CN1148198C - Non-toxic cotton seed extractions and their extraction process, medicinal composite and use as medicine for nervous system - Google Patents
Non-toxic cotton seed extractions and their extraction process, medicinal composite and use as medicine for nervous system Download PDFInfo
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- CN1148198C CN1148198C CNB98106650XA CN98106650A CN1148198C CN 1148198 C CN1148198 C CN 1148198C CN B98106650X A CNB98106650X A CN B98106650XA CN 98106650 A CN98106650 A CN 98106650A CN 1148198 C CN1148198 C CN 1148198C
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- Prior art keywords
- extract
- nontoxic
- water
- cotton seed
- semen gossypii
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- 231100000252 nontoxic Toxicity 0.000 title claims abstract description 34
- 230000003000 nontoxic effect Effects 0.000 title claims abstract description 34
- 239000003814 drug Substances 0.000 title claims abstract description 11
- 229920000742 Cotton Polymers 0.000 title claims description 21
- 238000000605 extraction Methods 0.000 title claims description 9
- 210000000653 nervous system Anatomy 0.000 title description 4
- 239000002131 composite material Substances 0.000 title 1
- 239000000284 extract Substances 0.000 claims abstract description 22
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 23
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims description 19
- 208000019901 Anxiety disease Diseases 0.000 claims description 12
- 210000000582 semen Anatomy 0.000 claims description 11
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims description 10
- QBKSWRVVCFFDOT-UHFFFAOYSA-N gossypol Chemical compound CC(C)C1=C(O)C(O)=C(C=O)C2=C(O)C(C=3C(O)=C4C(C=O)=C(O)C(O)=C(C4=CC=3C)C(C)C)=C(C)C=C21 QBKSWRVVCFFDOT-UHFFFAOYSA-N 0.000 claims description 8
- 230000036506 anxiety Effects 0.000 claims description 7
- 238000002481 ethanol extraction Methods 0.000 claims description 7
- 238000000034 method Methods 0.000 claims description 7
- 230000000994 depressogenic effect Effects 0.000 claims description 5
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- QHOPXUFELLHKAS-UHFFFAOYSA-N Thespesin Natural products CC(C)c1c(O)c(O)c2C(O)Oc3c(c(C)cc1c23)-c1c2OC(O)c3c(O)c(O)c(C(C)C)c(cc1C)c23 QHOPXUFELLHKAS-UHFFFAOYSA-N 0.000 claims description 4
- 238000009395 breeding Methods 0.000 claims description 4
- 229930000755 gossypol Natural products 0.000 claims description 4
- 229950005277 gossypol Drugs 0.000 claims description 4
- 239000003208 petroleum Substances 0.000 claims description 4
- 239000004480 active ingredient Substances 0.000 claims description 3
- 230000001488 breeding effect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 235000013399 edible fruits Nutrition 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 239000012259 ether extract Substances 0.000 claims 2
- 229960004551 cotton seed extract Drugs 0.000 abstract description 13
- 238000002360 preparation method Methods 0.000 abstract description 5
- 239000000203 mixture Substances 0.000 abstract 1
- 241000700159 Rattus Species 0.000 description 9
- 238000002474 experimental method Methods 0.000 description 8
- 230000000694 effects Effects 0.000 description 7
- 239000007788 liquid Substances 0.000 description 7
- 230000037396 body weight Effects 0.000 description 5
- 239000003960 organic solvent Substances 0.000 description 5
- 230000004071 biological effect Effects 0.000 description 4
- AAOVKJBEBIDNHE-UHFFFAOYSA-N diazepam Chemical compound N=1CC(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 AAOVKJBEBIDNHE-UHFFFAOYSA-N 0.000 description 4
- 229960003529 diazepam Drugs 0.000 description 4
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- WFDIJRYMOXRFFG-UHFFFAOYSA-N Acetic anhydride Chemical compound CC(=O)OC(C)=O WFDIJRYMOXRFFG-UHFFFAOYSA-N 0.000 description 3
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 239000001117 sulphuric acid Substances 0.000 description 3
