CN102600240A - Compound oil-in-water Chinese magnoliavine fruit oil nano-emulsion composition and preparation method thereof - Google Patents
Compound oil-in-water Chinese magnoliavine fruit oil nano-emulsion composition and preparation method thereof Download PDFInfo
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- CN102600240A CN102600240A CN2012100564999A CN201210056499A CN102600240A CN 102600240 A CN102600240 A CN 102600240A CN 2012100564999 A CN2012100564999 A CN 2012100564999A CN 201210056499 A CN201210056499 A CN 201210056499A CN 102600240 A CN102600240 A CN 102600240A
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Abstract
The invention discloses a compound oil-in-water Chinese magnoliavine fruit oil nano-emulsion composition and a preparation method thereof. The compound oil-in-water Chinese magnoliavine fruit oil nano-emulsion composition is characterized in that: the particle diameter of the nano-emulsion composition is between 1 nanometer and 100 nanometers; the nano-emulsion composition consists of the following raw materials in percentage by mass: 0.1-8.0 percent of Chinese magnoliavine fruit oil, 0.1-7.0 percent of Chinese thorowax root oil, 0.1-6.0 percent of Chinese angelica oil, 19.0-35.0 percent of a surfactant and the balance of distilled water; and the sum of the mass percentages of the components is 100 percent. The compound oil-in-water Chinese magnoliavine fruit oil nano-emulsion has the effects of resisting liver injury, lowering the content of glutamic-pyruvic transaminase in blood serums, recovering liver functions, effectively improving a liver protecting effect on a clinical symptom, treating various liver diseases of human beings, caring liver daily, preventing, treating and caring various infective liver diseases of livestock, and the like. The compound oil-in-water Chinese magnoliavine fruit oil nano-emulsion composition has high intestinal absorption rate, high stability, high bioavailability and a remarkable curative effect after being taken orally, and has a wide market prospect in the medical field.
Description
Technical field
The invention belongs to field of medicaments, relate to a kind of a kind of compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition that can be used for people and poultry liver disease treatment and liver daily health caring and preparation method thereof.The present invention can be used for the treatment of people's various hepatopathys and the health care of daily liver, prevention, treatment and the health care etc. of the various infectiousness hepatopathys of poultry.
Background technology
Hepatopathy is meant the pathological changes that occurs in liver.Common have hepatitis, liver cirrhosis, liver abscess, a primary hepatocarcinoma etc.Hepatitis is main with chronic hepatitis mainly, is divided into chronic viral hepatitis, autoimmune hepatitis, drug toxicity hepatitis, heritability hepatitis and other agnogenic chronic hepatitis by the cause of disease.And viral hepatitis is the most common with hepatitis B, and global according to statistics hepatitis B surface antigen carries number and surpasses 2.8 hundred million, is known as " the three big pertinacious diseases " that threaten human health.The performance of hepatopathy is that very obscure, the most outstanding symptom is lassitude and weak and anorexia.Common sympton has the abdominal part distending pain, feel sick, food back distension or jaundice is arranged, xerostomia, it is dried or half congealed to defecate, yellow urine, as develop into liver cirrhosis then symptom can increase the weight of.
The avian infectious hepatopathy of family is perplexing numerous raisers for a long time always; The primary disease pathogen is a lot, and antibacterial (like escherichia coli, Salmonella etc.), virus (like infectious bursal disease, newcastle etc.), fungus (like Aspergillus flavus etc.) and parasite (like Histomoniasis etc.) are arranged, and these cause of diseases all can cause hepar damnification; Liver function descends; Detoxification ability reduces, and toxin accumulates in blood and causes that Abwehrkraft des Koepers descends, and brings out and infects multiple disease.Traditional treatment all is to be main to kill cause of disease with improving immunity, has ignored the protection link of liver, and if liver function can not get not recovering, then the state of an illness can be shown effect repeatedly.The Chinese powder medicine that adopts clinically also causes utilization ratio of drug low because of poultry appetite is low, digestive tract function descends, and curative effect is undesirable, and aquaculture cost is raise.
