Composition of rheinic acid or rheinic acid compounds, its preparing method and its use in preparing medicine for preventing intestinal adhesion

A rhein and compound technology, applied in the field of medicinal compounds, can solve the problems of poor stability of preparations, high pH value of water injection, unacceptable, 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

[0013] 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 preventing intestinal adhesion
  • Composition of rheinic acid or rheinic acid compounds, its preparing method and its use in preparing medicine for preventing intestinal adhesion
  • Composition of rheinic acid or rheinic acid compounds, its preparing method and its use in preparing medicine for preventing intestinal adhesion

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] Example 1, the extraction and refining of rhein

[0082] 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

[0083] Embodiment 2, the preparation of rhein

[0084] 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

[0085] Embodiment 3, preparation containing 50% effective fraction of rhein

[0086] 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) stirred for more than 10min, centrifuged to obtain a precipitate, added 5% NaHCO3 equal to the volume of the concentrated solution, heated to dissolve, centrifuged, took the supernatant, added ethanol to make the ethanol content 60-90%, stirred, Centrifuge, take the supernatant, add concentrated hydrochloric acid to pH below 2, centrifuge, and dry to obtain a brown powder.

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Abstract

The present invention discloses application of compositions of rheinic acid or rheinic acid compound in preparation of drugs for treating stomach and intestine function recover or recovering the stomach and intestine function. The left side of the compound shown in the general formal (I) is one of the two: (1) the rheinic acid or rheinic acid compound monomer, wherein R2-R3, R6-R7 have 1-2 substitutions: -COOH and R1-R8, other positions are optional substitutions: -H, -O-glucose, -OH, -OCH3, and -CH3, at least two of R1-R8 are ..CH; (2) effective parts containing the rheinic acid and extracted from plants. M in the general formula (l) represents nitrogenous organic alkali or alkaline amino acid. The rheinic acid or the rheinic acid compound and the nitrogenous organic alkali or alkaline amino acid are joined through intermolecular forces to form the compound. The invention is a weak acid and weak alkalis compound and its solution is near neutral. The compound of the invention has easily acceptable pharmaceutical performance, better human body compliance and steady and less irritation.

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 preparing and treating gastrointestinal function recovery And the application in the medicine of preventing intestinal adhesion. Background technique [0002] Abdominal surgery is the most common operation in surgery. Generally, the gastrointestinal function of the patient is relatively weak after the operation. The recovery of the gastrointestinal function after the operation is of great significance to the patient's recovery, including the recovery of the disease, and the reduction of intestinal adhesions and other complications. [0003] Postoperative intestinal adhesion is still an unresolved clinical surgical problem. Research reports in recent years have pointed out that: 90% to 100% of patients who have undergone abdominal surgery have...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61K31/198A61K31/205A61K31/496A61K31/7008A61K9/19A61K9/20A61K9/48A61K36/708A61K36/704A61K36/482A61P1/14A61P1/00
Inventor 丛晓东
Owner 南京中敬医药科技研究所
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