CN1075378C - 'Futekang' traditional Chinese medicine emulsion and preparation method thereof - Google Patents

'Futekang' traditional Chinese medicine emulsion and preparation method thereof Download PDF

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CN1075378C
CN1075378C CN97118344A CN97118344A CN1075378C CN 1075378 C CN1075378 C CN 1075378C CN 97118344 A CN97118344 A CN 97118344A CN 97118344 A CN97118344 A CN 97118344A CN 1075378 C CN1075378 C CN 1075378C
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emulsion
semen coicis
oil
emulsion preparation
water
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CN1212874A (en
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陈金义
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Abstract

The present invention discloses an emulsion preparation and a preparation method thereof, and the emulsion preparation is formed by extracting and compounding natural medicines and has an antitumor function. The emulsion preparation is composed of coix seed oil, brucea javanica oil, fabaceous lecithin, pure glycerol and injection water. The active substances of the pure Chinese herbal medicines can be protected from losing by intravenous administration. The emulsion preparation is convenient for an organism to directly absorb, and can exert optimal effect. The emulsion preparation has the effect of heat clearing, detoxication, kidney nourishment and Yin supplement, and is especially suitable for inhibiting Ehrlich carcinoma, cervical cancers and the proliferation of ascitic type liver cancer cells and preventing atherosclerosis, etc. The emulsion preparation is clinically used for antitumor effect and is mainly used for treating cancers.

