CN103877274A - Chinese stellera root extract power injection - Google Patents
Chinese stellera root extract power injection Download PDFInfo
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Abstract
The invention relates to a Chinese stellera root extract power injection. The extract is prepared by adopting the following method comprising the steps of extracting a Chinese stellera root acetone and ethanol mixed solution, enabling the extract to pass through macroporous resin, and then carrying out gradient elution by the preparative chromatography, wherein a moving phase A is water, and a moving phase B is acetonitrile; collecting eluent in the time period of 10-15 minutes, concentrating and drying to obtain the extract.
Description
Technical field:
The present invention relates to a kind of anti-tumor Chinese medicine extract, the antineoplastic extract particularly extracting and extracting method thereof and purposes from Chinese medicine Stellera chamaejasme L..
Background technology:
Chinese crude drug Stellera chamaejasme L., English name: RADIX STELLERAE CHAMAEJASMES is the dry root of Isolated From Thymelaeaceae Species Stellera chamaejasme L..Excavate autumn, remove impurity, dry, medical material is spindle, taper shape or elongated cylindrical, slightly bending, single or have a branch, varying length, root head has aerial stem of plant vestiges, surface is brown to sepia, has the longitudinal furrow of distortion and hole skin and the lateral root trace of the protuberance that grows wild, and white flexible fibre is exposed in cork exfoliation.Body is light, and matter is tough, not frangibility, and it is fibrous that section is.Skin zone's off-white color, woody part is faint yellow.Feeble QI, taste is micro-pungent, and toxicity is more lower slightly than the Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae).
Its nature and flavor: pungent, temperature; Poisonous, function has cured mainly: heat-clearing and toxic substances removing, detumescence, rushes down inflammation, only ulcer, putrefaction-removing granulation-promoting.To Chemical Components in Stellera Chamaejasme L, analysis shows, the root of Stellera chamaejasme L. is containing sterol, phenolic constituent, aminoacid, triterpenes, anthracene glycoside, Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae) glycoside and poisonous polymeric organic acid.Containing Coumarins bergenin (pimpinelline), isopimpinellin (isopimpinelline), different Fructus Citri Sarcodactylis propyl ester (isobergapten), sphondin (sphondin), umbelliferone (umbelliferone, umbelliferone), daphnoritin.Also get multiple pair of hydrogen bisflavones chamaejasmine (chamaejasmine), 7-methyl chamaejasmine (7-methoxy chamaejasmin), chamaejasmine methyl-derivatives (chamaejasmenin A, B, C), Neochamaejovsmin A (+)-Neochamaejasmin A, B (neochamaejasmin A and B), Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae) chromone (chamaechromone), different chamaejasmine (isochamejasmin).
Stellera chamaejasme L. has following drug effect:
Antitumor action: zoopery shows that Stellera chamaejasme L. truly has certain inhibitory action to mice transplanted tumor, as its alcohol extract of lumbar injection or water extraction liquid are respectively 70.2% and 59.9% to Mice Bearing Lewis Lung Cancer tumour inhibiting rate; Water extract is 36.8% to rat liver cancer tumour inhibiting rate, to mouse cervical cancer 14 (U
14) cancer suppressing ratio be 48.5%; Volatile matter is 42.5% to hepatocarcinoma tumour inhibiting rate, be 50.5% to the tumour inhibiting rate of U14, its tumor killing effect and Herba Crotalariae sessiliflorae (40.2%), cantharidin (38.2%), fluorouracil (39.0%), vincristine (43.8%) etc. quite or slightly high, thereby think that this medical instrument has significant antitumaous effect.
Antibacterial action: the effective ingredient chamaejasmine of Stellera chamaejasme L. is an antibiotic property material, energy Antifungi, staphylococcus aureus and streptococcic growth.The Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae) has inhibitory action to 7 kinds of Gram-positive enteral pathogenic bacterium such as escherichia coli, sonne bacillus, Bacillus proteus, Bacillus typhi, Salmonella paratyphi, bacillus pyocyaneus and vibrio cholera in vitro.The water logging agent (1: 3) of the Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae) all has inhibitory action in various degree to dermatophytess such as yellow trichophyton, Trichophyton concentricunm, rust budlet spore tinea bacterium, oidium schoenleinii, the little sporeformer of Du Ang Shi difficult to understand, ulotrichy budlet spore tinea bacterium, epidermophyton inguinale, star nocardias in vitro.
