CN104147557A - Shogaol extract soft capsule and preparation method thereof - Google Patents
Shogaol extract soft capsule and preparation method thereof Download PDFInfo
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- CN104147557A CN104147557A CN201410319646.6A CN201410319646A CN104147557A CN 104147557 A CN104147557 A CN 104147557A CN 201410319646 A CN201410319646 A CN 201410319646A CN 104147557 A CN104147557 A CN 104147557A
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Abstract
The invention relates to a shogaol extract preparation and in particular relates to a shogaol extract soft capsule and a preparation method thereof. The shogaol extract soft capsule is prepared from the components in parts by weight: 3-10 parts of shogaol extract and 40-60 parts of oiliness matrix; preferentially, the shogaol extract soft capsule is prepared from the following components in parts by weight: 6 parts of shogaol extract and 54 parts of corn oil. As a supercritical CO2 extraction method is adopted, the extraction method of a shogaol extract has the advantages of high extraction ratio and high content of 6-shogaol. Meanwhile, the shogaol extract soft capsule is good in stability.
Description
Technical field
The present invention relates to a kind of ginger phenols extract preparation, specifically, relate to a kind of ginger phenols extract soft capsule and preparation method thereof.
Background technology
The economy, culture and the social life that develop rapidly the mankind of the modern means of communication and aerospace industry have been brought into play important facilitation, but also make some people move disease simultaneously.Motion sickness is that the nervous function causing after the uncomfortable conditioning being subject in movement environment is lacked of proper care, and main manifestations is autonomic nervous system dysfunction.Symptom is conventionally carries out sexual development, by gastric area discomfort, feel sick, salivation increase, pale complexion, be in a cold sweat, dizzy, headache, and then develop into retch, vomiting, drowsiness, indifferent.Vomiting severe patient even can dewater, exhaustion.When it betides people's riding vehicle, ship, aircraft, recreation facility or navigation, Aeronautics and Astronautics simulation and actual job.Because of residing movement environment difference, motion sickness has again different titles, as carsick, airsick (motion sickness), seasick (navigation motion sickness or sea are dizzy), space motion sickness (space flight disease), simulator sickness etc.Motion sickness sickness rate is higher, also larger with the different variations of movement environment.
The pathogenesis of motion sickness: according to many Chinese and overseas scholars for many years to the pathogenetic research understanding of motion sickness, can think that abnormal motion stimulates sensigenous conflict in central nervous system, cause many transmitter in central nervous system systemic-function loss of equilibrium, endocrine function, cerebral cortex functional disorder, regulating and controlling effect to brain stem autonomic center is not normal, causes vestibular sensations extremely and autonomic nervous dysfunction.The motion sickness resistant medicament of clinical practice at present mainly contains following a few class: anticholinergic agent, antihistaminic, dopamine-receptor antagonist, 5-hydroxytryptamine receptor antagonist, sympatheticomimetic etc.But these side effects of pharmaceutical drugs are all very large, and anticholinergic agent can suppress central nervous system, cause drowsinessly, also can make the dimness of vision, xerostomia, impair one's memory etc., should not be used for carrying out the personnel of operation.Antihistaminic kind is more, the most conventional with dimenhydrinate (generally claiming dimenhydrinate, dimenhydrinate), also the side effect that has maincenter to suppress, can cause drowsinessly, while especially increasing consumption for stiffening effect, thereby can not be used for carrying out the personnel of operation.In a word, the motion sickness resistant medicament of clinical practice mostly at present is cholinolytic and Loratadine, acts on stronger, but side effect is also more, little in the urgent need to toxic and side effects, do not affect normal operation, go sightseeing, the motion sickness resistant medicament of operation, the space flight operation etc. such as particularly sail across a sea.
Chinese medicine Rhizoma Zingiberis Recens is the fresh rhizome of zingiber (Zingiber officinale Rosc), nature and flavor are pungent, warm, return lung, spleen, stomach warp, there is the effects such as the cold expelling of inducing sweat, warming middle-JIAO to stop vomiting, preventing phlegm from forming and stopping coughing, cure mainly anemofrigid cold, gastrofrigid vomiting, cold-phlegm cough.