Description

A kind of antineoplastic Chinese medicine Emulsion and preparation method thereof
The present invention relates to a kind of antineoplastic Chinese medicine emulsion formulations, particularly relate to a kind of antitumor emulsion formulations that forms by natural drug extract compatibility, the invention still further relates to the preparation method of this emulsion formulations.
At present, cancer is one of several diseases that sickness rate is the highest in the world today, seizes thousands of people's life every year, does not still have the good medicine of radical cure so far.The chemotherapy cure rate that adopts is not high at present, and side effect is big.More domestic producers also develop some Chinese herbal compound preparations, though can reach certain antitumous effect, general effect is not good.Extracting the active substance smelting and treat tumor from natural drug, be the content of present Chinese medicine research exploitation, but difficulty is very big, and achievement in research is very few.
Semen Coicis is the dry kernel of grass Semen Coicis, the record that from ancient times just has Semen Coicis treatment disease, body-building to prolong life, external anticancer in the sixties have begun Semen Coicis, enhance immunity, provide the research of active ingredient one Semen Coicis oil of energy nutrient, CN1070680 discloses a kind of Semen Coicis neutral fat and preparation method thereof, this adlay oil extracts from Semen Coicis, has anticancer function.CN1080176 discloses a kind of Coixenolide neutral fat emulsion, mainly is made up of the Semen Coicis neutral fat, has the enhancing human body immunity function, high-energy nutrition, treatment cardiovascular system diseases is provided, suppresses effect of malignant tumors.Human colon cancer, hepatocarcinoma, pulmonary carcinoma etc. all there is certain treatment effect.
Fructus Bruceae is the seed of bitter subject plant Fructus Bruceae, and it is full to be used for treating the feeling of stuffiness in chest, miasma, and amebic dysentery, diseases such as wart are not seen the report of other further investigation.
Utilization is extracted active substance and is carried out compatibility from natural drug, because the difference that compatibility is formed, and the difference of medicine compatibility method, performance and difference on effect are very big.
The object of the present invention is to provide a kind of emulsion formulations that forms by natural drug extract compatibility with anti-tumor function.
Another object of the present invention is to provide a kind of preparation method of making quiet injectable emulsion by the natural drug extract.
Consisting of in per 100 milliliters of emulsions of natural drug extract Chinese medicine Emulsion of the present invention contains:
Semen Coicis oil 3.60~4.50 gram Oleum Fructus Bruceae 3.60~4.50 grams
Fabaceous lecithin 0.80~1.00 gram pure glycerin 2.50~3.10 grams
Surplusly become in per 100 milliliters of emulsions and contain for its preferred group of water for injection:
Semen Coicis oil 4.10 gram Oleum Fructus Bruceae 4.10 grams
Fabaceous lecithin 0.90 gram pure glycerin 2.80 grams
Surplus is the preparation method of a kind of antineoplastic Chinese medicine of water for injection Emulsion, may further comprise the steps successively:
(1). with fabaceous lecithin, glycerol and be preheated to 80 ℃ an amount of water for injection and mix, change in the high-speed tissue mashing machine, change with per minute 8000 and stirred 3 minutes, carry out repeatedly 3 times, until the fabaceous lecithin full and uniform dispersion;
(2). in above-mentioned dispersion liquid, adding is preheated to 80 ℃ Semen Coicis oil, Oleum Fructus Bruceae, changes in the high-speed tissue mashing machine, changes with per minute 8000 and stirs 3 minutes, carries out repeatedly 3 times, until Semen Coicis oil, Oleum Fructus Bruceae full and uniform dispersion;
(3). get above-mentioned colostrum and add the water for injection that is preheated to 80 ℃ and make and reach full dose, be transferred in the high pressure dispersing emulsification machine, carry out homogenize 3 times, microscopy is carried out in sampling, to oil droplet be 1 micron;
(4). get above-mentioned Emulsion and filter the back embedding in 10 milliliters of ampoule bottles, fill nitrogen, under 100 ℃, sterilized 30 minutes, promptly.
Oleum Fructus Bruceae, Semen Coicis oil can mix with water after adding water to form oil/water emulsion, so can supply intravenous drip.Because the decentralized photo surface area is big, absorb rapidly, the human body reticuloendothelial system has the external foreign body effect of engulfing simultaneously, bruceolic oil emulsion and Semen Coicis oil breast enter in the body by human vein, oil droplet is just stored at the abundant position of reticuloendothelial cell as foreign body, drug level is greatly improved, reach the curative effect height, the purpose that drug effect is long and side effect is little.
Press down in the cancer process of the test external, microdroplet and the cancerous cell of finding bruceolic oil emulsion have affinity preferably, can be in the intensive adhesion long period property on every side of cancerous cell, help contacting of medicine and cancerous cell, make anticarcinogen increase the chance of infiltrating, produce and directly kill or the effect of anticancer to cancerous cell.Histopathology is observed, and the combined effect of Oleum Fructus Bruceae and Semen Coicis oil microdroplet makes the cancerous cell degeneration, and broken, necrosis has effect.Therefore, Oleum Fructus Bruceae and Semen Coicis oil being made vein emulsion, is present domestic optimal route of administration and dosage form.
The present invention carries out compatibility with the active substance that extracts from natural drug, saving pure Chinese herbal medicine and nutrition from damage does not suffer a loss, being convenient to body directly absorbs it, and performance optimum effect, the directly intravenous drip of this Emulsion, heat-clearing and toxic substances removing, support the kidney nourishing YIN, be particularly useful for suppressing ehrlich carcinoma and cervical cancer, ascites hepatoma cells propagation, stop atherosclerosis etc., have antitumor efficacy.
Selected Semen Coicis oil is a commodity Semen Coicis neutral fat, be faint yellow transparent oily liquid, its Main Ingredients and Appearance is triglyceride, diglyceride, monoglyceride, fatty alkanyl ester etc., pressing fatty oil detects, its physicochemical constant (20 ℃) is: proportion is 0.915~0.918, and index of refraction is 1.470~1.475, and acid value is not more than 0.2, iodine value is 95.00~107.00, and saponification value is 185.00~195.00.
The process for purification of selected Oleum Fructus Bruceae is: with the fragmentation of Fructus Bruceae kernel, soak more than 12 hours with an amount of petroleum ether, after the reflux, extract,, collect extracting solution and reclaim solvent, get the Oleum Fructus Bruceae crude product, crude product makes purified Oleum Fructus Bruceae through active-carbon finely.
