CN101496833B - Liquid external preparation for preparing total alkaloids in nux vomica - Google Patents

Liquid external preparation for preparing total alkaloids in nux vomica Download PDF

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CN101496833B
CN101496833B CN2009100427152A CN200910042715A CN101496833B CN 101496833 B CN101496833 B CN 101496833B CN 2009100427152 A CN2009100427152 A CN 2009100427152A CN 200910042715 A CN200910042715 A CN 200910042715A CN 101496833 B CN101496833 B CN 101496833B
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semen strychni
total alkaloids
preparation
external preparation
liquid external
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CN101496833A (en
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吴萍
汤淮波
胡海
孙必强
唐武
杨占京
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Xiangtan University
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Xiangtan University
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Abstract

The invention relates to a preparation formulation for an externally applied liquid preparation prepared from total strychnos alkaloids, and preparation thereof. The preparation formulation is prepared from the total strychnos alkaloids and auxiliary materials such as a transdermal sorbefacient, a solvent, a humectant and an antiseptic according to certain proportion. The externally applied liquid preparation of the total strychnos alkaloids comprises a pharmaceutically described externally applied liquid preparation such as a spraying agent, a wet application, a liniment or a pigmentum, and is used for treating diseases such as injuries from falls, carbuncle-abscess pain, rheumatic obstinate paralysis, rheumatoid arthralgia and anesthesia and paralysis. The preparation can overcome the defect that people are easy to be poisoned when orally taking strychnos. As proved by research results, the preparation is safe and effective, is convenient and comfortable to use, has small skin irritation and low production cost, is easy to be accepted by patients, and can generate good social benefit and economic benefit.

Description

The liquid external preparation of total alkaloids in Semen Strychni preparation
Technical field
The present invention relates to a kind of liquid external preparation by the total alkaloids in Semen Strychni preparation.
Background technology
Semen Strychni is 2005 editions kinds of recording of pharmacopeia, and its nature and flavor hardship, cold, very toxic is returned liver, spleen channel, and the effect of mass dissipating and swelling eliminating, removing obstruction in the collateral to relieve pain is arranged, and is used for diseases such as traumatic injury, ulcer sore pain, rheumatism paralysis, rheumatoid arthrosis pain, paralysis and numbness.Semen Strychni contains multiple alkaloids such as strychnine, strychnine, vomicine, novacine, pseudostrychnine, pseudobrucine, 4-hydroxyl vomicine, brucine nitrogen oxide, NSC 118079, icajine, 4-hydroxyl 3-methyl brucine, still contains fatty oil, protein, chlorogenic acid, loganin etc. in addition.Its main effective ingredient is strychnine and strychnine, and strychnine content is 1.2-2.2% in the pharmacopeia regulation Semen Strychni, and strychnine content is no less than 0.8%.Semen Strychni should not be given birth to usefulness, should not obey clothes of a specified duration more, go into ball after concocting and loose, and consumption is 0.3-0.6g.
The strychnine amount is 3.6-13.2mg when taking Semen Strychni by pharmacopeia regulation, and strychnine toxicity is extremely strong, and poisoning symptom can appear in oral 5-10mg, thus the Semen Strychni oral administration poison easily, clinical little with safety.Strychnine has the selective excitement effect of height to spinal cord.Low dose can improve spinal reflex, shortens reflex time, improves reflex strength and strengthens bone road myotility, simultaneously can excited corticocerebral analysis of sensation device, and make vision, audition and olfactory sensation more sharp; Dosage is big slightly, the very easy excessive poisoning that causes: it is strong excessively to show as spinal reflex, and excitement is diffused into whole spinal cord, destroyed the mutual process of inhibition of antagonist, body presents the complete tetanus spasm, and to be that so-called spinal cord is frightened jump, small stimulation occurs and just caused complete tetanus, last dead because of dyspnea eventually.Taking orally has digestion promoting function.Strychnine has good analgesia, antiinflammatory action; Suppressing hematoblastic cohesion and antithrombotic forms; Can obviously reduce the early apoptosis that NO induces chondrocyte; The tool antitumor action can be used for treating cancerous pain; Mouse peritoneal injection strychnine 350 μ g/kg, producing excited, activity increases, but that lumbar injection strychnine 14~23rng/kg mice occurs is obviously calm, close order, activity reduces.