In traditional Chinese medical science classical literature, there is the report of a large amount of Rhizoma Zingiberis Recens treatment vomitings.Physician Li Gao claims " Rhizoma Zingiberis Recens is patient suffering from habitual vomiting panacea ".Tao Hongjing: " rheumatism cold and heat are told, removed to Rhizoma Zingiberis Recens preventing or arresting vomiting." property of medicine opinion " recorded Rhizoma Zingiberis Recens preventing or arresting vomiting and can not told any more food." Bencao Congxin " recorded: Roast Rhizoma Zingiberis Recens, and middle emesis." dietitian's heart mirror " record " stopping vomiting is told, and hundred medicines are not poor: Rhizoma Zingiberis Recens one or two, cut and close with vinegar slurry seven greatly as Semen phaseoli radiati, take four in silverware and close, on an empty stomach and dregs revolve sip it "." Medical Treasures of the Golden Chamber " Rhizoma Zingiberis Recens Rhizoma Pinelliae soup people that cures the disease seemingly breathes heavily in the heart, seemingly vomits, and like vomiting, muddled right helpless person in the heart." Medical Treasures of the Golden Chamber " Zingiberis-Ginseng-Pinelliae Pill controls incesant vomiting during pregnancy.
Five, the sixties, China has developed a series of Chinese herb compounds in Chinese herbal medicine motion, as anti-corona clever sheet, formed anti-corona by the 10 taste Chinese medicines such as Rhizoma Zingiberis Recens, Caulis Perillae, formed by Flos Daturae, Rhizoma Zingiberis, Pericarpium Zanthoxyli etc., ginger, is made up of the 6 taste Chinese medicines such as Rhizoma Zingiberis Recens, the Rhizoma Pinelliae, for preventing and treating motion sickness, effect is strong compared with dimenhydrinate, and side effect is not obvious.There is in recent ten years the report of a large amount of Rhizoma Zingiberis Recens anti-kinetosis both at home and abroad.
Rhizoma Zingiberis Recens section is spread on to Neiguan acupoint, and carsickness-proof in advance, tries out in 39 routine carsick persons, and carsick phenomenon does not occur 38 examples, and being used for the treatment of serious symptom vomiting has good effect, and Rhizoma Zingiberis Recens is mashed as mud shape spreads on Neiguan acupoint and also had the effect of pre-carsickness-proof.
The emptying sluggishness of rat stomach that Rhizoma Zingiberis Recens juice is sluggish to the gastric emptying of Canis familiaris L. due to cisplatin and 1,2,3,-thrihydroxy-benzene causes has significant inhibitory action, and its effect is better than ondansetron.To CuSO
4due to pigeon vomiting, Rhizoma Zingiberis Recens juice can significant prolongation occur vomiting incubation period, reduce vomiting number of times, town is told intensity and is reached 85%.
By Rhizoma Zingiberis Recens airing, wearing into fine powder is loaded in capsule oral, at random, double blind shows: Rhizoma Zingiberis Recens powder can suppress vomiting and be in a cold sweat, there is significant pre-Anti-seasickness, carsick effect, effect is better than dimenhydrinate, do not find any obvious untoward reaction, but preparation is unstable, places effect in two weeks and greatly reduce.Rhizoma Zingiberis Recens powder can significantly alleviate the nausea and vomiting that multiple operation occurs afterwards, acts on quite with metoclopramide, and has no side effect.70 routine women's 5 months randomized controlled result of the test is remarkable, the vomiting that Rhizoma Zingiberis Recens powder gestation causes, and inhibitory action and metoclopramide are suitable, and have no side effect.Rhizoma Zingiberis Recens powder causes thermostimulation dizzyly has a significant inhibitory action.
12 routine volunteer's result of the tests demonstrations, Rhizoma Zingiberis Recens extract significantly strengthens harmonization of the stomach duodenum intestinal motive force.Effect and metoclopramide that oral Rhizoma Zingiberis Recens acetone extract strengthens digestive tract power are suitable.The gastric emptying sluggishness that Rhizoma Zingiberis Recens acetone and ethanol extraction are sluggish to the gastric emptying of Canis familiaris L. due to cisplatin and 1,2,3,-thrihydroxy-benzene causes has significant inhibitory action, and the effect of acetone extract is better than ethanol extraction, and suitable with ondansetron.To CuSO
4due to pigeon vomiting, gingerade decoct can significant prolongation occur vomiting incubation period, reduce vomiting number of times and vomiting number of elements.The ethanol of Rhizoma Zingiberis Recens and acetone extract have significant inhibitory action to the vomiting of the Canis familiaris L. due to the chemotherapy such as cisplatin.
The anti-kinetosis mechanism of Rhizoma Zingiberis Recens is also completely not clear and definite at present.Most research thinks that the anti-kinetosis effect of Rhizoma Zingiberis Recens is mainly by the direct impact on gastronintestinal system, improves digestive tract power.The research of Jiang Zhenglin etc. is found, the anti-kinetosis effect of Rhizoma Zingiberis Recens is similar to anticholinergic agent scopolamine, the effect of the anti-kinetosis of lumbar injection Rhizoma Zingiberis Recens juice to rat is better than gastric infusion, the effect of prompting Rhizoma Zingiberis Recens anti-kinetosis, except outside the Pass having with its direct effect to gastrointestinal, may also have other mechanism of action.The research of Qian Dongsheng etc. is thought, Rhizoma Zingiberis Recens plays anti-kinetosis effect by maincenter and periphery cholinolytic and antihistamine, the process of inhibition of Rhizoma Zingiberis Recens juice cerebral cortex is strengthened, inhibited to corticocerebral conductive process for the front stimulation impulsion of bringing out, thereby can alleviate dizzy and nauseating reaction.
