CN105997848A - Tangut anisodus radix and musk gel and preparation method thereof - Google Patents
Tangut anisodus radix and musk gel and preparation method thereof Download PDFInfo
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- CN105997848A CN105997848A CN201610510544.1A CN201610510544A CN105997848A CN 105997848 A CN105997848 A CN 105997848A CN 201610510544 A CN201610510544 A CN 201610510544A CN 105997848 A CN105997848 A CN 105997848A
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- gel
- musk
- extract
- anisodamine
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- A61K36/32—Burseraceae (Frankincense family)
- A61K36/324—Boswellia, e.g. frankincense
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- A61K36/185—Magnoliopsida (dicotyledons)
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Abstract
The invention relates to a tangut anisodus radix and musk gel and a preparation method thereof, and belongs to the technical field of gels. The tangut anisodus radix and musk gel is prepared from the following raw materials in parts by weight: 50 to 70 parts of Daphne tangutica Maxim, 6 to 10 parts of tangut anisodus radix, 2 to 6 parts of dried ginger, 1 to 3 parts of frankincense, 1 to 3 parts of myrrh, 1 to 3 parts of borneol, 1 to 3 parts of camphor, 8 to 13 parts of methyl salicylate, 0.01 to 0.25 part of musk, 3 to 9 parts of matrix, 0.2 to 3.6 parts of azone, 2 to 6 parts of moisturizer, and 12 to 117 parts of solvent. The preparation method of the tangut anisodus radix and musk gel comprises the steps of preparing an extract, medicinal powder and a gel. The tangut anisodus radix and musk gel provided by the invention has the advantages of high percutaneous penetration rate, high bioavailability, and relatively good pharmacological effects.
Description
Technical field
The present invention relates to anisodamine-musk gel and preparation method thereof, belong to gel technical field.
Background technology
Joint disease has a strong impact on human health, reduces quality of life, and general Therapeutic Method is difficult to cure, therefore
The Global Health theme of 2000 ~ 2010 years is defined as " B&J 10 years " by World Health Organization (WHO) especially.Arthritis is one
Plant chronic disease, have the title of " No.1 disabling disease ".Arthritic kind is more than 100 kinds, and modal arthritis is bone joint
Inflammation and rheumatoid arthritis.The whole world has 3.55 hundred million arthritics scorching.Updated statistics shows, the arthritic of China
More than 100,000,000 people.Existing treatment arthrosis method, doctor trained in Western medicine is frequently with oral non-steroidal anti-inflammatory class antipyretic analgesic or operation
Therapy.Oral drugs side effect is many;The operative treatment cycle is long, costly, painful big, and preferably recurs.Chinese medicine is in treatment joint
Disease aspect, unique advantage, extract oral, external application, fumigation and wash method, acupuncture, sunburn treatment etc. have positive effect.Chinese medicine " inner disease outer treat "
Theoretical with a long history, have accumulated a large amount of good recipe, proved recipe, but external therapy of Chinese herb medicine generally exists dosage form and falls behind, dosage is big, uses not
The shortcoming such as just, as used the plaster of the traditional Chinese medical science, airtight due to it, also can be irritating to the skin, the untoward reaction such as allergy, therefore profit
Evident in efficacy persistently with Modern preparations technological development, Chinese medicine for outer use easy to use become the modernization of Chinese medicine one is important
Problem.
Applicant finds under study for action, although there is the report for anisodamine-musk preparation in prior art, but in system
Agent aspect has following defects that existing anisodamine-musk preparation mostly is rubber plaster and the oral formulations of external patch lamellar, external
The rubber plaster of paster shape easily stimulates skin, causes anaphylaxis, and during oral formulations long-term taking, side effect is bigger;When using it instead
During his dosage form, owing to dosage form changes, ingredient there occurs change, is easily caused under the bioavailability of anisodamine-musk preparation
Fall, drug effect are not stable in performance.At present, skin good penetrability the least in the urgent need to a kind of side effect, lasting release medicine can be stablized
Anisodamine-musk preparation.
Summary of the invention
The technical problem to be solved in the present invention is: overcome the deficiencies in the prior art, it is provided that anisodamine-musk gel and
Preparation method, the transdermal penetration rates of this anisodamine-musk gel is high, bioavailability is high, has preferable pharmacological action.
The technical solution adopted for the present invention to solve the technical problems is: this anisodamine-musk gel, it is characterised in that
Raw material including following weight portion: Tang Gute winter daphne 50 ~ 70 parts, Radix Anisodi Tangutici 6 ~ 10 parts, Rhizoma Zingiberis 2 ~ 6 parts, Olibanum 1 ~ 3 part, Myrrha
1 ~ 3 part, Borneolum Syntheticum 1 ~ 3 part, Camphora 1 ~ 3 part, methyl salicylate 8 ~ 13 parts, 0.01 ~ 0.25 part of Moschus, substrate 3 ~ 9 parts, azone
0.2 ~ 3.6 part, wetting agent 2 ~ 6 parts, solvent 18 ~ 144 parts.
This anisodamine-musk gel, it is characterised in that include the raw material of following weight portion: Tang Gute winter daphne 60 ~ 70 parts,
Radix Anisodi Tangutici 7 ~ 9 parts, Rhizoma Zingiberis 3 ~ 4 parts, Olibanum 1.5 ~ 3 parts, Myrrha 1.5 ~ 3 parts, Borneolum Syntheticum 1.5 ~ 3 parts, Camphora 1 ~ 2 part, salicylic acid first
Ester 9 ~ 11 parts, 0.02 ~ 0.2 part of Moschus, substrate 4 ~ 7.5 parts, azone 0.4 ~ 2.5 part, wetting agent 3 ~ 5 parts, solvent 36 ~ 90 parts.
Described wetting agent is that two or three in glycerol, Polyethylene Glycol, propylene glycol is mixed by any mass ratio, described
Solvent be water.
Described substrate is by polyacrylamide, sodium polyacrylate, methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl first
Any one in base cellulose, tragcanth, xanthan gum, alginic acid, forms with polyvinyl alcohol and carbomer.
Described substrate is by polyvinyl alcohol, carbomer and sodium polyacrylate 0.5 ~ 2:0.5 in mass ratio ~ 2:0.5 ~ 2 group
Become.
Described raw material also includes Radix Lamiophlomidis Rotatae 5 ~ 12 parts.
The preparation method of above-described anisodamine-musk gel, it is characterised in that: include preparing extractum, preparing medicated powder
With prepare gel step;
The concrete operations preparing extractum step are: weigh Tang Gute winter daphne, Radix Anisodi Tangutici and Rhizoma Zingiberis by weight, through mixing, pulverizing,
Boiling 2 ~ 3 times, decocts 1 ~ 2 hour used time every time, merges decoction liquor, is concentrated into runny plaste shape, adds the second of 85 ~ 95v/v%
Alcoholic solution mixed extraction, filters and concentrated filtrate, is dried to obtain extract powder;
The concrete operations preparing medicated powder step are: Moschus, Myrrha, Olibanum, Borneolum Syntheticum, Camphora and methyl salicylate finely ground mistake respectively
100 ~ 200 mesh sieves, after mix homogeneously, obtain medicated powder;
The concrete operations preparing gel step are: mixed powder and wetting agent by weight, prepare medicated powder dispersion liquid;By substrate
With solvent mixing, swelling, it is thus achieved that swelling solution, swelling solution is mixed with extract powder and transdermal enhancer, it is thus achieved that extract dispersion liquid;Will
Extract dispersion liquid mixes with medicated powder dispersion liquid, stirs and i.e. obtains anisodamine-musk gel.