Over nearly 30 years people transmission has produced great interest to the medicine percutaneous.Mainly concentrate on and have the medicine that commercial value can provide the whole body blood level, as scopolamine, nitroglycerin, clonidine, estradiol, testosterone, fentanyl.The advantage of transdermal delivery system can be avoided the gastrointestinal local irritation, can avoid the blood drug level big ups and downs of medicine and minimizing to give number of times and improve patient's compliance.A large amount of in recent years bibliographical informations adopts the percutaneous dosing approach that medicine is distributed seldom and arrival agents area deep tissues at whole body, and the drug level of the tissue of agents area lower floor is higher than oral or injection administration far away.Simultaneously during percutaneous dosing medicine with constant speed slowly by skin, it is constant that blood drug level can keep, and can avoid the violent medicine of some property of medicine the toxic and side effects that peak concentration produces to occur because of oral or drug administration by injection, even if it is easy the poisoning symptom processing method to occur.
Go into ball raw edge clothes after Semen Strychni is concocted, external is generally compound preparation.Drug standard records kind and mostly is conventional dosage forms: the medical material of will writing out a prescription directly is ground into medicated powder such as JIUFEN POWDER, and the time spent transfer to apply with wine, uses extremely inconveniently, and effective ingredient is difficult for being dissolved out from medicated powder that to cause effective ingredient concentration low, and onset is slow; Also have and will be prepared into rubber plaster such as DIEDA ZHENTONG GAO after the prescription medicinal material extract, but rubber plaster exists many shortcomings such as drug loading is low, skin irritation.The effective site total alkaloids in Semen Strychni of Semen Strychni is extracted, and the content may command of preparation sergeant's peace strychnine and the quality of the pharmaceutical preparations are stable, add novel transdermal absorption accelerator and can improve effective ingredient transdermal amount and improve clinical efficacy.Reports such as Guo Liwei are made liniment with total alkaloids in Semen Strychni, and it only was two weeks to its preparation stabilization Journal of Sex Research in the literary composition, in two weeks, occur slight layering, and had many operation factors all can influence the quality of preparation in the preparation process, be unsuitable for industrialized great production.Other has had many pieces of the bibliographical informations external absorption of strychnine, vauqueline liposome and analgesia, antiphlogistic research, the contained multiple alkaloid of Semen Strychni all has strong pharmacological action, list is unfavorable for keeping the original clinical efficacy of Semen Strychni medical material with strychnine, may strengthen along with strychnine concentration increases its toxic and side effects simultaneously.
Summary of the invention
The purpose of this invention is to provide total alkaloids in Semen Strychni and be prepared into the liquid exterior-applied formulation, can make total alkaloids in Semen Strychni be absorbed in the higher drug level of formation under the topical skin well and improve clinical efficacy by skin, this preparation is with on the skin simultaneously, drug absorption constant rate and speed are slower, and the phenomenon of poisoning peak concentration appears and in strychnine in the time of can avoiding the Semen Strychni oral administration.
The objective of the invention is to realize by following manner:
Total alkaloids in Semen Strychni liquid external preparation is prepared from by principal agent total alkaloids in Semen Strychni and proper supplementary material, principal agent 0.1g≤total alkaloids in Semen Strychni≤200g; Adjuvant is:
10ml≤penetrating promoter≤2000ml
0<wetting agent≤3000ml
0.5g≤antiseptic≤50g or 1000≤antiseptic≤3500ml
Solubilizer is to 10000ml.
The heat preserving agent preferred range is 1000ml≤wetting agent≤3000ml.
Described solvent is constituted jointly by following one or more: water, glycerol, ethanol, propylene glycol, Polyethylene Glycol, ethyl acetate, vegetable oil.
The preferred proportioning of the present invention is:
Principal agent total alkaloids in Semen Strychni 1g≤total alkaloids in Semen Strychni≤40g; Adjuvant is:
Penetrating promoter 100ml≤penetrating promoter≤2000ml
Wetting agent 1500ml≤wetting agent≤3000ml
Antiseptic 2000ml≤antiseptic≤3500ml
Add water to 10000ml.
The content of the strychnine in the total alkaloids in Semen Strychni is less than 40%, and strychnine content is greater than 20%.
Described wetting agent is constituted jointly by following one or more: glycerol, propylene glycol, Polyethylene Glycol, sorbitol; Described antiseptic is constituted jointly by following one or more: Nipagin ester, benzoic acid and salt thereof, sorbic acid and salt thereof; Ethanol, glycerol; Eucalyptus oil, Oleum menthae.
