CN1102583A - Application of Chinese herb Job's tears seed extract - Google Patents

Abstract

Coix seed as a Chinese-medicinal material is extracted to prepare injection and cream for respectively curing cancer and intractable dermatosis with high curative effect. By taking it for 15-30 days, most of symptoms may be cured without toxic by-effect.

Description

Application of Chinese herb Job's tears seed extract

The invention belongs to injection and the new application of cream that TRADITONAL CHINESE MEDICINAL HERB COIX LACHRYMA-JOBI core extract is produced through processing.

Semen Coicis is a kind of Chinese medicine, for the acetone extract of Semen Coicis, can suppress the generation of Mus body ehrlich carcinoma cell, thereby by the extract of wherein isolating anticancer active ingredient.Because Semen Coicis extract has active anticancer, its extracting method and applied research all there is report, for example Japan Patent is openly speciallyyed permit clear 58-213719 to provide a kind of is that raw material acetone is the method for solvent extraction Semen Coicis extract with the Semen Coicis.The method of having reported need be used a large amount of acetone solvent (1Kg raw material need 15L acetone), so the solvent processing difficulty, expands the scale of production to be subjected to restriction with certain; Utilize the very easily emulsifying of aqueous slkali washing operation, therefore make to separate to be difficult to carry out; Aluminium oxide needs to handle with bromothymol blue, and a large amount of chloroforms of loss, increases manufacturing cost; Product yield is low only to be about 0.2% of raw material.

The extracting method that the present inventor once applied for a kind of Semen Coicis extract in 91 years, this application number be disclose in 91106269.0 the method at reporting the use solvent that extracting method exists big, carry out major defects such as easy emulsifying of alkali cleaning and alumina chromatographic column preparation cost height, carried out big technological improvement and proposed a kind of simple and be suitable for the process that industrialization is adopted.Its extracting method comprises with acetone being the solvent extraction Semen Coicis, carry out the separation and purification Semen Coicis oil with petroleum ether, with the petroleum ether flushing Semen Coicis oil is carried out the silica gel column chromatography separating treatment and carries out the alumina column chromatography separating treatment with the chloroform flushing obtaining the product Semen Coicis extract, said extract is meant with the Semen Coicis to be a kind of product that raw material adopts following method to extract, and also incites somebody to action wherein Semen Coicis fat among the present invention.The extraction that refluxes in apparatus,Soxhlet's of the acetone extract Semen Coicis of this technology can reduce the use amount of solvent acetone significantly, is 1/4～1/5 of common extracting process only.Save the trouble of handling a large amount of solvents like this, reduced unsafe factor; Used chromatographic column adsorbent aluminium oxide gives processing with alkali or ammonia spirit earlier, make the alkali alumina adsorbent and make chromatographic column again, not only aluminium oxide needn't reuse bromothymol blue indicator be handled, reduce complicated processing procedure, save a large amount of chloroform solvents and prepare indicator, and can save among the common preparation technology and carry out alkaline cleaning procedure with potassium hydroxide, avoid the easy emulsifying of alkaline cleaning procedure effectively and not segregative technical problem, the purification thing can be directly as product behind the alkali alumina adsorpting column chromatography.The products therefrom yield also improves 3～5 times than former technology.Above-mentioned aqueous slkali is handled alumina process and can be adopted sodium hydroxide or potassium hydroxide aqueous solution to carry out, and also can replace aluminium oxide to make adsorbent with active carbon, is directly used in chromatographic column and separates.Raw material can directly utilize exsiccant Semen Coicis kernel and will not pulverize by raw material in this external above-mentioned technology, has both reduced operation and equipment, also reduces the loss of raw material, reduces production costs.Specifically exsiccant Semen Coicis kernel is directly placed apparatus,Soxhlet's, with the acetone extracting that refluxes, the extracting time should be no less than 10 hours to guarantee that coixenolide is fully extracted.Extracting solution reclaims acetone through (decompression) distillation can be re-used as the solvent use, and obtains thick Semen Coicis oil; Thick product adds petroleum ether and leaches insoluble matter, reclaims petroleum ether subsequently and gets Semen Coicis oil; Get extract and be dissolved in petroleum ether, be added to silica gel column chromatography, make eluant flushing silica gel column chromatography with petroleum ether, distillation is reclaimed eluant and is got the yellow oily extract; Utilize alkali or ammonia spirit to give to handle aluminium oxide to make the alkali alumina adsorbent and make chromatographic column, the yellow oily extract is dissolved in chloroform, be added in alkali alumina or the activated carbon chromatography post, wash chromatographic column with chloroform as eluant, distillation recovery eluant obtains light yellow neutral grease and is the product coixenolide, and its yield can reach 0.6%.Provide an example of the present invention below.

