CN1029293C - Coix seed neutral oil emulsion - Google Patents
Coix seed neutral oil emulsion Download PDFInfo
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- CN1029293C CN1029293C CN 93100735 CN93100735A CN1029293C CN 1029293 C CN1029293 C CN 1029293C CN 93100735 CN93100735 CN 93100735 CN 93100735 A CN93100735 A CN 93100735A CN 1029293 C CN1029293 C CN 1029293C
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- emulsion
- coix seed
- injection
- neutral oil
- neutral fat
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Abstract
The present invention relates to a medicament for resisting malignant tumors, namely a coix seed neutral oil emulsion (also called a Kanglaite vein emulsion) used for arterial and intravenous injection or oral application. Every 100 ml of the coix seed neutral oil emulsion contains 5 to 20g of coix seed neutral oil, 0.75 to 2.5g of emulsion, 2.5 to 5.0g of isotonizing agent and injection water as the rest and the coix seed neutral oil emulsion is emulsified in a two-step uniform emulsification dispersion method. The emulsion of the present invention has the advantages of high safety and reliability, reasonable formula, body immune function enhancement in clinic, high energy nutrition supply, cardiovascular system disease treatment, malignant tumor inhibition, and certain therapeutic effect on colon cancers, liver cancers, lung cancers, etc. so that the emulsion is a novel effective tumor resistant medicine.
Description
The present invention relates to a kind of anti-malignant tumor medicament, it be a kind of be the Emulsion of main component with Semen Coicis (claiming Semen Coicis again) neutral fat, can be used for artery and vein injection or oral.
States such as Japan have begun italian-jobi jen is carried out the basic research of anticancer effective component (italian-jobi jen ester) extraction and pharmacological screening before and after the sixties, but do not see the document and the patent report of relevant anti-tumor agent.Domestic once had a report (" Zhejiang pharmacy " for preparing the vein breast with the Petroleum ether extraction Semen Coicis oil; The 3rd the volume the 6th phase, in December, 1986) this Emulsion be with the Semen Coicis oil be the prescription principal agent, make with chemosynthesis emulsifier span, tween emulsifying, its prescription is:
Coix seed oil 10g
Arlacel-80 1g
Tween 80 1.5g
Water for injection adds to 100ml
This vein breast is mainly used in distribution test in preparation research and the body, and will reach the clinical use of people is still had following deficiency:
1. the coix seed oil purity of principal agent employing is not high, and its acid value is controlled at below 36, and this must have influence on Emulsion quality and drug safety, does not reach the requirement of Chinese Pharmacopoeia.
2. tween has haemolysis, can freely pass through cell membrane, makes emulsifying agent with it, need add could stop hemolytic generation after suitable grade is oozed adjustment agent adjustment.The commercial vein breasts of state such as English, moral, U.S., method, day all do not adopt the Tweens synthetic emulsifier at present, the domestic report that does not yet have employing.
3. do not have the vein breast must assist the isotonic agent that adds in the prescription, it is reasonable inadequately to fill a prescription.
The objective of the invention is in order to overcome the deficiency of prior art, a kind of principal agent purity height, emulsifying agent are safe and reliable, prescription is the Emulsion of principal agent with the Semen Coicis neutral fat reasonably and provide.
Semen Coicis neutral fat extracting method is open in Chinese patent application 92110839.7:
Semen Coicis powder extracts with acetone infusion process or percolation, and the crude product of extraction is rufous grease (according to Japanese document: think that the employing petroleum ether directly extracts, prove no obvious tumor killing effect, our pharmacological testing is also confirmed).Owing to contain a large amount of unhelpful deleterious impurity and the acid more than a times (as free fatty, pigment etc.) almost in the crude product, carry out the adsorption bleaching processing so be about to crude product earlier.Extract after treatment is a yellow oil.The present invention does not adopt silica gel column chromatography technology, thereby separation costs descends greatly.Yellow oil contains a large amount of acid fat, thus to adopt the alkali refining saponification handle with in and acid ingredient, separate milk.Utilize two utmost point characteristics of acetone molecules, add the dissolving of capacity acetone breakdown of emulsion, milk begins to become clear and bright thing, adds an amount of petroleum ether this moment again and extracts, acid ingredient (comprising the moisture in the former milk) changes the acetone layer over to: discard the acetone layer, neutrals is then stayed in the petroleum ether layer.If be difficult to eliminate acid ingredient and unnecessary alkali with conventional physical method, and cost dearly, operation is loaded down with trivial details.After reclaiming petroleum ether, pour in the vacuum distilling boiling water and fully boil, then can wash the residue of most organic solvent and alkali, discard water layer, heating in vacuum makes the water content in oil volatilization to the greatest extent for 100 ℃ again.Obtain the higher Semen Coicis neutral fat of purity thus.After once more adsorbing separation promptly obtain Semen Coicis neutral fat of the present invention.