- 235000011149 sulphuric acid Nutrition 0.000 description 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 241000700157 Rattus norvegicus Species 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 230000001430 anti-depressive effect Effects 0.000 description 2
- 229940125713 antianxiety drug Drugs 0.000 description 2
- 239000002249 anxiolytic agent Substances 0.000 description 2
- QWCRAEMEVRGPNT-UHFFFAOYSA-N buspirone Chemical compound C1C(=O)N(CCCCN2CCN(CC2)C=2N=CC=CN=2)C(=O)CC21CCCC2 QWCRAEMEVRGPNT-UHFFFAOYSA-N 0.000 description 2
- 229960002495 buspirone Drugs 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 235000013305 food Nutrition 0.000 description 2
- 239000007921 spray Substances 0.000 description 2
- 238000007619 statistical method Methods 0.000 description 2
- 238000005728 strengthening Methods 0.000 description 2
- 238000012360 testing method Methods 0.000 description 2
- 238000003809 water extraction Methods 0.000 description 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 1
- 229910021578 Iron(III) chloride Inorganic materials 0.000 description 1
- 208000012902 Nervous system disease Diseases 0.000 description 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 description 1
- 244000061458 Solanum melongena Species 0.000 description 1
- KXKVLQRXCPHEJC-UHFFFAOYSA-N acetic acid trimethyl ester Natural products COC(C)=O KXKVLQRXCPHEJC-UHFFFAOYSA-N 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- 150000001298 alcohols Chemical group 0.000 description 1
- 150000001350 alkyl halides Chemical class 0.000 description 1
- 238000000540 analysis of variance Methods 0.000 description 1
- 239000000935 antidepressant agent Substances 0.000 description 1
- 229940005513 antidepressants Drugs 0.000 description 1
- 239000007864 aqueous solution Substances 0.000 description 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 1
- 229910052794 bromium Inorganic materials 0.000 description 1
- 239000002021 butanolic extract Substances 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 239000000460 chlorine Substances 0.000 description 1
- 239000000571 coke Substances 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 230000005611 electricity Effects 0.000 description 1
- 150000002148 esters Chemical class 0.000 description 1
- RSEOPLGIFDMYKN-UHFFFAOYSA-N ethanol;naphthalen-1-ol Chemical compound CCO.C1=CC=C2C(O)=CC=CC2=C1 RSEOPLGIFDMYKN-UHFFFAOYSA-N 0.000 description 1
- 150000002170 ethers Chemical class 0.000 description 1
- 239000000706 filtrate Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- GNBHRKFJIUUOQI-UHFFFAOYSA-N fluorescein Chemical compound O1C(=O)C2=CC=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 GNBHRKFJIUUOQI-UHFFFAOYSA-N 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 239000011630 iodine Substances 0.000 description 1
- RBTARNINKXHZNM-UHFFFAOYSA-K iron trichloride Chemical compound Cl[Fe](Cl)Cl RBTARNINKXHZNM-UHFFFAOYSA-K 0.000 description 1
- YKYONYBAUNKHLG-UHFFFAOYSA-N n-Propyl acetate Natural products CCCOC(C)=O YKYONYBAUNKHLG-UHFFFAOYSA-N 0.000 description 1
- -1 potassium ferricyanide Chemical compound 0.000 description 1
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 1
- 229940090181 propyl acetate Drugs 0.000 description 1
- 230000002787 reinforcement Effects 0.000 description 1
- 230000035939 shock Effects 0.000 description 1
- 239000002893 slag Substances 0.000 description 1
- 235000012976 tarts Nutrition 0.000 description 1
- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical compound CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 1
- 238000009834 vaporization Methods 0.000 description 1
- 230000008016 vaporization Effects 0.000 description 1
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- Medicines Containing Plant Substances (AREA)
Abstract
The present invention relates to non-toxic cotton seed extract, a preparation thereof, a medicine composition containing the extract, and the medicament purpose thereof.