Dosage form of the present invention is spray, liniment, varnish or wet application.
The most preferred proportioning of the present invention is: 10g≤total alkaloids in Semen Strychni≤30g, and 100ml≤azone≤500ml, 200ml≤propylene glycol≤1000ml, 2000ml≤glycerol≤3000ml adds water to 10000ml again.
Because skin covering in human body whole body surface, directly contacts with external environment, and important barrier and protective effect are arranged, and can stop that foreign body and microorganism intrusion and body fluid exosmose, also stop the absorption of external used medicine simultaneously.Skin is made up of epidermis, corium, subcutaneous tissue and skin accessory organ.The outermost layer of skin is an epidermis, and horny layer is positioned at the top layer of epidermis.Horny layer is closely arranged by flat keratinocyte and is formed, and is dead cell, is the main barrier of medicine percutaneous absorption.The inventor discovers that the total alkaloids in Semen Strychni that will extract from Semen Strychni is dissolved in an amount of solvent, adding adjuvants such as a certain amount of penetrating promoter, wetting agent again makes and is prepared into the liquid external preparation, can promote total alkaloids in Semen Strychni to absorb effectively, reach higher drug concentration and reach clinical efficacy in the pathological changes part through skin; The drug slow constant speed sees through skin and may be absorbed by the blood capillary of dermal sites and enter blood circulation and produce the whole body therapeutic effect, also can avoid the oral very high blood drug level of Semen Strychni and the phenomenon that occurs poisoning.In addition, the penetrating promoter that the present invention adds is the material of the temporary transient adjusting percutaneous permeability of a kind of energy, and barrier function that can reversible change keratodermatitis does not damage the chemical substance of any competent cell again.The penetrating promoter that preparation of the present invention can be used is as follows: (1) azone.(2) menthol, Camphora, Oleum menthae, eucalyptus oil, Borneolum Syntheticum etc.(3) ethanol, isopropyl alcohol, isobutanol, n-dodecanol, propylene glycol, glycerol, ethyl acetate.(4) oleic acid, lauric methyl ester or ethyl ester, isopropyl myristate.Be preferably azone, propylene glycol, eucalyptus oil or Oleum menthae especially.
It is solvent that preparation optimizing prescriptions of the present invention adopts water, and can reduce has zest to skin, avoids easy dirty medicated clothing.Whole invention has should use Energy and comfort, the low characteristics of explained hereafter cost of raw material and preparation.Simultaneously water can impel the horny layer aquation and increase the permeability of medicine percutaneous.In addition, the present invention has also added wetting agent especially, and preferable amount is 20-30%, and the present invention can prevent that by the adding of wetting agent the medicinal liquid on the skin from volatilizing fast, thereby makes medicine percutaneous absorption and prolong drug action time in long-time.Compare with the liniment of bibliographical information, this preparation process thereof is simple, and quality is easy to control, and product stability is good, is suitable for industrialized great production; Use this preparation can cutaneous normal function simultaneously, Energy and comfort, patient's compliance height.The preparation process of total alkaloids in Semen Strychni is:
Method one: Semen Strychni coarse powder water or 0.5%-1% ore deposit acid liquid extract.After extracting solution was condensed into proper volume, reuse alkali (as ammonia, lime cream etc.) alkalized and dissociates alkaloid, extracts with organic solvent such as chloroform, benzene etc. then, and last concentrated extract gets the lipotropy total alkaloids.
Method two: after Semen Strychni Pulveratum was used aqueous alkali (lime cream, ammonia etc.) moistening, reuse organic solvent such as chloroform or benzene etc. directly carried out solid-liquid and extract.Promptly get the lipotropy total alkaloids after reclaiming organic solvent.
Whether to skin zest significantly, and can't produce effective product for total alkaloids in Semen Strychni liquid external preparation of the present invention, and the present invention is at antiinflammatory, the analgesic drug effect is how, and corresponding research has been done in invention per capita, and experiment method and result are as follows:
1. total alkaloids in Semen Strychni liquid external preparation is to rabbit intact skin acute toxicity testing
1.1 material
1.1.1 animal: healthy adult white man exempts from 12, is provided by the Xiangya Medical College, Zhongnan Univ Experimental Animal Center.