Oleum Fructus Bruceae is yellow transparent liquid, and its composition is three oleic acid glycerol, oleic acid etc., and its physicochemical constant (20 ℃) is: proportion is 0.9061~0.9110, index of refraction is 1.4670~1.4685, acid value is not more than 8.88, and iodine value is 85.82~88.50, and saponification value is 186.3~192.6.
Because Oleum Fructus Bruceae, Semen Coicis oil are intravenously administrable, should select for use in human body nontoxicly, have emulsifying capacity efficiently, and the stable emulsifying agent of chemical property.Through repetition test repeatedly, selecting purified fabaceous lecithin for use is emulsifying agent, and it mainly contains lecithin, also contains a small amount of other phospholipid, as cephalin.The phosphorous acid group of lecithin molecules, the polar end of choline base, the tool hydrophilic, the non-polar end of being made up of hydrocarbon chain has lipotropy, thus have the good emulsifying performance, and have than characteristics such as other phospholipid are stable, toxicity is little.Fabaceous lecithin should be made with extra care before using, and removes the impurity that wherein can cause blood pressure lowering, pyrogenicity etc.
The process for purification of selected fabaceous lecithin is: saltout (1): get 1 part of the full fabaceous lecithin of powdery, 12 parts of distilled water, in boiling water bath, stir into colloidal dispersions, drop into 1.8 parts of anhydrous sodium sulfates, continue slowly to stir, treat that phospholipid is bulk and separates out, discard saturated metabisulfite solution, carry out pickle change again, 5 parts of adding distil waters, 0.3 part of anhydrous sodium sulfate, method is the same; (2) extract pure dissolubility lecithin part, the fabaceous lecithin that salts out is placed in the vacuum desiccator, in moving to wide mouthed bottle behind the drying under reduced pressure below 75 ℃, 95% ethanol that adds 8.7 times of raw material inventorys, stirring and refluxing was extracted 3 hours in water-bath (80 ℃), the cooling hypsokinesis goes out to contain the mother solution of fabaceous lecithin, separates out through the freezing cephalin precipitation that makes.(3) alcoholic solution of phospholipid places in the water-bath and heats, and when treating that the ethanol temperature rises to 35 ℃, adds the activated alumina of 0.5 times of material quantity, fully stirs 1 hour after-filtration.(4) add 0.22 times active carbon in the above-mentioned alcoholic solution, fully stir 1 hour after-filtration and decolour.(5) alcoholic solution is placed alembic, under nitrogen (through washing, purifying) and 70 ℃ of heating in water bath, ethanol is removed in distilling under reduced pressure.(6) ether that adds 0.75 times of material quantity dissolves the fabaceous lecithin of evaporate to dryness in alembic.Nitrogen, airtight, freeze overnight are filled in the diethyl ether solution bottling.After the filtration mother solution is put vacuum evaporator, under logical nitrogen,, get the powdery fabaceous lecithin in 40 ℃ of pressure reducing and steaming ether of water-bath.(7) add anhydrous propanone in above-mentioned powdery fabaceous lecithin, grind repeatedly and embathe remaining oils and fats, moisture, the pigment of removing in the fabaceous lecithin.(8) the refining fabaceous lecithin that acetone was washed is contained in brown container, adds the anhydrous propanone submergence, airtight, lucifuge cold preservation.
Above-mentioned refining fabaceous lecithin meets the intravenous injection requirement through being up to the standards, and can be used as emulsifying agent and uses.
Glycerol oozes the adjustment agent as the grade of this Emulsion.Ooze because of general grade and to adjust dispersion and the outward appearance that agent such as sodium chloride, glucose all influence emulsion.Be subjected to the influence of sodium chloride electrolysis matter, the emulsion spherolite that makes is big, to thermally labile; Glucose is heated easy to change, influences the outward appearance of emulsion.Through test, adopt content to ooze the adjustment agent at the pharmaceutical grade glycerol work more than 97% etc., can reach optimum efficiency.
It is about 1 micron more than 90% that this Emulsion requires oil droplet, and oil droplet is excessive thromboembolism danger capillaceous, and the too small microemulsion that then forms of oil droplet owing to absorb too fastly, may increase toxicity.Can pass through the distribution of the oil droplet size of this Emulsion of laser scattering method, after measured, a kind of antineoplastic Chinese medicine Emulsion oil droplet that makes by said method is about 1 micron more than 90%.
The present invention is further illustrated below in conjunction with embodiment.
Embodiment 1:
Get 80 gram fabaceous lecithins, 250 gram glycerol mix with an amount of water for injection that is preheated to 80 ℃, change in the high-speed tissue mashing machine, change stirrings 3 minutes with per minute 8000, carry out repeatedly 3 times, until the fabaceous lecithin full and uniform dispersion; In above-mentioned dispersion liquid, add Semen Coicis oil 360 grams, Oleum Fructus Bruceae 360 grams that are preheated to 80 ℃, change in the high-speed tissue mashing machine, change with per minute 8000 and stirred 3 minutes, carry out repeatedly 3 times, until Semen Coicis oil, Oleum Fructus Bruceae full and uniform dispersion; Get above-mentioned colostrum and add the water for injection that is preheated to 80 ℃ and make and reach full dose, be transferred in the high pressure homogenization machine, carry out homogenize 3 times, microscopy is carried out in sampling, to oil droplet be about 1 micron; Get above-mentioned Emulsion and filter the back embedding in 10 milliliters of ampoule bottles, fill nitrogen, under 100 ℃, sterilized 30 minutes, promptly get a kind of antineoplastic Chinese medicine Emulsion.
Embodiment 2:
Get 100 gram fabaceous lecithins, 310 gram glycerol mix with an amount of water for injection that is preheated to 80 ℃, change in the high-speed tissue mashing machine, change stirrings 3 minutes with per minute 8000, carry out repeatedly 3 times, until the fabaceous lecithin full and uniform dispersion; In above-mentioned dispersion liquid, add Semen Coicis oil 450 grams, Oleum Fructus Bruceae 450 grams that are preheated to 80 ℃, change in the high-speed tissue mashing machine, change with per minute 8000 and stirred 3 minutes, carry out repeatedly 3 times, until Semen Coicis oil, Oleum Fructus Bruceae full and uniform dispersion; Get above-mentioned colostrum and add the water for injection that is preheated to 80 ℃ and make and reach full dose, be transferred in the high pressure homogenization machine, carry out homogenize 3 times, microscopy is carried out in sampling, to oil droplet be about 1 micron; Get above-mentioned Emulsion and filter the back embedding in 10 milliliters of ampoule bottles, fill nitrogen, under 100 ℃, sterilization in 30 minutes promptly gets a kind of antineoplastic Chinese medicine Emulsion.