Convulsion, antiepileptic action: Stellera chamaejasme L. finds to have antiepileptic activity, and its six kinds of crude extracts all have anticonvulsant action in various degree to many animals convulsion model, and wherein acetone extract antiepileptic action is stronger, and toxic and side effects is less.Experimental result shows that Stellera chamaejasme L. can effectively resist maximal electroshock convulsive attack, extends the convulsive attack incubation period that pentylenetetrazole brings out, and improves convulsions threshold value, can extend the time-to-live of convulsions mice simultaneously, reduces mortality rate; Sound source convulsive attack is also had to good antagonism; Also can obviously improve stimulation in rats motor cortex and bring out convulsions threshold value, further this medical instrument has anticonvulsant action certainly.Its anticonvulsant action mechanism is relevant with the interior amino acid neurotransmitter proportional imbalance of animal brain, also may be relevant with apoptosis etc.
To immune effect: the Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae) has very significantly inducing action to Epstein-Barr virus in Raji cell, and drug level is 1～100 μ g, and Epstein-Barr virus EA cell positive rate is 31.8%～52.0%; And can promote significantly Epstein-Barr virus to lymphocytic transformation.Also report and have the Stellera chamaejasme L. of activation the same with short cancer thing TPA to Epstein-Barr virus, can promote Adenovirus Type 5 to transform Mus blastocyte.Thereby prove that the Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae) not only has activation to Epstein-Barr virus, and adenovirus transformant is also had to facilitation.
Clinical research
Treatment tumor: by Stellera chamaejasme L. volatilize liquid, ethanol extract, water extract treatment malignant tumor 54 examples, wherein hepatocarcinoma 43 examples (II, III phase account for 94%), pulmonary carcinoma 6 examples, cervical cancer 1 example, carcinoma of corpus uteri 1 example, ovarian cancer 1 example, cancer of pancreas 1 example, brain colloid carcinoma 1 example.Result is alleviated 3 examples completely, partial rcsponse 9 examples, and effective 8 examples, improve 14 examples, and its objective effective percentage is 63%.Treatment tuberculosis: respond well with Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae) Fructus Jujubae, Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae) cream treatment tuberculosis, except pulmonary tuberculosis is not tried out energetically, the tuberculars such as other glands, bone, skin, epididymis, while declining as not yet crossed without severe complication and muscle power, can adhere to long-term treatment, can obtain satisfied recovery from illness or the effect alleviating, to Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae) cream therapy for tuberculosis of skin, more can accelerate to produce effects.
Treatment sciatica: Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae) medicated wine orally taken for curing sciatica 50 examples, pain relief after most of patient's medication 2d, effective percentage 90%.
Existing stellera chamaejasme L extract, extracting method has multiple, mainly comprises water extraction, alcohol extraction, ethyl acetate is carried, and acetone is carried, petroleum ether is carried, and methanol is carried etc., also comprise in all sorts of ways after extraction further separating extractive as: separate different active substances by different chromatographic columns.
Existing Stellera chamaejasme L. preparation comprises Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae) injection, Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae) solution (external), Radix Euphorbiae Fischerianae (Radix Euphorbiae Ebracteolatae) ointment etc., main active is ethanol extraction or water extract, because extraction process is simple, wherein contains a large amount of blending constituents, cause preparation side effect large, preparation stability is poor, unsatisfactory curative effect.
Adopt the high extract of purity, some is difficult to make suitable preparation, some poor stability, and some is insoluble in water, and bioavailability is not high.