Comprehensively above data can be found out, Rhizoma Zingiberis Recens has definite and significant anti-kinetosis effect and without obvious toxic and side effects, is comparatively ideal motion sickness resistant medicament.Europe and American Pharmacopeia have been classified Rhizoma Zingiberis Recens as anti-dizzy antiemetic.But different preparation methoies are larger to the anti-kinetosis function influence of Rhizoma Zingiberis Recens, wherein the anti-dizzy antiemetic effect of Rhizoma Zingiberis Recens juice is the strongest, significantly be better than dimenhydrinate etc., the medicines such as the effect of dry Rhizoma Zingiberis Recens powder and dimenhydrinate, metoclopramide and scopolamine are suitable, anti-kinetosis effect and the dimenhydrinate etc. of Rhizoma Zingiberis Recens acetone extract is quite or slightly, the effect of Rhizoma Zingiberis Recens ethanol extraction and water extract is less, even not anti-dizzy antiemetic effect.But Rhizoma Zingiberis Recens juice and Rhizoma Zingiberis powder are all unstable, be difficult to be prepared into stable, dosage form easily.With organic solvent extraction, in the time reclaiming solvent, easily make a part of composition lose or destroy.Be the main component of its anti-dizzy emesis according to the phenolic constituent such as gingerol, shogaol in Rhizoma Zingiberis Recens, we select supercritical CO through systematic research
2fluid extraction method, prepares ginger phenols extract, and further prepares that anti-kinetosis effect is strong, side effect is little, the Jiang Su soft gelatin capsule that dosage form is stable.
Summary of the invention
Primary goal of the invention of the present invention is to provide a kind of ginger phenols extract soft capsule;
The second goal of the invention of the present invention is to provide the preparation method of this ginger phenols extract soft capsule.
In order to complete object of the present invention, the technical scheme of employing is:
A kind of ginger phenols extract soft capsule, the consisting of of described soft capsule content: ginger phenols extract 3～10 weight portions, oleaginous base 40～60 weight portions; Be preferably: ginger phenols extract 4～8 weight portions, oleaginous base 50～56 weight portions; More preferably: ginger phenols extract 6 weight portions, oleaginous base 52～56 weight portions.
The first optimal technical scheme of the present invention is: described oleaginous base is selected from least one in Semen Maydis oil, Oleum Arachidis hypogaeae semen, soybean oil, olive oil.
The second optimal technical scheme of the present invention is: the consisting of of described soft capsule content: ginger phenols extract 6 weight portions, Semen Maydis oil 54 weight portions.
The 3rd optimal technical scheme of the present invention is: the consisting of of described soft capsule rubber: gelatin 25～40 weight portions, glycerol 10～20 weight portions, water 30～48 weight portions; Be preferably gelatin 30～36 weight portions, glycerol 12～18 weight portions, water 36～42 weight portions.
The 4th optimal technical scheme of the present invention is: in described soft capsule, the extracting method of ginger phenols extract is:
(1) Rhizoma Zingiberis Recens is cut into 2～5mm thin slice, 40～45 DEG C of aeration-drying to water content are less than 10%, pulverize 40 mesh sieves, obtain Rhizoma Zingiberis Recens powder;
(2) pack Rhizoma Zingiberis Recens powder into supercritical CO
2in extraction equipment, be that 40～55 DEG C, pressure are 20～30Mpa, CO in temperature
2flow velocity is to extract under the condition of 10kg/h.kg raw material, and extraction time is 1～3 hour, and the separating still that is then 10Mpa in pressure is collected ginger phenols extract.
The 5th optimal technical scheme of the present invention is: the super CO of supercritical
2extraction conditions, temperature is 53～55 DEG C, preferably 55 DEG C.
The 6th optimal technical scheme of the present invention is: the super CO of supercritical
2extraction conditions, pressure is 28～30Mpa, preferably 30Mpa.
The 7th optimal technical scheme of the present invention is: the preparation method of described soft capsule is:
(1) preparation of content: take by weight ginger phenols extract and oleaginous base, fully stir and make whole dissolvings in 55～65 DEG C; Put common filter paper filtration under diminished pressure in buchner funnel, filtrate is filtered through G3 sintered glass funnel again, obtains clear and bright solution;
(1) preparation of glue: take by weight water and glycerol, be heated to 70～80 DEG C, mix homogeneously, adds gelatin by weight, stirs, and melting, is incubated 1～2 hour, leaves standstill, and after foam floating, removes, and filters heat preservation for standby use;
(2) prepare soft gelatin capsule, the soft gelatin capsule of making is placed in to 21～24 DEG C of relative humidity 20～30%, temperature, under air blast condition, be dried, making glue shell water content is 6～10%.
