CN102058530A - Ganoderma lucidum polysaccharide oral nanoemulsion and preparation method thereof - Google Patents
Ganoderma lucidum polysaccharide oral nanoemulsion and preparation method thereof Download PDFInfo
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- CN102058530A CN102058530A CN2010105881962A CN201010588196A CN102058530A CN 102058530 A CN102058530 A CN 102058530A CN 2010105881962 A CN2010105881962 A CN 2010105881962A CN 201010588196 A CN201010588196 A CN 201010588196A CN 102058530 A CN102058530 A CN 102058530A
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Abstract
The invention belongs to the field of pharmaceutic preparation, and relates to ganoderma lucidum polysaccharide oral nanoemulsion and a preparation method thereof. The preparation method is characterized in that transparent or semi-transparent nanoemulsion is prepared by mixing and uniformly emulsifying 18.9%-78.6% of oil phase, 0.1%-2.2% of ganoderma lucidum polysaccharide, 19.9%-76.6% of surfactant and cosurfactant and the balance of distilled water by weight at a temperature between 45 DEG C and 60 DEG C in turn. The preparation method is simple and convenient and is low in energy consumption; and the prepared ganoderma lucidum polysaccharide nanoemulsion has lymph affinity, and can reduce damage of the gastrointestinal tract to ganoderma lucidum polysaccharide, enhance organism absorption rate and bioavailability, and make best of medicine.
Description
Technical field
The invention belongs to field of pharmaceutical preparations, relate to a kind of ganoderan nano-emulsion and preparation method thereof.
Background technology
Ganoderan is the main active substances of Ganoderma, and it is present in the mycelium and sporophore of Ganoderma fungus, the mixture of being made up of peptide polysaccharide, glucosan, heteropolysaccharide etc.Wherein major part is a beta glucan in the glucosan, and minority is an alpha-glucans, brings into play active main component and beta glucan is it.Ganoderan has pharmacologically active widely, comprises human body immunity improving power, inhibition tumor, enhancing body hypoxia-bearing capability, eliminates effects such as free radical, defying age, blood sugar lowering, blood fat reducing.In recent years more for the antitumor action research of ganoderan.Ganoderan is owing to have the non-specific resistance of stimulation of host, and immune specific reaction and inhibition tumor characteristic are subjected to Chinese scholars and more and more pay close attention to.
In recent years, the medicament nano technology more and more comes into one's own.Compare with traditional molecular medicine, medicine is behind nanorize, because architectural characteristics such as the porous that the small-size effect of nano-particle, specific surface area be big, have, hollow, multilamellars, make it have medicament curative effect enhancement, reduce administration number of times, reduce adverse effect, be easy to advantage such as medicament slow release controlled release.And for this class hydrophilic biopharmaceutical macromolecular drug of ganoderan, the nanorize technology can not only overcome it and be difficult to directly stride across biomembrane, the shortcoming that bioavailability is low, and can be by selecting the suitable carriers material, be prepared into suitable nano medicament carrying system, thereby reduce the degraded to medicine of gastrointestinal tract acidic materials and enzyme, prolong half-life reaches the purpose that improves bioavailability.
Nano-emulsion normally particle diameter is that the emulsion droplet of 10-100nm is dispersed in the dispersion system of colloid that forms in the another kind of liquid, be transparent or semitransparent, it is spherical that its emulsion droplet mostly is, and size is more even, through pressure sterilizing or centrifugally all can not make it layering, belong to the thermodynamically metastable fixed system usually.Nanometer emulsified technology has been penetrated into fields such as daily-use chemical industry, fine chemistry industry, petrochemical industry, material science, biological medicine technology and environmental science, becomes the research field that has the huge applications potentiality now in the world.After medicine is prepared to the nano-emulsion dosage form, its major advantage comprises: toxicity is little, safe, can increase the dissolubility of insoluble drug, improve the facile hydrolysis stability of drug, also can be used as the carrier of slow release or targeting drug delivery system, nano-emulsion stability is high, particle diameter and turbidity change or change slower hardly in time, are not subject to the influence of serum albumin, and the life-span in blood circulation is very long etc.