Preferably, the concrete operations preparing gel step are: mixed powder and wetting agent by weight, and prepared medicated powder divides
Dissipate liquid;By swelling for polyvinyl alcohol solubilizer 22 ~ 26 hours, it is thus achieved that the first swelling solution;By swelling for carbomer solubilizer 22 ~ 26 little
Time, add polyacrylamide, sodium polyacrylate, methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl methyl cellulose, Calculus Bovis from Northwest of China
Over sixty years of age glue, xanthan gum, any one in alginic acid, stir acquisition the second swelling solution;Extractum and transdermal enhancer are added
First swelling solution stirs evenly, adds the second swelling solution and stir evenly, it is thus achieved that extract dispersion liquid;By extract dispersion liquid and medicated powder dispersion liquid
Mixing, stirs and i.e. obtains anisodamine-musk gel.
Preferably, the concrete operations preparing gel step are: mixed powder and wetting agent by weight, and prepared medicated powder divides
Dissipate liquid;By each for substrate component mix homogeneously, add solvent mixing, swelling 22 ~ 26 hours, it is thus achieved that swelling solution, swelling solution is divided into
Etc. 2 ~ 3 parts of quality, use and add 1 part every time and stir the mode of mixing, divide 2 ~ 3 times and swelling solution is added extractum and transdermal rush
In the mixture of penetration enhancer, it is thus achieved that extract dispersion liquid;Extract dispersion liquid is mixed with medicated powder dispersion liquid, stirs and i.e. obtain Radix Anisodi Tangutici
Moschus gel.
When raw material is added with Radix Lamiophlomidis Rotatae, the preparation method of anisodamine-musk gel, it is characterised in that: include preparation
Extractum, prepare medicated powder and prepare gel step;
The described concrete operations preparing extractum step are: by Radix Lamiophlomidis Rotatae 42 ~ 95 v/v% ethanol solution reflux, extract, 2 ~ 3 times,
Extract 2 ~ 3 hours every time, merge ethanol extract, concentrating under reduced pressure, vacuum drying, obtain Radix Lamiophlomidis Rotatae extract;Weigh by weight
Tang Gute winter daphne, Radix Anisodi Tangutici, Rhizoma Zingiberis and Radix Lamiophlomidis Rotatae, through mixing, pulverize, boiling 2 ~ 3 times, decoct 1 ~ 2 hour used time every time,
Merge decoction liquor, be concentrated into runny plaste shape, add the ethanol solution mixed extraction of 85 ~ 95 v/v %, filter and concentrated filtrate, add
Radix Lamiophlomidis Rotatae extract mixes, and is dried to obtain extract powder;
The concrete operations preparing medicated powder step are: Moschus, Myrrha, Olibanum, Borneolum Syntheticum, Camphora and methyl salicylate finely ground mistake respectively
100 ~ 200 mesh sieves, after mix homogeneously, obtain medicated powder;
The concrete operations preparing gel step are: mixed powder and wetting agent by weight, prepare medicated powder dispersion liquid;By substrate
With solvent mixing, swelling 22 ~ 26 hours, it is thus achieved that swelling solution, swelling solution is mixed with extract powder and transdermal enhancer, it is thus achieved that extractum
Dispersion liquid;Extract dispersion liquid is mixed with medicated powder dispersion liquid, stirs and i.e. obtain anisodamine-musk gel.
Applicant is described as follows for inventive formulation:
Tang Gute winter daphne, pungent, bitter, temperature.Poisonous.Expelling wind and removing dampness, eliminating stasis to stop pain.For syphilitic rhinitis, primary sore, osteodynia and joint
Chamber hydrops.
Radix Anisodi Tangutici, bitter, pungent, temperature.Very toxic.Function cures mainly: analgesia spasmolytic, blood circulation and promoting silt, hemostasia and promoting granulation.For ulcer
Disease, acute and chronic gastroenteritis, gastrointestinal function of nervous system disease, ascariasis of biliary tract, cholelithiasis, traumatic injury, fracture, traumatic hemorrhage.
Rhizoma Zingiberis, pungent, hot.Return spleen, stomach, kidney, the heart, lung meridian.Function cures mainly: Rhizoma Zingiberis warming spleen and stomach for dispelling cold, and recuperating depleted YANG is promoted blood circulation, and dampness disappears
Expectorant.For coldness and pain in the epigastrium, vomiting is had loose bowels, cold extremities faint pulse, and phlegm retention is breathed with cough.
Olibanum, property is worked hard, warm.Enter the heart, liver, spleen channel.Function: regulating qi and activating blood, analgesic therapy, chase after poison.Cure mainly: coagulation of QI-blood, the heart
Abdomen pain, ulcerative carbuncle toxic swelling, traumatic injury, dysmenorrhea, postnatal blood stasis twinge.
Myrrha, property is bitter, flat.GUIXIN, liver, spleen channel.Function is for dissipating blood and relieving pain, detumescence and promoting granulation.For ulcer sore pain, trusted subordinate,
The all pains of muscles and bones, traumatic blood stasis, external can expelling pus and promoting granulation.Promoting blood circulation to remove blood stasis eases pain.External has convergence and antiinflammation.In addition Myrrha pair
Various skin tinea bacterium has inhibitory action in various degree.
Borneolum Syntheticum, pungent, bitter, it is slightly cold.GUIXIN, spleen, lung meridian.Function cures mainly: refreshment of having one's ideas straightened out, clearing away heat to alleviate pain.For calentura coma,
Convulsion is fainted, apoplexy syncope due to accumulation of phlegm, stagnation of QI sudden syncope, and attacked by pestiferous factors is gone into a coma, and conjunctival congestion, aphtha, laryngopharynx swelling and pain, auditory meatus is suppurated.
Camphora, pungent, temperature.Function cures mainly: sensible ward off dirty, warming middle-JIAO to relieve pain, dampness removing parasite killing.Vomit and diarrhoea for cold-damp, stomach abdomen pain;
Scabies is controlled in external, tinea, dental caries are had a pain.
Methyl salicylate, colourless oil liquid, there is Folium Ilicis Purpureae fragrance.Slightly soluble in water, can be with volatile oil, fatty oil
Arbitrarily mixing.Function cures mainly: can promote local blood circulation, has antiinflammatory and analgesic activity.
Moschus, pungent, temperature.GUIXIN, spleen channel.Function cures mainly: refreshment of having one's ideas straightened out, promoting blood circulation to restore menstrual flow, reducing swelling and alleviating pain.For calentura god
Dusk, apoplexy syncope due to accumulation of phlegm, stagnation of QI sudden syncope, attacked by pestiferous factors stupor, amenorrhea, abdominal mass, stillborn fetus of having difficult labour, trusted subordinate's sudden pain, carbuncle scrofula, laryngopharynx swelling and pain,
Falling and flutter the pain of injury, arthralgia pain is numb.