1.1.2 medicine and reagent:
Total alkaloids in Semen Strychni liquid external preparation is provided by pharmacy teaching and research room of University Of Xiangtan chemistry institute, and total alkaloid content is respectively 2mg/kg in the liquid, 4mg/kg or do not contain alkaloidal fluid matrix.
1.2 method
12 families are exempted to be divided at random 3 groups, A group: matched group; B group: Semen Strychni liquid external preparation small dose group (2mg/kg); C group: Semen Strychni liquid external preparation high dose group (4mg/kg).24h before the experiment beginning cuts off hair just with animal spinal column both sides with shears, and the reuse electric shaver is shaved hair, and the depilation area is approximately every side 5 * 10cm 2Get and tried thing 1ml and evenly be coated on skin of back unhairing district, animal left side, cover with one deck PE thin film then, non-stimulated immobilization with adhesive tape behind the 24h, is removed the residual reagent thing that is subjected to normal saline.The conventional raising observed the change of body weight, skin and hair, eyes and mucosa and breathing, circulation, autonomic nerve and central nervous system, limb motion and the behavioral activity etc. of 1 all rabbit continuously.In-particular its notice whether animal occurs trembling, symptoms such as tic, sialorrhea, diarrhoea, drowsiness and stupor.
1.3 result
Behavior, activity, diet, fur gloss and body weight (table 1) that the external of Semen Strychni liquid was exempted from the intact skin man with preparation small dose group (2mg/kg) and heavy dose of group (4mg/kg) outer time spent do not have influence, observe earlier in 7 days houselessness and exempt from death, acute toxic reaction do not occur.Be coated with tried thing after 20~40min, three groups of rabbit all have the phenomenon of panting, and may be due to the operating process rabbit struggles.
2. skin irritation test
2.1 the processing of animal subject
(1.5 ± 0.2kg) 8, male and female half and half are divided into intact skin group and damaged skin group to get healthy rabbits.
48h before the experiment beginning cuts off hair just with animal spinal column both sides with shears, and the reuse electric shaver is shaved hair, and whether slough the back 24h inspection of hair skin of unhairing injured because of unhairing.The making of damaged skin: with the operating scissors after the sterilization unhairing skin of sterilizing is scratched, the degree of being with the oozing of blood, the damaged degree of control left and right sides skin is consistent substantially.
2.2 method
Self left and right sides contrast is adopted in experiment.Rabbit left side unhairing district coating 1.0ml Strychnos alkaloid liquid preparation (1mg/ml) and the blank substrate of right side unhairing district coating 1.0ml are used PE film and immobilization with adhesive tape in contrast.Every animal sub-cage rearing, give tried thing after 24 hours with warm water flush away residue, remove to be tried behind the thing to observe in the 1st, 24,48,72 hour and smear the position and have or not situations such as erythema and edema, and mark standards of grading table 2, table 3.
When table 1 is used for intact skin to the influence (g) of rabbit body weight (X ± SD, n=4)
Figure G2009100427152D00071
Table 2 skin irritation reaction standards of grading
Figure G2009100427152D00072
Table 3 skin irritation intensity evaluation standard
2.3 result
Strychnos alkaloid liquid external preparation is respectively to rabbit intact skin and damaged skin administration, in 72h, observe, rabbit intact skin group is not found anaphylactic reactions such as erythema, edema, and the damaged skin group has indivedual rabbit damage location to occur the edema phenomenon is arranged, but can alleviate gradually in 72h, total stimulus intensity score value belongs to non-stimulated between 0-0.49, illustrate that Strychnos alkaloid liquid external preparation all has no stimulation to rabbit intact skin and damaged skin, the results are shown in Table 4.
3. xylol causes the experiment of mice auricle swelling
3.1 method
Choose 30 of healthy mices, be divided into 3 groups at random, be respectively and 1. tried the thing group: Strychnos alkaloid liquid preparation (1mg/ml) by body weight; 2. positive control drug group: (company limited by shares of YUNNAN BAIYAO group produces Yunnan Baiyao aerosol, product batch number: 20071108); 3. blank group: normal saline.Each is organized the mouse right ear two sides and only is coated with the corresponding thing that tried by 0.05ml/ respectively, 0.02ml proinflammatory agent dimethylbenzene on the repaste; Left side ear is left intact.Behind the 30min, animal is taken off neck put to death, cut ears, lay round auricle at same position respectively, weigh with analytical balance with 9mm diameter card punch along auricle.With left and right sides ear weight difference is swelling degree index, and matched group and administration group are carried out statistical procedures.Auricle edema suppression ratio=(the average swelling degree of the average swelling degree one administration group of matched group)/average swelling degree of matched group
3.2 result
The result shows that the Strychnos alkaloid spray has the effect of significant inhibition mice caused by dimethylbenzene xylene auricle edema, has antiinflammatory action preferably, sees Table 5.