Based on the advantage of nano-emulsion, ganoderan is prepared into the nano-emulsion dosage form and has following significant advantage by oral form administration:
(1) stability of raising ganoderan reduces the degraded of gastrointestinal tract to medicine.
(2) prolong ganoderan macromolecular drug soak time, improve bioavailability.
(3) have the lymph affinity, overcome first pass effect.
(4) oral administration route is convenient, compliance is good.
(5) compare with existing other nanotechnology, nano-emulsion preparation technology is easy, energy consumption is low, repeatability is high.
Research contents
The technical problem to be solved in the present invention is intended to provide a kind of ganoderan that can promote to absorb, and improves its bioavailability and is fit to ganoderan oral administration nanometer Emulsion of suitability for industrialized production and preparation method thereof.Described ganoderan oral administration nanometer Emulsion can be rolled into ganoderan the nanoscale preparation, reduces the destruction of ganoderan at human gastrointestinal tract, and the absorbance of enhancing body and bioavailability play a role medicine more.
Ganoderan oral administration nanometer breast of the present invention, the clear emulsion of forming by oil phase, surfactant, cosurfactant and water.Its raw material and mass percent thereof are: oil phase 18.9%-78.6%, and ganoderan 0.1%-2.2%, surfactant and surfactant 19.9%-76.6%, surplus is a distilled water, above-mentioned raw materials percentage ratio sum is 100%.
Ganoderan oral administration nanometer breast of the present invention is characterized in that described ganoderan derives from Ganoderma sporophore, is water soluble polysaccharide, and its range of molecular weight distributions is for releasing 5kDa-40kDa.
Ganoderan oral administration nanometer breast of the present invention is characterized in that described oil phase preferably is rich in any in the Oleum Glycines of long-chain triglyceride, Semen Maydis oil, the isopropyl myristate.
Ganoderan oral administration nanometer breast of the present invention is characterized in that described surfactant is one or more the mixture in glyceryl monostearate, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, castor oil hydrogenated polyoxyethylene ether, castor oil polyoxyethylene ether, lecithin or soybean phospholipid, the fatty glyceride.
Ganoderan oral administration nanometer breast of the present invention is characterized in that one or more the mixture in the preferred sorbitan fatty acid ester of described surfactant, polyoxyethylene sorbitan fatty acid ester, castor oil hydrogenated polyoxyethylene ether, the castor oil polyoxyethylene ether.
Ganoderan oral administration nanometer breast of the present invention is characterized in that described cosurfactant is the long-chain monoglyceride, ethanol, the mixture of one or more in the propylene glycol.
Ganoderan oral administration nanometer breast of the present invention, it is directly oral to it is characterized in that described ganoderan nano-emulsion is used for, or pack into hard gelatin capsule or Perle or enteric solubility hard gelatin capsule or enteric solubility Perle are prepared into oral formulations.
Ganoderan oral administration nanometer Emulsion of the present invention is used in the medicine for preparing prevention or treatment tumor, human body immunity improving.
The present invention detects through transmission electron microscope, and droplet diameter distribution is between 10-100nm.
Description of drawings
Fig. 1, Fig. 2 are respectively embodiment 1, the ganoderan nano-emulsion transmission electron microscope picture that embodiment 2 is prepared into.
The specific embodiment
Embodiment 1: the ganoderan nano-emulsion
Composition weight (g)
Injection stage soybean oil 2.25
Tween 80 0.5
Sorbester p17 1
Ganoderan 0.032
Distilled water 0.4
Precision takes by weighing recipe quantity injection stage soybean oil, Tween 80, sorbester p17, and under 45-60 ℃ of condition, magnetic agitation is even.Other gets ganoderan, be dissolved in be prepared into water in the distilled water after, slowly drop in the said mixture, the magnetic agitation while adding is added into fully to water, when promptly system becomes clarification suddenly, the ganoderan nano-emulsion.