Radix Lamiophlomidis Rotatae, bitter, it is slightly cold.Slightly poisonous.Function cures mainly: blood circulation promoting and blood stasis dispelling, reducing swelling and alleviating pain.For traumatic injury, fracture, waist
Portion sprains.
The form of medication of gel made by anisodamine-musk preparation by applicant in the present invention.Gel is that a class contains two
More than component or two components, by solid-liquid two phase composition, there is semi-solid property macromolecular network system.Inventive gel agent
Can by medicine dissolution or be dispersed in gel, and can the long period with site of action tight adhesion, have preferably
Biocompatibility, preparation method is simple, uses comfortable.Further, the hydrated gel layer formed after inventive gel agent water absorption and swelling is right
Medicine has the effect controlling rate of release, has prolongation antiinflammatory, the effect of analgesic onset time.The anisodamine-musk of the present invention
Gel can percutaneous or mucosa delivery, for controlling of many-sided especially arthritis disease such as antiinflammatory, pain relieving, local hemorrhage
Treating, instant effect and zest are little, are difficult to cause anaphylaxis.
Applicant finds under study for action: although disclosing the formula at anisodamine-musk in prior art, but its component and
Consumption adds unreasonable, it is impossible to play optimal drug effect.First, it is found by the applicant that work as and add Tang Gute winter daphne 60 ~ 70 parts, mountain
Hyoscyami 7 ~ 9 parts, Rhizoma Zingiberis 3 ~ 4 parts, Olibanum 1.5 ~ 3 parts, Myrrha 1.5 ~ 3 parts, Borneolum Syntheticum 1.5 ~ 3 parts, Camphora 1 ~ 2 part, methyl salicylate
9 ~ 11 parts, 0.02 ~ 0.2 part of Moschus, substrate 4 ~ 7.5 parts, azone 0.4 ~ 2.5 part, wetting agent 3 ~ 5 parts, solvent 36 ~ 90 parts.Part
Time, the analgesic effect performance of gained gel is preferably.It is further preferred that include the raw material of following weight portion: Tang Gute winter daphne
66 ~ 70 parts, Radix Anisodi Tangutici 7.5 ~ 8 parts, Rhizoma Zingiberis 3 ~ 3.5 parts, Olibanum 2 ~ 2.5 parts, Myrrha 2 ~ 2.5 parts, Borneolum Syntheticum 1.5 ~ 2 parts, Camphora 1
~ 1.5 parts, methyl salicylate 10 ~ 10.5 parts, 0.05 ~ 0.1 part of Moschus, substrate 4 ~ 6 parts, azone 0.4 ~ 2 part and wetting agent 4 ~ 5
Part, solvent 36 ~ 72 parts, during this consumption, analgesic effect is preferable, and relatively small to the zest of skin.Secondly, applicant sets
Meter with the addition of Radix Lamiophlomidis Rotatae in formula, and Radix Lamiophlomidis Rotatae can improve work further with Tang Gute winter daphne, Rhizoma Zingiberis, Olibanum, Moschus combination
Blood and dissolving stasis, the effect of analgesia detumescence, have the collaborative effect strengthening drug effect.Preferably consumption is: Radix Lamiophlomidis Rotatae 9 ~ 11 parts, and adding should
During consumption, the raising of analgesic effect is the most obvious.
It addition, also use water and ethanol preparing extractum step in medicated powder step with preparing, this water and ethanol volatilization dissipate
Lose, be not present in the anisodamine-musk gel finally obtained, and consumption changes final gained anisodamine-musk gel
The drug effect impact of agent is inconspicuous.The ethanol preparing extractum step and prepare different volumes specific concentration used in medicated powder step is molten
Liquid, those skilled in the art can allocate the most voluntarily.The solvent prepared in gel step is ultimately present in Radix Anisodi Tangutici
In Moschus gel, it is preferred that solvent is distilled water, belongs to commercially available prod.
Preferably, the mass percent shared by anisodamine-musk gel mesostroma of final gained is 0.5 ~ 7%, azone
Content be 0.4 ~ 2.5%.Preferably, the mass percent shared by anisodamine-musk gel mesostroma of final gained be 4 ~
6%, the content of azone is 0.5 ~ 2%.
Applicant uses azone as transdermal enhancer in the present invention, is owing to applicant finds through numerous studies: solidifying
Medicine contained in colloid has selectivity for transdermal enhancer, in the present invention, uses azone as transdermal enhancer energy
Enough play optimal mechanism.Azone is a kind of nonpolar penetration enhancer, and its sphere of action is wide, no color or smell, and zest is low, right
Hydrophilic and oleophilic type medicine all has the saturating effect of rush.Applicant studies discovery Borneolum Syntheticum and has collaborative enhancing drug transdermal effect with azone,
Owing to containing Borneolum Syntheticum in raw material of the present invention, therefore this test is with the skin permeation rate of the effective ingredient daphnetin of Tang Gute winter daphne for referring to
Mark, selection azone is as transdermal enhancer, and its consumption has been carried out further investigation.It is found by the applicant that: work as anisodamine-musk
During gel external coating, in anisodamine-musk gel, the content of azone has considerable influence to the permeability of medicine.Through grinding
Studying carefully confirmation, when the weight portion shared by transdermal enhancer is 1 ~ 3.6, its mechanism is optimal, more or less than the equal nothing of this consumption
Method reaches optimal mechanism.
Applicant have selected specific composition in the present invention as substrate.Preferably, substrate is polyvinyl alcohol, carbomer
With polyacrylamide, sodium polyacrylate, methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl methyl cellulose, tragcanth,
Any one in xanthan gum, alginic acid, three is mixed by any mass ratio.As gel after polyvinyl alcohol, carbomer are swelling
The support frame that agent is main, and add polyacrylamide, sodium polyacrylate, methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl
Any one in methylcellulose, tragcanth, xanthan gum, alginic acid, forms form stable, slow release effect excellent
Pluralgel substrate.Preferably, substrate is by polyvinyl alcohol, carbomer and sodium polyacrylate 1 ~ 2:1 in mass ratio ~ 2:0.5 ~ 1
Composition.Use polyvinyl alcohol, carbomer and sodium polyacrylate collocation use can form preferable slow-releasing system, extend drug effect
The performance time.Preferably, substrate is made up of polyvinyl alcohol, carbomer and sodium polyacrylate 1:1:0.5 in mass ratio, this quality
Ratio lower slow release effect performance optimum, can effectively extend analgesia time.
It is that two or three in glycerol, Polyethylene Glycol, propylene glycol is by arbitrarily that applicant designs wetting agent in the present invention
Mass ratio mixes,
In preparation method: prepare extractum step and the order preparing medicated powder step can overturn, prepare gel step and be positioned at
After preparing extractum step and preparing medicated powder step.
Applicant adopts and uses water as solvent, forms water-soluble gel, it is simple to extract powder dissolving in gel and dispersion.