The present invention is studied stellera chamaejasme L extract, find a kind of suitable extract, and find that unexpectedly it has antitumor action and antiinflammatory action concurrently, there is the prospect for the treatment of rheumatic or rheumatoid arthritis, for this reason, this extract is prepared into pharmaceutical preparation by the present invention, itself and other antitumor drug and anti-inflammatory drug combined to use simultaneously, there is the effect of the existing curative effect of medication of remarkable increase, play synergistic function.The present invention has also carried out the research of preparation aspect to extract of the present invention, found multiple operable dosage form comprise be applicable to part take, gastrointestinal tract is taken, and the dosage form that parenteral route is taken, for the modernization of Chinese medicine provides a kind of product having good prospects.
Summary of the invention:
The invention provides a kind of stellera chamaejasme L extract, described extract is prepared by following methods:
Step 1, Stellera chamaejasme L. is extracted with the mixed solution of acetone and ethanol, obtain extracting solution;
Step 2, reclaim solvent, concentrate drying obtains dry extract, gets macroporous resin and dry extract and mixes and mix sample; First use the mixed solution of ethanol and ethyl acetate as mobile phase eluting, then change ethanol as mobile phase, eluting obtains eluent, this eluent is reclaimed after ethanol to concentrate drying;
Step 3, sample is further carried out with preparative liquid chromatography gradient elution separation, collect different time flow out eluent,
Obtain extract.
Preferably, extract of the present invention, its preparation method is as follows,
Step 1, will after 1kg Stellera chamaejasme L. pulverizing medicinal materials, add 10L acetone: ethanol=2:1(v:v) mixed solution, reflux 1 hour, leach extracting solution, again add 10L acetone: ethanol=2:1(v:v) mixed solution, reflux 1 hour, leach extracting solution, merging filtrate obtains extracting solution;
Step 2, by merge after extracting solution decompression and solvent recovery, concentrate drying obtains dry extract 85g, gets HPD100 type macroporous resin 2kg, mixes and mixes sample with dry extract; First, adopting ethanol: ethyl acetate=1:1(v:v) 5L is as mobile phase eluting, then changes 95% ethanol 5L as mobile phase, and eluting obtains eluent, and this eluent is reclaimed after ethanol, and concentrate drying obtains 15g sample;
Step 3, the sample preparative liquid chromatography that step 2 is obtained further carry out gradient elution separation, collect the eluent that different time flows out, and obtain extract; Wherein, the chromatography eluant condition of gradient elution is: chromatographic column is preparative column YMC-PackPro C18; 30mm × 250mm, mobile phase A is water, and Mobile phase B is acetonitrile, and gradient elution program is as follows:
| Time (min) | Mobile phase A (%) | Mobile phase B (%) |
| 0 | 90 | 10 |
| 5 | 80 | 20 |
| 20 | 50 | 50 |
| 40 | 20 | 80 |
| 60 | 10 | 90 |
| 75 | 5 | 95 |
Flow velocity is 20ml/min, and column temperature is room temperature; Sample 95% dissolve with ethanol, gradient elution separation through preparative liquid chromatography, at time period 10-15 minute, 20-25 minute, 30-35 minute, 40-45 minute, 50-55 minute, within 60-65 minute, collect eluent, measure through HPLC, wherein the eluent of 10-15 minute has multiplet, and all the other are without peak, to wherein obtaining extract after the eluent concentrate drying of 10-15 minute, extract with 95% ethyl alcohol recrystallization once; Obtain pale yellow powder (hereinafter referred to as extract 1).
Carried out Pharmacodynamic screening for above extract 1, the selection result is as follows:
Hepatoma carcinoma cell HepG2, the BEL-7402 that experiment one, stellera chamaejasme L extract 1 are originated to people, the inhibitory action of SMMC-7721
The results are shown in Table 1.
Table 1 stellera chamaejasme L extract is external to the originate inhibiting IC of hepatoma carcinoma cell of people
50(unit: μ g/ml)
| Cell line | HepG-2 | SMMC-7721 | BEL-7402 |
| Blank group | ＞100 | ＞100 | ＞100 |
| Extract 1 | 58.6 | 39.2 | 66.8 |
Experiment two, the hepatoma carcinoma cell HL-60 tumor cell of stellera chamaejasme L extract 1 to people source, K562 tumor cell, the inhibitory action of MCF-7 tumor cell
The results are shown in Table 2.