Explanation that the technical solution of the present invention is further explained below:
The present invention proposes a kind of soft capsule of ginger phenols extract, because the crude drug of preparation of the present invention is semifluid, be difficult to make solid preparation, if make tablet etc., not only need to add a large amount of adjuvants, and due to the pungent abnormal smells from the patient of crude drug, make the compliance variation of medicine.And because ginger phenols extract of the present invention is soluble in vegetable oil, and because it has acid, oral rear local concentration may produce stimulation to gastrointestinal when higher, with after vegetable oil dilution, delay it and discharge, reduce local excitation.Therefore, ginger phenols extract is prepared into soft capsule, can overcomes above-mentioned defect.Meanwhile, due to ginger phenols extract less stable, dissolve and prepare after soft gelatin capsule with vegetable oil, suppress its oxidation thereby reduce with contacting of oxygen, can also prevent volatilization, increase stability.Meanwhile, because Semen Maydis oil does not almost affect blood fat, and the large-scale production of medicinal Semen Maydis oil, resource abundance, steady quality, can reach medicinal standard, and price is lower.The results showed that the Semen Maydis oil solution of ginger phenols extract still keeps clear and bright state through long-time place (2～3 years), without precipitation, metachromatism, assay is stablized constant.So the present invention preferably adopts Semen Maydis oil and ginger phenols extract to prepare soft capsule, to find through contrast test, the stability of ginger phenols extract of the present invention in Semen Maydis oil is higher than other oleaginous bases.Known through stability test, the stability of soft capsule prepared by formula of the present invention is good.And find by stability test, adopt ginger phenols extract: the ratio that Semen Maydis oil is 1:9, stability the best of the soft capsule obtaining, is better than other ratios.
The preparation of the ginger phenols extract in soft capsule of the present invention has adopted the method preparation of supercritical carbon dioxide extraction, and the method, with respect to other organic solvent extracting access method, has simple to operate, extraction ratio advantages of higher.The present invention improves the method:
First, Rhizoma Zingiberis Recens is dry, and under lower temperature conditions, aeration-drying, prevents the volatilization of effective ingredient; And impact experiment by extraction ratio and the dried water content of Rhizoma Zingiberis Recens finds, water content is larger on the productive rate impact of extract between 10～20% time, and water content be less than 10% productive rate change little, therefore select to be dried to water content lower than 10%.Meanwhile, the granularity of material has double influence to extraction ratio, and on the one hand, material attenuates has increased mass transfer area, has reduced mass transfer distance and resistance to mass tranfer, is beneficial to extraction; On the other hand, material is too thin, under high pressure, is easily compacted, and has increased resistance to mass tranfer, is unfavorable for extraction.The present invention by experiment, finds Rhizoma Zingiberis powder to be prepared into 40 object granularities, extraction yield the best.
Then, pack Rhizoma Zingiberis Recens powder into supercritical CO
2in extraction equipment, be that 50～55 DEG C, pressure are 25～30Mpa, CO in temperature
2flow velocity is to extract under the condition of 10kg/h.kg raw material, and extraction time is 2～3 hours; Preferred condition is that temperature is that 55 DEG C, pressure are 30Mpa, CO
2flow velocity is 10kg/h.kg; Then the separating still that is 10Mpa in pressure is collected ginger phenols extract.Carrying out supercritical CO
2in extraction process, find, can obtain oleoresin shape thing when adjusting when the pressure of separator I is 10Mpa, temperature 50 C, at separator II (pressure is 6.5Mpa), what obtain is grease.GC-MS analysis result shows, in extract II, containing compositions such as monoterpene, sesquiterpenes, is mainly volatile oil.Extract I mainly contains phenols component, is therefore called ginger phenols extract.And learn the extract of the ginger phenols just preparing by extraction preparation method of the present invention, its drug effect the best by further pharmacodynamic experiment; And extraction conditions of the present invention, its productive rate can reach 3～12.0%, and in preparation-obtained ginger phenols extract, the content of 6-gingerol can reach 22.5～28.5%.
Brief description of the drawings:
Fig. 1 is the high-efficient liquid phase chromatogram of the ginger phenols extract for preparing in embodiment;
Fig. 2 is the influence curve of Rhizoma Zingiberis Recens powder water content to extraction yield in experimental example 2.
The specific embodiment of the present invention only limits to content of the present invention to make further explanation, and content of the present invention is not enough become to restriction.