No matter be the sort of hepatopathy, clinical all with recovering liver function, reduce the first step of hepatic injury for treatment.Have only liver function to recover, hepatic injury has been prevented, and the state of an illness could be controlled, and liver just can be protected, and just can carry out next step treatment.Hepatic on the society is a lot, and like five clever balls, HUGAN PIAN etc., its main component all be unable to do without Fructus Schisandrae Chinensis, this just Fructus Schisandrae Chinensis have the proof of good liver-protecting efficacy.
Fructus Schisandrae Chinensis is the fruit of magnoliaceae schisandra, gains the name because of it has sweet, sour, hot, bitter, the salty five tastes; Warm in nature, return lung, the heart, kidney channel; Effect with astringent or styptic treatment for spontaneous sweating, the supplementing QI for promoting the production of body fluid of convergence, kidney calming, the clinical chronic cough dyspnea due to deficiency that is usually used in, emission, enuresis frequent micturition, incessant chronic diarrhea etc.Fructus Schisandrae oil is the volatile oil that from Fructus Schisandrae Chinensis, extracts; Main active is australene, nopinene, myrcene, limonene etc.; Have liver protection preferably, it can promote hepatic glycogen to decompose, and the glucose phosphorylation process of fructose in brain, liver, the muscle is strengthened; Can obviously reduce serum glutamic pyruvic transminase content, the hepar damnification that carbon tetrachloride is caused has protective effect, the clinical treatment that is mainly used in treatment various acute, chronic hepatitis, viral hepatitis and chronic persistent hepatitis etc.
At present people mainly are confined on the former medicine the utilization of Fructus Schisandrae oil, though certain curative effect is arranged, the effective ingredient of medicine are utilized insufficient, and concentration is low.Oral formulations on the market etc. are not high with the back drug bioavailability, and assimilation effect is undesirable, has directly influenced the utilization and extention of Fructus Schisandrae oil.Therefore, be necessary to develop the deficiency that a kind of novel form comes the replace old dosage form.
Summary of the invention
The present invention is directed to the defective of the problems referred to above and prior art, provide a kind of bioavailability good, the compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition of the hepatic disease of people and poultry is treated in high being used to of stability.Said composition safely, have no side effect, evident in efficacy.
The technical scheme that realizes the foregoing invention purpose is a compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition, and it is made up of the material of following mass percent:
Fructus Schisandrae oil 0.1%～8.0%
Oleum Bupleuri 0.1%～7.0%
Radix Angelicae Sinensis oil 0.1%～6.0%
Surfactant 19.0%～35.0%
Surplus is a distilled water
Above-mentioned total component is 100%.
On surfactant selection, the present invention selects the nonionic surfactant of avirulence and good biocompatibility for use.Nonionic surfactant is more stable in solution, is not subject to the influence of strong electrolyte, inorganic salts, also is not subject to the influence of soda acid, and good with the compatibility of other surfactants, and haemolysis is less.In theory; The HLB value that the preparation of O/W type nanometer emulsion needs surfactant is between 8～18; Consider preparation technology's simplicity; Be the easy formation property of nano-emulsion and the stability of the nano-emulsion for preparing, the present invention selects the liquid nonionic surfactant of HLB between 10～15 for use, preferably uses tween 80.
The present invention with Fructus Schisandrae oil, Oleum Bupleuri and Radix Angelicae Sinensis oil as combination; Be because Fructus Schisandrae oil has tangible anti-liver injury; Reduce the effect of serum glutamic pyruvic transminase; Can improve glutathion peroxidase in the liver, superoxide dismutase and catalatic activity, thereby reach the liver-protective purpose of recovering liver function, in this prescription as monarch drug; The Oleum Bupleuri main component is bupleurumol, eugenol, saikoside etc., has the effect of reducing fever by reconciliation, depressed liver-energy dispersing and QI regulating, elevate a turnable ladder yang-energy, cures mainly alternate attack of chill and fever, incoordination between the liver and spleen, stagnation of QI due to depression of the liver etc.Pharmacological action shows as and can significantly reduce hepatocellular degeneration and the necrosis that chemicals causes, effectively improves symptom, retraction liver spleen, recovers liver function, and hepatitis B antigen is turned out cloudy has better action, in this prescription as ministerial drug; Radix Angelicae Sinensis oil is that main component is ligustilide, n-butene base Phthalide, angelicone etc., can increase liver to oxygen absorption from the volatile oil of the dry root extraction of Radix Angelicae Sinensis; Purify the blood, thereby nutrition brain, the heart, spleen and protecting liver and detoxication can increase the bile secretion rate; Facilitating digestion; To the liver plasma membrane damage, liver cell mitochondria damage and lysosome membrane damage have the improvement effect, are used as adjuvant drug in this prescription; Three flavor Chinese medicine composition can reduce the hepatocyte injury that is caused by a variety of causes effectively, improve clinical symptoms, significantly reduce glutamate pyruvate transaminase content in the blood, recover liver function, and facilitating digestion reaches the purpose that protects the liver.
