CN102068419A - Curcumin composition - Google Patents
Curcumin composition Download PDFInfo
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- CN102068419A CN102068419A CN2010106099192A CN201010609919A CN102068419A CN 102068419 A CN102068419 A CN 102068419A CN 2010106099192 A CN2010106099192 A CN 2010106099192A CN 201010609919 A CN201010609919 A CN 201010609919A CN 102068419 A CN102068419 A CN 102068419A
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Abstract
The invention discloses a curcumin composition. The composition comprises the following components in part by weight: 1 part of curcumin phospholipid compound, and 0.6 to 2.5 parts of nonionic surfactant, wherein the curcumin phospholipid compound consists of 1 part of curcumin, and 0.4 to 1.8 parts of phospholipid. The combined components have remarkable synergetic effect, and can remarkably improve the bioavailability of the curcumin.
Description
Technical field
The present invention relates to pharmaceutical product, specifically a kind of Chinese medicine composition that contains plant extract.
Background technology
Curcumin is a kind of phenolic compound that extracts from the conventional Chinese medicine Rhizoma Curcumae Longae, also is present in other zingiberaceous plant.Modern study finds that curcumin has wide biological activity and pharmacological action, as blood fat reducing, atherosclerosis, antiplatelet aggregation, inflammation-inhibiting reaction, antioxidation, resisting rheumatoid disease etc., curcumin is used to prevent and treat the tumor that various derivants cause as chemoprophylactic drug and obtains extensive studies in recent years, and animal model test confirms curcumin safety, effectively.But because the curcumin utmost point is insoluble in water, do not dissolve to highly acid (stomach) aqueous medium at weak acid (duodenum and small intestinal), therefore common curcumin preparation (as curcumin sheet, curcumin capsule) is difficult for absorbing at gastric, and during through intestinal easily by enzyme in the intestinal or bacterial metabolism.So existing curcumin preparation exists absorption difference, problem that bioavailability is low.
In order to improve the bioavailability of curcumin, there is research worker to carry out curcumin and phospholipid compound, physicochemical property and biological nature to curcumin improves thus, make and had dispersibility preferably, promoted medicine to absorb, can improve the bioavailability of curcumin effectively at gastrointestinal.Disclose a kind of phospholipid complexes of curcumin as CN200410036402.3, the bioavailability of this complex is higher relatively, but still remains further to be improved.
Summary of the invention
Purpose of the present invention is exactly that a kind of new curcumin compositions will be provided, with the further dispersion of curcumin, the absorption rate and the bioavailability of medicament of raising curcumin improved.
The object of the present invention is achieved like this:
Curcumin compositions provided by the present invention is made of the component of following weight part ratio:
1 part of phospholipid complexes of curcumin, non-ionic surface active agent 0.6-2.5 part; Phospholipid complexes of curcumin wherein part is made of 1 part of curcumin, phosphatidase 10 .4～1.8.
The more preferred proportioning of phospholipid complexes of curcumin is by 1 part of curcumin, phosphatidase 10 .4～0.8 part.
Wherein phospholipid can be selected natural phospholipid or synthetic phospholipid for use.Natural phospholipid is optional from soybean phospholipid or egg phosphatide, and synthetic phospholipid can be selected from two palmityl phosphatidyl cholines or two palmityl PHOSPHATIDYL ETHANOLAMINE.
Above-mentioned non-ionic surface active agent is one or more the mixture in the agent of ethers non-ionic surface, esters non-ionic surface active agent or the high score subclass non-ionic surface active agent.
The mixture of one or more in ethers non-ionic surface agent preferred fatty acid polyoxyethylene ether, the polyoxyethylene lauryl ether;
One or more mixture of esters non-ionic surface active agent preferred fatty acid Pyrusussuriensis ester, lauric acid polyoxy glycol glyceride, sucrose fatty acid ester, polyoxyethylene carboxylate, Span-20, sorbitan fatty acid ester, sorbitan fatty acid ester ethylene oxide adduct; Wherein sucrose fatty acid ester more helps absorption of human body, is easy to biodegradation so be highly preferred non-ionic surface active agent among the present invention.
The mixture of one or more in Arlacel-20, Arlacel-40, the Arlacel-80 more preferably in the sorbitan fatty acid ester.
The mixture of one or more in tween 80, the tween 20 more preferably in the sorbitan fatty acid ester ethylene oxide adduct.
In the agent of high score subclass non-ionic surface more preferably molecular weight be the poloxalkol of 4000-8000.