Detailed description of the invention
Embodiment 1 prepares ginger phenols extract soft capsule
1. formula is:
2 preparation technologies
2.1 extraction of ginger by supercritical carbon dioxide phenols extract things:
(1) Rhizoma Zingiberis Recens is cut into 2～5mm thin slice, 45 DEG C of aeration-drying to water content are less than 10%, pulverize 40 mesh sieves, obtain Rhizoma Zingiberis Recens powder;
(2) pack Rhizoma Zingiberis Recens powder into supercritical CO
2in extraction equipment, be that 55 DEG C, pressure are 30Mpa, CO in temperature
2flow velocity is to extract under the condition of 10kg/h.kg raw material, and extraction time is 2 hours, and the separating still that is then 10Mpa in pressure is collected and obtained ginger phenols extract, and its high-efficient liquid phase chromatogram as shown in Figure 1.
2.2 solution preparation
The preparation of content solution: accurately take ginger phenols extract 600g, add medicinal Semen Maydis oil 5400g, fully stir and make whole dissolvings in 60 DEG C; Put common filter paper filtration under diminished pressure in buchner funnel, filtrate is filtered through G3 sintered glass funnel again, obtains clear and bright solution.
The preparation of glue: by formulation weight, take gelatin, G & W, first G & W mixing post-heating to 70～80 DEG C, add gelatin by formula, stirs, and melting, is incubated 1～2 hour, leaves standstill, and after foam floating, removes, and filters heat preservation for standby use.2.3 soft gelatin capsule preparations
Adopt the standby Jiang Su soft gelatin capsule of RJWJ-1 type soft capsule capsule mechanism processed; The soft gelatin capsule of making is spread out and put in tray, put into drying alley, at 20～30% relative humiditys, 21～24 DEG C of temperature, are dried under air blast condition, make glue shell water content in 6～10% scopes; Every ball soft gelatin capsule weighs 0.3 gram, includes 30mg ginger phenols extract.
Embodiment 2～6 prepares ginger phenols extract soft capsule
Fill a prescription as shown in table 1:
Table 1:
| ? | Ginger phenols extract | Refined maize oil | Gelatin | Glycerol | Water |
| Embodiment 2 | 400g | 5000g | 3600g | 1800g | 4200g |
| Embodiment 3 | 300g | 6000g | 3000g | 1200g | 3600g |
| Embodiment 4 | 1000g | 4000g | 3600g | 1200g | 4000g |
| Embodiment 5 | 600g | 5200g | 4000g | 2000g | 3600g |
| Embodiment 6 | 600g | 5600g | 2500g | 1000g | 3000g |
Preparation method is with embodiment 1.
Embodiment 7～12: prepare ginger phenols extract soft capsule
Fill a prescription as shown in table 2:
Table 2:
| ? | ? | Oleaginous base |
| Embodiment 7 | Ginger phenols extract | Oleum Arachidis hypogaeae semen |
| Embodiment 8 | Ginger phenols extract | Olive oil |
| Embodiment 9 | Ginger phenols extract | Soybean oil |
| Embodiment 10 | Ginger phenols extract | Semen Maydis oil: olive oil=1:1 |
| Embodiment 11 | Ginger phenols extract | Semen Maydis oil: Oleum Arachidis hypogaeae semen=2:1 |
| Embodiment 12 | Ginger phenols extract | Soybean oil: olive oil=1:2 |
All the other compositions and preparation method are with embodiment 1.
Experimental example 1: the extraction of ginger phenols extract
Adopt the method for embodiment 1, Rhizoma Zingiberis Recens is carried out to supercritical carbon dioxide extraction, wherein, the baking temperature of Rhizoma Zingiberis Recens is carried out to grouping experiment, be divided into 4 groups: 30 DEG C of groups, 40 DEG C of groups, 60 DEG C of groups and 80 DEG C of groups; Make respectively fresh ginger sheet be dried to water content below 10% at 30,40,60 and 80 DEG C, all the other conditions are with embodiment 1.Get respectively the dry Rhizoma Zingiberis Recens powder of 200g and carry out supercritical CO
2extraction, measures extract content and 6-gingerol content, and result is as table 3.
Table 3. Rhizoma Zingiberis Recens powder baking temperature is on the impact of extracting
Experimental result shows, on the extraction impact of 6-gingerol obviously, when temperature is 60～80 DEG C, the content that extracts 6-gingerol in product reduces baking temperature, and therefore the present invention is chosen in 40～45 DEG C and is dried under ventilation condition.Affect the factor that walks extraction effect under Rhizoma Zingiberis Recens powder and may be due to temperature too Gao Zehui make a part of composition lose or destroy, therefore must control baking temperature.
