Composition of rheinic acid or rheinic acid compounds, its preparing method and its use in preparing medicine for treating diabetic nephrosis

A technology of rhein and compounds, applied in drug combination, drug delivery, urinary system diseases, etc., can solve the problems of poor stability of preparations, unacceptable, high pH value of water injection, etc.

Inactive Publication Date: 2007-01-24
南京中敬医药科技研究所 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The purpose of the present invention is to provide a new complex of rhein compounds and different bases, which not only increases the water solubility, but also overcomes the alkalinity of the strong alkali salt solution of rhein compounds, and makes water needles The pH value is high, which is difficult for the human body to accept physiologically; if the pH value is lowered, the preparation stability is not good.

Method used

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  • Composition of rheinic acid or rheinic acid compounds, its preparing method and its use in preparing medicine for treating diabetic nephrosis
  • Composition of rheinic acid or rheinic acid compounds, its preparing method and its use in preparing medicine for treating diabetic nephrosis
  • Composition of rheinic acid or rheinic acid compounds, its preparing method and its use in preparing medicine for treating diabetic nephrosis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0079] Example 1, the extraction and refining of rhein

[0080] Take 500g of rhubarb powder, add 5 times the amount of 60% ethanol, heat and reflux twice, 1 hour each time, combine the extracts, concentrate to about 1000ml, add 100ml concentrated hydrochloric acid, hydrolyze at 50°C for 1 hour, let cool, filter to obtain a precipitate, add 1000ml 5% NaHCO3 solution, heat to dissolve, filter, add ethanol to the filtrate to make the ethanol concentration reach 50-90%, filter, adjust the pH of the filtrate below 3 with concentrated hydrochloric acid, filter to obtain a yellow precipitate, wash with water until neutral, and recrystallize with glacial acetic acid to obtain Rhein, the content is more than 98%.

Embodiment 2

[0081] Embodiment 2, the preparation of rhein

[0082] Add 6 g of chrysophanol to a mixed solution of 150 ml of acetic anhydride and pyridine (1:1), room temperature overnight, pour the reactant into cold water to crystallize, filter, dry, put in 300 ml of mixed solution of acetic anhydride and glacial acetic acid (1:1) , add chromium trioxide solution dropwise at 45°C, stir at 65°C for 8 hours, pour the reactant into water, crystallize, filter, add 1000ml 25% Na2CO3 solution, extract 3 times with chloroform, heat the Na2CO3 solution to boil, cool, add hydrochloric acid to acidify , after exhausting a large amount of gas, heat and boil for 1 hour, let cool, crystallize, wash with suction and water, recrystallize with glacial acetic acid to obtain 2 g of rhein, with a content of more than 98%.

Embodiment 3

[0083] Embodiment 3, preparation containing 50% effective fraction of rhein

[0084] Rhubarb coarse powder 100g, add 5 times the amount of 60% ethanol, heat and reflux for hydrolysis for 1 hour, filter with suction, combine the filtrates and concentrate under reduced pressure to 30% of the volume of the stock solution to obtain a dilute syrup, add concentrated HCL (1 volume of concentrated hydrochloric acid / 10 times the amount of medicinal materials) Stir for more than 10min, centrifuge to obtain a precipitate, add 5% NaHCO3 equal to the volume of the concentrated solution, heat to dissolve, centrifuge, take the supernatant, add ethanol to make the ethanol content by weight 60-90%, stir , centrifuge, take the supernatant, add concentrated hydrochloric acid to below pH 2, centrifuge, and dry to obtain a brown powder.

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Abstract

The present invention discloses compositions of rheinic acid or rheinic acid compound as shown in the general expression and nitrogen-containing organic base or basic amino acid combined through intermolecular force. The present invention discloses the preparation process of the compositions and their application in preparing medicine for treating diabetic nephrosis.

Description

technical field [0001] The present invention relates to a medicinal compound, in particular to a compound formed of rhein or rhein-like compounds and different bases, a preparation method of the compound, and the use of the compound in preventing and treating diabetic nephropathy application in medicines. Background technique [0002] In the prior art, rhein or rhein-like compounds have been used in the preparation of various drugs, such as the rhein salt disclosed in Chinese patent application 200410049948. [0003] The following two general formulas represent rhein and rhein salts respectively: [0004] [0005] In the general formula, M represents an alkali metal, an alkaline earth metal or an organic base residue. [0006] Rhein compounds are defined as: rhubarb (Rheum palmatum L., Rheumtanguticum Maxim.ex Balf. or Rheum officinale Baill.), Polygonum cuspidum Sieb.et Zucc., Folium sennae, Polygonum multiflorum Thunb.), cassia (Semen cassiae) and other plants contai...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61K31/198A61K31/205A61K31/496A61K31/7008A61K9/00A61K9/02A61K9/06A61K9/08A61K9/10A61K9/107A61K9/12A61K9/14A61K9/19A61K9/20A61K9/48A61K36/708A61K36/704A61K36/482A61P3/10A61P13/12
Inventor 丛晓东
Owner 南京中敬医药科技研究所
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