Table 2 stellera chamaejasme L extract is external to HL-60 tumor cell, K562 tumor cell, the inhibitory action of MCF-7 tumor cell
Anti-inflammatory activity-mice auricle swelling method of experiment three, stellera chamaejasme L extract 1
The results are shown in Table 3.
The inhibitory action of table 3 stellera chamaejasme L extract gastric infusion to mice auricle swelling
Analgesic activities-acetic acid twisting method of experiment four, stellera chamaejasme L extract 1
The results are shown in Table 4.
The inhibitory action of table 4 stellera chamaejasme L extract gastric infusion to mouse writhing number of times
Extract 1 of the present invention has good anti-tumor activity through evidence above, has antiinflammatory action simultaneously:
For this reason, the present invention is further prepared into by extract 1 of the present invention the pharmaceutical composition that is applicable to taking.Pharmaceutical composition of the present invention, comprises active component (being extract 1 of the present invention), and said composition can also add medicine acceptable carrier as required.
Compositions of the present invention, is the pharmaceutical dosage forms of unit dose, and described unit dosage form refers to the unit of preparation, as every of tablet, and every capsules of capsule, every bottle of oral liquid, every bag of granule etc.
Compositions of the present invention active component wherein, its shared percentage by weight in preparation can be 0.01-99.99%, all the other are medicine acceptable carrier.
Compositions of the present invention, by being mixed with above-mentioned active component and medicine acceptable carrier to obtain.
Compositions of the present invention, its pharmaceutical dosage forms can be any pharmaceutically useful dosage form, and these dosage forms comprise: tablet, sugar coated tablet, film coated tablet, enteric coated tablet, capsule, hard capsule, soft capsule, oral liquid, suck agent, granule, electuary, pill, powder, unguentum, sublimed preparation, suspensoid, powder, solution, injection, suppository, ointment, plaster, cream, spray, drop, drop pill, patch.Preparation of the present invention, preferably peroral dosage form, as: capsule, tablet, oral liquid, granule, pill, powder, sublimed preparation, unguentum etc.
Compositions of the present invention, the preparation of its oral administration can contain conventional excipient, such as binding agent, filler, diluent, tablet agent, lubricant, disintegrating agent, coloring agent, flavoring agent and wetting agent, can carry out coating to tablet if desired.
Applicable filler comprises cellulose, mannitol, lactose and other similar filler.Suitable disintegrating agent comprises starch, polyvinylpyrrolidone and starch derivatives, for example sodium starch glycollate.Suitable lubricant comprises, for example magnesium stearate.The acceptable wetting agent of suitable medicine comprises sodium lauryl sulphate.
Can, by mixing, fill, the method that tabletting etc. are conventional is prepared solid oral composition.Repeatedly mix and can make active substance be distributed in those compositionss of a large amount of filleies of whole use.
The form of oral liquid can be for example aqueous or oily suspensions, solution, Emulsion, syrup or elixir, or can be a kind of available water before use or the composite dry products of other suitable carrier.This liquid preparation can contain conventional additive, such as suspending agent, for example sorbitol, syrup, methylcellulose, gelatin, hydroxyethyl-cellulose, carboxymethyl cellulose, aluminium stearate gel or hydrogenation edible fat, emulsifying agent, for example lecithin, anhydro sorbitol monooleate or arabic gum; Non-aqueous carrier (they can comprise edible oil), for example almond oil, fractionated coconut oil, such as oily ester, propylene glycol or the ethanol of the ester of glycerol; Antiseptic, for example para hydroxybenzene methyl ester or propyl p-hydroxybenzoate or sorbic acid, and if need, can contain conventional flavouring agent or coloring agent.
For injection, the liquid unit dosage forms of preparation contains active substance of the present invention and sterile carrier.According to carrier and concentration, this compound can be suspended or dissolve.The preparation of solution, normally by active substance being dissolved in a kind of carrier, being packed into filter-sterilized before a kind of suitable bottle or ampoule, then seals.Adjuvant for example a kind of local anesthetic, antiseptic and buffer agent also can be dissolved in this carrier.In order to improve its stability, can be by freezing this compositions after packing bottle into, and under vacuum, water is removed.