Experimental example 2
Adopt the method for embodiment 1, Rhizoma Zingiberis Recens is carried out to supercritical carbon dioxide extraction, wherein, water content in Rhizoma Zingiberis Recens powder is carried out to grouping experiment, its experimental result is as shown in table 4, and all the other conditions are with embodiment 1.See accompanying drawing 2.
Table 4. Rhizoma Zingiberis Recens powder water content is on the impact of extracting
From accompanying drawing 1, can find out, water content between 10～20% time the productive rate impact on extract larger, and water content be less than 10% productive rate change little, therefore select to be dried to water content lower than 10%.
Experimental example 3
Adopt the method for embodiment 1, Rhizoma Zingiberis Recens is carried out to supercritical carbon dioxide extraction, wherein, the condition of supercritical carbon dioxide extraction is carried out grouping experiment, and its experimental result is as shown in table 5, and all the other conditions are with embodiment 1.
Table 5:
| ? | Temperature | Pressure | CO 2Flow velocity | Productive rate (%) | 6-gingerol content (%) |
| Embodiment 1 | 55 | 30 | 10 | 11.39 | 28.12 |
| Comparative example 1 | 50 | 30 | 10 | 10.56 | 26.78 |
| Comparative example 2 | 55 | 25 | 10 | 10.21 | 26.45 |
| Comparative example 3 | 55 | 35 | 10 | 10.36 | 26.12 |
| Comparative example 4 | 50 | 25 | 10 | 9.89 | 25.76 |
| Comparative example 5 | 45 | 30 | 10 | 9.95 | 25.53 |
| Comparative example 6 | 40 | 25 | 10 | 9.68 | 24.87 |
Known according to above-mentioned contrast test, adopt the temperature and pressure condition in embodiment 1, the productive rate of prepared ginger phenols extract is the highest, and the content of 6-gingerol is the highest.Therefore the condition in the preferred embodiment of the present invention 1 is extraction conditions, carries out large-scale production.
Experimental example 4: stability test
1 sample source
Get 3 batches (0101,0102,0103) of ginger phenols extract soft capsule prepared by embodiment 1.
2 test apparatuses
Shimadzu UV-2501PC ultraviolet spectrophotometer;
High pressure liquid chromatograph, Waters600 pump, 996 diode array detectors, 717 automatic samplers, 2010 chromatographic work stations.
3 contents of the test
Get 3 batches (0101,0102,0103) of ginger phenols extract soft capsule prepared by embodiment 1, deposit 18 months at normal temperature with listing packaging (aluminum-plastic blister), observe respectively at sampling in 1,2,3,6,9,12,18 month, measure content.
4 investigation project and methods: the relevant code according to pharmacopeia is measured:
Appearance character: directly observe.
Differentiate: thin layer chromatography.
Disintegration time, the ball method of double differences are different: pertinent regulations under capsule item.
Every of total phenol content contains 15～24mg: ultraviolet spectrophotometry, make blank with Semen Maydis oil, and adopt dual wavelength to measure.
6-gingerol content: high performance liquid chromatography.
5. investigate result
Investigate result as table 10-12.This preparation was through the investigation of 18 months, and its physicochemical property and assay are showed no significant change, illustrated that said preparation primary stability is investigated to meet the requirements.
Table 6. Jiang Su soft gelatin capsule primary stability experimental result
Table 7. Jiang Su soft gelatin capsule primary stability experimental result
Table 8. Jiang Su soft gelatin capsule primary stability experimental result
Embodiment 5: pharmacodynamic experiment
1. the preparation of medicine:
1.1 extract ginger phenols extract according to the method in embodiment 1;
1.2 extract ginger phenols extract according to the method in comparative example 1;
1.3 extract ginger phenols extract according to the method in comparative example 3;
1.4 extract ginger phenols extract according to the method in comparative example 5;
1.5 extract ginger phenols extract according to the method in comparative example 6.
2. pharmacodynamic experiment:
2.1: the prevention experiment that guinea pig eye trembles:
Cavia porcellus is divided into 6 groups at random, 20 of every treated animals; 300～400 grams of body weight, ♀
dual-purpose.
Matched group only gives Semen Maydis oil 0.5ml/; All the other 5 groups of dosages are 20mg/kg;
Medication and time are gastric infusion one time, and administration time is the front 30min of test.