Embodiment: get the 100kg Semen Coicis powder, use acetone extraction, obtain acetone extraction crude product 5kg behind the recovery acetone, adsorb, decolour.Add 152g NaOH(or KOH) to be made into concentration be that 2% heat alkali liquid carries out abundant alkali refining saponification, adding alkali number is decide according to the crude product acid value, heating then is in order to accelerate saponification speed and to make saponification abundant, leave standstill to abundant layering, separate milk.After being washed till milk and being neutral (about pH6-7) with 2-3 hot distilled water, it is clear and bright to add acetone breakdown of emulsion dissolving in 1: 1, and an amount of petroleum ether of restock extracts, and discards the acetone layer after making the abundant layering of solution, and neutrals is then stayed petroleum ether layer.Add residual substances such as adsorbents adsorb pigment and pyrogen.Filter back solution recovery petroleum ether and get neutral oil.Neutral oil is moved to boiling half an hour in the vacuum distilling boiling water, leave standstill to abundant layering, get 100 ℃ of neutral oil heating in vacuum and make the water content in oil volatilization to the greatest extent, the neutral fluid that obtains adds adsorbents adsorb once more and separates, get the about 2kg of faint yellow neutral fat, last packing is purified Semen Coicis neutral fat of the present invention through 160 ℃ of dry heat sterilizations 2 hours, and it can be for preparation artery and vein breast and oral breast.
Described adsorbent can be 1% active carbon, 3% kaolin, 10% aluminium oxide or other adsorbents.
Its main component of Semen Coicis neutral fat is triglyceride (91.48 ± 3.43%), diglyceride (1.47 ± 0.63%), monoglyceride (5.75 ± 3.19%), fatty alkanyl ester (1.00 ± 0.78%).Fatty acid residue after the esterlysis is hexadecanoic acid, octadecanoid acid, octadecenic acid, 18 diene acid.The Semen Coicis neutral fat is a kind of faint yellow transparent oily liquid, presses fatty oil and detects, and its physicochemical constant is: acid value＜0.20, proportion 0.915～0.918(20 ℃); Iodine value: 95.00～107.00; Saponification value: 185.00～195.00; Index of refraction 1.470～1.475(20 ℃).
The present invention is a principal agent with the Semen Coicis neutral fat, and content is 5-20g in per 100 milliliters of Emulsions; Emulsifying agent can be used Semen sojae atricolor (or egg yolk) lecithin, soybean phospholipid, Pu Lulang Garrick (Pluronic), polyglycereol Palmic acid glycol etc., and consumption is 0.75～2.5g; Isotonic agent (report that claims isotonic agent is abroad also arranged) can be used glycerol, sorbitol, xylitol, glucose etc., and consumption is 2.5g-5.0g, and the osmotic pressure that makes preparation is near the Human Physiology osmotic pressure.Water for injection adds to 100ml, carries out emulsifying with the even dispersion method of two step breasts, makes described Emulsion.Usually, the Semen Coicis neutral fat is got 10～20g; During the system vein emulsion, more safe and reliable with naturally occurring emulsifying agent such as Semen sojae atricolor (or egg yolk) lecithin, consumption is 0.75～1.5g; Isotonic agent adopts glycerol, and consumption is 2.5g; Water for injection adds to 100ml.
Prove that through zoopery Canis familiaris L. 7.5ml/kg, 15ml/kg, the continuous intravenously administrable of 30ml/kg untoward reaction do not occur more than 45 days; The maximum tolerated dose of mouse vein administration is 90ml/mg.The clinical use result of people 100～200ml/50kg/ time, successive administration is more than 20 days, and routine intravenous drip surplus 80,30 routine livers, the administration of pulmonary artery intubate have no adverse reaction, and human hepatocellular, pulmonary carcinoma, human colon cancer etc. are all had certain therapeutic effect.
