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Derivative of fibrauretine, and preparation method

A technology of palmetine and its derivatives, which is applied in the field of palmetine derivatives and its preparation, can solve the problems of affecting clinical efficacy and clinical application range, low bioavailability of oral preparations, limiting administration routes and dosage forms, etc., achieving Improved bioavailability, improved water solubility and absorbability, and low manufacturing cost

Inactive Publication Date: 2007-05-09
吴晓枫
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, during clinical use, it was also found that a small number of patients had allergic reactions such as palpitations, general numbness, shortness of breath, chest tightness, pale complexion, irritability, fever all over the body, skin itching, rashes, etc., which limited the clinical application to a certain extent.
[0003] Palmatine is an alkaloid substance, and its own structural characteristics determine that there is a relatively large shortcoming and deficiency, that is, poor water solubility, low solubility in water, and a solubility of about 4 grams at room temperature, thus causing oral preparations Low bioavailability limits the route of administration and dosage form, which greatly affects the clinical efficacy and clinical application range

Method used

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  • Derivative of fibrauretine, and preparation method
  • Derivative of fibrauretine, and preparation method

Examples

Experimental program
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Effect test

example 1

[0028] Select 1 kg of pure palmatine, and another 0.238 kg of pure sodium bicarbonate (that is, the same molar quantity), add water for injection and dilute to 212 liters, mix and place in a water bath at 55°C until completely dissolved to obtain an orange-yellow to wine 212 liters of red clear solution can obtain 0.5% solution. Add acid-base buffer to the solution, filter and sterilize it, and pack it into 106,000 2ml injections, each containing about 10 mg of dry product of the new drug.

example 2

[0030] Take 1 kg of pure palmetine, add 80 kg of water for injection, heat it in a water bath at 55°C until it dissolves to obtain a yellow clear liquid, add 0.238 kg of sodium bicarbonate to 20 kg of water for injection until completely dissolved, and mix the two solutions , stir evenly, after the reaction, an orange-red clear liquid is obtained, add an appropriate amount of acid-base buffer pair and a cosolvent (such as Tween-80) to settle to 106 liters to obtain a 1% solution, filter and sterilize, and pack into 53000 5 ml vials placed in a freeze dryer. After vacuum drying at low temperature for 24 to 36 hours, freeze-dried powder injections are obtained, each containing about 20 mg of the new drug.

example 3

[0032] Take 1 kg of pure palmetine, add 80 kg of water for injection, heat it in a water bath at 55°C until it dissolves to obtain a yellow clear liquid, add 0.238 kg of sodium bicarbonate to 20 kg of water for injection until completely dissolved, and mix the two solutions , stirred evenly, after the reaction, an orange-red clear liquid was obtained, adding an appropriate amount of acid-base buffer pair and a cosolvent (such as Tween-80) to constant volume to 106 liters to obtain a 1% solution, and drying or low-temperature drying to obtain a dry product of 1.2 to 1.3 Add dextrin, medicinal starch, etc. after one kilogram of crushing, add distilled water and stir evenly, press into 60,000 to 65,000 tablets and dry, each containing about 20 mg of the drug.

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Abstract

This invention discloses a method for preparing fibrauretine derivative with antibacterial, anti-inflammatory, cardiomyocyte protective and anti-arrhythmia functions. The method comprises: dissolving fibrauretine in 0-100 deg.C water, adding the same mol amount of alkali or salt containing Na+ or K+, reacting under stirring and normal pressure to obtain transparent liquid with the color from orange to bordeaux and a pH value of 7.0-12.5, sterilizing, filtering, and heating or vacuum-drying at low temperatures to obtain solid fibrauretine derivative with the color from light yellow to dark brown. The fibrauretine derivative has improved water solubility, absorbency, bioavailability and therapeutic effects, newly developed administration method and dosage form, and widened clinical applications.

Description

technical field [0001] The invention relates to a palmatine derivative and a preparation method thereof. This new compound can be made into pharmaceutical preparations as raw materials (solid dosage forms such as: tablets, capsules, granules, drop pills, etc.; liquid dosage forms such as: powder injection, water injection, infusion, eye drops, oral liquid etc.), a new technical field of medicines with antibacterial and anti-inflammatory properties, cardiomyocyte protection and anti-arrhythmia effects. It can be widely used in medicine, health products, food, beverage, cosmetics, animal medicine and other fields. Background technique [0002] As we all know, traditional Chinese medicine, as a pearl in the world's medical treasure house, has made great contributions to the health of human beings, especially the Chinese people. Palmatine hydrochloride or palmatine hydrochloride is an alkaloid extracted from the dry cane of Phantasmus chinensis (also known as rhubarb vine), al...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D455/03A61K31/4375A61K9/08A61K9/00A61P31/04A61P29/00A61P9/06A61P9/00
Inventor 吴晓枫
Owner 吴晓枫
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