Experimental technique
Having in the darkroom of sound insulation and lucifuge, clear-headed Cavia porcellus is placed in special fixed bin, two fronts at eye level, at the subcutaneous insertion of right and left eyes outer canthus 3/8# medical suture needle, as positive and negative electrode, auris dextra outer rim is reference electrode.Put into Cavia porcellus external auditory meatus edge with an infusion plastic pipe and connect syringe, draw 4 DEG C of cold water of 5ml with syringe, in 30s, inject fast complete.Lead physiograph with RM-6000 more, be equipped with nystagmus that preposition biological amplifier AB-600G traces the horizontal or vertical direction that 4 DEG C of cold water stimulating Cavia porcellus external auditory meatuss bring out the continuously ripple that quivers.Instrument record condition is, time constant 2, sensitivity 0.02mV/DIV, filtering 30Hz, chart drive speed 10mm/s, 1 °=1mm of calibration.Be normal eye movement ripple writing time, and after filling with cold water, 30s, 1min nystagmus involve the nystagmus ripple end time.
Observation index
The nystagmus incidence rate (%) of quivering: observe after cold water stimulating Cavia porcellus external auditory meatus, the animal that occurs continuously 5 same directions (to the left or to the right) sawtooth like wave certain time is the nystagmus positive (+) that quivers.
Experimental result is as shown in Table 15:
The preventive effect that the each extract of table 9. Rhizoma Zingiberis Recens trembles to guinea pig eye
2.2 histamine phosphates bring out the antagonism experiment of Guinea pig Gastric smooth muscle contraction:
Test is established six groups, matched group, 1 group of embodiment, 1 group of experimental example, 3 groups of experimental examples, 5 groups of experimental examples, 6 groups of experimental examples altogether.
Animal: 36 of Cavia porcelluss, 300～400 grams of body weight, ♀
dual-purpose.Every group 6.
Method: Cavia porcellus is tapped the head and causes dusk with blunt, get rapidly stomach, after taking out stomach, cut stomach bottom, cut off stomach along lesser gastric curvature and remove mucosa (cut-out ring muscle), at the stomach smooth muscle that is cut into 3mm along longitudinal muscle direction level crossing, one end of long 2cm specimen is fixed on L-type pipe portion hook, the other end is connected on tension pick-up, is placed in Tyrode ' s liquid, Tyrode ' s liquid composition (NaCl137mM, KCl2.7mM, CaCl
20.2mM, MgCl
20.1mM, NaH
2pO
20.05mM, NaHCO
31.0mM, glucose 1.0mM), pH7.4,37 DEG C of constant temperature, volume is 15ml, passes into and contains 95%O
2and 5%CO
2mist, predetermined tension is 1g, balance 1h records stomach, smooth muscle contraction amplitude by tension pick-up with balance recorder.Add in advance His1 × 10
-4mg/ml brings out Guinea pig Gastric contraction and reaches ceiling effect.Rinse after 3 times, add and be subject to reagent back balance 10min, then add isodose His, observe the stomach shrinkage curve adding after following each group of medicine.Experimental result is as shown in table 10:
The each extract of table 10. Rhizoma Zingiberis Recens brings out the antagonism of Guinea pig Gastric smooth muscle contraction to histamine phosphate
* * P < 0.01 compared with matched group, * P < 0.05.
2.3: to the antagonism experiment of Acetylcholine-induced Guinea pig Gastric smooth muscle contraction
Test is established six groups, matched group, 1 group of embodiment, 1 group of experimental example, 3 groups of experimental examples, 5 groups of experimental examples, 6 groups of experimental examples altogether.
Animal: 36 of Cavia porcelluss, 300～400 grams of body weight, ♀
dual-purpose.Every group 6.
Method: Cavia porcellus is tapped the head and causes dusk with blunt, get rapidly stomach, after taking out stomach, cut stomach bottom, cut off stomach along lesser gastric curvature and remove mucosa (cut-out ring muscle), at the stomach smooth muscle that is cut into 3mm along longitudinal muscle direction level crossing, one end of long 2cm specimen is fixed on L-type pipe portion hook, the other end is connected on tension pick-up, is placed in Tyrode ' s liquid, Tyrode ' s liquid composition (NaCl137mM, KCl2.7mM, CaCl
20.2mM, MgCl
20.1mM, NaH
2pO
20.05mM, NaHCO
31.0mM, glucose 1.0mM), pH7.4,37 DEG C of constant temperature, volume is 15ml, passes into and contains 95%O
2and 5%CO
2mist, predetermined tension is 1g, balance 1h records stomach, smooth muscle contraction amplitude by tension pick-up with balance recorder.Add in advance Ach1 × 10
-5mg/ml brings out Guinea pig Gastric contraction and reaches ceiling effect.Rinse after 3 times, add and be subject to reagent back balance 10min, then add isodose Ach, observe the stomach shrinkage curve adding after agonist.
The antagonism (drug dose be 0.18mg/ml) of the each extract of table 11. Rhizoma Zingiberis Recens to Acetylcholine-induced Guinea pig Gastric smooth muscle contraction
* * P < 0.01 compared with matched group, * P < 0.05.
