CN1044444C - Pharmaceutic usage of Chinese medicine coix seed - Google Patents

Abstract

The present invention discloses the new medical application of coix seed to the preparation of medicament for resisting AIDS, relieving pain and protecting gastric mucosa.

Description

The pharmaceutic usage of TRADITONAL CHINESE MEDICINAL HERB COIX LACHRYMA-JOBI core

The invention belongs to the new purposes invention of TRADITONAL CHINESE MEDICINAL HERB COIX LACHRYMA-JOBI core, specifically is the invention about the new medical application of TRADITONAL CHINESE MEDICINAL HERB COIX LACHRYMA-JOBI core anti-AIDS, pain relieving and protection gastric mucosa.

Semen Coicis is a kind of conventional Chinese medicine, has multiple medical application.Many scholars had once carried out many-sided research to Semen Coicis, adopted diverse ways that Semen Coicis is extracted, and were prepared into different pharmaceutical preparation.It is that raw material acetone is the method for solvent extraction Semen Coicis extract with the Semen Coicis that the clear 58-213719 of Japan Patent Publication Laid-Open provides a kind of.The inventor once with regard to the specific extraction thing of Semen Coicis and preparation application thereof patent (CN1080176), and proved antitumor action, immunoregulation effect, effect for reducing blood fat, the effect of increase coronary flow, protection hepatic injury effect, antiinflammatory action, antifatigue effect, the anti-aging effects of Semen Coicis.The Semen Coicis broad research is shown Semen Coicis has a lot of medical applications and remains R and D, however, up to the present, yet there are no the report of relevant Semen Coicis anti-AIDS, pain relieving and the effect of protection gastric mucosa.

One of purpose of the present invention just provides the new purposes of anti-AIDS of Semen Coicis, has invented the application of Semen Coicis in the medicine of preparation treatment acquired immune deficiency syndrome (AIDS);

Another object of the present invention provides the new purposes of pain relieving of Semen Coicis, has invented the application of Semen Coicis in the preparation analgesic drug product;

Another object of the present invention provides the new purposes of the protection gastric mucosa of Semen Coicis, has invented the application of Semen Coicis in the medicine of preparation protection gastric mucosa;

Semen Coicis can be that the Semen Coicis crude drug directly is processed into medicine when the medicine of the above-mentioned new purposes of preparation, also can extract Semen Coicis, and extract is prepared into medicine.Can be to be that active constituents of medicine is made medicament with Semen Coicis or its extract separately, also can be Semen Coicis or its extract to be cooperated with other active constituents of medicine make compound preparation.

When Semen Coicis directly is processed into medicine, earlier Semen Coicis is picked, washed quietly, oven dry is pulverized then, crosses 120 mesh sieves, makes the fine powder of Semen Coicis.Fine powder is encapsulated, perhaps make electuary, tablet, pill etc.

To the extraction of Semen Coicis, can adopt the whole bag of tricks of the prior art to extract.For example, extract with aqueous solvent, perhaps with organic solvent extraction.Preferably with organic solvent extraction.

To the preferred extracting method of Semen Coicis, referring to disclosed method in the Chinese patent application 92110839.7.The extract that uses this method to extract can better reach the said medical effect of the present invention.Therefore, be used for the Semen Coicis neutral fat that Semen Coicis extract of the present invention preferably extracts with this method.

The extract of Semen Coicis is prepared into medicament, and can be prepared into clinically can received various medicaments.For example, tablet, pill, oral liquid, injection, infusion solution etc.

Semen Coicis extract is prepared into the method for injection, referring to Chinese patent application publication number CN1080176.

With the medicament that Semen Coicis or its extract are made, has the new medical application of anti-AIDS, pain relieving and protection gastric mucosa.

1, the effect of AIDS virus resisting

Experiment showed, the injection made from Semen Coicis extract (commodity are called KANGLAITE), the simian acquired immunodeficiency syndrome infective virus is produced and cytopathy all has in various degree inhibitory action.

(1) to Hut-78 cytotoxicity assay

When heavy dose of the Hut-78 cell there is direct killing effect, cellular atrophy death, its IC is 4 μ l/ml (cultivating 72 hours), sees Fig. 1.

(2) to the influence of SIV positive cell infection rate

By the SIV infection cell, express virus protein, utilize immune antibody to detect.Experiment shows that with the injection 5 μ l/ml that Semen Coicis extract is made, 0.5 μ l/ml concentration all can suppress the positive cell infection rate, and is dose dependent.See Fig. 2.

(3) to the influence of SIV virus titer

Generation has certain inhibitory action to the injection made from Semen Coicis extract to SIV/ virus, especially when dosage is 5 μ l/ml, influences more obvious.See Fig. 3.

(4) to the cytopathic influence of Hut-78

The fused cell that the injection made from Semen Coicis extract produces SIV infection Hut-78 cell has certain inhibitory action.See Table 1.