The present invention constitutes compositions with phospholipid complexes of curcumin and non-ionic surface active agent, can effectively improve the bioavailability of curcumin, but the raising of its bioavailability and the non-linear relation of the consumption of surfactant, when phospholipid complexes of curcumin adds the amount of surfactant 〉=0.6, its bioavailability increases along with the increase of dosage of surfactant, and when the amount of surfactant greater than 2.5 the time, bioavailability does not then have significant change again.So the invention provides phospholipid complexes of curcumin and the effective proportional quantity of non-ionic surface active agent, both improved the bioavailability of curcumin with this, therefore the consumption of non-ionic surface active agent can be controlled at reasonable category again, also avoid the excessive and inconvenience that bring to preparation process of non-ionic surface active agent consumption.
Each component is share and is had significant synergism in the present composition, therefore under the fixed situation of curcumin consumption, can effectively reduce the consumption of phospholipid.As among the present invention the phospholipid in the phospholipid complexes of curcumin being reduced to 0.4～0.8 part, can significantly improve the bioavailability of curcumin.
Curcumin compositions of the present invention can be prepared in order to the below method:
Curcumin extraction, phospholipid, 1: 0.4～1.8 weight part ratio are taken by weighing each component, curcumin extraction is mixed with phospholipid after the back adds the appropriate amount of organic dissolving, after decompression or the spray drying, obtain phospholipid complexes of curcumin; Be 1 according to phospholipid complexes of curcumin and non-ionic surface active agent weight part ratio again: 0.6-2.5 takes by weighing each component, with the two mix homogeneously.Add pharmaceutically acceptable pharmaceutic adjuvant such as diluent, absorbent, binding agent, wetting agent, disintegrating agent, lubricant and slow-release material at last, stirring or ground and mixed are even, are prepared into acceptable clinically various dosage forms.
Above-mentioned organic solvent can be selected from chloroform, ether, acetone, dichloromethane, ethyl acetate, dioxane, oxolane, normal hexane, C1-C6 straight or branched low-grade alkane alcohol (as methanol, ethanol, propanol or butanols) etc.
The medical usage of the present composition and usage, consumption all can be with reference to the curcumin soft capsules.
Description of drawings
Fig. 1 is blood drug level-time plot in the rat body.
Among the figure:
The specific embodiment
Following examples are used for that the present invention is further illustrated, but with this protection scope of the present invention are not limited.
The preparation of embodiment 1 curcumin composition soft
Prescription: phospholipid complexes of curcumin 140.g (curcumin: soybean phospholipid=1: 0.4)
Sucrose fatty acid ester 135g
Soybean oil 1485g
Make 1000
Get gelatin, water and glycerol and be mixed with gelatin solution, be incubated standby.
After taking by weighing curcumin and soybean phospholipid adding anhydrous alcohol solution by weight proportion, make phospholipid complexes of curcumin after the spray drying, with the sucrose fatty acid ester mix homogeneously, being dissolved in must yellow clear and bright medicinal liquid in the soybean oil.The medicinal liquid for preparing is added in the feed tank, carry out pelleting, dry under 24-30 ℃, relative humidity 20-45% condition, promptly get the curcumin composition soft.
The preparation of embodiment 2 curcumin composition sustained-release sheets
Prescription: phospholipid complexes of curcumin (curcumin: two palmityl phosphatidyl cholines=1: 0.8)
180g
Arlacel-20 180g
Hypromellose 150g
Calcium hydrogen phosphate 60g
Pregelatinized Starch 150g
The 1.0%PVP alcoholic solution is an amount of
Magnesium stearate 40g
Make 1000
Take by weighing curcumin and two palmityl phosphatidyl cholines by weight proportion, with the two mixing, after adding the chloroform dissolving, decompression makes phospholipid complexes of curcumin, grinds with calcium hydrogen phosphate and Arlacel-20, after making it fully absorb liquid, with phospholipid complexes of curcumin, hypromellose, pregelatinized Starch mix homogeneously, with an amount of 1.0%PVP alcoholic solution system soft material, 18 mesh sieves are granulated, 60 ℃ of dry back granulate, with recipe quantity magnesium stearate mix homogeneously, tabletting, promptly get curcumin composition sustained-release sheet.
The preparation of embodiment 3 curcumin composition oral liquid
Prescription: phospholipid complexes of curcumin 100g (curcumin: egg yolk lecithin=1: 1.0)
Lauric acid polyoxyethylene ether 100g
Icing Sugar 800g
Mannitol 400g
Carmethose 8g
Sodium benzoate 4g
Essence is an amount of
Purified water 1500g
Make 1000
Take by weighing curcumin by weight proportion and egg yolk lecithin makes phospholipid complexes of curcumin, recipe quantity Icing Sugar, mannitol, carmethose, sodium benzoate is soluble in water, add phospholipid complexes of curcumin and polyoxyethylene lauryl ether, after suspendible is even, add an amount of essence, promptly get curcumin composition oral liquid.