Example one, the king * *, the man, 58 years old, be diagnosed as pulmonary carcinoma on inspection, invalid through secondary arterial cannulation chemotherapy, after a week behind this medicine arterial perfusion, left central type carcinoma of lung is obviously dwindled, and former left pulmonary atelectasis complete expansion is restored, and clinical symptoms is clearly better.
Example two, slowly * *, the man, 39 years old, be diagnosed as primary hepatocarcinoma on inspection, through once in a week behind totally three arterial cannulations, the ultrasound diagnosis lump is contracted to 4.4 * 4.6cm from former 9.2 * 8.4cm.Clinical symptoms is greatly improved, and has no adverse reaction.
Example three, Rhizoma Zingiberis Recens * *, the man, 67 years old, be diagnosed as small cell lung cancer on inspection, through intravenously administrable was followed treatment in oral 15 days after 10 days after, hematochrome rose near normal, the doing well,improving uncomfortable in chest of panting, appetite increases, and the X-ray examination of shadow piece disappears.
Example four, Yu * *, the woman, 49 years old, be diagnosed as hepatocarcinoma on inspection, through west, Chinese medicine control 40 days invalid, the back intravenously administrable 40 days continuously of being in hospital, lump narrows down to 8cm from 11cm, hematochrome rises to 11 grams, weight increase, self-doing well,improving from 6 grams.
Coixenolide neutral fat emulsion of the present invention.Emulsifying agent is safe and reliable, prescription is reasonable, and the effect of eliminating pathogenic factor for supporting vital QI is arranged.In clinical, has the enhancing human body immunity function, the treatment cardiovascular system diseases, suppress malignant growth, anticancer cell transfer does not have influence and preventing is arranged and reduce the effect of aspects such as bone marrow depression that chemotherapy causes, leukopenia, hepatic and renal function injure normal leukocyte, the state of an illness of patient with advanced cancer is alleviated to some extent, some cases also dwindles focus, and improve patient's life quality and prolonged life cycle, be another effective PTS.
Simultaneously, a large amount of experimental result data of warp prove that this Emulsion cooperates in low dose of chemotherapy or the preparation of this Emulsion has collaborative summation action behind the low dose of chemotherapeutics of adding (as cyclophosphamide, fluorouracil etc.), can improve curative effect.
Embodiment 1, and soybean lecithin for injection 1.5g and glycerol for injection 2.5g are inserted high-speed tissue mashing machine, adds an amount of water for injection, is prepared into the homodisperse phase with 1.2 ten thousand rev/mins of speed; Decentralized photo and Semen Coicis neutral fat 10g are distinguished 60～80 ℃ of preheatings, make colostrum after the mixing; Colostrum is added the injection water to 100ml, insert the emulsifying repeatedly of high-pressure emulsification machine,, fill nitrogen fill, sterilization again, promptly make the vein breast by 3 μ m filtering with microporous membranes, also can be oral.
Embodiment 2, and injection lecithin 1.2g is prepared into homodisperse earlier mutually with glycerol for injection 2.5g and water for injection; The Semen Coicis neutral fat 10g that adds preheating makes colostrum, is assigned to 100ml; High-pressure emulsification by 3 μ m filtering with microporous membranes, fills nitrogen fill, sterilization again, promptly makes the vein breast.
Embodiment 3, and Pu Lulang Garrick F88 2.0g is prepared into homodisperse earlier mutually with glycerol for injection 2.5g and water for injection; The Semen Coicis neutral fat 15g that adds preheating makes colostrum, is assigned to 100ml; High-pressure emulsification fills nitrogen fill, sterilization again, promptly makes oral liquid.
Embodiment 4, and soybean lecithin 2.0g is prepared into homodisperse earlier mutually with glycerol for injection 2.5g and water for injection; The Semen Coicis neutral fat 15g that adds preheating makes colostrum, is assigned to 100ml; High-pressure emulsification by 3 μ m filtering with microporous membranes, fills nitrogen fill, sterilization again, promptly makes the vein breast.