Embodiment 2: the ganoderan nano-emulsion
Composition weight (g)
Isopropyl myristate 2.25
Tween 80 0.5
Sorbester p17 1
Ganoderan 0.088
Propylene glycol 0.2
Distilled water 1.1
Precision takes by weighing recipe quantity isopropyl myristate, Tween 80, sorbester p17, and under 45-60 ℃ of condition, magnetic agitation is even.After other gets ganoderan, propylene glycol and is dissolved in and is prepared into water in the distilled water, slowly drop in the said mixture, the magnetic agitation while adding is added into fully to water, when promptly system becomes clarification suddenly, the ganoderan nano-emulsion.
Embodiment 3: the ganoderan nano-emulsion
Composition weight (g)
Injection stage soybean oil 3
Sorbester p17 1.5
Castor oil hydrogenated polyoxyethylene ether 0.5
Ganoderan 0.024
Distilled water 0.3
Precision takes by weighing recipe quantity injection stage soybean oil, sorbester p17, castor oil hydrogenated polyoxyethylene ether, and under 45-60 ℃ of condition, magnetic agitation is even.Other gets ganoderan, be dissolved in be prepared into water in the distilled water after, slowly drop in the said mixture, the magnetic agitation while adding is added into fully to water, when promptly system becomes clarification suddenly, the ganoderan nano-emulsion.
Embodiment 4: the ganoderan nano-emulsion
Composition weight (g)
Injection stage soybean oil 2.1
Sorbester p17 0.6
Castor oil polyoxyethylene ether 0.8
Ganoderan 0.028
Distilled water 0.35
Precision takes by weighing recipe quantity injection stage soybean oil, sorbester p17, castor oil polyoxyethylene ether, and under 45-60 ℃ of condition, magnetic agitation is even.Other gets ganoderan, be dissolved in be prepared into water in the distilled water after, slowly drop in the said mixture, the magnetic agitation while adding is added into fully to water, when promptly system becomes clarification suddenly, the ganoderan nano-emulsion.
Embodiment 5: the ganoderan nano-emulsion
Composition weight (g)
Semen Maydis oil 1.5
Tween 80 0.5
Sorbester p17 1
Ganoderan 0.036
Ethanol 0.2
Distilled water 0.45
Precision takes by weighing recipe quantity Semen Maydis oil, Tween 80, sorbester p17, and under 45-60 ℃ of condition, magnetic agitation is even.After other gets ganoderan, ethanol and is dissolved in and is prepared into water in the distilled water, slowly drop in the said mixture, the magnetic agitation while adding is added into fully to water, when promptly system becomes clarification suddenly, the ganoderan nano-emulsion.
Claims (9)
1. ganoderan oral administration nanometer breast, the clear emulsion of forming by oil phase, surfactant, cosurfactant and water.Its raw material and mass percent thereof are: oil phase 18.9%-78.6%, and ganoderan 0.1%-2.2%, surfactant and cosurfactant 19.9%-76.6%, surplus is a distilled water, above-mentioned raw materials percentage ratio sum is 100%.
2. ganoderan oral administration nanometer breast according to claim 1 is characterized in that described ganoderan derives from Ganoderma sporophore, is water soluble polysaccharide, and its range of molecular weight distributions is 5kDa-40kDa.
3. ganoderan oral administration nanometer breast according to claim 1 is characterized in that described oil phase is one or more a mixture of long-chain triglyceride, long-chain two sweet esters, long-chain monoglyceride, long-chain fat isopropyl propionate.
4. according to claim 1,3 described ganoderan oral administration nanometer breasts, it is characterized in that described oil phase preferably is rich in any in the Oleum Glycines of long-chain triglyceride, Semen Maydis oil, the isopropyl myristate.
5. ganoderan oral administration nanometer breast according to claim 1 is characterized in that described surfactant is one or more the mixture in glyceryl monostearate, sorbitan fatty acid ester, polyoxyethylene sorbitan fatty acid ester, castor oil hydrogenated polyoxyethylene ether, castor oil polyoxyethylene ether, lecithin or soybean phospholipid, the fatty glyceride.
6. according to claim 1,5 described ganoderan oral administration nanometer breasts, it is characterized in that one or more the mixture in the preferred sorbitan fatty acid ester of described surfactant, polyoxyethylene sorbitan fatty acid ester, castor oil hydrogenated polyoxyethylene ether, the castor oil polyoxyethylene ether.
