CN102552453B - Application of gingerol and rhizoma coptidis composition to preparation of medicine for resisting vomiting - Google Patents
Application of gingerol and rhizoma coptidis composition to preparation of medicine for resisting vomiting Download PDFInfo
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- CN102552453B CN102552453B CN201210038339.1A CN201210038339A CN102552453B CN 102552453 B CN102552453 B CN 102552453B CN 201210038339 A CN201210038339 A CN 201210038339A CN 102552453 B CN102552453 B CN 102552453B
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- 239000003814 drug Substances 0.000 title claims abstract description 67
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- 206010047700 Vomiting Diseases 0.000 title claims abstract description 40
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- 235000002780 gingerol Nutrition 0.000 title claims abstract description 36
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- 230000008673 vomiting Effects 0.000 title claims abstract description 36
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- ZUFQODAHGAHPFQ-UHFFFAOYSA-N pyridoxine hydrochloride Chemical compound Cl.CC1=NC=C(CO)C(CO)=C1O ZUFQODAHGAHPFQ-UHFFFAOYSA-N 0.000 description 3
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Abstract
The invention relates to a natural medicinal composition, a preparation method thereof and application thereof to preparation of a medicine for resisting vomiting. According to the natural medicinal composition, the ratio of a rhizoma coptidis extract to gingerol is (5-30): (1-2). The composition has a good curative effect on vomiting.
Description
Technical field
The present invention relates to a kind of natural drug composition, relate more specifically to a kind of natural drug composition be made up of Rhizoma Coptidis extract and gingerol, the preparation method of this natural drug composition and its purposes as the medicine of resisting emesis.
Background technology
Vomiting is mankind's misery reactions unbearably.Improper diet, psychentonia, gastroenteropathy, carcinosis radiotherapy and chemotherapy, drug toxicity, postoperative, cinetosis and gestation etc. can cause nausea and vomiting and all can cause vomiting, frequently and tempestuously vomit can cause malnutrition, the complication such as de-water and rock-soil coupling, the particularly vomiting that causes of carcinosis radiotherapy and chemotherapy is one of patient's abandoning cure reason.
At present, clinical conventional Bendectin mainly contains histamine, acetylcholine, dopamine receptor antagonistic, Kallidin I (NK
1) and 5-hydroxy tryptamine (5-HT
3) short of money dose of receptor etc., but these medicines are to the weak curative effect of vomit duo to chemotherapy, and toxic and side effects is strong, and application is very limited.Novel Bendectin, as NK
1and 5-HT
3receptor antagonist, though antiemetic effect is good, expensive, the scope of application is narrow, and the toxicity of maincenter and periphery is large, clinically needs drug combination more, therefore the initiative of urgently novel resisting emesis medicine.
Chinese medicine Rhizoma Zingiberis Recens (zingiber) is described as " vomiting panacea ".Gingerol is the active ingredient extracted from Rhizoma Zingiberis Recens, the present inventor observes gingerol can resist inorganic and organic poison copper sulfate and Cisplatin-induced Vomiting, and suppress intestinal pheochromocyte to discharge to cause and tell factor 5-HT and Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2, gingerol acts on the maximally related NK of emesis of chemotherapy
1and 5-HT
3deng receptor, be Mutiple Targets, natural low toxicity Bendectin.This product be the dry rod of ranunculaceae plant Rhizoma Coptidis Contischinensis Franch. Coptis deltoidea C.Y.Cheng et Hsiao Coptis deltoidea C.Y.Chenget Hsiao or Coptis Teeta Wall Coptis teeta Wall. wantonly for damp and hot feeling of fullness, vomiting acid regurgitation, dysentery etc.The present inventor, through the research of a large amount of each formula proportion and experiment and clinical practice, finally obtains optimal drug comparative compositions of the present invention, and demonstrates it and have good curative effect to vomiting, this completes the present invention.
Summary of the invention
The present invention's first object is to provide a kind of natural drug composition, and said composition low toxicity is efficient, determined curative effect, is convenient to application and promotes, and can be used as the medicine of resisting emesis.
A kind of natural drug composition provided by the invention, is made up of in the ratio of 5-30: 1-2 by weight Rhizoma Coptidis extract and gingerol.