Compositions of the present invention, in the time being prepared into medicament, optionally add applicable medicine acceptable carrier, described medicine acceptable carrier is selected from: mannitol, sorbitol, sodium pyrosulfite, sodium sulfite, sodium thiosulfate, cysteine hydrochloride, TGA, methionine, vitamin C, EDETATE SODIUM, Ethylenediaminetetraacetic Acid Calcium Salt, the alkali-metal carbonate of monovalence, acetate, phosphate or its aqueous solution, hydrochloric acid, acetic acid, sulphuric acid, phosphoric acid, aminoacid, sodium chloride, potassium chloride, sodium lactate, xylitol, maltose, glucose, fructose, dextran, glycine, starch, sucrose, lactose, mannitol, silicon derivative, cellulose and derivant thereof, alginate, gelatin, polyvinylpyrrolidone, glycerol, POLYSORBATE 80, agar, calcium carbonate, calcium bicarbonate, surfactant, Polyethylene Glycol, cyclodextrin, beta-schardinger dextrin-, phospholipid material, Kaolin, Pulvis Talci, calcium stearate, magnesium stearate etc.
Compositions of the present invention is determined usage and dosage according to patient's situation in use, can take every day three times, each 1-20 agent, as: 1-20 bag or grain or sheet.
The present invention, as Chinese medicine extract, can combine use with existing antitumor drug and anti-inflammatory drug, and described existing medicine comprises Chinese patent medicine and chemical drugs, as is selected from following antitumor drug:
Cyclophosphamide, the card mustard that disappears, chlorambucil, lomustine, semustine, busulfan, Drogenil, hexamethylmelamine, mercaptopurine, fluorouracil, ftorafur, UFT, doxifluridine, hydroxyurea, etoposide, tamoxifen, aminoglutethimide, ondansetron.Ankangxin capsule,
fUFANG BANMAO JIAONANG, PINGXIAO JIA0NANG, precious balosam capsule, anticancer pill ball, capsule with pseudo-ginseng and Chinese fanpalm seed, the precious capsule of stilbene, the multiple recovery oral liquid of gold, Wei Mai Ning Capsule, HUISHENG KOUFUYE, Fufang Luxiancao granule, gan fu le, Fushengkang Capsule, Jinlong capsule, Auricularia Sophorae granule, Shenyi capsule, compound recipe wood chicken granule
As be selected from following anti-inflammatory drug:
Aspirin,
diclofenac, nimesulide, meloxicam, indomethacin, ibuprofen, diclofenac, naproxen, methotrexate, sulfasalazine, dexamethasone, leflunomide, oxychloroquine, chloroquine, auranofin, penicillamine, azathioprine, ciclosporin, cyclophosphamide, Mycophenolate mofetil.The celestial capsule of elder brother, Radix Paeoniae Alba total glucosides, seven taste Orally taken Bi-dredging liquid, blood stasis dispelling spirit, Tong Zhi Su Run Capsules, YISHEN JUANBI WAN, compound Nanxing pain paste, Radix Tripterygii Wilfordii total glycosides, ZHENGQINGFENGTONGNING.
The present invention finds, combines and uses the effect with the existing medicine of remarkable increase with extract 1 of the present invention and existing antitumor drug, plays synergistic function.
Relevant experiment is as follows:
Experiment 1, mice H22 hepatoma model
Table 5 stellera chamaejasme L extract 1 and the impact of fluorouracil use in conjunction gastric infusion on subcutaneous transplantation tumor H22
The present invention finds, combines and uses the effect with the existing medicine of remarkable increase with extract 1 of the present invention and existing anti-inflammatory drug, plays synergistic function.