Preferably, prepare in gel step: substrate and solvent 1:6 ~ 16 in mass ratio mix, can be formed under this ratio and be easy to be coated with
Cover, the gel of form stable;Preferably, substrate and solvent 1:9 ~ 12 in mass ratio mix, it is found by the applicant that the adding of aqueous solvent
Dosage is crossed conference and the slow release of medicine is brought harmful effect, and addition is crossed that I haven't seen you for ages and the stretchability of gel can be brought bad shadow
Ringing, when substrate and solvent 1:9 ~ 12 in mass ratio mix, the slow release effect of medicine and stretchability can show optimum.
Preferably, the concrete operations preparing extractum step are: weigh Tang Gute winter daphne, Radix Anisodi Tangutici and Rhizoma Zingiberis by weight,
Through mixing, pulverize, boiling 2 times, decoct 1 ~ 1.5 hour used time every time, merge decoction liquor, be concentrated into runny plaste shape, add 85 ~
The ethanol solution mixed extraction of 90v/v%, filters and concentrated filtrate, is dried to obtain extract powder, and under these process conditions, extract powder carries
Take efficiency the highest;Prepare the concentration in extractum step to be decompression recycling ethanol and concentrate, be dried as vacuum drying.
When composition of raw materials includes Radix Lamiophlomidis Rotatae, the concrete operations preparing extractum step are:
It is conventional ethanol reflux extraction method preparing the reflux, extract, described in Radix Lamiophlomidis Rotatae extract.Preferably, in preparation solely
Simply during extract, Radix Lamiophlomidis Rotatae 75 ~ 85/v% ethanol solution reflux, extract, 2 ~ 3 times, Extracting temperature 79.5 ~ 83 DEG C, extracts every time
2 ~ 3 hours, merge ethanol extract (i.e. lixiviating solution in reflux, extract, container), concentrating under reduced pressure, vacuum drying, obtain Radix Lamiophlomidis Rotatae and carry
Take thing.In the ethanol solution mixed extraction of addition 85 ~ 95 v/v % prepared described in extractum step, refer at normal temperatures,
The ethanol solution adding 85 ~ 95 v/v % mixes with the stirring of described runny plaste shape concentrate.
Preferably, the concrete operations preparing medicated powder step are: Moschus, Myrrha, Olibanum, Borneolum Syntheticum, Camphora and methyl salicylate
Respectively finely ground mistake 200 mesh sieve, after mix homogeneously, obtains medicated powder, 200 mesh medicated powder good dispersions, is easier to point when mixing with wetting agent
Dissipate;The ethanol solution of Moschus with 90 ~ 95v/v% of quality is mixed, grinds in process of lapping by Moschus, to accelerate grinding of Moschus
Mill efficiency, the ethanol solution of 90 ~ 95v/v% can quickly volatilize lost, finally be not present in medicated powder after grinding.
Preferably, prepare in gel step: when swelling solution is mixed with extractum and transdermal enhancer, use swelling solution
It is divided into etc. 2 ~ 3 parts of quality, according to adding the form of 1 part every time, swelling solution is divided 2 ~ 3 times and add extractum and transdermal penetration enhancer
In mixture, it is thus achieved that extract dispersion liquid.
Compared with prior art, anisodamine-musk gel of the present invention and preparation method thereof is had the advantage that
It is: 1, this anisodamine-musk gel transdermal penetration rates is high, bioavailability is high, has preferable pharmacological action.Tang Gute
Winter daphne has and grows stomach-fire, expelling wind and removing dampness, effect of pain relieving dissipating blood stasis.Radix Anisodi Tangutici has analgesia spasmolytic, blood circulation and promoting silt, hemostasia and promoting granulation
Effect.Myrrha has promoting blood circulation to remove blood stasis, reducing swelling and alleviating pain effect.The most each medicine share, invigorating blood circulation analgesia, expelling wind and removing dampness.To rheumatic arthralgia,
Arthritis, rheumatoid arthritis, the disease such as traumatic injury has preferable therapeutical effect.Applicant in inventive formulation with nitrogen
Ketone is as transdermal enhancer, and limits in anisodamine-musk gel the mass percent shared by transdermal enhancer as 0.5 ~ 2%,
This consumption significantly improves the skin permeation rate of medicine, improves the bioavailability of medicine, has preferable pharmacological action.
2, this anisodamine-musk gel can stablize lasting release medicine, and the analgesic effect persistent period is long.Applicant exists
The present invention devises specific matrix components, and limit mass percent shared by anisodamine-musk gel mesostroma as
0.5 ~ 5% so that the medicine in anisodamine-musk gel can stablize lasting release, and the analgesic effect persistent period is long.
3, this anisodamine-musk gel can improve further to traumatic injury, arthritis and rheumatoid arthritis
Therapeutic effect.First, applicant optimizes proportioning raw materials, and applicant have chosen the optimum amount proportioning of raw material of Chinese medicine after deliberation:
Tang Gute winter daphne 60 ~ 70 parts, Radix Anisodi Tangutici 9.5 ~ 10 parts, Rhizoma Zingiberis 4.5 ~ 6 parts, Olibanum 1.5 ~ 3 parts, Myrrha 1.5 ~ 3 parts, Borneolum Syntheticum 1.5
~ 3 parts, Camphora 1.5 ~ 3 parts, methyl salicylate 8.7 ~ 12 parts, 0.02 ~ 0.25 part of Moschus, substrate 3 ~ 8 parts, transdermal enhancer 0.5
~ 2 parts and during wetting agent 3 ~ 5 parts, for traumatic injury, arthritis and rheumatoid arthritis therapeutic effect more preferably.Secondly, Shen
Ask someone to improve the formula of raw material, formula with the addition of raw material Radix Lamiophlomidis Rotatae, it is found by the applicant that;When adding Radix Lamiophlomidis Rotatae in the feed
After 5 ~ 12 parts, it is possible to improve blood circulation promoting and blood stasis dispelling, the effect of analgesia detumescence further, there is the collaborative effect strengthening drug effect.
Detailed description of the invention
Embodiment 1 ~ 10 is the detailed description of the invention of the anisodamine-musk gel of the present invention and preparation method thereof, Qi Zhongshi
Execute example 1 for most preferred embodiment.
Embodiment 1
The present embodiment comprises the raw material of following weight portion: Tang Gute winter daphne 70 parts, Radix Anisodi Tangutici 8 parts, Rhizoma Zingiberis 3 parts, Olibanum 2.5 parts,
Myrrha 2.5 parts, Borneolum Syntheticum 2 parts, Camphora 1 part, methyl salicylate 10.5 parts, 0.06 part of Moschus, substrate 4.5 parts, azone 0.8 part,
Wetting agent 5 parts and solvent 45 parts.Wetting agent is the mixture of glycerol, Polyethylene Glycol and propylene glycol 1:1:0.5 in mass ratio.Substrate
Being made up of polyvinyl alcohol, carbomer and sodium polyacrylate 1:1:0.5 in mass ratio, solvent is water;
The preparation method of the present embodiment comprises the steps:
Prepare extractum: weigh Tang Gute winter daphne, Radix Anisodi Tangutici and Rhizoma Zingiberis by weight, through mixing, pulverize, boiling 2 times, every time
Decoct 1 ~ 2 hour used time, merge decoction liquor, be concentrated into runny plaste shape, add the ethanol solution mixed extraction of 85 ~ 95v/v%, filter
And concentrated filtrate, it is dried to obtain extract powder;
Prepare medicated powder: Moschus, Myrrha, Olibanum, Borneolum Syntheticum, Camphora and methyl salicylate finely ground mistake 100 ~ 200 mesh sieve respectively, mixing is all
After even, obtain medicated powder;
Prepare gel: medicated powder, wetting agent are mixed to prepare medicated powder dispersion liquid;By swelling for polyvinyl alcohol solubilizer 24 hours, it is thus achieved that
First swelling solution;By swelling for carbomer solubilizer 24 hours, adding sodium polyacrylate, stir acquisition the second swelling solution;Will
Extractum adds in the first swelling solution and stirs evenly, and adds the second swelling solution and stirs evenly, it is thus achieved that extract dispersion liquid;By extract dispersion liquid and medicine
Powder dispersion liquid mixes, and stirs and i.e. obtains anisodamine-musk gel.