Above-mentioned natural drug composition, wherein the usage ratio of Rhizoma Coptidis extract and gingerol is 23: 2.
Wherein, Rhizoma Coptidis extract and gingerol are by well known to a person skilled in the art that conventional method is carried out purification and obtained, gingerol can business be buied, and the natural drug of the present invention that these compositions adopting conventional method to obtain or the one-tenth adopting business to buy are grouped into all can obtain identical curative effect.The method below listed is only that inventor thinks and is not intended to preferred method make special restriction to the extracting method of composition each in this natural drug composition.
In above-mentioned natural drug composition, the preparation method of Rhizoma Coptidis extract is:
Get Rhizoma Coptidis, 10 times amount distilled water immersion 1h, on the electric furnace adding asbestos gauge, heating decocts 1h, and silk filters, preserve filtrate, medicinal residues add 6 times of distilled water again, soak, decoct, filter with method, by twice filtrate mixing, heating is concentrated into small size, ultrafiltration membrance filter, adopts vacuum drying oven 70 DEG C of drying under reduced pressure 36h, is Rhizoma Coptidis extract.
In above-mentioned natural drug composition, the preparation method of gingerol is:
Rhizoma Zingiberis Recens is thinly sliced, natural drying, break into powder with high speed Universalpulverizer, cross 30 mesh sieves, then the fine powder that will sieve puts into the large port grinding bottle of 5000mL, to soak 72h under 6 times amount acetone room temperature; At 40 DEG C, supersound extraction 15min under the ultrasonic frequency of 40KHz, centrifugally obtains supernatant, and residue discards; By supernatant decompress filter again, filtrate is placed in Rotary Evaporators vacuum concentration and obtains Rhizoma Zingiberis Recens and extract mixture, then this mixture is carried out repeatedly concentrate drying purification and obtain gingerol.
Present invention also offers the preferred preparation method of this natural drug composition, comprising:
(1) preparation of Rhizoma Coptidis extract
Get Rhizoma Coptidis, 10 times amount distilled water immersion 1h, on the electric furnace adding asbestos gauge, heating decocts 1h, and silk filters, preserve filtrate, medicinal residues add 6 times of distilled water again, soak, decoct, filter with method, by twice filtrate mixing, heating is concentrated into small size, ultrafiltration membrance filter, adopts vacuum drying oven 70 DEG C of drying under reduced pressure 36h, is Rhizoma Coptidis extract.
(2) preparation of gingerol
Rhizoma Zingiberis Recens is thinly sliced, natural drying, break into powder with high speed Universalpulverizer, cross 30 mesh sieves, then the fine powder that will sieve puts into the large port grinding bottle of 5000mL, to soak 72h under 6 times amount acetone room temperature; At 40 DEG C, supersound extraction 15min under the ultrasonic frequency of 40KHz; Centrifugally obtain supernatant, residue discards; By supernatant decompress filter again, filtrate is placed in Rotary Evaporators vacuum concentration and obtains Rhizoma Zingiberis Recens oily mixture, then this mixture is carried out repeatedly concentrate drying purification and obtain gingerol.
(3) choose Rhizoma Coptidis extract and gingerol in proportion, Homogeneous phase mixing, to obtain final product.
The preparation method of above-mentioned natural drug composition, also comprise: product obtained for step (3) is made capsule containing natural drug composition 100mg or 200mg specification further by the pharmacy means of routine, maybe will make the tablet containing natural drug composition 100mg or 200mg specification by wet granulation technology.
The present invention also comprises natural drug composition and reduces the purposes of vomitting in medicine in preparation.
The instructions of taking of natural drug composition of the present invention: the treatment available capsule of vomiting or tablet, for each person every day 600mg, point three one after each meals.
Detailed description of the invention
Set forth the preparation of natural drug composition of the present invention further below by embodiment and test example, and it is at the beneficial effect of resisting emesis.
Embodiment
The first step: the preparation of various extract
(1) preparation of Rhizoma Coptidis extract
Get Rhizoma Coptidis, 10 times amount distilled water immersion 1h, on the electric furnace adding asbestos gauge, heating decocts 1h, and silk filters, preserve filtrate, medicinal residues add 6 times of distilled water again, soak, decoct, filter with method, by twice filtrate mixing, heating is concentrated into small size, ultrafiltration membrance filter, adopts vacuum drying oven 70 DEG C of drying under reduced pressure 36h, is Rhizoma Coptidis extract.
