CN104434824A - Method for preparing xanthophylls solid dispersion - Google Patents
Method for preparing xanthophylls solid dispersion Download PDFInfo
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- CN104434824A CN104434824A CN201310435782.7A CN201310435782A CN104434824A CN 104434824 A CN104434824 A CN 104434824A CN 201310435782 A CN201310435782 A CN 201310435782A CN 104434824 A CN104434824 A CN 104434824A
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- lutein
- crystal
- solid dispersoid
- phylloxanthin
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Abstract
The invention provides a method for preparing a xanthophylls solid dispersion. A solid dispersion preparation process is adopted to mix a xanthophylls crystal with a carrier and a plasticizer, and the xanthophylls solid dispersion is prepared by adopting such methods as thermal melting, solvent method, hot-melt extrusion and the like. The method provided by the invention has the advantages of high efficiency and simple production process, and the xanthophylls solid dispersion prepared according to the method provided by the invention has good solubility, thus the bioavailability of xanthophylls is improved.
Description
Technical field
The invention belongs to medicine, food technology field, specifically, the present invention relates to a kind of preparation method of lutein solid dispersoid.
Background technology
Phylloxanthin is a Carotenoids, is a kind of natural pigment, and it is bright in colour, strong coloring force, good in oxidation resistance, and safety non-toxic evil, has abundant nutritive value.Be a kind of natural materials be extensively present in vegetable, flowers, fruit and some algae, be widely used in multiple fields such as food, health product, cosmetics, medicine, Nicotiana tabacum L. and dynamic bird feed.FDA (Food and Drug Adminstration) was used in food as food supplement with regard to approved phylloxanthin as far back as nineteen ninety-five.Because phylloxanthin is widely used, in the international market, 1g phylloxanthin is suitable with 1g gold, therefore has the laudatory title of " plant gold ".
The result of current research shows that phylloxanthin has protection used to vision; in addition it also has the effects such as prevention, prevention of arterial sclerosis, enhancing immunity, particularly prevents the generation of canceration, delays the focus that the aspects such as cancer become current scientist research.
Owing to there are ten conjugated double bonds in phylloxanthin chemical constitution, light and heat all easily causes it that degeneration and its biological activity is reduced occurs, thus limits its application in medicine and food service industry.Due to these character of phylloxanthin, this makes them in production and processing and application, there is significant limitation.Limited dissolubility and the hypersensitivity to oxidation, hinder the direct use of thick product in food and feed dyeing of synthesizing and obtaining, because the material of coarse crystallization form only can obtain poor absorption and produce poor Color.For increasing tinctorial yield and increasing absorbability and bioavailability, the particle diameter of active substance must be reduced to less than 10 μm, what even have reaches nanoscale, because the painted effect of phylloxanthin and bioavailability are directly related with its particle diameter in media as well and dispersibility.The feature that permeability is high according to the dissolubility of carotenoid is low, the means only by reducing carotenoid particle diameter reach and strengthen painted and sorbefacient object, and therefore, the water dispersible and the stability that improve phylloxanthin are extremely important.
Solid dispersions technique, is be dispersed in by certain method a kind of without in the carrier of physiologically active by medicine, obtains the solid dispersion of medicine and carrier.Medicine particle diameter is in the carrier between 0.001 μm-0.1 μm.Solid dispersion be mainly used in increase insoluble drug dissolution rate, improve its bioavailability, also for reducing adverse effect, covering drug smell etc.
Applying solid dispersion technology can improve the water-soluble of phylloxanthin, and can improve the bioavailability of phylloxanthin further, can be applied to the exploitation of medicine, food, beverage.
Summary of the invention
A preparation method for lutein solid dispersoid, comprises the following steps: by high purity lutein crystal or extraction extractum, medicinal polymer carrier and dispersion additives mix homogeneously, prepare lutein solid dispersoid.It is characterized in that: comprise lutein crystal, carrier material, additives, its weight ratio is lutein crystal: carrier material: additives are 1: 20 ~ 80: 0 ~ 19.