The present invention detects through transmission electron microscope, and droplet diameter distribution is between 1～100nm, and outward appearance is yellow or flaxen transparency liquid, has good stability:
1, ageing stability
Ageing stability is meant when nano-emulsion is preserved under room temperature nature change condition, and outward appearance prolongs and the degree that changes in time.This compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition through the lasting clear of check outward appearance, is not found breakdown of emulsion situation such as muddiness or deposition behind storage, explain that ageing stability is good.
2, heat storage stability
This compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition is sub-packed in several vials, places 50 ℃ of calorstats to store 15d after the sealing, the every sampling at a distance from 5d observed.The result shows that this liquid heat storage back check outward appearance still keeps the outward appearance of clear, does not find breakdown of emulsion situation such as muddiness or layering, explains that heat storage stability is good.
3, anti-freeze-stable property
With this compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition in refrigerator-10 ℃ preserve a week after.Return to room temperature.If nano-emulsion is solid at-10 ℃, return to room temperature, the outward appearance clear still through dilution check back, and place all continued and check, do not find breakdown of emulsion situation such as muddiness or deposition, think that then freezing-resistance is good.
4, accelerated stability
This compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition is placed test tube, sealing, under the rotating speed of 15000r/min centrifugal 20 minutes, the profit layering does not appear, and clear still after dilution is checked is not found breakdown of emulsion situation such as muddiness or deposition.
5, light stability experiment
This compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition of part is loaded in the vial, and sealing places under the daylight, and light at room temperature is according to 10d, in 1d, 3d, 5d, 10d sampling.The result shows that this nanoemulsions still keeps clear, and breakdown of emulsion situation such as no muddiness or layering show that light stability is good.
Compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition of the present invention has the effect of treatment people and poultry liver disease and liver health care.
Usage and dosage: oral or drinking-water (poultry), the each 0.2ml of people, every day 3 times; The every 100ml of poultry converts 1 ton in water, freely drinks.
Compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition of the present invention compared with prior art has the following advantages:
1) higher thermodynamic stability is arranged.The nano-emulsion of preparation stores not phase-splitting, does not precipitate between-10 ℃ and 50 ℃, stability improves;
2) high-absorbility.This compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition emulsion droplet particle diameter can be better by intestinal absorption after oral between 1 ~ 100nm;
3) method technology is simple, is fit to large-scale production.
The specific embodiment
Below come further to set forth the beneficial effect of medicine according to the invention through pharmacodynamics test and contrast test.
Test Example 1Compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition (is example with embodiment 1) the anti-liver injury test of pesticide effectiveness
30 healthy mices are divided into blank group, CCl at random
43 groups of model group and Fructus Schisandrae oil nano emulsion composition groups, 10 every group.Every nanoemulsions 0.4ml that irritates stomach 8% drug loading of Fructus Schisandrae Chinensis nano emulsion composition group mice, blank group and CCl
4Model group is irritated the solvent that makes up a prescription of stomach equivalent respectively, once a day, and one week of continuous irrigation stomach.Behind the last administration 3h, blank control group mouse peritoneal injection liquid paraffin 0.2ml, CCl
4Model group and Fructus Schisandrae oil nano-emulsion group be lumbar injection 3.0% CCl respectively
4Solution 0.2ml, three groups of equal fasting of mice are only drunk water then.Take a blood sample separation of serum behind the 24h from eyeball.Adopt automatic clinical chemistry analyzer to measure glutamate pyruvate transaminase (ALT) content in the blood.