Embodiment 2
The present embodiment comprises the raw material of following weight portion: Tang Gute winter daphne 70 parts, Radix Anisodi Tangutici 8 parts, Rhizoma Zingiberis 3 parts, Olibanum 2.5 parts,
Myrrha 2.5 parts, Borneolum Syntheticum 2 parts, Camphora 1 part, methyl salicylate 10.5 parts, 0.06 part of Moschus, substrate 4.5 parts, azone 0.4 part,
Wetting agent 5 parts and solvent 45 parts.Solvent, wetting agent and matrix components are with embodiment 1.
Preparation method is with embodiment 1.
Embodiment 3
The present embodiment comprises the raw material of following weight portion: Tang Gute winter daphne 70 parts, Radix Anisodi Tangutici 8 parts, Rhizoma Zingiberis 3 parts, Olibanum 2.5 parts,
Myrrha 2.5 parts, Borneolum Syntheticum 2 parts, Camphora 1 part, methyl salicylate 10.5 parts, 0.06 part of Moschus, substrate 4.5 parts, azone 1.6 parts,
Wetting agent 5 parts and solvent 45 parts.Solvent, wetting agent and matrix components are with embodiment 1.
Preparation method is with embodiment 1.
Embodiment 4
The present embodiment comprises the raw material of following weight portion: Tang Gute winter daphne 66 parts, Radix Anisodi Tangutici 8 parts, Rhizoma Zingiberis 3 parts, Olibanum 2.5 parts,
Myrrha 2.5 parts, Borneolum Syntheticum 1.5 parts, Camphora 1.5 parts, methyl salicylate 10 parts, 0.1 part of Moschus, substrate 7.5 parts, azone 3 parts and guarantor
Humectant 3.5 parts, solvent 75 parts.Wetting agent is the mixture of glycerol, Polyethylene Glycol and propylene glycol 2:1:0.5 in mass ratio;Substrate
Mixing for polyvinyl alcohol, carbomer and sodium polyacrylate 1:1:1. in mass ratio, solvent is water;
The preparation method of the present embodiment comprises the steps:
Prepare extractum: weigh Tang Gute winter daphne, Radix Anisodi Tangutici and Rhizoma Zingiberis by weight, through mixing, pulverize, boiling 3 times, every time
Decoct 1 hour used time, merge decoction liquor, be concentrated into runny plaste shape, add the ethanol solution mixed extraction of 85 ~ 95v/v%, filter also
Concentrated filtrate, is dried to obtain extract powder;
Prepare medicated powder: Moschus, Myrrha, Olibanum, Borneolum Syntheticum, Camphora and methyl salicylate finely ground mistake 100 ~ 200 mesh sieve respectively, mixing is all
After even, obtain medicated powder;
Prepare gel: medicated powder, wetting agent are mixed to prepare medicated powder dispersion liquid;Each for substrate component being stirred, solubilizer is swelling
24 hours, it is thus achieved that swelling solution;By 3 parts of the quality such as swelling solution is divided into, use and add 1 part of side being then uniformly mixed every time
Formula, divides in the mixture that swelling solution adds for 3 times extractum and transdermal penetration enhancer, it is thus achieved that extract dispersion liquid;By extract dispersion liquid with
Medicated powder dispersion liquid mixes, and stirs and i.e. obtains anisodamine-musk gel.
Embodiment 5
The raw material that the present embodiment comprises following weight portion: Tang Gute winter daphne 60 parts, Radix Anisodi Tangutici 9 parts, Rhizoma Zingiberis 3 parts, Olibanum 3 parts, do not have
Medicine 1.5 parts, Borneolum Syntheticum 3 parts, Camphora 1 part, methyl salicylate 11 parts, 0.02 part of Moschus, substrate 8 parts, azone 2 parts, wetting agent 5 parts
With solvent 88 parts.Wetting agent is the mixture of glycerol, Polyethylene Glycol and propylene glycol 1:0.5:1 in mass ratio;By poly-second in substrate
Enol, carbomer and xanthan gum 0.5:1:1. in mass ratio forms, and solvent is water;
The preparation method of the present embodiment comprises the steps:
Prepare extractum: weigh Tang Gute winter daphne, Radix Anisodi Tangutici and Rhizoma Zingiberis by weight, through mixing, pulverize, boiling 3 times, every time
Decoct 1 hour used time, merge decoction liquor, be concentrated into runny plaste shape, add the ethanol solution mixed extraction of 85 ~ 95v/v%, filter also
Concentrated filtrate, is dried to obtain extract powder;
Prepare medicated powder: Moschus, Myrrha, Olibanum, Borneolum Syntheticum, Camphora and methyl salicylate distinguish finely ground mistake 200 mesh sieve, mix homogeneously
After, obtain medicated powder;
Prepare gel: medicated powder, wetting agent are mixed to prepare medicated powder dispersion liquid;By swelling for polyvinyl alcohol solubilizer 24 hours, it is thus achieved that
First swelling solution;By swelling for carbomer solubilizer 24 hours, adding xanthan gum, stir acquisition the second swelling solution;By extractum
Add in the first swelling solution and stir evenly, add the second swelling solution and stir evenly, it is thus achieved that extract dispersion liquid;Extract dispersion liquid is divided with medicated powder
Dissipate liquid mixing, stir and i.e. obtain anisodamine-musk gel.
Embodiment 6
The present embodiment comprises the raw material of following weight portion: Tang Gute winter daphne 70 parts, Radix Anisodi Tangutici 7 parts, Rhizoma Zingiberis 4 parts, Radix Lamiophlomidis Rotatae 8 parts,
Olibanum 1.5 parts, Myrrha 3 parts, Borneolum Syntheticum 1.5 parts, Camphora 2 parts, methyl salicylate 9 parts, 0.2 part of Moschus, substrate 3 parts, azone 0.5
Part, wetting agent 3 parts and solvent 36 parts.Wetting agent is the mixture of glycerol, Polyethylene Glycol and propylene glycol 0.5:1:1 in mass ratio.