2 kilograms of exsiccant Semen Coicis kernel are placed the device of getting of Soxhlet, add acetone 2.5 liters and reflux and extract 14 hours, acetone distillation (but distilling under reduced pressure) is reclaimed, about 70 grams of rufous syrup.Return petroleum ether 450ml in extracting syrup, separate and remove petroleum ether insoluble, distillation is reclaimed petroleum ether and is got rufous syrup 50 grams.The a small amount of petroleum ether dissolution of last 50 gram syrup, adorn 150 in being added to and restrain on the silica gel adsorption columns, with the flushing of 500ml petroleum ether, distillation gets yellow oil 35 grams after reclaiming the eluant petroleum ether.With 0.5N sodium hydrate aqueous solution impregnated alumina, dipping back is dry do alkali alumina adsorbent and dress up alumina chromatographic column.Above-mentioned 35 gram yellow oily extracts are added adorn in the 500 gram alkali alumina chromatographic columns in being added to after the minimum of chloroform dissolving, with chloroform wash present yellow to the alumina column bottom till.Distillation is reclaimed behind the chloroform must the light yellow neutral grease of about 12 grams, is the coixenolide product, and product yield can reach 0.6%.

The Semen Coicis fat that adopts said method to extract by equivalent method (doubly mensuration) principle of progressively increasing, adds and adds the solvent tween 80, again with normal saline merge stir evenly injection; Its proportioning is Semen Coicis fat 25g～50g, tween 80 375～750g, normal saline 20000～40000ml.Concrete preparation steps is to be provided by following: 25 gram coixenolides+25 gram tween 80s=50 grams are ground to clear liquid (mixed liquor 1); 50 gram (mixed liquor 1)+50 gram tween 80=100 grams are ground to clear liquid (mixed liquor 2); 100 gram (mixed liquor 2)+100 gram tween 80=200 grams are ground to clear liquid (mixed liquor 3); 200 gram (mixed liquor 3)+200 gram tween-8=400 grams are ground to clear liquid (mixed liquor 4).

Promptly 25 gram Semen Coicis fat+375 gram tween 80s are made clear liquid, and it is to stir in the 20000m normal saline solution more than 50 ℃ that gained 400g mixed liquor is gone into temperature, then molten in the time of slightly, with G3 or G4 funnel sucking filtration, then with the packing of peace bottle, sterilization.

The cream made from coixenolide is the tasteless vanishing cream (the commercially available vanishing cream that does not add essence) that adopts Cosmetics Plant to produce, add molten the mixing of coixenolide and get final product, add coixenolide amount be advisable with 0.1～5%.It is characterized in that made injection and cream can be used for treating cancer and skin stubborn disease.The cancer of treatment comprises pulmonary carcinoma, gastric cancer, esophageal carcinoma, uterus carcinoma, intestinal cancer and skin carcinoma; The skin stubborn disease of treatment comprises warm rash, core class seborrheic keratosis, keratosis erythematosa, erythroderma, skin pruritus etc.

The present invention makes injection and white liquid with coixenolide, is feasible as a kind of new drug and in new application.Use it to obtain significant curative effect at cancer and treating for skin disease, clinical effectiveness shows that most symptoms can obtain recovery from illness at first quarter moon to January.It has curative effect height, advantages such as safe without toxic side effect.Can become a kind of anticancer and dermopathic medicine of treatment.

About Therapeutic Method is such: be used for treating for skin disease and be adopting (2ml) intramuscular injection every day of coixenolide injection, and be aided with the coixenolide frost and embrocate affected part; Be the method that adopts coixenolide injection vein to splash into when treatment of cancer, each 20, be a course of treatment January.

Provide the observation of curative effect statistical table below:

Efficacy analysis:

All types of wet treatment group total cure rates 75.3%, total effective rate 94.6%, effective time is many in a week, weak point person 1～2 day, elder 10 days, healing time is organized general course of treatment of first quarter moon to 3 month, erythroderma group 6～10 months for the treatment of wetting; Whether curative effect and disease, age, sex, occupation and the past treat and do not see any dependency; This group is cured case and is observed respectively and do not wait in 2 years half to 3 months, and no case was recurrence, because of after certain reason carries out drug withdrawal, and the normal basicly stable level after taking a turn for the better of skin lesion, no rebound phenomenon becomes obvious contrast with hormone therapy.

Claims (3)

1, a kind of new purposes of TRADITONAL CHINESE MEDICINAL HERB COIX LACHRYMA-JOBI core extract is characterized in that it can be used for treating cancer and skin stubborn disease.

2,, it is characterized in that this extract can be made into injection and cream according to the described new purposes of claim 1.

3,, it is characterized in that the cancer for the treatment of comprises pulmonary carcinoma, gastric cancer, esophageal carcinoma, uterus carcinoma, intestinal cancer and skin carcinoma according to the described new purposes of claim 1; The skin stubborn disease of treatment comprises warm rash, erythroderma, keratosis erythematosa, erythroderma, skin pruritus etc.