Table 1Compound recipe oil-in-water type Fructus Schisandrae oil nano-emulsion anti-liver injury effect experiment result
Can find out by the result: CCl
4Successfully caused the hepatic injury of mice, Serum ALT content is obviously raise; CCl
4The ALT content difference of model group and Fructus Schisandrae oil nano-emulsion group is remarkable.The result shows that compound recipe oil-in-water type Fructus Schisandrae oil nano-emulsion is anti-liver injury effectively, plays liver protective effect.
Test Example 2Compound recipe oil-in-water type Fructus Schisandrae oil nanometer (is example with newborn embodiment 1) and other preparation for treating hepatic injury effect comparison tests
Choose 40 of healthy mices, be divided into blank, CCl at random
44 groups of model group, bifendate group and compound recipe oil-in-water type Fructus Schisandrae oil nano-emulsion groups, 10 every group.The bifendate group is irritated the bifendate medicinal liquid 0.3ml of stomach 20g/L, and compound recipe oil-in-water type Fructus Schisandrae oil nano-emulsion group is irritated the compound recipe oil-in-water type Fructus Schisandrae oil nano-emulsion 0.3ml of stomach 8%, blank group and CCl
4Model group is irritated the solvent that makes up a prescription of stomach equivalent, and continuous irrigation stomach 8d irritates stomach every day 1 time, behind the last administration 3h, and blank group lumbar injection saxol 0.2ml, CCl
4Model group, bifendate group and compound recipe oil-in-water type Fructus Schisandrae oil nano-emulsion group lumbar injection 3% CCl
4Solution 0.2ml then, to each group mice fasting, only drinks water.The blood sampling of 24h posterior orbit, separation of serum detects glutamate pyruvate transaminase (ALT) content.Mice is put to death, the aseptic part hepatic tissue of getting same position, in stripping and slicing fast on ice, size is about 1mm
3, carry out step by step processed 4 ℃ of fixing down backs with ethanol with 4% glutaraldehyde, process electron microscopic section after the epoxy resin embedding, observe ultrastructure of hepatic cell.
The Electronic Speculum criterion:
Not damaged: hepatocyte is normal, the nucleus clear in structure, and neat in edge, structure of mitochondria is normal, and ridge is prominent clear, is evenly distributed, and the rough endoplasmic reticulum regularity of distribution is the flat structure, marshalling;
General damage: slight hepatic cell swelling, the nucleus structure is fuzzyyer, and the edge is not whole, and structure of mitochondria is normal basically, and ridge is prominent fuzzy, and rough endoplasmic reticulum has the expansion phenomenon, and is flourishing;
Severe injury: hepatocyte is destroyed serious, the volume enlargement, and nuclear structure is fuzzy, and the edge is whole, and mitochondrial crista is dashed forward unclear, and part disappears, and rough endoplasmic reticulum quantity reduces, and the fracture that has is arranged in a jumble, and there have fat to ooze in the Cytoplasm that has to be existing.
Table 2Compound recipe oil-in-water type Fructus Schisandrae oil nano-emulsion and bifendate treatment hepatic injury effect comparison result of the test
Can be found out by the result: compound recipe oil-in-water type Fructus Schisandrae oil nano-emulsion has significant anti-liver injury effect, and liver protective effect is certain, and its effect is superior to bifendate.
Below come further to set forth medicine according to the invention through specific embodiment composition and method for preparing.
Embodiment 1
Fructus Schisandrae oil 5.0g, Oleum Bupleuri 1.5g, Radix Angelicae Sinensis oil 0.7g, tween 80 29.0g, distilled water 63.8g.
Above-mentioned each component is processed compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition, comprises the following steps:
1) accurately take by weighing the quality of tween 80, Fructus Schisandrae oil, Oleum Bupleuri, Radix Angelicae Sinensis oil, distilled water by filling a prescription, subsequent use;
2) with Fructus Schisandrae oil, Oleum Bupleuri, the Radix Angelicae Sinensis oil mixing and stirring of said amount, as oil phase;
3) join the surfactant tween 80 of said amount in the middle of the oil phase and stir;
4) with distilled water as water; At room temperature stir oil phase and tween 80 mixture rapidly; Slowly drip distilled water when stirring, this mixture system can occur by rare retrogradation, and is last again by thick thinning a series of variations; Be transparent liquid until system, promptly get compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition.
Embodiment 2
Fructus Schisandrae oil 5.4g, Oleum Bupleuri 0.7g, Radix Angelicae Sinensis oil 0.7g, tween 80 34.0g, distilled water 59.2g.