Table 4 rabbit single-dose skin irritation test
Table 5 xylol cause mice auricle swelling influence (X ± SD, n=10)
Figure G2009100427152D00091
Compare with the blank group: * P<0.05, * * P<0.01
4. Dichlorodiphenyl Acetate causes the influence of mouse writhing reaction
4.1 method
Choose 30 of healthy mices, be divided into 3 groups at random by body weight, grouping is with experiment 3, and preserved skin is at first promptly cut with elbow and carefully carefully wiped out the about 5cm of hair from mouse back to the both sides abdominal part 2To the syringe coating medicine-feeding of three groups of mices with the removal syringe needle, the equal administration 0.5ml of every Mus fixes with being about to mice, prevents from himself or lick mutually to bait.The cover that is fixed behind the assurance medicinal liquid absorption 1h is removed, and does corresponding experiment.Behind the percutaneous dosing 1h, good chemical irritant 0.6% acetum of configured in advance only is injected in the mouse peritoneal with 0.2ml/.Observe and write down mouse writhing number of times in 15 minutes.The results are shown in following table.
Table 6 Dichlorodiphenyl Acetate cause mouse writhing reaction influence (X ± SD, n=10)
Figure G2009100427152D00092
Annotate: compare with the blank group: * P<0.05, * * P<0.01
4.2 result
With normal saline group ratio, the external of total alkaloids in Semen Strychni liquid has significant inhibitory effect with preparation Dichlorodiphenyl Acetate induced mice writhing response, shows that this preparation has significant analgesia role.
Strychnine toxicity is extremely strong in the total alkaloids in Semen Strychni, might absorb the appearance poisoning by percutaneous.This product is the transdermal fluid external preparation, and the medicine percutaneous absorbs the administration area direct ratio with skin, and relevant with the kind of skin, human body administration area generally can not surpass 50cm yet 2, and the human body skin horny layer is thicker than rabbit skin keratin, and medicine percutaneous absorptance rabbit is slow.And this preparation is 100cm to administration area in the intact skin acute toxicity testing 2, the actual medication process of old friend's body can tolerate the concentration of total alkaloids in Semen Strychni can be higher.In sum, total alkaloids in Semen Strychni liquid external preparation shows that to intact skin acute toxicity testing and skin irritation test result preparation external preparation for skin administration safety of the present invention is better.Strychnos alkaloid liquid external preparation can significantly suppress the mice auricle swelling due to the dimethylbenzene, point out this preparation that the effect of obvious inhibition inflammatory swelling is arranged in early days in inflammation, can suppress hemorrhage in early days in tissue injury, acceleration is to the absorption of congestion, edema, help exudation and promote that damaged tissues restores as early as possible, have significant antiinflammatory action; Acetic acid induced mice writhing response is the result show: preparation of the present invention has significant analgesic activity.Above-mentioned experimental result shows that this preparation is safe in utilization effectively, has realized the re-set target of invention.
The specific embodiment
Following examples are intended to illustrate the present invention rather than limitation of the invention further, and the present invention can implement by the described any mode of summary of the invention.
Embodiment 1:
Total alkaloids in Semen Strychni 0.2g
Azone 5ml
Propylene glycol 30ml
Ethyl hydroxybenzoate 0.1g
Add water to 100ml
Total alkaloids in Semen Strychni is a principal agent in the prescription, and azone is penetrating promoter, and propylene glycol has penetrating promoter, preserve moisture and the effect of solvent, and ethyl hydroxybenzoate is an antiseptic, and water is solvent.
Precision takes by weighing total alkaloids in Semen Strychni and dissolves in the propylene glycol, adds azone and ethyl hydroxybenzoate; Add suitable quantity of water again to 100ml.To can make liniment or varnish in its Packaging Bottle of packing into; Pack into being spray in the aerosol container of special sprayer unit; Medicinal liquid is adsorbed with special dressing, and sealing promptly can be used as wet application.