(2) preparation of gingerol
Rhizoma Zingiberis Recens is thinly sliced, natural drying, break into powder with high speed Universalpulverizer, cross 30 mesh sieves, then the fine powder that will sieve puts into the large port grinding bottle of 5000mL, to soak 72h under 6 times amount acetone room temperature; At 40 DEG C, supersound extraction 15min under the ultrasonic frequency of 40KHz; Centrifugally obtain supernatant, residue discards; By supernatant decompress filter again, filtrate is placed in Rotary Evaporators vacuum concentration and obtains Rhizoma Zingiberis Recens oily mixture, then this mixture is carried out repeatedly concentrate drying purification and obtain gingerol.
Second step: the preparation of preparation
(1) preparation of natural drug composition capsule preparations of the present invention
Take Rhizoma Coptidis extract 92mg, gingerol 8mg prepared by above-mentioned steps respectively, take starch 395mg, magnesium stearate 5mg, Homogeneous phase mixing, filled capsules simultaneously, make the capsule of each pure heavy 500mg.
(2) preparation of natural drug composition tablet of the present invention
Take Rhizoma Coptidis extract 92mg, gingerol 8mg prepared by above-mentioned steps respectively, take starch 295mg, lactose 100mg, Homogeneous phase mixing simultaneously, with wet granulation, drying, mix with 5mg magnesium stearate after granulate, tabletting, make the tablet of the pure heavy 500mg of every sheet.
Test example 1: natural drug composition treatment cisplatin causes the pharmacodynamic study of vomiting effect
1, test material
(1) Rhizoma Coptidis, bought by large pharmacy, medical insurance city, Qingdao, Rhizoma Zingiberis Recens, is purchased from Shandong Pingdu.
(2) cisplatin (cisplatin), Shandong Qilu Pharmaceutical Factory produces, lot number: 903005CE, 20mg/ prop up.
(3) Ondansetron Hydrochloride injection, the pharmacy of Olympic Competition health, lot number: 090102,2ml: 4mg.
(4) healthy adult mink, body weight 1.3=1.8kg, male, provided by special cultivation animal feeding center, Qingdao, every animal is placed in separately the ferrum cage of 75cm × 50cm × 50cm, 24h natural light irradiation, ad lib drinking-water before experiment.
2, test method:
Mink is divided into 4 groups at random, and often organize 6, A group is cisplatin model control group, and B group is ondansetron positive drug group, and C group is gingerol, and D group is natural drug composition of the present invention (Rhizoma Coptidis extract mixes in 23: 2 ratios with gingerol).A group gives normal saline pretreatment; B group gives ondansetron 7.5m g.kg
-1pretreatment; C group is to giving gingerol 10g.kg
-1(being equivalent to containing crude drug amount) ig pretreatment; D group gives natural drug composition 10g.kg of the present invention
-1(being equivalent to containing crude drug amount) ig pretreatment, each group all gives cisplatin 7.5mg.kg at administration 30min
-1ip.For the vomiting reaction in observation mink upon administration 6h, record its vomiting incubation period, retch and vomiting number of times.
3, experimental result
Compare with matched group, each treatment group all can obviously alleviate retches and also prolongation vomiting incubation period (P < 0.01) of vomiting number of times.Gingerol group and natural drug composition of the present invention all can reduce and cause the rate of vomitting.The results are shown in Table 1.
Table 1 compositions to cisplatin (7.5mg/kg, ip) cause vomit effect impact (
n=6)
Note: a is equivalent to, containing crude drug amount, compare with matched group
cp < 0.01
Test example 2: natural drug composition is to the pharmacodynamic study of copper sulfate induced Vomiting
1, test material
(1) copper sulfate, Tianjin recovery fine chemistry industry institute
(2) Ondansetron Hydrochloride injection, the pharmacy of Olympic Competition health
(3) healthy adult mink, body weight 1.3-1.8kg, male, provided by special cultivation animal feeding center, Qingdao, every animal is placed in separately the ferrum cage of 75cm × 50cm × 50cm, 24h natural light irradiation, ad lib drinking-water before experiment.
