment 2

[0064] Embodiment 2: Epiphylline hydrochloride

[0065] 2.1 Preparation

[0066] Get 2 grams of epiphylline (extracted by the method in Example 1), be dissolved in 50 milliliters of chloroform, pass into excessive dry hydrogen chloride gas in the chloroform solution under the stirring situation, press every mole of alkaloid (each composition) with 1 ~2 moles of hydrogen chloride are used to react with hydrogen chloride gas to form a precipitate of boxicine hydrochloride insoluble in chloroform. After the reaction is completed, filter out the precipitate, wash the precipitate twice with an appropriate amount of ethanol, and dry it under reduced pressure at 80°C. - Recrystallize from chloroform, dry under reduced pressure at 80°C to constant weight, and obtain boxyrine hydrochloride.

[0067] Solubility The solubility of boxicine hydrochloride in commonly used solvents is measured in Table 3. Compared with salicine, its solubility in water is significantly increased. The solu...

Embodiment 3

[0079] Embodiment 3: epiphylline injection

[0080] Injections made of epiphylline and / or its hydrochloride, including small needle solutions for injection, injections for intravenous infusion, sterile powders for injections, freeze-dried products, etc. The boxyline prepared in Example 1 was used for the boxyline, and the boxyline hydrochloride prepared in Example 2 was used for the boxylate hydrochloride.

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PUM

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Abstract

The invention discloses buxine. It is made up of cyclovirobuxine D, cyclovirobuxine D, and cyclovirobune C. And their weight content respectively is 60%-95%, 1.0%-30%, and 0.5%-20%. It also discloses buxine hydrochloride and its preparation method and their preparation. The formed product has clear composition and structure, effective quality control to ensure stable curative effect and easy to form various modern preparations. Its preparation technology is simple. And its cost is low.

Description

technical field [0001] The present invention relates to extracting, separating and preparing from boxwood-Buxus microphylla, which contains three main alkaloid components, cyclovirbuxine D, cycloboxine D and cycloevergreen boxwood C, and has synergistic therapeutic effect on cardiovascular and cerebrovascular diseases. The effective part of the alkaloid of the "Buxusine", its hydrochloride raw materials, and their pharmaceutical preparations, as well as their preparation methods and quality analysis and control methods. Background technique [0002] Boxwood is used as medicine and recorded in Materia Medica. Cyclovitamin D is an alkaloid monomer isolated from boxwood. The raw material of Cyclovitamin D and its preparations are included in the 2005 edition of the "Chinese Pharmacopoeia". "Buxus Ning Tablets" made from Huowei Buxus D raw material. The raw material of Cycloviral Buxusin D recorded in the Pharmacopoeia and Buxusin Tablets are Cycloviral Buxusin D monomer. It ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J53/00A61K9/08A61K9/20A61K9/14A61K31/56
Inventor 杭太俊张正行梁秉文袁厚亮安登魁刘洁方泰惠
Owner 杭太俊
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