Relevant experiment is as follows:
Experiment 2, rat carrageenan foot swelling model
Table 6 stellera chamaejasme L extract 1 and dexamethasone use in conjunction gastric infusion are to paw swelling comparison due to the anti-carrageenin of the different time points of rat
| Grouping | Cause scorching rear right foot volume (120 minutes) ml |
| Blank group | 0.65 |
| Model group | 1.13 |
| 1 group of extract (10mg/kg) | 0.95 |
| Dexamethasone group (1mg/kg) | 0.86 |
| Extract 1 (10mg/kg)+Dexamethasone group (1mg/kg) | 0.73 |
Beneficial effect of the present invention is:
By the research of Stellera chamaejasme L. extracting method, find unexpectedly extract of the present invention, through measuring, products therefrom is stable, has good pharmacologically active, is applicable to being prepared into oral formulations.The present invention obtains the active component of given activity first from medical material, and is used in first in the treatment of inflammation, because activity is good, is suitablely developed to new new Chinese medicine, for the treatment of rheumatism or rheumatoid arthritis and other inflammation.
The specific embodiment:
Further illustrate by the following examples the present invention.
Embodiment 1
The preparation of stellera chamaejasme L extract 1:
A kind of stellera chamaejasme L extract, is characterized in that, is to be prepared by following methods:
Step 1, will after 1kg Stellera chamaejasme L. pulverizing medicinal materials, add 10L acetone: ethanol=2:1(v:v) mixed solution, reflux 1 hour, leach extracting solution, again add 10L acetone: ethanol=2:1(v:v) mixed solution, reflux 1 hour, leach extracting solution, merging filtrate obtains extracting solution;
Step 2, by merge after extracting solution decompression and solvent recovery, concentrate drying obtains dry extract 85g, gets HPD100 type macroporous resin 2kg, mixes and mixes sample with dry extract; First, adopting ethanol: ethyl acetate=1:1(v:v) 5L is as mobile phase eluting, then changes 95% ethanol (v:v) 5L as mobile phase, and eluting obtains eluent, and this eluent is reclaimed after ethanol, and concentrate drying obtains 15g sample;
Step 3, the sample preparative liquid chromatography that step 2 is obtained further carry out gradient elution separation, collect the eluent that different time flows out, and obtain extract; Wherein, the chromatography eluant condition of gradient elution is: chromatographic column is preparative column YMC-Pack Pro C18; 30mm × 250mm, mobile phase A is water, and Mobile phase B is acetonitrile, and gradient elution program is as follows:
| Time (min) | Mobile phase A (%) | Mobile phase B (%) |
| 0 | 90 | 10 |
| 5 | 80 | 20 |
| 20 | 50 | 50 |
| 40 | 20 | 80 |
| 60 | 10 | 90 |
| 75 | 5 | 95 |
Flow velocity is 20ml/min, and column temperature is room temperature; Sample 95% dissolve with ethanol, gradient elution separation through preparative liquid chromatography, time period 10-15 minute collect eluent, this eluent obtains extract 390mg after concentrate drying, with 95% ethanol (v:v) recrystallization once; Obtain pale yellow powder 350mg.(being extract 1 of the present invention).
Embodiment 2
The preparation of tablet
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, starch 200mg, Icing Sugar 100mg, magnesium stearate is appropriate,,, granulates through mixing as binding agent with gelatinized corn starch, air-dry, granulate, tabletting, obtains tablet.
Tablet stability experiment:
Tablet prepared by 100mg extract 1 and said method is placed in 40 ℃ of incubators, after 3 months, observes, and its outward appearance, there is not any variation in color.
Embodiment 3
The preparation of sugar coated tablet
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, starch 200mg, Icing Sugar 100mg, magnesium stearate is appropriate,,, granulates through mixing as binding agent with gelatinized corn starch, air-dry, granulate, tabletting, obtains tablet, obtains coated tablet with syrup coat.
Embodiment 4
The preparation of film coated tablet
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, starch 200mg, Icing Sugar 100mg, magnesium stearate is appropriate,,, granulates through mixing as binding agent with gelatinized corn starch, air-dry, granulate, tabletting, obtains tablet., obtain as coating material film coating with hydroxypropyl cellulose.
Embodiment 5
The preparation of enteric coated tablet
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, starch 200mg, Icing Sugar 100mg, magnesium stearate is appropriate,,, granulates through mixing as binding agent with gelatinized corn starch, air-dry, granulate, tabletting, obtains tablet., obtain as coating material film coating with enteric solubility acrylic resin.