2, test method:
Mink is divided into 4 groups at random, and often organize 6, A group is copper sulfate model control group, and B group is ondansetron positive drug group, and C group is gingerol, and D group is natural drug composition of the present invention (Rhizoma Coptidis extract mixes in 23: 2 ratios with gingerol).A group gives normal saline pretreatment; B group gives ondansetron 7.5m g.kg
-1pretreatment: C group is to giving gingerol 10g.kg
-1(being equivalent to containing crude drug amount) ig pretreatment; D group gives natural drug composition 10g.kg of the present invention
1(being equivalent to containing crude drug amount) i g pretreatment, each group all presses 40mgkg at administration 30min
-1gavage gives copper sulfate.For the vomiting reaction in observation mink upon administration 2h, record its vomiting incubation period, retch and vomiting number of times.
3, experimental result
Compare with matched group, each group all obviously can alleviate retch and also prolongation vomiting incubation period (P < 0.01) of vomiting number of times, and compositions resisting emesis effect of the present invention is better than gingerol group.The results are shown in Table 2.
Table 2 compositions on copper sulfate (40mg/kg) cause vomit effect impact (
n=6)
Note: a is equivalent to, containing crude drug amount, compare with matched group
cp < 0.01
Test example 3: natural drug composition is to the pharmacodynamic study of apomorphine induced Vomiting
1, test material
(1) apomorphine, sigma company
(2) Ondansetron Hydrochloride injection, the pharmacy of Olympic Competition health
(3) healthy adult mink, body weight 1.3-1.8kg, male, provided by special cultivation animal feeding center, Qingdao, every animal is placed in separately the ferrum cage of 75cm × 50cm × 50cm, 24h natural light irradiation, ad lib drinking-water before experiment.
2, test method:
Mink is divided into 4 groups at random, and often organize 6, A group is apomorphine model control group, and B group is ondansetron positive drug group, and C group is gingerol, and D group is natural drug composition of the present invention (Rhizoma Coptidis extract mixes in 23: 2 ratios with gingerol).A group gives normal saline pretreatment; B group gives ondansetron 7.5m g.kg
1pretreatment; C group is to giving gingerol 10g.kg
1(being equivalent to containing crude drug amount) ig pretreatment; D group gives natural drug composition 10g.kg of the present invention
1(being equivalent to containing crude drug amount) ig pretreatment, each group all gives apomorphine 0.25mgkg at administration 30min
-1ip.For the vomiting reaction in observation mink upon administration 2h, record its vomiting incubation period, retch and vomiting number of times.
3, experimental result
Compare with matched group, each group all can alleviate retch and also prolongation vomiting incubation period (P < 0.01) of vomiting number of times.And compositions resisting emesis effect of the present invention is better than gingerol group.The results are shown in Table 3.
Table 3 compositions is to apomorphine (0.25mgkg
1, ip) cause vomit effect impact (
n=6)
Note: a is equivalent to, containing crude drug amount, compare with matched group
cp < 0.01
Test example 4: the acute toxicity test of natural drug composition of the present invention
1, experimental animal:
Kunming mouse, body weight 20 ± 2g, is provided by medicine inspecting institute of Qingdao City Experimental Animal Center
2, medicine:
Natural drug composition of the present invention, tragakanta
3, test method:
Promulgate on November in 999 year 12 according to National Drug Administration one " the study of tcm new drug technical requirement " of revision, acute toxicity testing is carried out to natural drug of the present invention.Because limiting by drug level and volume, LD cannot be measured
50, therefore carry out maximum dosage-feeding experiment.Get Kunming mouse 30, female half and half, ig, give capsule Chinese medicine 1g/mL, every 0.8mL, be i.e. the maximum gavage volume of mice, by observation post administration mice active state, diet, feces, breathing, body weight and death condition, Continuous Observation 14d.
4, result of the test:
Well-grown after each group of mouse stomach administration, body weight increases, and behavior is normal, is showed no death and significant reaction.After sacrifice of animal, each main organs of perusal phenomenon without exception.
Result shows, natural drug composition maximal dose oral application of the present invention, and to animal without obvious damage, not finding the toxic reaction produced body, is a kind of safe and reliable antiemetic.
