CN1583783A - Licorice acid double salt, preparing method and use thereof - Google Patents
Licorice acid double salt, preparing method and use thereof Download PDFInfo
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- CN1583783A CN1583783A CN 200410024178 CN200410024178A CN1583783A CN 1583783 A CN1583783 A CN 1583783A CN 200410024178 CN200410024178 CN 200410024178 CN 200410024178 A CN200410024178 A CN 200410024178A CN 1583783 A CN1583783 A CN 1583783A
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- double salt
- acid double
- glycyrrhizic acid
- organic solvent
- matrine
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Abstract
Glycyrrhizic acid double salt and its pharmaceutics are prepared from start materials of glycyrrhizic acid to (sophocarpidine ) matrine with weight ratio of 1 to 1-10 by: putting raw materials into organic solvent with weight ratio of 1 to 10- 100 , reflux heating at 25-80deg.C for 1-5 hours , recovering organic solvent , then drying the solid resultant to get the products. Solvent is alcohol or methanol or acetone. This pharmaceutics can be used in therapy of acute or chronic hepatitis, virus hepatitis and hepatic injury.
Description
Technical field
The present invention relates to medicine and preparation method thereof, relate in particular to a kind of glycyrrhizic acid double salt and its production and use.
Background technology
Potenlini is a most important effective constituent in the Radix Glycyrrhizae, and Potenlini has anti-inflammatory, antiviral, and biological activity such as raise immunity, is used for the treatment of hepatitis, bronchitis, stomach ulcer, AIDS and some cancer clinically.But because its molecular weight big (＞800), polar group is more, water-soluble and fat-soluble all relatively poor reason, cause that oral gastrointestinal absorption is poor, bioavailability is low, limited it in Clinical Application.Matrine is the alkaloid that extracts from the Chinese medicine kuh-seng, it is antiviral that matrine has (is its main pharmacological, but hepatitis B virus resisting and hepatitis C virus), immunomodulatory, protect the liver pharmacological actions such as (anti peroxidation of lipid, anti-hepatocellular apoptosis), anti-hepatic fibrosis, be widely used in diseases such as treatment hepatitis, dermatitis and eczema clinically.Still there is not the open report that Potenlini (comprising its extract and acid salt) and matrine (comprising Oxymatyine and Radix Sophorae Flavescentis extract) generate double salt at present.
Summary of the invention
One of purpose of the present invention is at disadvantages of background technology, and providing a kind of is glycyrrhizic acid double salt of making of raw material and uses thereof with Potenlini and matrine; Two of purpose provides the preparation method of this glycyrrhizic acid double salt.
One of purpose of the present invention can realize by following technical measures
This glycyrrhizic acid double salt is with Potenlini: matrine=1: 1～10 weight part proportionings are the mixture that raw material is made, and structural formula is as follows
R=glucose
Can be made into the medicine of said various formulations on any pharmaceutics with glycyrrhizic acid double salt of the present invention; Described formulation is various oral dosage forms or injection powder pin, liquid drugs injection Injectable compound preparation etc.Use glycyrrhizic acid double salt treatment acute, chronic hepatitis, viral hepatitis and liver injury of the present invention.
Two of purpose of the present invention can realize by following technical measures
Earlier according to Potenlini: matrine=1: 1～10 weight part proportioning constitutive materials, again according to raw material: the weight part proportioning of organic solvent=1: 10～100 is dissolved in the organic solvent, through reflux 1～5 hour, reclaims organic solvent, with the solids drying, promptly get product again.Described organic solvent is meant ethanol or methyl alcohol or acetone; Described reflux temperature is 25～80 ℃.
Potenlini of the present invention comprises its extract and acid salt, and described matrine comprises Oxymatyine and Radix Sophorae Flavescentis extract, and these raw materials are present city's pin product, raw materials used being easy to get.
Glycyrrhizic acid double salt of the present invention can improve the water-soluble of Potenlini, increases its oral absorption; And Potenlini and matrine all have good anti-hepatitis hepatoprotective effect, but Potenlini matrine is based on antiviral based on anti-inflammatory action, the two forms double salt, can produce synergistic therapeutic action, reduces simultaneously because the side effect of using matrine to produce separately.Experimentation on animals shows: use separately with Potenlini or matrine and compare, glycyrrhizic acid double salt of the present invention is significantly improved to the therapeutic action of acute, chronic hepatitis, viral hepatitis and liver injury.