The preparation of embodiment 4 curcumin composition softs
Prescription: phospholipid complexes of curcumin 100g (curcumin: soybean phospholipid=1: 1.25)
Polyoxyethylene sorbitan monoleate 135g
Soybean oil 1485g
Make 1000
Get gelatin, water and glycerol and be mixed with gelatin solution, be incubated standby.Take by weighing curcumin by weight proportion and soybean phospholipid makes phospholipid complexes of curcumin, with the polyoxyethylene sorbitan monoleate mix homogeneously, be dissolved in the soybean oil yellow clear and bright medicinal liquid.The medicinal liquid for preparing is added in the feed tank, carry out pelleting, dry under 24-30 ℃, relative humidity 20-45% condition, promptly get the curcumin composition soft.
Prescription: phospholipid complexes of curcumin 100g (curcumin: soybean phospholipid=1: 1.8)
Tween 20 60g
Distilled water 1000ml
Make 1000ml
Take by weighing curcumin by weight proportion and soybean phospholipid makes phospholipid complexes of curcumin, the recipe quantity tween 20 is slowly added, add an amount of correctives, make suspension.
Beneficial effect of the present invention has obtained checking by following test.
Test example 1
Dosage regimen: the SD rat, male, body weight 180-230g.Purify and feed 7d, fasting 12h, whole process be can't help water.Distinguish 5 groups at random, every group 10, be respectively curcumin group (giving curcumin), phospholipid complexes of curcumin group (giving phospholipid complexes of curcumin), curcumin compositions A organizes (curcumin compositions shown in the embodiment 1), curcumin compositions B organizes (curcumin compositions shown in the embodiment 2), curcumin compositions C organizes (curcumin compositions shown in the embodiment 3), each group is scattered in the radiacmeter of 0.2g/kg curcumin in 0.5% the carboxymethylcellulose sodium solution, make the suspension oral gavage administration, respectively at 0.08,0.25,0.5,0.75,1,1.5,2,2.5,3,4,5h gets blood 0.5ml from rat eye socket venous plexus.
Sample treatment: blood sample is placed the centrifugal 5min of centrifuge tube 1200r/min that scribbles the anticoagulant heparin agent, get 0.2ml blood plasma, add 0.5ml chromatograph methanol, vortex vibration 30s, the centrifugal 5min of 12000r/min, protein precipitation, extract curcumin, supernatant is measured the concentration of curcumin through HPLC.
Chromatographic condition: chromatographic column DiamonsilC18 (4.6mm * 250mm, 5 μ m); Mobile phase methanol-water-acetic acid (77: 22: 1); Detect wavelength 428nm; Flow velocity 1.0ml/min, column temperature are room temperature.
Curcumin blood drug level data see Table 1 in the rat body, are abscissa with the sample time, and the concentration of curcumin is vertical coordinate in the blood plasma, mapping, and blood medicine (curcumin) concentration-time curve is seen Fig. 1 in the rat body.
Curcumin blood drug level (μ g/ml) in the table 1 rat body
Date processing: use the 3P97 medicine to handle for calculation procedure, the curcumin compositions of match meets the one compartment model one-level at the rat physiological disposition and absorbs, with AUC, the C of curcumin compositions and curcumin and phospholipid complexes of curcumin
Max, T
Max3 parameters have been carried out variance analysis and q check, and both kinetic parameters compare between any two, AUC, C
MaxSignificant difference (P＜0.05) is arranged.Relevant pharmacokinetic parameters sees table 2 for details.
Table 2 pharmacokinetic parameters (
N=10)
Annotate: * P＜0.05
The result shows that the degree of absorption of simple curcumin suspension is relatively poor, and the bioavailability of phospholipid complexes of curcumin increases, compositions provided by the invention, AUC, C
MaxAll be higher than phospholipid complexes of curcumin (P＜0.05), curcumin compositions provided by the invention blood drug level height in the rat body is described, can significantly improve curcumin, more help curcumin and bring into play drug effect in vivo in the intravital relative bioavailability of rat.
Claims (8)
1. curcumin compositions is characterized in that it is made of the component of following weight part ratio:
1 part of phospholipid complexes of curcumin, non-ionic surface active agent 0.6-2.5 part, phospholipid complexes of curcumin wherein part is made of 1 part of curcumin, phosphatidase 10 .4～1.8.
2. curcumin compositions according to claim 1 is characterized in that described phospholipid complexes of curcumin by 1 part of curcumin, phosphatidase 10 .4～0.8 part formation.
3. curcumin compositions according to claim 1 is characterized in that described non-ionic surface active agent is one or more the mixture in the agent of ethers non-ionic surface, the agent of esters non-ionic surface or the agent of high score subclass non-ionic surface.