Substrate is polyvinyl alcohol, carbomer and sodium carboxymethyl cellulose 0.5:1:1. in mass ratio composition, and solvent is water;
The preparation method of the present embodiment comprises the steps:
Prepare extractum: by Radix Lamiophlomidis Rotatae 42 ~ 95 v/v% ethanol solution reflux, extract, 2 times, extract 2 hours every time, merge ethanol and carry
Take liquid, concentrating under reduced pressure, vacuum drying, obtain Radix Lamiophlomidis Rotatae extract;Weigh Tang Gute winter daphne, Radix Anisodi Tangutici, Rhizoma Zingiberis and solely by weight
Simply, through mixing, pulverize, boiling 3 times, decoct 1 hour used time every time, merge decoction liquor, be concentrated into runny plaste shape, add 85
The ethanol solution mixed extraction of ~ 95%, filters and concentrated filtrate, adds Radix Lamiophlomidis Rotatae extract mixing, is dried to obtain extract powder;
Prepare medicated powder: Moschus, Myrrha, Olibanum, Borneolum Syntheticum, Camphora and methyl salicylate distinguish finely ground mistake 100 mesh sieve, mix homogeneously
After, obtain medicated powder;
Prepare gel: medicated powder, wetting agent are mixed to prepare medicated powder dispersion liquid;By swelling for polyvinyl alcohol solubilizer 24 hours, it is thus achieved that
First swelling solution;By swelling for carbomer solubilizer 24 hours, adding sodium carboxymethyl cellulose, the acquisition second that stirs is swelling
Liquid;Extractum is added in the first swelling solution and stir evenly, add the second swelling solution and stir evenly, it is thus achieved that extract dispersion liquid;Extractum is disperseed
Liquid mixes with medicated powder dispersion liquid, stirs and i.e. obtains anisodamine-musk gel.
Embodiment 7
The raw material that the present embodiment comprises following weight portion: Tang Gute winter daphne 70 parts, Radix Anisodi Tangutici 6 parts, Rhizoma Zingiberis 6 parts, Olibanum 3 parts, do not have
Medicine 3 parts, Borneolum Syntheticum 1 part, Camphora 3 parts, methyl salicylate 8 parts, 0.01 part of Moschus, substrate 3 parts, azone 0.5 part, wetting agent 2 parts and
Solvent 33 parts.Wetting agent is glycerol and the mixture of Polyethylene Glycol 1:1 in mass ratio.Substrate such as is at the polyvinyl alcohol of quality, the card
Ripple nurse and tragcanth 1:1:1. in mass ratio forms, and solvent is water;
The preparation method of the present embodiment comprises the steps:
Prepare extractum: weigh Tang Gute winter daphne, Radix Anisodi Tangutici and Rhizoma Zingiberis by weight, through mixing, pulverize, boiling 3 times, every time
Decoct 1 hour used time, merge decoction liquor, be concentrated into runny plaste shape, add the ethanol solution mixed extraction of 85 ~ 95v/v%, filter also
Concentrated filtrate, is dried to obtain extract powder;
Prepare medicated powder: Moschus, Myrrha, Olibanum, Borneolum Syntheticum, Camphora and methyl salicylate distinguish finely ground mistake 100 mesh sieve, mix homogeneously
After, obtain medicated powder;
Prepare gel: medicated powder, wetting agent are mixed to prepare medicated powder dispersion liquid;By swelling for polyvinyl alcohol solubilizer 24 hours, it is thus achieved that
First swelling solution;By swelling for carbomer solubilizer 24 hours, adding tragcanth, stir acquisition the second swelling solution;Will leaching
Cream adds in the first swelling solution and stirs evenly, and adds the second swelling solution and stirs evenly, it is thus achieved that extract dispersion liquid;By extract dispersion liquid and medicated powder
Dispersion liquid mixes, and stirs and i.e. obtains anisodamine-musk gel.
Embodiment 8
The present embodiment comprises the raw material of following weight portion: Tang Gute winter daphne 50 parts, Radix Anisodi Tangutici 10 parts, Rhizoma Zingiberis 2 parts, Olibanum 1 part,
Myrrha 1 part, Borneolum Syntheticum 3 parts, Camphora 1 part, methyl salicylate 13 parts, 0.25 part of Moschus, substrate 9 parts, azone 3.6 parts, wetting agent 6
Part and solvent 144 parts.Wetting agent is the mixture of glycerol, Polyethylene Glycol and propylene glycol 2:0.5:0.5 in mass ratio.Substrate by etc.
The polyvinyl alcohol of quality, carbomer and methylcellulose 1:1:1. in mass ratio forms, and solvent is water;
The preparation method of the present embodiment comprises the steps:
Prepare extractum: weigh Tang Gute winter daphne, Radix Anisodi Tangutici and Rhizoma Zingiberis by weight, through mixing, pulverize, boiling 2 times, every time
Decoct 2 hours used times, merge decoction liquor, be concentrated into runny plaste shape, add the ethanol solution mixed extraction of 85 ~ 95v/v%, filter also
Concentrated filtrate, is dried to obtain extract powder;
Prepare medicated powder: Moschus, Myrrha, Olibanum, Borneolum Syntheticum, Camphora and methyl salicylate distinguish finely ground mistake 200 mesh sieve, mix homogeneously
After, obtain medicated powder;
Prepare gel: medicated powder, wetting agent are mixed to prepare medicated powder dispersion liquid;Each for substrate component being stirred, solubilizer is swelling
22 hours, it is thus achieved that swelling solution;By 3 parts of the quality such as swelling solution is divided into, use and add 1 part every time and stir the mode of mixing, divide 3
In the secondary mixture that swelling solution is added extractum and transdermal penetration enhancer, it is thus achieved that extract dispersion liquid;Extract dispersion liquid is divided with medicated powder
Dissipate liquid mixing, stir and i.e. obtain anisodamine-musk gel.
Embodiment 9
The present embodiment comprises the raw material of following weight portion: Radix Lamiophlomidis Rotatae 12 parts, the component of remaining raw material and consumption are with embodiment 7;
The preparation method of the present embodiment comprises the steps:
Prepare extractum: by Radix Lamiophlomidis Rotatae 42 ~ 95 v/v% ethanol solution reflux, extract, 3 times, extract 2 hours every time, merge ethanol and carry
Take liquid, concentrating under reduced pressure, vacuum drying, obtain Radix Lamiophlomidis Rotatae extract;Weigh Tang Gute winter daphne, Radix Anisodi Tangutici and Rhizoma Zingiberis, warp by weight
Mixing, pulverize, boiling 3 times, decoct 1 hour used time every time, merge decoction liquor, be concentrated into runny plaste shape, add 85 ~ 95v/v%
Ethanol solution mixed extraction, filter and concentrated filtrate, add Radix Lamiophlomidis Rotatae extract mixing, be dried to obtain extract powder;
Prepare medicated powder step and prepare gel step with embodiment 7.