Primary raw material adopts phylloxanthin coarse crystal and the phylloxanthin high out-degree extractum of highly purified lutein crystal, arbitrarily lutein content; Carrier material is a kind of in Polyethylene Glycol, polyvidone, poloxamer, organic acid, saccharide, alcohols, carbamide, ethene polymers, cellulose family and derivant thereof, polyacrylic resin class, dextrin class, hydrophilic polymer or their mixture; Additives are a kind of of emulsifying agent and gelatin substance or their mixture.Emulsifying agent is a kind of in phospholipid, ten POGE-A POGE-B POGE-C Polyglycerin palmitate, sucrose fatty acid ester, ten polyglyceryl myristate or ten polyglycereol stearic acid esters or their mixture; Glue class is a kind of in gelatin, arabic gum, alginate, caseinate or their mixture; This solid dispersion adopts the one in solvent method, fusion method, solvent-fusion method, polishing, spray drying method, CO 2 supercritical method, ultrasonic method to prepare.Use solvent is the mixed solution of ethanol, isopropyl alcohol, n-butyl alcohol, oxolane, ethylene glycol, ethyl acetate, acetone.By the preparation method of lutein solid dispersoid according to claim 1, the dispersion made can be used for the fields such as medicine, functional food, beverage.
Of the present inventionly to be a little:
1, the lutein solid dispersoid produced by application torching mark can significantly improve the water-soluble of phylloxanthin, expands the range of application of phylloxanthin.
2, invention increases the stability of phylloxanthin, can be used for tabletting, micropill medicine carrying, various functional food, can be applied in beverage, milk product.
Detailed description of the invention
Example 1
Get proper proportion phylloxanthin and PVPK 1 mixing, with appropriate ethyl acetate-acetone solubilize, mixing.Solvent removed by evaporation at reduced pressure under 40 DEG C of water-baths, obtains dope, is put by this dope in 40 DEG C of vacuum drying ovens, and removing residual solvent, pulverizes, and crosses 80 mesh sieves, obtains white mobility powder, kept dry.Example 2
Adopt solvent-fusion method preparation.Carrier is placed in 65-80 DEG C of heating in water bath melting, adds the phylloxanthin with appropriate ethyl acetate-acetone solubilize while stirring, boil off solvent, pour in culture dish rapidly and tile, after freezing 6 hours, vacuum drying 24 hours, pulverized 80 mesh sieves, kept dry.
Example 3 supersound method
The stabilizing agent aqueous solution 100mL of variable concentrations is added in 250mL conical flask, it is placed in 0-5 DEG C of ice-water bath, under ultrasonic condition (50kHz), the phylloxanthin ethyl acetate-acetone solution of a certain amount of variable concentrations is slowly dripped until solution system becomes muddy with the speed of 1mL/min, after leaving standstill certain hour, high speed centrifugation is until be separated completely.By centrifugal for the washing of gained solid sample, the removing supernatant, the product obtained drying in the vacuum drying oven of 40 DEG C obtains final sample.Sample will be obtained in distilled water after ultrasonic disperse, carry out granularity and pattern test with ultramicroscope.
Example 4
Get 3g PEG or Poloxamer188 and be placed in beaker, about 63 DEG C heating in water bath make its melting, and the phylloxanthin added containing 0.15g is dissolved in ethyl acetate-acetone solution, and limit edged stirs, and then continue to stir 1h at maintenance 63 DEG C of temperature, until solvent evaporation eliminates.Then from water-bath, take out beaker, move to rapidly in the refrigerator of 20 DEG C, solidification 24h, take out and put the dry 24h of 37 DEG C of air dry ovens, take out from beaker, be cut into small pieces, grind, cross 80 mesh sieves, put exsiccator and keep in Dark Place.
Example 5
The phylloxanthin and the PVP3g that take 0.15g are dissolved in ethyl acetate-acetone solution, stir until phylloxanthin and PVP all dissolve and form yellowish-brown clear solution, transfer in eggplant-shape bottle, reduction vaporization ethanol, to time thick, be placed in rapidly .20 DEG C of refrigerator and solidify 24h, take out, be ground into 20 object granules, in 50 DEG C of air dry ovens, dry 24h thoroughly to remove desolventizing, porphyrize, cross 80 mesh sieves, put exsiccator and keep in Dark Place.
Example 6
Get phylloxanthin 0.15g and be placed in beaker, add 50mL ethyl acetate-acetone solubilize, then take 3g CrosPVP, be added to ethyl acetate-acetone solution molten in, beaker is placed on magnetic stirrer, is about 1h with stirring at low speed.Then decompression rotates evaporate to dryness ethanol, is placed in 40 DEG C of dry 24h of air dry oven, porphyrize, crosses 80 mesh sieves, puts exsiccator and keep in Dark Place.