4. curcumin compositions according to claim 3 is characterized in that the agent of described ethers non-ionic surface is one or more the mixture in aliphatic acid polyethenoxy ether, the polyoxyethylene lauryl ether.
5. curcumin compositions according to claim 3 is characterized in that described esters non-ionic surface active agent is one or more a mixture of fatty acid Pyrusussuriensis ester, lauric acid polyoxy glycol glyceride, sucrose fatty acid ester, polyoxyethylene carboxylate, Span-20, sorbitan fatty acid ester, sorbitan fatty acid ester ethylene oxide adduct.
6. curcumin compositions according to claim 5 is characterized in that described sorbitan fatty acid ester is one or more the mixture in Arlacel-20, Arlacel-40, the Arlacel-80.
7. curcumin compositions according to claim 5 is characterized in that described sorbitan fatty acid ester ethylene oxide adduct is one or more the mixture in tween 80, the tween 20.
8. curcumin compositions according to claim 3 is characterized in that the agent of described high score subclass non-ionic surface is the poloxalkol of molecular weight 4000-8000.
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| CN2010106099192A CN102068419A (en) | 2010-12-28 | 2010-12-28 | Curcumin composition |
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| CN2010106099192A CN102068419A (en) | 2010-12-28 | 2010-12-28 | Curcumin composition |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3203992A4 (en) * | 2014-10-08 | 2018-11-07 | Boston Biopharm, Inc. | Compositions and methods for increasing the bioavailability of one or more compounds |
| JP2018193307A (en) * | 2017-05-12 | 2018-12-06 | 小林製薬株式会社 | Curcuminoid-containing tablet |
| CN109481689A (en) * | 2018-12-25 | 2019-03-19 | 广州白云山汉方现代药业有限公司 | Water-soluble composition of a kind of enhancing curcumin and preparation method thereof |
| CN110960516A (en) * | 2018-09-27 | 2020-04-07 | 广州汝丽多食品科技有限公司 | Curcumin compound and preparation method thereof |
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| CN1657040A (en) * | 2004-11-22 | 2005-08-24 | 山东大学 | Curcumin and phosphatide composite and its preparation method |
| CN1772011A (en) * | 2005-11-04 | 2006-05-17 | 张钧寿 | Ginkgo leaf extract composition and its prepn |
| US20090131373A1 (en) * | 2006-03-09 | 2009-05-21 | Andrea Giori | Phospholipid complexes of curcumin having improved bioavailability |
| CN101618222A (en) * | 2008-06-30 | 2010-01-06 | 成都国嘉联合制药有限公司 | Anethol trithione and phospholipid compound and preparation method thereof |
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Patent Citations (4)
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| CN1657040A (en) * | 2004-11-22 | 2005-08-24 | 山东大学 | Curcumin and phosphatide composite and its preparation method |
| CN1772011A (en) * | 2005-11-04 | 2006-05-17 | 张钧寿 | Ginkgo leaf extract composition and its prepn |
| US20090131373A1 (en) * | 2006-03-09 | 2009-05-21 | Andrea Giori | Phospholipid complexes of curcumin having improved bioavailability |
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Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3203992A4 (en) * | 2014-10-08 | 2018-11-07 | Boston Biopharm, Inc. | Compositions and methods for increasing the bioavailability of one or more compounds |
| US11185507B2 (en) | 2014-10-08 | 2021-11-30 | Boston Biopharm Inc. | Compositions and methods for increasing the bioavailability of one or more compounds |
| JP2018193307A (en) * | 2017-05-12 | 2018-12-06 | 小林製薬株式会社 | Curcuminoid-containing tablet |
| CN110960516A (en) * | 2018-09-27 | 2020-04-07 | 广州汝丽多食品科技有限公司 | Curcumin compound and preparation method thereof |
| CN110960516B (en) * | 2018-09-27 | 2023-01-06 | 广州汝丽多食品科技有限公司 | Curcumin compound and preparation method thereof |
| CN109481689A (en) * | 2018-12-25 | 2019-03-19 | 广州白云山汉方现代药业有限公司 | Water-soluble composition of a kind of enhancing curcumin and preparation method thereof |
| CN109481689B (en) * | 2018-12-25 | 2021-12-03 | 广州白云山汉方现代药业有限公司 | Composition for enhancing water solubility of curcumin and preparation method thereof |
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Address after: South Luancheng County 051430 Hebei city of Shijiazhuang Province Applicant after: China Shineway Pharmaceutical Group Co., Ltd. Address before: South Luancheng County 051430 Hebei city of Shijiazhuang Province Applicant before: Shineway Pharmaceutical Co., Ltd. |
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Application publication date: 20110525 |