Description
The present invention relates to the non-toxic cotton seed extract, its extracting method contains their pharmaceutical composition and as the purposes of nervous system medicine.
Non-toxic cotton is by no gossypol that Cotton Gossypii is carried out obtain after selection-breeding or the breeding or the very low Cotton Gossypii of gossypol content.Non-toxic cotton seed is the seed of the mature fruit of non-toxic cotton, and it can be used as the feedstuff of domestic animal.But up to the present, the active ingredient and the biological activity of relevant non-toxic cotton seed do not see that utmost point road is arranged.
The objective of the invention is to seek and develop the new purposes of non-toxic cotton seed.
The inventor has now found that after deliberation the non-toxic cotton seed extract that obtains by following method demonstrates good nervous system biological activity, especially anxiety, antidepressant effect, the present invention is based on above discovery and is accomplished.
According to the present invention, extract of the present invention is following obtaining: with the non-toxic cotton seed organic solvent, and water-containing organic solvent or water extraction.Used organic solvent is selected from alcohols such as methanol, ethanol, propanol or butanols etc.; Halo alkanes such as dichloromethane, chlorine side etc.; Ethers such as petroleum ether or ether etc., esters such as methyl acetate, ethyl acetate or propyl acetate etc.
According to the present invention, non-toxic cotton seed extract of the present invention has following qualitative reaction:
A) 1% istain acetone soln and 10ml acetic acid are made into developer.Cotton seed is extracted object point on filter paper, spray above-mentioned developer on this filter paper, dry up, when treating that tart flavour is not too dense, filter paper is put into 100 ℃ of baking ovens bakings 5-10 minute, then show colors such as red, Huang on the filter paper with hair-dryer.
B) preparation of developer: A liquid is dissolved in 0.5 gram ferric chloride in the 50ml water and obtains; B liquid is dissolved in the 0.5 gram potassium ferricyanide in the 50ml water and obtains, and faces the time spent, and A, B two liquid equal-volumes are mixed.Cotton seed extract sample spot on paper, is sprayed above-mentioned solution, be the obvious blue speckle immediately.
C) with exsiccant cotton seed extract sample dissolution or be suspended in the 0.5ml acetic anhydride, drip 1 concentrated sulphuric acid, solution is aubergine, and the upper strata of solution gradually becomes green.
D) with the extraction object point of cotton seed on filter paper, spray 0.05% fluorescein aqueous solution, the scraps of paper are exposed to (or in iodine vapor) speckle displaing yellow, background become pale red soon in the bromine vapor.
E) with the dissolving of cotton seed extract, be placed into 10ml in vitro, add 10% alpha-Naphthol ethanol liquid.Shake up, drip a small amount of concentrated sulphuric acid along test tube again, the purpuric garland in the interface that liquid contacts with concentrated sulphuric acid in the test tube produces.
According to the present invention, first aspect present invention relates to the non-toxic cotton seed extract, and this extract demonstrates good biological activity to the human nervous system, especially anxiety and antidepressant activity.
According to the present invention, the invention still further relates to the method for preparing the non-toxic cotton seed extract, it comprises the non-toxic cotton seed organic solvent, water-containing organic solvent or water extraction.
According to the present invention, the invention still further relates to pharmaceutical composition, it comprises non-toxic cotton seed extract of the present invention and one or more pharmaceutical carriers or excipient as active ingredient.
According to the present invention, the invention still further relates to the purposes that the non-toxic cotton seed extract is used to prepare treatment nervous system disease such as anxiety, depressed medicine.
According to the present invention, non-toxic cotton seed extract of the present invention can use separately or with pharmaceutical compositions, and its administering mode can be decided as the case may be, but preferred oral.The dosage that gives non-toxic cotton seed of the present invention is generally the 1-300mg/kg body weight/day, preferred 5-150mg/kg body weight/day.
Further specify the present invention below by embodiment and biotic experiment, but this does not mean that any limitation of the invention.