Embodiment 10
The present embodiment comprises the raw material of following weight portion: Radix Lamiophlomidis Rotatae 5 parts, the component of remaining raw material and consumption are with embodiment 8;
Prepare extractum: by Radix Lamiophlomidis Rotatae 42 ~ 95 v/v% ethanol solution reflux, extract, 2 times, extract 2 hours every time, merge ethanol and carry
Take liquid, concentrating under reduced pressure, vacuum drying, obtain Radix Lamiophlomidis Rotatae extract;Weigh Tang Gute winter daphne, Radix Anisodi Tangutici and Rhizoma Zingiberis, warp by weight
Mixing, pulverize, boiling 2 times, decoct 2 hours used times every time, merge decoction liquor, be concentrated into runny plaste shape, add 85 ~ 95v/v%
Ethanol solution mixed extraction, filter and concentrated filtrate, add Radix Lamiophlomidis Rotatae extract mixing, be dried to obtain extract powder;
Prepare medicated powder step and prepare gel step with embodiment 8.
Comparative example
Comparative example 1 ~ 3 is the comparative example that applicant designs to verify technical solution of the present invention.
Comparative example 1
Proportioning raw materials and the preparation method of this comparative example resides in reduced the consumption of azone, gained Radix Anisodi Tangutici with embodiment 1, difference
In Moschus gel, mass percent shared by azone is 0.25%.
Comparative example 2
Proportioning raw materials and the preparation method of this comparative example are to add the consumption of azone, gained Radix Anisodi Tangutici with embodiment 1, difference
In Moschus gel, mass percent shared by azone is 3%.
Comparative example 3
This comparative example is rubber-emplastrum group, and rubber-emplastrum used is the anisodamine-musk that Qinghai Bao Jiantang traditional Chinese medicines company limited produces
Cream.
Performance test
One, the assay of preparation
1. the assay of daphnetin
1.1 chromatographic conditions: Agilent ZORBAX (4.6 mm × 250 mm, 5 μm) post, with methanol-0.04% phosphoric acid water (22:
78) for flowing phase;Detection wavelength 325nm;Column temperature: 30 DEG C;Flow velocity 1 mL/min.
1.2 assay methods: it is appropriate that precision weighs daphnetin reference substance, add methanol solution constant volume in the volumetric flask of 10mL,
Make the storing solution solution of every l mL daphnetin reference substance containing 0.46 mg;With methanol dilution, 0.046 mg/mL's of system is right
According to product solution.Take this product 0.05g, put in round-bottomed flask, add ethanol 5ml, after standing 30 minutes, supersound extraction 1 hour, take out
Filter, is concentrated to dryness filtrate with Rotary Evaporators, and again with methanol is dissolved and is settled in the volumetric flask of 25ml, molten as sample
Liquid;Take reference substance solution and sample solution 10 μ l respectively, inject high performance liquid chromatograph, measure and calculation.
Two, the selection of transdermal enhancer
In order to keep this unitary variant of transdermal enhancer azone, applicant chooses embodiment 1 ~ 3 and comparative example 1 ~ 2 is carried out
Detection, to obtain: when the mass percent shared by azone in anisodamine-musk gel changes, daphnetin skin permeation rate
Situation of change.
Experimental apparatus and reagent: Agilent 1200 high performance liquid chromatograph;(iron of fine quality triumphant instrument in Shanghai is limited for Franz diffusion cell
Company);YB-P6 type intelligence penetrating absorption instrument (Tianjin Pharmacopoeia Standard Instrument Factory);Azone and other reagent are analytical pure.
Experimental technique: select 200 scholar's 20g healthy rats.Belly wool is cut off, puts to death, take off skin of abdomen, remove subcutaneous
Fat, normal saline is clean, and cold preservation is standby, by the above-mentioned skin keratin aspect processed, repeatedly pastes with adhesive tape 20 times, will
Horny layer is peelled off, and is smooth surface to skin, translucent.Skin is fixed on Franz diffusion cell to coyote hole and acceptance pool
Between, corium side contacts with acceptable solution, emptying bubble.Take certain area containing same matrix, wetting agent, different transdermal enhancer
The gel sample of the present invention be attached to, on coyote hole skin, be allowed to and skin close contact.Fluid Contacting is about 10mlpH7.4's
Phosphate buffer, magnetic agitation speed is about 100r/min, and bath temperature is (37 ± 0.5) DEG C.Every necessarily in 24 hours
Time inclines and takes whole acceptable solution, supplements equal-volume acceptable solution immediately after.The acceptable solution taken out is placed in dry evaporating dish, water-bath
50% methanol constant volume is added in 1ml measuring bottle after being evaporated.According to the content assaying method of above-mentioned preparation, daphnetin is measured, meter
Calculate skin permeation rate, the results are shown in Table 1.
Table 1 transdermal enhancer Selection experiment
。
By table 1 data it can be seen that in embodiment 1 ~ 3 mass percent of azone be 0.5% ~ 2%, transdermal facilitation effect
Optimum.In the anisodamine-musk gel of comparative example 1 ~ 2, the mass percent of azone is all outside 0.5% ~ 2% scope, although its
Skin permeation rate is below the skin permeation rate of embodiment 1 ~ 3, but the skin permeation rate of comparative example can reach more than 25%, preferable.
Three, pharmacological testing
The mice of blank group does not uses any medicine.Writhing response number of times is the fewest, represents that analgesic effect is the best.Hot plate reaction
Time is the longest, shows that analgesic effect duration is the longest, drug effect more lasting stability.
1, analgesic test
1.1 impacts on mouse hot-plate induced pain effect
Female mice (body weight 20 scholar 2g) 40 divides 4 groups at random, and ibid, successive administration 5 days, last is given for packet and medication
After medicine, each Mus is individually fixed in the hot-plate instrument of 55 ± 0.5 DEG C by 1h, and to lick the metapedes indicator reaction as " pain ", observation is given
After medicine, in the mice response time to hot plate pain, the results are shown in Table 2.
The impact of the writhing response that 1.2 Dichlorodiphenyl Acetates cause
Take female mice (body weight 20 scholar 2g) 40, packet and medication ibid, successive administration 5 days, last be administered after 1h,
Lumbar injection 0.6% acetum 0.2ml/20g body weight, observes the mouse writhing number of times in 10min, the results are shown in Table 2.
Table 2 analgesic test result (X ± SD)
。
Note: compare with blank group:*P < 0.05;**P < 0.01;
Table 2 result shows: inventive gel agent has preferable analgesic activity, with blank group, the gel of comparative example 2 and
The rubber-emplastrum group of comparative example 3 compares, and the analgesic activity of invention formulation is notable.Applicant is by the gel of embodiment 2 ~ 10 gained
Agent carries out table 2 respectively and tests, find the hot plate pain response time of embodiment 2 ~ 10 be all longer than one-armed in, and be all longer than contrast
Example 3, but all it is shorter than embodiment 1;The writhing number of times of embodiment 2 ~ 10 is all less than comparative example 2, and all less than comparative example 3, but all
More than embodiment 1, embodiment 1 is most preferred embodiment the most in sum.
The above, be only presently preferred embodiments of the present invention, is not the restriction that the present invention makees other form, appoints
What those skilled in the art changed possibly also with the technology contents of the disclosure above or be modified as equivalent variations etc.
Effect embodiment.But every without departing from technical solution of the present invention content, the technical spirit of the foundation present invention is to above example institute
Any simple modification, equivalent variations and the remodeling made, still falls within the protection domain of technical solution of the present invention.