Embodiment 3
Fructus Schisandrae oil 3.5g, Oleum Bupleuri 0.1g, Radix Angelicae Sinensis oil 3.5g, tween 80 27.9g, distilled water 65.0g.
Embodiment 4
Fructus Schisandrae oil 8.0g, Oleum Bupleuri 0.2g, Radix Angelicae Sinensis oil 0.5g, tween 80 28.8g, distilled water 62.5g.
Embodiment 5
Fructus Schisandrae oil 4.4g, Oleum Bupleuri 0.7g, Radix Angelicae Sinensis oil 0.7g, tween 80 35.0g, distilled water 59.2g.
Embodiment 6
Fructus Schisandrae oil 1.8g, Oleum Bupleuri 0.1g, Radix Angelicae Sinensis oil 6.0g, tween 80 29.6g, distilled water 62.5g.
Embodiment 7
Fructus Schisandrae oil 1.0g, Oleum Bupleuri 1.0g, Radix Angelicae Sinensis oil 1.0g, tween 80 30.0g, distilled water 67.0g.
Embodiment 8
Fructus Schisandrae oil 7.2g, Oleum Bupleuri 0.5g, Radix Angelicae Sinensis oil 0.5g, tween 80 29.0g, distilled water 62.8g.
Embodiment 9
Fructus Schisandrae oil 8.0g, Oleum Bupleuri 6.0g, Radix Angelicae Sinensis oil 0.2g, tween 80 30.0g, distilled water 55.8g.
Embodiment 10
Fructus Schisandrae oil 4.5g, Oleum Bupleuri 2.0g, Radix Angelicae Sinensis oil 1.0g, tween 80 30.0g, distilled water 62.5g.
Embodiment 11
Fructus Schisandrae oil 4.0g, Oleum Bupleuri 0.8g, Radix Angelicae Sinensis oil 2.0g, tween 80 27.0g, distilled water 66.2g.
Claims (3)
1. a compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition is characterized in that, is made up of following raw materials by weight percentage:
Fructus Schisandrae oil 1.0%～8.0%, Oleum Bupleuri 0.1%～7.0%, Radix Angelicae Sinensis oil 0.1%～6.0%, surfactant 19.0%～35.0%, surplus are distilled water, and the mass percent sum of above-mentioned raw materials is 100%;
Described glass or plastic containers tween 80.
2. compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition according to claim 1 is characterized in that the particle diameter of this nano emulsion composition is between 1～100nm.
3. the method for preparing of the described a kind of compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition of claim 1 is characterized in that, may further comprise the steps:
Take by weighing surfactant, Fructus Schisandrae oil, Oleum Bupleuri, Radix Angelicae Sinensis oil, distilled water, subsequent use;
With Fructus Schisandrae oil, Oleum Bupleuri, Radix Angelicae Sinensis oil mixing and stirring, as oil phase;
Surfactant is joined in the middle of the oil phase and stirs;
Distilled water as water, is at room temperature stirred oil phase and surfactant mixture rapidly, slowly drip distilled water in the time of stirring, constantly stirring is transparent liquid until system, promptly gets compound recipe oil-in-water type Fructus Schisandrae oil nano emulsion composition.
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2959911A4 (en) * | 2013-06-12 | 2016-01-06 | Xiaoyan Zhang | Compound fructus forsythiae-radix bupleuri oil nanoemulsion preparation |
| CN114470042A (en) * | 2022-03-18 | 2022-05-13 | 四川农业大学 | Composition for preventing and treating animal liver injury and preparation method and application thereof |
-
2012
- 2012-03-06 CN CN2012100564999A patent/CN102600240A/en active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2959911A4 (en) * | 2013-06-12 | 2016-01-06 | Xiaoyan Zhang | Compound fructus forsythiae-radix bupleuri oil nanoemulsion preparation |
| CN114470042A (en) * | 2022-03-18 | 2022-05-13 | 四川农业大学 | Composition for preventing and treating animal liver injury and preparation method and application thereof |
| CN114470042B (en) * | 2022-03-18 | 2023-09-05 | 四川农业大学 | Composition for preventing and treating liver injury of animals as well as preparation method and application thereof |
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Application publication date: 20120725 |