Embodiment 2:
Total alkaloids in Semen Strychni 0.1g
Azone 5ml
Propylene glycol 10ml
Glycerol 35ml
Add water to 100ml
Total alkaloids in Semen Strychni is a principal agent in the prescription, and azone, propylene glycol are penetrating promoter, and glycerol has preserves moisture and antisepsis, and water is solvent.
Precision takes by weighing total alkaloids in Semen Strychni and dissolves in the propylene glycol, adds azone and glycerol; Add suitable quantity of water again to 100ml.To can make liniment or varnish in its Packaging Bottle of packing into; Pack into being spray in the aerosol container of special sprayer unit; Medicinal liquid is adsorbed with special dressing, and sealing promptly can be used as wet application.
Embodiment 3:
Total alkaloids in Semen Strychni 0.4g
Oleic acid 10ml
Propylene glycol 10ml
Ethanol 25ml
Glycerol 25ml
Add water to 100ml
Total alkaloids in Semen Strychni is a principal agent in the prescription, and oleic acid, propylene glycol are penetrating promoter, and glycerol has the effect of preserving moisture, and ethanol is antiseptic and solvent, and water is solvent.
Precision takes by weighing total alkaloids in Semen Strychni and dissolves in the ethanol, adds oleic acid, propylene glycol, glycerol; Add suitable quantity of water again to 100ml.To can make liniment or varnish in its Packaging Bottle of packing into; Pack into being spray in the aerosol container of special sprayer unit; Medicinal liquid is adsorbed with special dressing, and sealing promptly can be used as wet application.
Embodiment 4:
Total alkaloids in Semen Strychni 0.1g
Eucalyptus oil 2ml
Propylene glycol l0ml
Glycerol 35ml
Solubilizer is to 100ml
Total alkaloids in Semen Strychni is a principal agent in the prescription, and eucalyptus oil, propylene glycol are penetrating promoter, and glycerol has the effect of preserving moisture, and eucalyptus oil has the antiseptical effect, and water is solvent.
Precision takes by weighing total alkaloids in Semen Strychni and dissolves in the propylene glycol, adds eucalyptus oil; Add suitable quantity of water again to 100ml.To can make liniment or varnish in its Packaging Bottle of packing into; Pack into being spray in the aerosol container of special sprayer unit; Medicinal liquid is adsorbed with special dressing, and sealing promptly can be used as wet application.
Embodiment 5:
Total alkaloids in Semen Strychni 0.3g
Oleum menthae 5ml
Ethanol 30ml
Glycerol 25
Add water to 100ml
Total alkaloids in Semen Strychni is a principal agent in the prescription, and Oleum menthae, propylene glycol are penetrating promoter, and glycerol has the effect of preserving moisture, and ethanol has the antiseptical effect, and water is solvent.
Precision takes by weighing total alkaloids in Semen Strychni and dissolves in the ethanol, adds azone and glycerol; Add suitable quantity of water again to 100ml.To can make liniment or varnish in its Packaging Bottle of packing into; Pack into being spray in the aerosol container of special sprayer unit; Medicinal liquid is adsorbed with special dressing, and sealing promptly can be used as wet application.
Embodiment 6:
Total alkaloids in Semen Strychni 0.4g
Eucalyptus oil 5ml
Glycerol 25ml
Ethanol 25ml
Add ethanol to 100ml
Total alkaloids in Semen Strychni is a principal agent in the prescription, and eucalyptus oil has penetrating facilitation, and ethanol is as antiseptic 25ml, and simultaneously as solvent and have penetrating promotion and antisepsis concurrently, glycerol has the effect of preserving moisture.
Get in the biological adding of the semen strychni total adequate amount of ethanol, add eucalyptus oil and glycerol again, add ethanol, can make liniment or varnish in the Packaging Bottle of packing into to 100ml; Pack into being spray in the aerosol container of special sprayer unit; Medicinal liquid is adsorbed with special dressing, and sealing promptly can be used as wet application.
Embodiment 7:
Total alkaloids in Semen Strychni 0.4g
Azone 5ml
Glycerol 25ml
Ethanol 25ml
Add ethanol to 100ml
Total alkaloids in Semen Strychni is a principal agent in the prescription, and azone has penetrating facilitation, and ethanol is that solvent and anticorrosion ethanol are 25ml as antiseptic,, general needs to contain 20% above ethanol in medicinal liquid and can have anti-corrosion function.In addition, in the present embodiment ethanol also and have certain penetrating facilitation concurrently, glycerol has the effect of preserving moisture.
