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

A technology of rhein and compounds, applied in the application field of medicine, can solve the problems of poor preparation stability, 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

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Example 1, the extraction and refining of rhein

[0083] 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

[0084] Embodiment 2, the preparation of rhein

[0085] 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

[0086] Embodiment 3, preparation containing 50% effective fraction of rhein

[0087] 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 compositions of rheinic acid or rheinic acid compound used in preparing medicine for treating osteoarthritis, rheumatic and rheumatoid arthritis, a left side of a general formula (1) of the compositions being one of the following two: (1) rhein or rhein compound monomer component, wherein R2-R3, R6-R7 have 1-2 substituent groups ..CCOOH, R1-R8 are arbitrary substitutent groups: -H, -O-glucose, -OH, -OCH3, and -CH3, at least two of the R1-R8 are ..CHs, (2) effective parts containing the rhein and extracted from plants; wherein M represents an organic base containing nitrogen or basic amino acid, the rhein or the rhein compound is combined with the organic base containing the nitrogen or the basic amino acid by using intermolecular forces to form the compositions. The compositions of the invention are weak acid and weak base compositions. The solution of the compositions is approximately neutral. The compositions are acceptable in pharmacy. Human body compliance is better, the composition is more stable and the thrill is smaller.

Description

technical field [0001] The present invention relates to a pharmaceutical compound, in particular to a compound formed of rhein or rhein compound and different bases, a preparation method of the compound, and the preparation of the compound in the treatment of osteoarthritis, Drug use in rheumatism and rheumatoid arthritis. Background technique [0002] Osteoarthritis, rheumatoid arthritis and rheumatoid arthritis are joint diseases with a high incidence rate. Taking the former as an example, the incidence rate is about 10% of the total population. For patients over 60 years old, more than 50% of the patients It affects 2%, 30% and 68% of women under the age of 45, 45 to 60 and over 65, respectively; and 3%, 24.5% and 58% of men. As the population ages, the proportion of the diseased population to the total population will increase. [0003] The current drugs for the treatment of osteoarthritis mainly include steroidal and non-steroidal anti-inflammatory drugs. Adverse eff...

Claims

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Application Information

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IPC IPC(8): A61K31/192A61K31/198A61K31/205A61K31/496A61K31/7008A61K9/00A61K9/02A61K9/06A61K9/08A61K9/10A61K9/107A61K9/12A61K9/14A61K9/19A61K9/20A61K9/48A61K36/708A61K36/704A61K36/482A61P19/02A61P29/00
Inventor 丛晓东
Owner 南京中敬医药科技研究所
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