Claims (10)
1. anisodamine-musk gel, it is characterised in that include the raw material of following weight portion: Tang Gute winter daphne 50 ~ 70 parts, mountain Liang
Henbane 6 ~ 10 parts, Rhizoma Zingiberis 2 ~ 6 parts, Olibanum 1 ~ 3 part, Myrrha 1 ~ 3 part, Borneolum Syntheticum 1 ~ 3 part, Camphora 1 ~ 3 part, methyl salicylate 8 ~ 13
Part, 0.01 ~ 0.25 part of Moschus, substrate 3 ~ 9 parts, azone 0.2 ~ 3.6 part, wetting agent 2 ~ 6 parts, solvent 18 ~ 144 parts.
Anisodamine-musk gel the most according to claim 1, it is characterised in that include the raw material of following weight portion: Tang
Ancient special winter daphne 60 ~ 70 parts, Radix Anisodi Tangutici 7 ~ 9 parts, Rhizoma Zingiberis 3 ~ 4 parts, Olibanum 1.5 ~ 3 parts, Myrrha 1.5 ~ 3 parts, Borneolum Syntheticum 1.5 ~ 3 parts, Camphor tree
1 ~ 2 part of brain, methyl salicylate 9 ~ 11 parts, 0.02 ~ 0.2 part of Moschus, substrate 4 ~ 7.5 parts, azone 0.4 ~ 2.5 part, wetting agent 3 ~ 5
Part, solvent 36 ~ 90 parts.
Anisodamine-musk gel the most according to claim 1, it is characterised in that: described wetting agent is glycerol, poly-second
In glycol, propylene glycol two or three is mixed by any mass ratio, and described solvent is water.
Anisodamine-musk gel the most according to claim 1, it is characterised in that: described substrate by polyacrylamide,
Sodium polyacrylate, methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl methyl cellulose, tragcanth, xanthan gum, alginic acid
In any one, form with polyvinyl alcohol and carbomer.
Anisodamine-musk gel the most according to claim 1, it is characterised in that: described substrate is by polyvinyl alcohol, card
Ripple nurse and sodium polyacrylate 0.5 ~ 2:0.5 in mass ratio ~ 2:0.5 ~ 2 composition.
Anisodamine-musk gel the most according to claim 1, it is characterised in that: described raw material also includes Radix Lamiophlomidis Rotatae
5 ~ 12 parts.
7. the preparation method of the anisodamine-musk gel described in any one of claim 1 ~ 4, it is characterised in that: include preparation leaching
Cream, prepare medicated powder and prepare gel step;
The concrete operations preparing extractum step are: weigh Tang Gute winter daphne, Radix Anisodi Tangutici and Rhizoma Zingiberis by weight, through mixing, pulverizing,
Boiling 2 ~ 3 times, decocts 1 ~ 2 hour used time every time, merges decoction liquor, is concentrated into runny plaste shape, adds the second of 85 ~ 95v/v%
Alcoholic solution mixed extraction, filters and concentrated filtrate, is dried to obtain extract powder;
The concrete operations preparing medicated powder step are: Moschus, Myrrha, Olibanum, Borneolum Syntheticum, Camphora and methyl salicylate finely ground mistake respectively
100 ~ 200 mesh sieves, after mix homogeneously, obtain medicated powder;
The concrete operations preparing gel step are: mixed powder and wetting agent by weight, prepare medicated powder dispersion liquid;By substrate
With solvent mixing, swelling, it is thus achieved that swelling solution, swelling solution is mixed with extract powder and transdermal enhancer, it is thus achieved that extract dispersion liquid;Will
Extract dispersion liquid mixes with medicated powder dispersion liquid, stirs and i.e. obtains anisodamine-musk gel.
The preparation method of anisodamine-musk gel the most according to claim 7, it is characterised in that: prepare gel step
Concrete operations be: mixed powder and wetting agent by weight, prepare medicated powder dispersion liquid;By swelling for polyvinyl alcohol solubilizer 22 ~
26 hours, it is thus achieved that the first swelling solution;By swelling for carbomer solubilizer 22 ~ 26 hours, add polyacrylamide, sodium polyacrylate,
Any one in methylcellulose, sodium carboxymethyl cellulose, hydroxypropyl methyl cellulose, tragcanth, xanthan gum, alginic acid
Kind, stir acquisition the second swelling solution;Extractum and transdermal enhancer are added in the first swelling solution and stirs evenly, add second molten
Swollen liquid stirs evenly, it is thus achieved that extract dispersion liquid;Being mixed with medicated powder dispersion liquid by extract dispersion liquid, stirring, it is solidifying i.e. to obtain anisodamine-musk
Colloid.
The preparation method of anisodamine-musk gel the most according to claim 7, it is characterised in that: prepare gel step
Concrete operations be: mixed powder and wetting agent by weight, prepare medicated powder dispersion liquid;By each for substrate component mix homogeneously, add
Enter solvent mixing, swelling 22 ~ 26 hours, it is thus achieved that swelling solution, by 2 ~ 3 parts of the quality such as swelling solution is divided into, use and every time add 1 part
And stir the mode of mixing, point 2 ~ 3 times swelling solution is added in the mixture of extractum and transdermal penetration enhancer, it is thus achieved that extractum disperses
Liquid;Extract dispersion liquid is mixed with medicated powder dispersion liquid, stirs and i.e. obtain anisodamine-musk gel.
10. the preparation method of the anisodamine-musk gel described in claim 6, it is characterised in that: include preparing extractum, preparation
Medicated powder and prepare gel step;
The described concrete operations preparing extractum step are: by Radix Lamiophlomidis Rotatae 42 ~ 95 v/v% ethanol solution reflux, extract, 2 ~ 3 times,
Extract 2 ~ 3 hours every time, merge ethanol extract, concentrating under reduced pressure, vacuum drying, obtain Radix Lamiophlomidis Rotatae extract;Weigh by weight
Tang Gute winter daphne, Radix Anisodi Tangutici, Rhizoma Zingiberis and Radix Lamiophlomidis Rotatae, through mixing, pulverize, boiling 2 ~ 3 times, decoct 1 ~ 2 hour used time every time,
Merge decoction liquor, be concentrated into runny plaste shape, add the ethanol solution mixed extraction of 85 ~ 95 v/v %, filter and concentrated filtrate, add
Radix Lamiophlomidis Rotatae extract mixes, and is dried to obtain extract powder;
The concrete operations preparing medicated powder step are: Moschus, Myrrha, Olibanum, Borneolum Syntheticum, Camphora and methyl salicylate finely ground mistake respectively
100 ~ 200 mesh sieves, after mix homogeneously, obtain medicated powder;
The concrete operations preparing gel step are: mixed powder and wetting agent by weight, prepare medicated powder dispersion liquid;By substrate
With solvent mixing, swelling 22 ~ 26 hours, it is thus achieved that swelling solution, swelling solution is mixed with extract powder and transdermal enhancer, it is thus achieved that extractum
Dispersion liquid;Extract dispersion liquid is mixed with medicated powder dispersion liquid, stirs and i.e. obtain anisodamine-musk gel.
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CN116676355A (en) * | 2023-08-03 | 2023-09-01 | 成都第一制药有限公司 | Method for catalytic synthesis of anisodamine |
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