Get in the biological adding of the semen strychni total adequate amount of ethanol, add azone and glycerol again, add ethanol, can make liniment or varnish in the Packaging Bottle of packing into to 100ml; Pack into being spray in the aerosol container of special sprayer unit; Medicinal liquid is adsorbed with special dressing, and sealing promptly can be used as wet application.

Claims (9)

1. the liquid external preparation of total alkaloids in Semen Strychni preparation is prepared from by principal agent total alkaloids in Semen Strychni and proper supplementary material, it is characterized in that principal agent total alkaloids in Semen Strychni 0.1g≤total alkaloids in Semen Strychni≤200g; The content of strychnine is less than 40% in the total alkaloids in Semen Strychni, and strychnine content is greater than 20%;
Adjuvant is:
10ml≤penetrating promoter≤2000ml
0≤wetting agent≤3000ml
0.5g≤antiseptic≤50g or 1000ml≤antiseptic≤3500ml
Solubilizer is to 10000ml.
2. the liquid external preparation of total alkaloids in Semen Strychni preparation according to claim 1 is characterized in that 1000ml≤wetting agent≤3000ml.
3. the liquid external preparation of total alkaloids in Semen Strychni preparation according to claim 1 is characterized in that described solvent is constituted jointly by following one or more: water, glycerol, ethanol, propylene glycol, Polyethylene Glycol, ethyl acetate, vegetable oil.
4. the liquid external preparation of total alkaloids in Semen Strychni preparation according to claim 1 is prepared from by principal agent total alkaloids in Semen Strychni and proper supplementary material, it is characterized in that principal agent total alkaloids in Semen Strychni 1g≤total alkaloids in Semen Strychni≤40g; Adjuvant is:
5. according to the liquid external preparation of claim 1 or 2 or 3 or 4 described total alkaloids in Semen Strychni preparations, it is characterized in that described penetrating promoter is constituted jointly by following one or more: (1) azone; (2) menthol, Camphora, Oleum menthae, eucalyptus oil, Borneolum Syntheticum; (3) ethanol, isopropyl alcohol, isobutanol, n-dodecanol, propylene glycol, glycerol, ethyl acetate; (4) oleic acid, lauric methyl ester or ethyl ester, isopropyl myristate.
6. the liquid external preparation of total alkaloids in Semen Strychni preparation according to claim 5 is characterized in that described penetrating promoter is azone, propylene glycol, eucalyptus oil or Oleum menthae.
7. according to the liquid external preparation of claim 1 or 2 or 3 or 4 described total alkaloids in Semen Strychni preparations, it is characterized in that described wetting agent is constituted jointly by following one or more: glycerol, propylene glycol, Polyethylene Glycol, sorbitol; Described antiseptic is constituted jointly by following one or more: Nipagin ester, benzoic acid and salt thereof, sorbic acid and salt thereof; Ethanol, glycerol; Eucalyptus oil, Oleum menthae.
8. the liquid external preparation of total alkaloids in Semen Strychni preparation according to claim 1 is characterized in that described dosage form is spray, liniment, varnish or wet application.
9. the liquid external preparation of total alkaloids in Semen Strychni preparation according to claim 4 is characterized in that 10g≤total alkaloids in Semen Strychni≤30g, 100ml≤azone≤500ml, 200ml≤propylene glycol≤1000ml, 2000ml≤glycerol≤3000ml adds water to 10000ml again.
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CN101804096B (en) * 2010-02-08 2011-11-09 南京中医药大学 Method for extracting purified total alkaloid of strychnos nux-vomica and application thereof in pharmacy
CN102949450B (en) * 2012-11-27 2014-08-20 湘潭大学 Nux vomica alkaloid patch for treating local myalgia and arthralgia and preparation method
CN106692112B (en) * 2016-12-06 2019-07-16 湘潭大学 A kind of strychnia patch for treating local soft tissue inflammatory pain
CN112870255A (en) * 2021-03-22 2021-06-01 内蒙古医科大学 Mongolian medicine film coating agent for treating peripheral facial paralysis and preparation method thereof

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CN1718190A (en) * 2004-07-09 2006-01-11 蔡宝昌 Nux vomica alkaloid liposome, and its prepn. method

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CN1718190A (en) * 2004-07-09 2006-01-11 蔡宝昌 Nux vomica alkaloid liposome, and its prepn. method

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