Solvent method and solvent one fusion method is adopted all successfully to prepare solid dispersion.Wherein solvent method preparation process is simple, pumps products therefrom after solvent more loose through vacuum, easily pulverizes and mobility is fine, but product collection is more difficult; Solvent one fusion method is many compared with solvent method step, but more suitable to the carrier that fusing point is lower.
Claims (7)
1. a preparation method for lutein solid dispersoid, comprises the following steps: by high purity lutein crystal or extraction extractum, medicinal polymer carrier and dispersion additives mix homogeneously, prepare lutein solid dispersoid.It is characterized in that: comprise lutein crystal, carrier material, additives, its weight ratio is lutein crystal: carrier material: additives are 1:20 ~ 80:0 ~ 19.
2. by lutein solid dispersoid according to claim 1, it is characterized in that: lutein crystal is phylloxanthin coarse crystal and the phylloxanthin high out-degree extractum of highly purified lutein crystal, arbitrarily lutein content.
3. by lutein solid dispersoid according to claim 1, it is characterized in that: carrier material is a kind of in Polyethylene Glycol, polyvidone, poloxamer, organic acid, saccharide, alcohols, carbamide, ethene polymers, cellulose family and derivant thereof, polyacrylic resin class, dextrin class, hydrophilic polymer or their mixture.
4. by lutein solid dispersoid according to claim 1, it is characterized in that: additives are a kind of of emulsifying agent and gelatin substance or their mixture.Emulsifying agent is a kind of in phospholipid, ten POGE-A POGE-B POGE-C Polyglycerin palmitate, sucrose fatty acid ester, ten polyglyceryl myristate or ten polyglycereol stearic acid esters or their mixture; Glue class is a kind of in gelatin, arabic gum, alginate, caseinate or their mixture.
5. by lutein solid dispersoid according to claim 1, it is characterized in that: described solid dispersion adopts the one in solvent method, fusion method, solvent-fusion method, polishing, spray drying method, CO 2 supercritical method, ultrasonic method to prepare.
6. a preparation method for lutein solid dispersoid as claimed in claim 1, its feature: described solvent is ethanol, isopropyl alcohol, n-butyl alcohol, oxolane, ethylene glycol, ethyl acetate, acetone.
7., by the preparation method of lutein solid dispersoid according to claim 1, the dispersion made can be used for the fields such as medicine, functional food, beverage.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310435782.7A CN104434824A (en) | 2013-09-18 | 2013-09-18 | Method for preparing xanthophylls solid dispersion |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201310435782.7A CN104434824A (en) | 2013-09-18 | 2013-09-18 | Method for preparing xanthophylls solid dispersion |
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| CN104434824A true CN104434824A (en) | 2015-03-25 |
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| CN201310435782.7A Pending CN104434824A (en) | 2013-09-18 | 2013-09-18 | Method for preparing xanthophylls solid dispersion |
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107088186A (en) * | 2017-04-28 | 2017-08-25 | 华南理工大学 | A kind of solid dispersions containing lutein and preparation method thereof |
| CN107308114A (en) * | 2017-06-09 | 2017-11-03 | 广州百花香料股份有限公司 | A kind of solid dispersions containing lutein and its microwave fusion preparation method |
| CN113018266A (en) * | 2019-12-25 | 2021-06-25 | 晨光生物科技集团股份有限公司 | Preparation method of cannabidiol solid dispersion, cannabidiol solid dispersion prepared by preparation method and application of cannabidiol solid dispersion |
-
2013
- 2013-09-18 CN CN201310435782.7A patent/CN104434824A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN107088186A (en) * | 2017-04-28 | 2017-08-25 | 华南理工大学 | A kind of solid dispersions containing lutein and preparation method thereof |
| CN107308114A (en) * | 2017-06-09 | 2017-11-03 | 广州百花香料股份有限公司 | A kind of solid dispersions containing lutein and its microwave fusion preparation method |
| CN113018266A (en) * | 2019-12-25 | 2021-06-25 | 晨光生物科技集团股份有限公司 | Preparation method of cannabidiol solid dispersion, cannabidiol solid dispersion prepared by preparation method and application of cannabidiol solid dispersion |
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Addressee: Newly help and revive Pharmaceutical Science and Technology Ltd. in Tianjin Document name: Notification that Application Deemed to be Withdrawn |
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Application publication date: 20150325 |