Embodiment 6
The preparation of hard capsule
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, starch 200mg, Icing Sugar 100mg, magnesium stearate is appropriate,,, granulates through mixing as binding agent with gelatinized corn starch, air-dry, and granulate is encapsulated.
Embodiment 7
The preparation of soft capsule
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, soybean oil 100mg, Polyethylene Glycol 100mg, makes softgel shell with gelatin, is prepared into soft capsule.
Embodiment 8
The preparation of oral liquid
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, glycerol 50mg, sucrose 100mg, essence is appropriate, and water is added to 10ml.
Embodiment 9
The preparation of granule
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, dextrin 200mg, Icing Sugar 100mg, water, as binding agent, mixes, and granulates, air-dry, granulate, packing.
Embodiment 10
The preparation of pill
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, adds sodium carboxymethyl cellulose 200mg, is mixed evenly, and general pill, dry, make 1000 balls, film coating, to obtain final product.
Embodiment 11
The preparation of ointment
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, adds azone and vaseline appropriate, is prepared into ointment,
Embodiment 12
The preparation of injectable powder
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, mannitol 100mg, mix homogeneously.
Embodiment 13
The preparation of buccal tablet
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
1g extract 1, trehalose 6g, glycine 5g, xylitol 44g, sodium carboxymethyl cellulose 8g, erythritol 34gg jelly powder 2g, magnesium stearate 1g.With 50% ethanol soft material processed, granulate, air-dry, granulate, tabletting, packing.
Embodiment 14
The preparation of dry suspension
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10g extract 1, hydroxypropyl methylcellulose 100g, microcrystalline Cellulose 200g, sucrose 200g, mixes: with 50% ethanol soft material processed, granulate, air-dry, granulate, packing.
Embodiment 15
The preparation of suppository
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10g extract 1, cocoa butter 600g, melting substrate, adds medicine, mixes, and injection molding, cooling, scraping, taking-up, to obtain final product.
Embodiment 16
The preparation of ointment
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, adds azone, and water and hexadecanol are appropriate, are prepared into ointment,
Embodiment 17
The preparation of drop pill
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
5g extract 1,60g polyethylene glycol 6000,
Get extract 1, add in the polyethylene glycol 6000 of melting and mix, temperature is 60-90 ℃, after melting and stirring, moves in the drip irrigation of pill dripping machine (insulation 70-90 ℃), splash in the liquid Paraffin or methyl-silicone oil of 5-17 ℃, take out drop pill, remove liquid Paraffin or methyl-silicone oil, wash ball, dry, make drop pill 1000 balls.
Embodiment 18
The preparation of oral cavity disintegration tablet
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
5g extract 1, microcrystalline Cellulose (PH101) 350g, aspartame 40g, vitamin C 1g, low-substituted hydroxypropyl cellulose 40g, sodium lauryl sulphate 2.0g, Pulvis Talci 2.0g, magnesium stearate 1.5g, water, as binding agent, mixes, granulate, air-dry, granulate, tabletting.
Embodiment 19
The preparation of dispersible tablet
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
5g extract 1, lactose 18g, pregelatinized Starch 25g, microcrystalline Cellulose 35g, low-substituted hydroxypropyl cellulose 7g, polyvinylpyrrolidone 6g, micropowder silica gel 1g. water, as binding agent, mixes, and granulates, air-dry, granulate, tabletting.
Embodiment 20
The preparation of enteric coated capsule
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 2, starch 200mg, Icing Sugar 100mg, magnesium stearate is appropriate,,, granulates through mixing as binding agent with gelatinized corn starch, and air-dry, granulate, packs enteric capsule shell into.
Embodiment 21
The preparation of sugar free granule
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1 steviosin 4mg dextrin 440mg.Get extract 1, dextrin, steviosin and mix, add 95% ethanol and make soft material, 14 eye mesh screens are granulated, 50～55 ℃ of oven dry, and 12 order granulate, subpackage, to obtain final product.