Embodiment 5, soybean lecithin for injection 120g and glycerol for injection 250g and water for injection are made decentralized photo preheating (80 ℃), mix the even Emulsion that is prepared into 10000ml by two step high pressure homogenizers with Semen Coicis neutral fat (80 ℃ of preheatings) 1000g, by 3 μ m filtering with microporous membranes, fill the nitrogen fill again, sterilization promptly gets the vein breast.
Claims (5)
1, a kind of Coixenolide neutral fat emulsion is characterized in that containing in per 100 milliliters of Emulsions:
Semen Coicis neutral fat 5-20 gram
Emulsifying agent 0.75-2.5 gram
Isotonic agent 2.5-5.0 gram
Surplus is water for injection.
2, Coixenolide neutral fat emulsion as claimed in claim 1 is characterized in that containing in 100 milliliters of Emulsions:
Semen Coicis neutral fat 10-20 gram
Semen sojae atricolor (or egg yolk) lecithin 0.75-2.0 gram
Glycerol for injection 2.5 grams
Surplus is water for injection.
3, Coixenolide neutral fat emulsion as claimed in claim 2 is characterized in that containing in per 100 milliliters of Emulsions:
Semen Coicis neutral fat 10 grams
Semen sojae atricolor (or egg yolk) lecithin 1.5 grams
Glycerol for injection 2.5 grams
Surplus is water for injection.
4, as claim 1 or 2 or 3 described Coixenolide neutral fat emulsions, it is characterized in that containing antitumor drug.
5, Coixenolide neutral fat emulsion as claimed in claim 4 is characterized in that described antitumor drug is a chemotherapeutics.
Priority Applications (10)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 93100735 CN1029293C (en) | 1993-01-01 | 1993-01-01 | Coix seed neutral oil emulsion |
| PH46885A PH30249A (en) | 1992-09-16 | 1993-01-01 | Neutral lipids from endosperm of job's tears |
| US08/120,549 US5444089A (en) | 1992-09-16 | 1993-09-14 | Neutral lipids from endosperm of Job's tears |
| CA002106176A CA2106176C (en) | 1992-09-16 | 1993-09-14 | Neutral lipids from kernel of job's tears |
| DE69327284T DE69327284T2 (en) | 1992-09-16 | 1993-09-15 | Neutral lipids from the endosperm of Coix lacryma jobi and compositions containing them |
| EP93307278A EP0588621B1 (en) | 1992-09-16 | 1993-09-15 | Neutral lipids from endosperm of job's tears and compositions including them |
| DK93307278T DK0588621T3 (en) | 1992-09-16 | 1993-09-15 | Neutral endosperm lipids from job tears and preparations containing them |
| JP5263994A JP3005407B2 (en) | 1992-09-16 | 1993-09-16 | Neutral lipids from Juzudama endosperm |
| KR1019930018932A KR100263680B1 (en) | 1992-09-16 | 1993-09-16 | Neutral lipid extracted from Yulmu kernels and pharmaceutical composition containing it |
| HK98109310A HK1008305A1 (en) | 1992-09-16 | 1998-07-21 | Neutral lipids from endosperm of job's tears and compositions including them |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 93100735 CN1029293C (en) | 1993-01-01 | 1993-01-01 | Coix seed neutral oil emulsion |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1080176A CN1080176A (en) | 1994-01-05 |
| CN1029293C true CN1029293C (en) | 1995-07-12 |
Family
ID=4983197
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 93100735 Expired - Lifetime CN1029293C (en) | 1992-09-16 | 1993-01-01 | Coix seed neutral oil emulsion |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1029293C (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100367951C (en) * | 2005-12-16 | 2008-02-13 | 石药集团恩必普药业有限公司 | Butyl benzene phthalein vein emulsion and its application |
| CN101028461B (en) * | 2007-03-30 | 2010-05-19 | 吴敏 | Job's tears nut oil self-emusifying preparation and its making method |
| CN1809339B (en) * | 2003-06-18 | 2010-06-23 | B·布朗·梅尔松根有限公司 | Oil emulsion for postnatal hormone substitution |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1045257C (en) * | 1994-08-30 | 1999-09-29 | 李大鹏 | Medicine for cancer |
| CN100409852C (en) * | 2005-01-22 | 2008-08-13 | 姚长虹 | Chinese medicine for enhancing immunologic function |