Claims (5)
1. reduce a natural drug composition for vomiting reaction, it is characterized in that said composition is made up of in the ratio of 5-30: 1-2 by weight Rhizoma Coptidis extract and gingerol,
Wherein the preparation method of Rhizoma Coptidis extract is:
Get Rhizoma Coptidis, 10 times amount distilled water immersion 1h, on the electric furnace adding asbestos gauge, heating decocts 1h, and silk filters, preserve filtrate, medicinal residues add 6 times of distilled water again, soak, decoct, filter with method, by twice filtrate mixing, heating is concentrated into small size, ultrafiltration membrance filter, adopts vacuum drying oven 70 DEG C of drying under reduced pressure 36h, is Rhizoma Coptidis extract;
Wherein the preparation method of gingerol is:
Rhizoma Zingiberis Recens is thinly sliced, natural drying, break into powder with high speed Universalpulverizer, cross 30 mesh sieves, then the fine powder that will sieve puts into the large port grinding bottle of 5000mL, to soak 72h under 6 times amount acetone room temperature; At 40 DEG C, supersound extraction 15min under the ultrasonic frequency of 40KHz, centrifugally obtains supernatant, and residue discards; By supernatant decompress filter again, filtrate is placed in Rotary Evaporators vacuum concentration and obtains Rhizoma Zingiberis Recens and extract mixture, then this mixture is carried out repeatedly concentrate drying purification and obtain gingerol.
2. natural drug composition as claimed in claim 1, wherein the usage ratio of Rhizoma Coptidis extract and gingerol is 23: 2.
3., as the preparation method of the natural drug composition of claim 1 or 2, it is characterized in that the method comprises:
(1) preparation of Rhizoma Coptidis extract
Get Rhizoma Coptidis, 10 times amount distilled water immersion 1h, on the electric furnace adding asbestos gauge, heating decocts 1h, and silk filters, preserve filtrate, medicinal residues add 6 times of distilled water again, soak, decoct, filter with method, by twice filtrate mixing, heating is concentrated into small size, ultrafiltration membrance filter, adopts vacuum drying oven 70 DEG C of drying under reduced pressure 36h, is Rhizoma Coptidis extract;
(2) preparation of gingerol
Rhizoma Zingiberis Recens is thinly sliced, natural drying, break into powder with high speed Universalpulverizer, cross 30 mesh sieves, then the fine powder that will sieve puts into the large port grinding bottle of 5000mL, to soak 72h under 6 times amount acetone room temperature; At 40 DEG C, supersound extraction 15min under the ultrasonic frequency of 40KHz, centrifugally obtains supernatant, and residue discards; By supernatant decompress filter again, filtrate is placed in Rotary Evaporators vacuum concentration and obtains Rhizoma Zingiberis Recens oily mixture, then this mixture is carried out repeatedly concentrate drying purification and obtain gingerol;
(3) choose Rhizoma Coptidis extract and gingerol Homogeneous phase mixing in proportion, to obtain final product.
4. the preparation method of natural drug composition as claimed in claim 3, also comprise: product obtained for step (3) is made capsule containing natural drug composition 100mg or 200mg specification further by the pharmacy means of routine, maybe will make the tablet containing natural drug composition 100mg or 200mg specification by wet granulation technology.
5. the natural drug composition as described in any one of claim 1-2 reduces the purposes in vomiting reaction medicine in preparation.
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| CN103272014A (en) * | 2013-03-29 | 2013-09-04 | 阚兆云 | Traditional chinese medicine extract |
| CN103316112A (en) * | 2013-07-04 | 2013-09-25 | 石强 | Natural pharmaceutical composition |
| CN103919819A (en) * | 2014-04-21 | 2014-07-16 | 青岛中仁药业有限公司 | Poria cocos natural composition and anti-cancer vomit-preventing application thereof |
| CN104000876A (en) * | 2014-06-18 | 2014-08-27 | 青岛市市立医院 | Composition of mangnolia officinalis and gingerol and application thereof |
| CN105616442A (en) * | 2016-03-04 | 2016-06-01 | 青岛黄海学院 | Medicine composition for treating vomit and preparation method and application of medicine composition |
| CN107583003B (en) * | 2016-07-08 | 2021-06-18 | 香港大学 | Compound composition for preventing or treating diabetic eye disease, its preparation method and use |
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