The cytopathic influence of Hut-78 that table 1 couple SlV infects

Medicine	The cell contrast	Virus control	AZT (10μM)	KANGLAITE (5μl/ml)	KANGLAITE (5μl/ml)
						Pathological change	±	+++	+	++	++-+++

2, analgesic effect

Show also that through clinic trial the injection that Semen Coicis extract is made has significant pain relieving effect.As everyone knows, cancer pain is a Universal Problems.Effectively pain management is one of four emphasis in World Health Organization's cancer unified plan.Current narcoticness analgesia should be positive palliative treatment, can alleviate the hardship of cancer patient's pain, but want addiction.What Semen Coicis extract was made is injected at when killing and wounding cancerous cell, human body immunity improving power, also has significant analgesic effect concurrently, and can not cause addiction.Many patients use after a course of treatment pain sensation to die away or alleviate.102 routine tumour patients of Zhejiang Prov. Hospital of Traditional Chinese Medicine statistics have pain person's 45 examples, and after the injection treatment that Semen Coicis extract is made, pain relief rate (disappearing+alleviate) accounts for 91.1%.See Table 2.

Doing well,improving situation after table 2 medication

Symptom	The example number	Alleviate	Disappear	No change	Increase the weight of	Remission rate
							The pain heating anorexia abdominal distension weak cough expiratory dyspnea of having a sleepless night	45 29 84 38 41 70 28 11	31 11 57 19 21 37 14 5	10 8 16 2 11 16 6 1	4 7 10 12 9 9 8 5	0 3 1 5 0 8 0 0	91.1％ 65.5％ 73.0％ 55.3％ 78.0％ 75.7％ 71.4％ 54.5％

3, the effect of protection gastric mucosa

The experiment of rat anti gastric mucosa injury shows that the injection that Semen Coicis extract is made can protect gastric mucosa to avoid the damage of ethanol and 0.6N HCL significantly, and its ulcer index significantly reduces; To the gastric mucosa injury that 0.2N NaOH causes, its ulcer index has reduction trend.See Table 3.

Table 3 Semen Coicis injection is to the effect of gastric mucosa injury model (M ± SD)

Ulcer index
					The dehydrated alcohol model	0.6N salt acid profile	0.2N sodium hydroxide model
Lipomul (contrast) Semen Coicis injection	200.9±94.4 (n=12) 102.2±45.2 (n=13)	153.4±58.8 (n=9) 71.8±19.5 (n=8)	258.3±143 (n=8) 174.5±104 (n=10)

Description of drawings:

Fig. 1 is the toxic action of Semen Coicis injection to the Hut-78 cell, and wherein vertical coordinate is meant the percentage ratio that accounts for matched group, and abscissa is the concentration of injection.

Fig. 2 is the effect of Semen Coicis injection to the SIV protein expression of Hut-78 cell, wherein vertical coordinate is meant 200 positive cell numbers in the cell, CONTROL represents matched group in the abscissa, AZT is the present trade name of a kind of anti-AIDS drug commonly used in the world, ZCE-3 represents a kind of extract of Semen Coicis, indicated concentration in the bracket.

Fig. 3 is the effect of Semen Coicis injection to the SIV protein expression of Hut-174 cell, wherein vertical coordinate is meant the Log2 that virus produces, CONTROL represents matched group in the abscissa, AZT is the present trade name of a kind of anti-AIDS drug commonly used in the world, KANGLAITE represents a kind of extract of Semen Coicis, indicated concentration in the bracket

Embodiment

Semen Coicis be used to prepare have anti-AIDS, the injection of pain relieving and the effect of protection gastric mucosa

Get 100 kilograms of Semen Coicis powder, use acetone extraction, obtain 5 kilograms of acetone extraction crude products behind the recovery acetone, adsorb, decolour.Adding 152 gram NaOH (or KOH), to be made into concentration be that 2% heat alkali liquid carries out abundant alkali refining saponification, and adding alkali number is decide according to the crude product acid value, and 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 (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 about 2 kilograms of faint yellow neutral fat, last packing makes purified Semen Coicis neutral fat through 160 ℃ of dry heat sterilizations 2 hours, and is standby.

Soybean lecithin for injection 1.5 grams and glycerol for injection 2.5 grams are inserted high-speed tissue mashing machine, add an amount of water for injection, be prepared into the homodisperse phase with 1.2 ten thousand rev/mins of speed; Decentralized photo and Semen Coicis neutral fat 10 are restrained 60-80 ℃ of preheating respectively, make colostrum after the mixing; Colostrum is added injection water to 100 milliliter, insert the emulsifying repeatedly of high-pressure emulsification machine,, fill canned, the sterilization of nitrogen again, make used for intravenous injection Emulsion by 3 μ m filtering with microporous membranes.

Claims (9)

1, Semen Coicis has application in the medicine of anti-AIDS effect in preparation.

2, according to the application of claim 1, wherein said Semen Coicis is the extract of Semen Coicis.

3, according to the application of claim 2, wherein said Semen Coicis extract is the extractive with organic solvent of Semen Coicis.

4, Semen Coicis has application in the medicine of analgesic effect in preparation.

5, according to the application of claim 4, wherein said Semen Coicis is the extract of Semen Coicis.

6, according to the application of claim 5, wherein said Semen Coicis extract is the extractive with organic solvent of Semen Coicis.

7, Semen Coicis has application in the medicine of protection gastric mucosa effect in preparation.

8, according to the application of claim 7, wherein said Semen Coicis is the extract of Semen Coicis.

9, application according to Claim 8, wherein said Semen Coicis extract are the extractive with organic solvent of Semen Coicis.

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