Embodiment 22
The preparation of effervescent tablet
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, tartaric acid 150mg, pregelatinized Starch 105mg, sodium bicarbonate 110mg, PVPk3036mg, magnesium stearate 4.5mg, micropowder silica gel, 15mg, water, as binding agent, mixes, and granulates, air-dry, granulate, tabletting.
Embodiment 23
The preparation of floating in stomach sheet
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, lactose 10mg, hydroxypropyl cellulose 150mg, polyacrylic resin Ⅱ 30mg, sodium bicarbonate 50mg, HPMC30mg, octadecanol 30mg, sodium lauryl sulphate 5mg, micropowder silica gel 1mg, water is as binding agent, mix, granulate, air-dry, granulate, tabletting.
Embodiment 24
The preparation of gel
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
5g extract 1, hydroxypropyl methylcellulose 8.0g, Acritamer 940 2.5g, propylene glycol 160g, methyl hydroxybenzoate 0.15g, sodium hydroxide is appropriate, and water is added to 1000g.
Embodiment 25
The preparation of patch
The extract that embodiment 1 obtains, as active constituents of medicine, adds pharmaceutical carrier, prepares according to galenic pharmacy routine techniques, as following preparation method:
10mg extract 1, polyacrylic resin 60mg, ethyl acetate 30mg.By medicine and adjuvant mix homogeneously, be coated with into certain thickness, at the scope inner drying of 50 ℃-150 ℃, after suitable viscosity, be combined with each other with backing protective layer and antiseized protective layer, be die-cut into 10cm
2square, obtain patch.
Claims (1)
1. a stellera chamaejasme L extract injectable powder, is characterized in that, by the preparation of stellera chamaejasme L extract and pharmaceutical carrier
Become, described stellera chamaejasme L extract is to be prepared by following methods:
Step 1, will after 1kg Stellera chamaejasme L. pulverizing medicinal materials, add the mixed solution of 10L acetone: ethanol=2:1, reflux 1 hour, leaches extracting solution, again add the mixed solution of 10L acetone: ethanol=2:1, reflux 1 hour, leaches extracting solution, and merging filtrate obtains extracting solution;
Step 2, by merge after extracting solution decompression and solvent recovery, concentrate drying obtains dry extract 85g, gets HPD100 type macroporous resin 2kg, mixes and mixes sample with dry extract; First, adopt ethanol: ethyl acetate=1:15L as mobile phase eluting, then change 95% ethanol 5L as mobile phase, eluting obtains eluent, and this eluent is reclaimed after ethanol, and concentrate drying obtains 15g sample;
Step 3, the sample preparative liquid chromatography that step 2 is obtained further carry out gradient elution separation, collect the eluent that different time flows out, and obtain extract; Wherein, the chromatography eluant condition of gradient elution is: chromatographic column is preparative column YMC-PackPro C18; 30mm × 250mm, mobile phase A is water, and Mobile phase B is acetonitrile, and gradient elution program is as follows:
Flow velocity is 20ml/min, and column temperature is room temperature; Sample 95% dissolve with ethanol, gradient elution separation through preparative liquid chromatography, time period 10-15 minute collect eluent, this eluent obtains extract 390mg after concentrate drying, with 95% ethyl alcohol recrystallization once; Obtain pale yellow powder 350mg.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410127894.0A CN103877274A (en) | 2014-03-31 | 2014-03-31 | Chinese stellera root extract power injection |
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| Application Number | Priority Date | Filing Date | Title |
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| CN201410127894.0A CN103877274A (en) | 2014-03-31 | 2014-03-31 | Chinese stellera root extract power injection |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN110960599A (en) * | 2019-12-31 | 2020-04-07 | 西安交通大学医学院第二附属医院 | Method for extracting total alkaloids of stellera chamaejasme and application thereof |
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| CN110960599A (en) * | 2019-12-31 | 2020-04-07 | 西安交通大学医学院第二附属医院 | Method for extracting total alkaloids of stellera chamaejasme and application thereof |
| CN110960599B (en) * | 2019-12-31 | 2023-11-07 | 西安交通大学医学院第二附属医院 | Extraction method and application of stellera chamaejasme total alkaloids |
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Application publication date: 20140625 |