Claims (3)

1. antineoplastic Chinese medicine Emulsion, it consists of in per 100 milliliters of emulsions and contains:
Semen Coicis oil 3.60~4.50 gram Oleum Fructus Bruceae 3.60~4.50 grams
Fabaceous lecithin 0.80~1.00 gram pure glycerin 2.50~3.10 grams
Surplus is water for injection
2. a kind of antineoplastic Chinese medicine Emulsion according to claim 1, it consists of in per 100 milliliters of emulsions and contains:
Semen Coicis oil 4.10 gram Oleum Fructus Bruceae 4.10 grams
Fabaceous lecithin 0.90 gram pure glycerin 2.80 grams
Surplus is water for injection
3. the preparation method of a kind of antineoplastic Chinese medicine Emulsion according to claim 1 and 2 may further comprise the steps successively:
(1). with fabaceous lecithin, glycerol and be preheated to 80 ℃, water for injection mixes, and changes in the tissue mashing machine, change with per minute 8000 and stirred 3 minutes, 3 times repeatedly, until the fabaceous lecithin homodisperse;
(2). in above-mentioned dispersion liquid, adding is preheated to 80 ℃ Semen Coicis oil, Oleum Fructus Bruceae, changes in the tissue mashing machine, and change with per minute 8000 and stirred 3 minutes, 3 times repeatedly, until Semen Coicis oil, Oleum Fructus Bruceae homodisperse;
(3). get above-mentioned colostrum and add the water for injection that is preheated to 80 ℃ and make and reach full dose, be transferred in the high pressure dispersing emulsification machine, homogenize 3 times, the sampling microscopy, to oil droplet be 1 micron;
(4). get above-mentioned Emulsion and filter the back embedding in 10 milliliters of ampoule bottles, fill nitrogen, under 100 ℃, sterilized 30 minutes.
CN97118344A 1997-09-30 1997-09-30 'Futekang' traditional Chinese medicine emulsion and preparation method thereof Expired - Fee Related CN1075378C (en)

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CN1075378C true CN1075378C (en) 2001-11-28

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Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1485072A (en) * 2002-09-28 2004-03-31 Coix seed oil soft capsule for curing prostate diseases and the application thereof
CN105477554A (en) * 2015-12-31 2016-04-13 蒲敬北 Medicine for treating HPV infection and preventing cervical cancer and preparation method of medicine
CN110613808A (en) * 2019-09-26 2019-12-27 浙江工商大学 Emulsion for reducing skin melanoma and preparation method and application thereof

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
中国医院药学杂志1993,13(6) 2093.6.30 罗伯远,鸦胆子口服液的研制 *
中西医结合杂志1985,5(2) 2085.2.28 苏守元等,10%鸦胆子油静脉乳剂治疗肺癌脑转移16例临床疗效观察 *
浙江药爱1986,3(6) 2086.6.30 史沛海等,薏苡仁油提取与期静脉乳剂制备 *
浙江药爱1986,3(6) 2086.6.30 史沛海等,薏苡仁油提取与期静脉乳剂制备;中国医院药学杂志1993,13(6) 2093.6.30 罗伯远,鸦胆子口服液的研制;中西医结合杂志1985,5(2) 2085.2.28 苏守元等,10%鸦胆子油静脉乳剂治疗肺癌脑转移16例临床疗效观察 *

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