Embodiment 1
The preparation of non-toxic cotton seed ligroin extraction
Non-toxic cotton seed 5kg was pulverized 100 mesh sieves, used Petroleum ether extraction then, used 10 liters at every turn, extracted three times, merge extractive liquid,, reduction vaporization gets the 320g ligroin extraction to doing, and it has aforesaid qualitative reaction feature.
Embodiment 2
The alcoholic acid preparation of getting thing of non-toxic cotton seed
With embodiment 1 Chinese medicine slag ethanol extraction, use 15 liters at every turn, extract three times, merge extractive liquid,, be evaporated to dried, the 510g ethanol extraction, it also has aforesaid qualitative reaction feature.
Embodiment 3
The preparation of non-toxic cotton seed n-butyl alcohol and water extract
Ethanol extraction among the embodiment 2 is water-soluble, to filter, filtrate is distributed extraction between n-butyl alcohol and water, get 20g n-butanol extract and 490g water extract, and they all have aforesaid qualitative reaction feature.
The biological activity of extract of the present invention
The angst resistance effect experiment:
1. the rat safety signal is removed (safety signal withdrawol) experiment
(1) method (referring to people such as document Thiebot MH., spiritual pharmacology (Psychopharmacology), 1991,103:415-24): the experiment carry out with MED rat control box system (U.S. Med company).
Male Wistar rat, initial body weight 100-130g, body weight 170~220g when experiment finishes.The animal random packet.Branch is trained and is tested two stages.Allow rat association by fixed ratio (FR) during training
1Strengthen (FR
1, promptly every depression bar once obtains a food ball), then excessively to FR
2, FR
4And FR
8, 18 minutes every days, be divided into 5 successive time periods: 1,4 minute; 2,4 minutes; 3,3 minutes; 4,4 minutes; 5,3 minutes.Wherein, 1,3,5 is the non-punishment phase, and right lamp bright (safety signal) is pressed FR
8Strengthen, 2,4 are the punishment phase, and left lamp bright (punishment signal) is pressed FR
1When strengthening, give the foot electric shock of ratio 50% at random.Train to stablize and experimentized in 10 days.Experimental arrangement keep above-mentioned preceding 3 time periods (totally 11 minutes but close at 2 phases (promptly punishing the phase) right lamps (safety signal), still presses FR for electric shock
1Strengthen record security phase (FR
8, 7 minutes) and safety signal remove the phase (FR
1, 4 minutes) and rat obtains the number of times that the food ball is strengthened.Result's ANOVA statistical analysis, relatively Dunett ' st check between group.Antianxiety drugs is not influencing FR
8The dosage of strengthening increases FR
1Strengthen.The results are shown in Table 1.
Table 1. is removed the angst resistance effect of the Semen Gossypii water extract of embodiment 3 in the experiment at the rat safety signal
Medicine (mg/kg) n strengthens number
Safe period, safety signal was removed the phase
(FR
8) (FR
1)
Normal saline (contrast) n 47 ± 12 20 ± 10
Diazepam 1.0 38 46 ± 8 33 ± 9
*
Buspirone 1.0 16 47 ± 14 45 ± 8
*
The water extract 100.0 7 52 ± 10 24 ± 13 of embodiment 3
200.0 14 45±13 31±10
*
400.0 17 46±12 29±12
*
X ± SD, with the matched group ratio,
*P<0.05,
*P<0.01.
(2) discuss:
As can be seen from Table 1, antianxiety drugs diazepam and buspirone all can significantly increase the reinforcement number that safety signal is removed the phase at 1mg/kg, and to there not being influence Safe period.Embodiment 3 Semen Gossypii water extract 100~400mg/kg also has similar effect, and is certain dose relationship, shows angst resistance effect.