Experimentation on animals:
Get body weight and be 50 of the male mices of 18～22g, be divided into 5 groups at random: normal control group, model control group, Potenlini group, matrine group, glycyrrhizic acid double salt group.Gastric infusion, dosage 5g/20g body weight, normal control group and model control group give equal-volume distilled water, successive administration 7 days, after administration in the 6th day 6 hours, except that the normal control group, all abdominal injection gave 0.1% tetracol phenixin 10ml/, after the last administration 24 hours, get blood (fasting is 16 hours before getting blood) from angular vein, separation of serum is measured ALT, AST, cuts open simultaneously and gets liver, calculate liver index, comparative group differences after weighing.The results are shown in following table:
Table: different preparations cause the influence of chmice acute liver injury to tetracol phenixin
Group dosage (mg/kg) Serum ALT (U/L) serum AST liver index (g/100g body weight)
(U/L)
Normal control 5ml 41.7 ± 15.6 128. ± 26.8 5.866 ± 0.711
Model contrast 5ml 178. ± 47.5 243. ± 49.8 6.778 ± 0.624
Potenlini group 5g 48.3 ± 12.4 147. ± 45.4 6.428 ± 0.663
Matrine group 5g 47.1 ± 14.4 143 ± 25.4 6.304 ± 0.788
Glycyrrhizic acid double salt group 5g 40.4 ± 10.3 127 ± 24.5 5.898 ± 0.635
Embodiment 1:
Take by weighing Potenlini 24kg, matrine 74kg is dissolved in the 2000kg ethanol, 50 ℃ of reflux, reacts 3 hours, reclaims ethanol, and gained solids drying promptly gets product.
Embodiment 2:
Take by weighing the Radix Glycyrrhizae extract that contains Potenlini 46kg, contain the Radix Sophorae Flavescentis extract of matrine 48kg, be dissolved in the 3000kg acetone, 25 ℃ of reflux, reacted 5 hours, reclaim acetone, gained solids drying promptly gets product.
Embodiment 3:
Take by weighing Potenlini 30kg, Oxymatyine 300kg is dissolved in the 31000kg methyl alcohol, 70 ℃ of reflux, reacts 2 hours, reclaims methyl alcohol, and the gained solids is drying to obtain.
Embodiment 4:
Elder generation's extracting liquorice acid 1 weight part, matrine 5 weight parts are prepared into glycyrrhizic acid double salt, again with glycyrrhizic acid double salt in 60 ℃ of dryings, pulverized 100 mesh sieves, pregelatinized Starch, Microcrystalline Cellulose dry 1 hour, was pulverized 100 mesh sieves.Add medicinal adhesive, the system particle, 60 ℃ of dryings, whole grain adds 1% sodium starch glycolate and 1% Magnesium Stearate, and compressing tablet gets the glycyrrhizic acid double salt tablet.
Embodiment 5:
Elder generation's extracting liquorice acid 1 weight part, Oxymatyine 10 weight parts are prepared into glycyrrhizic acid double salt, again with glycyrrhizic acid double salt in 60 ℃ of dryings, pulverized 100 mesh sieves, pregelatinized Starch, Microcrystalline Cellulose dry 1 hour, was pulverized 100 mesh sieves.Add medicinal adhesive, the system particle, 60 ℃ of dryings, whole grain, the capsule of packing into No. 1 gets the glycyrrhizic acid double salt capsule preparations.
Embodiment 6:
Radix Glycyrrhizae extract, matrine 7 weight parts of elder generation's extracting liquorice acid 1 weight part are prepared into glycyrrhizic acid double salt, again glycyrrhizic acid double salt is dissolved in the purified water, stir fully dissolving, add 85% simple syrup again, adjustable value to 3.5～7.0, add 0.3% Sodium Benzoate again and make sanitas, heated and boiled 30 minutes, the filtering with microporous membrane of 0.8 μ m, embedding is in the brown oral vial of 20ml, sterilization in 100 ℃, 30 minutes gets the glycyrrhizic acid double salt oral liquid.
Embodiment 7:
Elder generation's extracting liquorice acid 1 weight part, Oxymatyine 4 weight parts are prepared into glycyrrhizic acid double salt, glycyrrhizic acid double salt are added in the water for injection, fully dissolving again, the gac of adding 0.1%, heated and boiled 15 minutes is filtered carbon removal, the gac of adding 0.03% stirs, transfer pH value to 5.0～7.0, survey intermediate content, pH value, qualified after, embedding in glass ampoule in, 100 ℃, 30 minutes circulation vapor sterilizations get Potenlini matrine injection.
Embodiment 8:
Elder generation's extracting liquorice acid 1 weight part, matrine 1 weight part are prepared into glycyrrhizic acid double salt, glycyrrhizic acid double salt are added in the water for injection, fully dissolving again, the gac of adding 0.3%, heated and boiled 15 minutes, sterile filtration carbon removal, embedding is in the ampoule of 20ml, and cool freeze-drying is dry, gets lyophilized powder.
Claims (7)
1, a kind of glycyrrhizic acid double salt is characterized in that it being with Potenlini: matrine=1: 1～10 weight part proportionings are the mixture that raw material is made, and structural formula is as follows
R=glucose
2, make the medicine of said various formulations on any pharmaceutics with the glycyrrhizic acid double salt of claim 1.
3, medicine according to claim 2 is characterized in that described formulation is various injections and oral dosage form.
4, the preparation method of the glycyrrhizic acid double salt of claim 1, it is characterized in that earlier raw material according to raw material: the weight part proportioning of organic solvent=1: 10～100 is dissolved in the organic solvent, through reflux 1～5 hour, reclaims organic solvent, with the solids drying, promptly get product again.
5, the preparation method of glycyrrhizic acid double salt according to claim 4 is characterized in that described organic solvent is meant ethanol or methyl alcohol or acetone.
6, the preparation method of glycyrrhizic acid double salt according to claim 4 is characterized in that described reflux temperature is 25～80 ℃.
7, the glycyrrhizic acid double salt of claim 1 is in the application of treatment acute, chronic hepatitis, viral hepatitis and liver injury.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410024178 CN1583783A (en) | 2004-06-03 | 2004-06-03 | Licorice acid double salt, preparing method and use thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200410024178 CN1583783A (en) | 2004-06-03 | 2004-06-03 | Licorice acid double salt, preparing method and use thereof |
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| CN1583783A true CN1583783A (en) | 2005-02-23 |
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| CN 200410024178 Pending CN1583783A (en) | 2004-06-03 | 2004-06-03 | Licorice acid double salt, preparing method and use thereof |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100395261C (en) * | 2004-06-22 | 2008-06-18 | 江苏恒瑞医药股份有限公司 | Compound salt of glycyrrhizin and kurarinol, its production and use |
| CN101367799B (en) * | 2008-10-06 | 2011-11-30 | 李国玉 | Matrine salviol acid B complex salt and kuh-seng native salviol acid B complex salt, preparation method and application thereof |
| CN103130865A (en) * | 2013-03-06 | 2013-06-05 | 天津赫而博生物科技有限公司 | Sophocarpidine, oxymatrine glycyrrhetinic acid double salt, and preparation method and use thereof |
| WO2023078004A1 (en) * | 2021-11-02 | 2023-05-11 | 深圳市萱嘉生物科技有限公司 | Matrine glycyrrhizine amino acid ionic salt, preparation method therefor and application thereof |
-
2004
- 2004-06-03 CN CN 200410024178 patent/CN1583783A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100395261C (en) * | 2004-06-22 | 2008-06-18 | 江苏恒瑞医药股份有限公司 | Compound salt of glycyrrhizin and kurarinol, its production and use |
| CN101367799B (en) * | 2008-10-06 | 2011-11-30 | 李国玉 | Matrine salviol acid B complex salt and kuh-seng native salviol acid B complex salt, preparation method and application thereof |
| CN103130865A (en) * | 2013-03-06 | 2013-06-05 | 天津赫而博生物科技有限公司 | Sophocarpidine, oxymatrine glycyrrhetinic acid double salt, and preparation method and use thereof |
| CN103130865B (en) * | 2013-03-06 | 2016-08-03 | 天津赫而博生物科技有限公司 | Matrine, oxymatrine enoxolone double salt and preparation method thereof, purposes |
| WO2023078004A1 (en) * | 2021-11-02 | 2023-05-11 | 深圳市萱嘉生物科技有限公司 | Matrine glycyrrhizine amino acid ionic salt, preparation method therefor and application thereof |
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