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Use of composition of rheinic acid or rheinic acid compounds in preparing medicine for treating osteoarthritis

A technology of osteoarthritis and rhein, applied in the application field of medicine

Inactive Publication Date: 2013-11-27
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

It not only increases the water solubility, but also overcomes the alkalinity of the strong alkali salt solution of rhein compounds, and the pH value of the water injection is high, which is difficult for the human body to accept; if the pH value is lowered, the stability of the preparation is not good. shortcoming

Method used

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  • Use of composition of rheinic acid or rheinic acid compounds in preparing medicine for treating osteoarthritis
  • Use of composition of rheinic acid or rheinic acid compounds in preparing medicine for treating osteoarthritis
  • Use of composition of rheinic acid or rheinic acid compounds in preparing medicine for treating osteoarthritis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0086] Embodiment 2, the preparation of rhein

[0087] 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 of 25% Na2CO3 solution, extract 3 times with chloroform, heat the Na2CO3 solution to boil, cool, add hydrochloric acid to acidify, After a large amount of gas is exhausted, heat and boil for 1 hour, let cool, crystallize, filter and wash with water, and recrystallize with glacial acetic acid to obtain 2 g of rhein with a content of more than 98%.

Embodiment 2

[0088] Embodiment 3, preparation containing 50% effective fraction of rhein

[0089] 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.

Embodiment 3

[0090] Example 4, Preparation of arginine complex containing 50% effective fraction of rhein

[0091] Take 40g of the effective part containing 50% rhein, put it in a suitable container, add water, add 22g of L-arginine to heat, let it cool, add ethanol to make the alcohol content reach 60-90%, stir until dissolved, filter, concentrate the filtrate, concentrate Add ethanol to the liquid to make the alcohol content reach 40-80%, let stand, filter, and dry to obtain 28 g of solid.

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Abstract

Application of rhein or a complex of rhein compounds in the preparation of medicines for the treatment of osteoarthritis, rheumatism and rheumatoid arthritis, the left side of the compound general formula (I) is one of the following two: (1) Rhein or rhein compound monomer components, wherein R2~R3, R6~R7 have 1~2 substituents -COOH, R1~R8, and the rest are any of the following substituents: -H, -O-glucose, -OH, -OCH3, -CH3, R1~R8, at least 2 of them are -H; (2) effective fractions extracted from plants containing rhein; where M represents nitrogen-containing organic bases or basic amino acids, rhubarb Acids or rhein compounds combine with nitrogen-containing organic bases or basic amino acids to form complexes through intermolecular forces. The invention is a compound of weak acid and weak base, the solution of which is nearly neutral, more acceptable in medicine, better in human body compliance, more stable and less irritating.

Description

technical field [0001] The present invention relates to a new application of a medicinal compound, in particular to a compound formed of rhein or rhein compound and different bases in the preparation of medicines for treating osteoarthritis, rheumatism and rheumatoid arthritis Applications. 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 effects of steroidal anti-inflammat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
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 丛晓东张云戴德哉戴茵陈国勋
Owner 南京中敬医药科技研究所
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