7. ganoderan oral administration nanometer breast according to claim 1 is characterized in that described cosurfactant is one or more the mixture in long-chain monoglyceride, ethanol, the propylene glycol.
8. ganoderan oral administration nanometer breast according to claim 1, it is directly oral to it is characterized in that described ganoderan nano-emulsion is used for, or pack into hard gelatin capsule or Perle or enteric solubility hard gelatin capsule or enteric solubility Perle are prepared into oral formulations.
9. use in the medicine for preparing treatment or prophylaxis of tumours, human body immunity improving according to the arbitrary described ganoderan oral administration nanometer Emulsion of claim 1-8.
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104473872A (en) * | 2014-12-11 | 2015-04-01 | 浙江大学 | Plant polysaccharide oil emulsion and preparation method and application thereof |
| CN108635577A (en) * | 2018-08-07 | 2018-10-12 | 河南牧业经济学院 | Radix Et Caulis Acanthopanacis Senticosi polysaccharide nano-emulsion and preparation method thereof |
| CN109646399A (en) * | 2019-02-15 | 2019-04-19 | 中国科学院上海药物研究所 | A kind of Orally taken emulsion and its preparation method and application comprising ganoderma lucidum spore oil and ganoderma lucidum polysaccharide |
| CN114246839A (en) * | 2020-09-22 | 2022-03-29 | 鲁南制药集团股份有限公司 | Oral nanoemulsion enteric capsule and preparation method thereof |
| CN115282089A (en) * | 2022-08-02 | 2022-11-04 | 安徽中医药大学 | Ganoderma lucidum extract nanoemulsion and preparation method and application thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1682753A (en) * | 2005-03-04 | 2005-10-19 | 山东省中医药研究院 | Paeonal injection emulsion for anti-tumor and its preparing method |
| WO2009087368A1 (en) * | 2008-01-04 | 2009-07-16 | The University Of Nottingham | Compositions comprising ganoderma lucidum extracts and uses thereof |
-
2010
- 2010-12-14 CN CN2010105881962A patent/CN102058530A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1682753A (en) * | 2005-03-04 | 2005-10-19 | 山东省中医药研究院 | Paeonal injection emulsion for anti-tumor and its preparing method |
| WO2009087368A1 (en) * | 2008-01-04 | 2009-07-16 | The University Of Nottingham | Compositions comprising ganoderma lucidum extracts and uses thereof |
Non-Patent Citations (1)
| Title |
|---|
| 林华型: "灵芝多糖抗肿瘤靶向作用机制研究进展", 《细胞与分子免疫学杂志》 * |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104473872A (en) * | 2014-12-11 | 2015-04-01 | 浙江大学 | Plant polysaccharide oil emulsion and preparation method and application thereof |
| CN104473872B (en) * | 2014-12-11 | 2017-09-26 | 杭州眺旺生物科技有限公司 | Plant polyose oil emu and its production and use |
| CN108635577A (en) * | 2018-08-07 | 2018-10-12 | 河南牧业经济学院 | Radix Et Caulis Acanthopanacis Senticosi polysaccharide nano-emulsion and preparation method thereof |
| CN109646399A (en) * | 2019-02-15 | 2019-04-19 | 中国科学院上海药物研究所 | A kind of Orally taken emulsion and its preparation method and application comprising ganoderma lucidum spore oil and ganoderma lucidum polysaccharide |
| CN114246839A (en) * | 2020-09-22 | 2022-03-29 | 鲁南制药集团股份有限公司 | Oral nanoemulsion enteric capsule and preparation method thereof |
| CN114246839B (en) * | 2020-09-22 | 2024-05-28 | 鲁南制药集团股份有限公司 | Oral nanoemulsion enteric capsule and preparation method thereof |
| CN115282089A (en) * | 2022-08-02 | 2022-11-04 | 安徽中医药大学 | Ganoderma lucidum extract nanoemulsion and preparation method and application thereof |
| WO2024027113A1 (en) * | 2022-08-02 | 2024-02-08 | 安徽中医药大学 | Ganoderma lucidum extract nanoemulsion, preparation method therefor, and use thereof |
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Application publication date: 20110518 |