The preventive effect experiment of Canis familiaris L. vomiting due to 2.4 pairs of morphine hydrochlorides:
Experimental animal: Hebei Province domesticated dog, body weight 13～17kg, male and female dual-purpose.
Dosage arranges and grouping
Test is established six groups, matched group, 1 group of embodiment, 1 group of experimental example, 3 groups of experimental examples, 5 groups of experimental examples, 6 groups of experimental examples altogether.Matched group gives 2ml/ Semen Maydis oil only, and all the other each group gives dosage is 0.36mg/kg.4 of every treated animal numbers.
Test method
Select the dog of relatively cooperating, and it is more responsive that subcutaneous injection morphine hydrochloride is caused to vomiting, interval 1 week can Reusability.Before experiment, fasting 18 hours, presses the weight of animals administration when test, and ginger phenols extract is filled in to the rear pharyngeal of dog, gives a small amount of beef simultaneously, allows animal take down voluntarily.After taking medicine, 30min starts subcutaneous injection morphine hydrochloride 0.1mg/kg.After injection, at once observe time started, vomiting number of times that abdomen (feeling sick), vomiting appear taking out in animal, be 30min observing time.Experimental result is as shown in table 12.
The preventive effect of table 12. Rhizoma Zingiberis Recens extract to Canis familiaris L. vomiting due to morphine hydrochloride
Claims (1)
1. a ginger phenols extract soft capsule with anti-dizzy emesis effect, is characterized in that, the formula of described soft capsule is: ginger phenols extract 600g, and Semen Maydis oil 5400g, gelatin 3600g, glycerol 1800g, water 3600g, makes 20000 of Jiang Su soft gelatin capsules; In described ginger phenols extract, the content of 6-gingerol is 28.12%, and the preparation method of described ginger phenols extract soft capsule is:
(1) extraction of ginger by supercritical carbon dioxide phenols extract: Rhizoma Zingiberis Recens is cut into 2～5mm thin slice, and 45 DEG C of aeration-drying to water content are less than 10%, pulverize 40 mesh sieves, obtain Rhizoma Zingiberis Recens powder; Pack Rhizoma Zingiberis Recens powder into supercritical CO
2in extraction equipment, be that 55 DEG C, pressure are 30Mpa, CO in temperature
2flow velocity is to extract under the condition of 10kg/h.kg raw material, and extraction time is 2 hours, and the separating still that is then 10Mpa in pressure is collected and obtained ginger phenols extract;
(2) solution preparation: the preparation of content solution: accurately take ginger phenols extract 600g, add medicinal Semen Maydis oil 5400g, fully stir and make whole dissolvings in 60 DEG C; Put common filter paper filtration under diminished pressure in buchner funnel, filtrate is filtered through G3 sintered glass funnel again, obtains clear and bright solution; The preparation of glue: by formulation weight, take gelatin, G & W, first G & W mixing post-heating to 70～80 DEG C, add gelatin by formula, stirs, and melting, is incubated 1～2 hour, leaves standstill, and after foam floating, removes, and filters heat preservation for standby use;
(3) soft gelatin capsule preparation: adopt the standby Jiang Su soft gelatin capsule of RJWJ-1 type soft capsule capsule mechanism processed; The soft gelatin capsule of making is spread out and put in tray, put into drying alley, at 20～30% relative humiditys, 21～24 DEG C of temperature, are dried under air blast condition, make glue shell water content in 6～10% scopes; Every ball soft gelatin capsule weighs 0.3 gram, includes 30mg ginger phenols extract.
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| CN105963705A (en) * | 2016-06-13 | 2016-09-28 | 湖北文理学院 | Compound stabilizer for preserving gingerol and use method of compound stabilizer |
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| CN1611240A (en) * | 2003-10-30 | 2005-05-04 | 苏少宁 | Fresh ginger soft capsule and its preparing method |
| CN1958057A (en) * | 2006-11-16 | 2007-05-09 | 南昌弘益科技有限公司 | Application of extractive of Daliangjiang, and application in medication |
| CN101347608A (en) * | 2008-09-01 | 2009-01-21 | 南京医科大学 | Chinese medicine soft capsules with cholagogic efficacy and preparation method thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN1611240A (en) * | 2003-10-30 | 2005-05-04 | 苏少宁 | Fresh ginger soft capsule and its preparing method |
| CN1958057A (en) * | 2006-11-16 | 2007-05-09 | 南昌弘益科技有限公司 | Application of extractive of Daliangjiang, and application in medication |
| CN101347608A (en) * | 2008-09-01 | 2009-01-21 | 南京医科大学 | Chinese medicine soft capsules with cholagogic efficacy and preparation method thereof |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105963705A (en) * | 2016-06-13 | 2016-09-28 | 湖北文理学院 | Compound stabilizer for preserving gingerol and use method of compound stabilizer |
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