2. rat Vogel (conflict experiment)
(1) method: experiment is considered instrument, list of references: Zhang Hanting etc., Chinese J Pharmacol Toxicol, 1995 with the Model-102 formed coke that U.S. Lafayette company produces; 9 (4): 254-7.Male Wistar rat, initial weight 180~220g, prohibit water after 48 hours body weight be 155~200g.The rat random packet is prohibited water and train it to lick water after 24 hours, does not add electric shock, licks water in 3 minutes and is no less than 300 times continuation and prohibits water and experimentize after 48 hours, and the vola gives the electric shock (whenever lick water give for 20 times 1 time shock by electricity) of 0.3mA simultaneously.Instrument record was automatically licked the waterside number in 3 minutes.Anti-burnt brave medicine increases this index.Statistical analysis is the same.The results are shown in Table 2.
The angst resistance effect of table 2. embodiment 3 water extracts on rat Vogel conflict model
Medicine (mg/kg) n licks the waterside number
Normal saline (contrast) 9 216 ± 151
Diazepam 3.0 8 467 ± 142
*
Embodiment 3 water extracts 100.0 7 356 ± 120
200.0 9 379±116
400.0 8 431±140
*
X ± SD. and matched group ratio,
*P<0.05.
(2) discuss
As seen from Table 2, diazepam 3mg/kg can obviously increase the rat conflict phase and lick the waterside number, but embodiment 3 water extracts 100~400mg/kg also increase the conflict phase and lick the waterside number in dose dependent ground, be angst resistance effect.
Claims (5)
1. be used for the treatment of anxiety and/or depressed nontoxic Semen Gossypii extract, wherein nontoxic Semen Gossypii is from the seed of non-toxic cotton mature fruit, non-toxic cotton is that described extract is following to be obtained by no gossypol that Cotton Gossypii is carried out obtain after selection-breeding or the breeding or the very low Cotton Gossypii of gossypol content:
A) nontoxic Semen Gossypii Petroleum ether extraction, or
B) with remaining medicinal residues ethanol extraction after a) PetroChina Company Limited.'s ether extracts, or
C) with b) in ethanol extraction in water and n-butyl alcohol, distribute, obtain the extract of water and n-butyl alcohol respectively.
2. prepare the method for nontoxic Semen Gossypii extract, it comprises:
A) nontoxic Semen Gossypii Petroleum ether extraction, or
B) with remaining medicinal residues ethanol extraction after a) PetroChina Company Limited.'s ether extracts, or
C) with b) in ethanol extraction in water and n-butyl alcohol, distribute, obtain the extract of water and n-butyl alcohol respectively.
3. be used for the treatment of anxiety and/or depressed pharmaceutical composition, it comprises nontoxic Semen Gossypii extract and one or more pharmaceutical carriers or excipient as claim 1 requirement of active ingredient.
4. nontoxic Semen Gossypii extract is used for preparing treatment anxiety and/or depressed medicine purposes.
5. the purposes of claim 4, wherein said nontoxic Semen Gossypii extract is the nontoxic Semen Gossypii extract in the claim 1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB98106650XA CN1148198C (en) | 1998-04-17 | 1998-04-17 | Non-toxic cotton seed extractions and their extraction process, medicinal composite and use as medicine for nervous system |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNB98106650XA CN1148198C (en) | 1998-04-17 | 1998-04-17 | Non-toxic cotton seed extractions and their extraction process, medicinal composite and use as medicine for nervous system |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1232675A CN1232675A (en) | 1999-10-27 |
| CN1148198C true CN1148198C (en) | 2004-05-05 |
Family
ID=5219040
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB98106650XA Expired - Fee Related CN1148198C (en) | 1998-04-17 | 1998-04-17 | Non-toxic cotton seed extractions and their extraction process, medicinal composite and use as medicine for nervous system |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1148198C (en) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002076473A1 (en) * | 2001-03-26 | 2002-10-03 | Academy Of Military Medical Sciences Institute Of Pharmacology And Toxicology | Quercetin derivative and its medicinal use |
-
1998
- 1998-04-17 CN CNB98106650XA patent/CN1148198C/en not_active Expired - Fee Related
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| Publication number | Publication date |
|---|---|
| CN1232675A (en) | 1999-10-27 |
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