| CN1990032B (en) * | 2005-12-31 | 2011-03-23 | 天津天士力制药股份有限公司 | Composite intravenous injection emulsion of glossy ganoderma spore oil and coix seed oil and method for making same |
| CN105250804A (en) * | 2014-07-18 | 2016-01-20 | 浙江康莱特集团有限公司 | Coix seed oil containing 11 triglycerides, preparation and applications thereof |
| CN104173824B (en) * | 2014-07-18 | 2017-02-15 | 浙江康莱特集团有限公司 | Coix seed oil containing 8 triglycerides as well as preparation and application of coix seed oil |
| CN105254498B (en) * | 2014-07-18 | 2017-11-21 | 浙江康莱特药业有限公司 | The glyceryl linoleate of 1,3 2 oleic acid of compound 2, preparation, preparation method and applications |
| US9884037B2 (en) * | 2014-07-18 | 2018-02-06 | Zhejiang Kanglaite Group Co., Ltd. | Pharmaceutical composition containing 8 triglycerides, and preparations and use thereof |
| US9585929B2 (en) * | 2014-07-18 | 2017-03-07 | Zhejiang Kanglaite Group Co., Ltd. | Coix seed oil containing 13 glycerides, and pharmaceutical preparation and use thereof |
| US9585858B2 (en) * | 2014-07-18 | 2017-03-07 | Zhejiang Kanglaite Group Co., Ltd. | Pharmaceutical composition containing 13 triglycerides, and preparations and use thereof |
| CN105311486A (en) * | 2014-07-18 | 2016-02-10 | 浙江康莱特集团有限公司 | Coix seed oil containing 16 glycerides, preparation and applications thereof |
-
1993
- 1993-01-01 CN CN 93100735 patent/CN1029293C/en not_active Expired - Lifetime
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1809339B (en) * | 2003-06-18 | 2010-06-23 | B·布朗·梅尔松根有限公司 | Oil emulsion for postnatal hormone substitution |
| CN100367951C (en) * | 2005-12-16 | 2008-02-13 | 石药集团恩必普药业有限公司 | Butyl benzene phthalein vein emulsion and its application |
| US10463614B2 (en) | 2005-12-16 | 2019-11-05 | Shijiazhuang Pharma Group Nbp Pharmaceutical Co. | Butylphthalide intravenous emulsion and application thereof |
| CN101028461B (en) * | 2007-03-30 | 2010-05-19 | 吴敏 | Job's tears nut oil self-emusifying preparation and its making method |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1080176A (en) | 1994-01-05 |
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Legal Events
| Date | Code | Title | Description |
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| C10 | Entry into substantive examination | ||
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| PB01 | Publication | ||
| C14 | Grant of patent or utility model | ||
| GR01 | Patent grant | ||
| ASS | Succession or assignment of patent right |
Owner name: ZHEJIANG PROV KANGLAITE GROUP CO.,LTD. Free format text: FORMER OWNER: ZHEJIANG PROV. HOSPITAL OF TRADITIONAL CHINESE MEDICINE Effective date: 20011023 |
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| C41 | Transfer of patent application or patent right or utility model | ||
| TR01 | Transfer of patent right |
Effective date of registration: 20011023 Address after: 310019 11 Xiasha Road, Zhejiang, Hangzhou Patentee after: Zhejiang Kanglaite Group Co., Ltd. Address before: 310006 postal circuit 54, Zhejiang, Hangzhou Patentee before: Zhejiang Chinese Medicine Hospital |
|
| EE01 | Entry into force of recordation of patent licensing contract |
Assignee: ZHEJIANG KANGLAITE PHARMACEUTICAL CO., LTD. Assignor: Zhejiang Kanglaite Group Co., Ltd. Contract fulfillment period: 2007.1.1 to 2011.12.31 contract change Contract record no.: 2008990000483 Denomination of invention: Coix seed neutral oil emulsion Granted publication date: 19950712 License type: Exclusive license Record date: 2008.9.22 |
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| LIC | Patent licence contract for exploitation submitted for record |
Free format text: EXCLUSIVE LICENCE; TIME LIMIT OF IMPLEMENTING CONTACT: 2007.1.1 TO 2011.12.31 Name of requester: ZHEJIANG KANGLAITE PHARMACEUTICAL CO., LTD. Effective date: 20080922 |
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| C17 | Cessation of patent right | ||
| CX01 | Expiry of patent term |
Expiration termination date: 20130104 Granted publication date: 19950712 |