CN1857673A - Curcumenol preparation - Google Patents
Curcumenol preparation Download PDFInfo
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- CN1857673A CN1857673A CN 200610020522 CN200610020522A CN1857673A CN 1857673 A CN1857673 A CN 1857673A CN 200610020522 CN200610020522 CN 200610020522 CN 200610020522 A CN200610020522 A CN 200610020522A CN 1857673 A CN1857673 A CN 1857673A
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- curcumenol
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Abstract
The present invention discloses a kind of curcumenol preparation, and applies curcumenol clinically through solving the problems of insolubility, toxic side effect and hemolytic reaction of zedoary oil. The curcumenol preparation may be injection, transfusion solution, freeze dried powder for injection, microemulsion, liposome, oral liquid, emulsion, etc. and may contains pharmaceutically acceptable supplementary material, such as solubilizer, surfactant, freeze dying protector, etc. The curcumenol preparation is safe and reliable, and may be used in treating tumor, early pregnancy, viral disease, mutation, etc.
Description
Technical field
The present invention relates to a kind of preparation of curcumenol, especially relate to injection of a kind of curcumenol and preparation method thereof.
Background technology
Curcumenol has another name called Rhizoma Curcumae Longae ring alcohol difficult to understand, curcumol, is the important activity composition in the Oleum Curcumae volatilization, have antitumor, antiearly pregnancy, antiviral, mutation, protect the liver, multiple pharmacological effect such as activating blood circulation to dissipate blood stasis, water-soluble hardly, dissolubility is low, does not reach the clinical administration requirement.So the preparation of curcumenol is the report of listing never.Listing is the volatility aromatic turmeric oil preparation now, as Oleum Curcumae capsule, Oleum Curcumae injection, Zedoary turmeric oil glucose injection, and Oleum Curcumae is the traditional medicine volatile oil that is grouped into by tens kinds of one-tenth, curative effect certainly, but composition is indeterminate, children's's toxic and side effects often taking place during clinical application, hemolytic reaction takes place, has caused the great attention of medical circle.How how to reduce toxic and side effects, be clinical service more effectively, benefits the patient; And curcumenol is the monomer of Oleum Curcumae and important effective ingredient, so the preparation of exploitation curcumenol has important reality and clinical meaning.
The formulation development of curcumenol is preparation research expert's pursuit always, as carrying out enclose with beta-schardinger dextrin-, but because the complex structure of curcumenol, generally form the part enclose only, and preparation clathrate influence factor is a lot, as rate of charge, enclose temperature, inclusion time, alr mode etc., so be difficult to the Development and Production listing.Its structure is transformed, synthesized its phthalic acid ester and phosphate ester list sodium salt, just increased dissolubility, synthetic cost is big, and also have a lot of job demand to finish, so its salt does not still have the report of listing, independent curcumenol preparation does not have the report of listing yet.
Summary of the invention
The present invention is intended to develop the preparation of curcumenol, has solved its dissolubility and toxic and side effects and the hemolytic reaction of having eradicated Oleum Curcumae, reaches the clinical application requirement.
This preparation can be liquid drugs injection, transfusion, freeze-dried powder, microemulsion, liposome, also comprises oral liquid, Emulsion etc.
The adjuvant that this preparation can suit by the pharmaceutical formulation requirement is as solubilizing agent, surfactant, freeze drying protectant, emulsifying agent, isotonic agent etc.
This preparation goes for having antitumor, antiearly pregnancy, antiviral, mutation, protect the liver, the treatment of activating blood circulation to dissipate blood stasis etc.
This preparation can realize in the following manner, but is not the restriction to this invention.
The specific embodiment
Embodiment 1
Curcumenol 15g
Tween 80 is an amount of
Make 1000 units
Curcumenol is dissolved with an amount of Tween 80, and adding correctives etc. can be made into oral liquid.
Embodiment 2
Curcumenol 10g
Tween 80 is an amount of
Make 1000 units
Curcumenol with an amount of Tween 80 dissolving, can be added isotonic agent, stabilizing agent, freeze drying protectant etc. and can be made into injection, lyophilizing and infusion solutions etc.
Embodiment 3
Curcumenol 10g
Hydroxypropyl is an amount of
Make 1000 units
Curcumenol with an amount of hydroxypropyl, can be added isotonic agent, stabilizing agent, freeze drying protectant etc. and can be made into injection, lyophilizing and infusion solutions etc.
Embodiment 4
Curcumenol 20.0g
Soybean oil 100g
Lecithin 12g
Glycerol 25g
Add the injection water to 1000ml
Glycerol 25g is dissolved in the water for injection, and refined lecithin 12g, curcumenol 20g are dissolved in the refined soybean oil, are heated to 80 ℃ respectively, mixing, earlier in tissue mashing machine's mid score emulsifying, again through the emulsifying of high speed dispersing emulsification machine to meeting the preparation particle diameter.Add the injection water to 1000ml, cooling, fill promptly gets the curcumenol injectable emulsion.
Embodiment 5
Curcumenol 10.0g
Soybean oil 100g
Soybean phospholipid 15g
Glycerol 22.5g
Add the injection water to 1000ml
Glycerol 22.5g, soybean phospholipid 15g are dissolved in the water for injection, and curcumenol 10g is heated to 60 ℃ respectively in refined soybean oil, mixing, earlier in tissue mashing machine's mid score emulsifying, again through the emulsifying of high speed dispersing emulsification machine to meeting the preparation particle diameter.Add the injection water to 1000ml, cooling, fill promptly gets the curcumenol injectable emulsion.
Stability test
The sample that makes is carried out study on the stability, investigated following table as a result.
Lot number: 050401 specification: 100ml:100mg, 40 ℃ of test temperatures.
| Time (moon) | 0 | 1 | 2 | 3 | 6 |
| Content (%) | 101.6 | 100.7 | 99.3 | 98.9 | 98.4 |
Above result of study shows: the curcumenol stable content in this product, this preparation is suitable for emodin.
Safety testing
Example is carried out anaphylaxis, hemolytic and irritation test, draw 1.0% curcumenol injectable emulsion and dilute in right amount in the back adding 2% rabbit erythrocyte normal saline, 37 ℃ of temperature were incubated 4 hours, and not seeing has haemolysis and red cell agglutination.Cavia porcellus anaphylaxis test shows behind the sensitizing injection 14 days and 21 days, and in 15 minutes, 1% curcumenol injectable emulsion anaphylaxis belongs to negative reaction after the booster injection.With rabbit ear auricular vein injection 5ml/kg1.0% curcumenol injectable emulsion, after suitably handling, once a day, continuous three days, the injection site is the swollen and erythema of water breakthrough not, and did not also find blood vessel irritation damage phenomenon through histopathologic examination.Injectable emulsion of the present invention does not have anaphylaxis, hemolytic, and also nonirritant reaction is safe.
Anxious poison test
Curcumenol injection of the present invention has carried out toxicity research on anxious malicious experimental basis, LD50 is greater than 260mg/kg for chmice acute toxicity, and subacute toxicity LD50 is greater than 170mg/kg, and it is very safe to show that this product applies to human body.
Claims (4)
1, a kind of preparation of curcumenol has solved its dissolubility and toxic and side effects and the hemolytic reaction of having eradicated Oleum Curcumae, reaches the clinical application requirement.
2, the feature of said preparation can be liquid drugs injection, transfusion, freeze-dried powder, microemulsion, liposome, also comprises oral liquid, Emulsion etc.
3, the feature of the said preparation adjuvant that can suit by the pharmaceutical formulation requirement is as solubilizing agent, surfactant, freeze drying protectant, emulsifying agent, isotonic agent etc.
4, said preparation go for having antitumor, antiearly pregnancy, antiviral, mutation, protect the liver, treatment such as activating blood circulation to dissipate blood stasis.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610020522 CN1857673A (en) | 2006-03-21 | 2006-03-21 | Curcumenol preparation |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200610020522 CN1857673A (en) | 2006-03-21 | 2006-03-21 | Curcumenol preparation |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1857673A true CN1857673A (en) | 2006-11-08 |
Family
ID=37296661
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200610020522 Pending CN1857673A (en) | 2006-03-21 | 2006-03-21 | Curcumenol preparation |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1857673A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101569606A (en) * | 2009-06-09 | 2009-11-04 | 沈阳药科大学 | Curcumol liposome and preparation method thereof |
-
2006
- 2006-03-21 CN CN 200610020522 patent/CN1857673A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101569606A (en) * | 2009-06-09 | 2009-11-04 | 沈阳药科大学 | Curcumol liposome and preparation method thereof |
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| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |