CN1806823B - Externally applied wind-expelling Chinese medicinal composition plaster - Google Patents
Externally applied wind-expelling Chinese medicinal composition plaster Download PDFInfo
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Abstract
The invention relates to an externally applied wind-expelling Chinese medicinal composition plaster, which is prepared clove basil oil, methyl salicylate, Radix Cinnamomi Camphorae oil, Cinnamomum cassia oil, cinnamic aldehyde, geranialdehyde, borneo camphor and specific hydrophilic base materials.
Description
[technical field] the present invention relates to a kind of Chinese medicine composition plaster of external, more particularly, the present invention relates to a kind of Chinese medicine composition plaster of externally applied wind-expelling, this plaster is to be medicine activity component by Oleum Ocimi Gratissimi, methyl salicylate, JIANGZHANGYOU, Oleum Cinnamomi, cinnamic aldehyde, citral, Borneolum Syntheticum, after being mixed and made into ointment with an amount of hydrophilic matrix, it is applied to backing and overlay film forms, this hydrophilic matrix mainly is made up of polymer binder, filler, wetting agent, cross-linking agent, organic acid regulator, surfactant and water.The main outer treatment that is used for rheumatic ostalgia, osteopatia sprain, headache due to invasion of exogenous pathogens, skin pruritus of this Chinese medicine composition plaster belongs to the field of Chinese medicines.
Classical medicament-safflower oil that [background technology] used as wind dispelling at present is stated from Drug Standard of Ministry of Public Health of the Peoples Republic of China " the 14th in Chinese traditional patent formulation preparation ", and its active medicine component is Oleum Ocimi Gratissimi, methyl salicylate, JIANGZHANGYOU, Oleum Cinnamomi, cinnamic aldehyde, citral, Borneolum Syntheticum.Wherein, Oleum Ocimi Gratissimi is the volatile oil of basil Flos Caryophylli, has the acaricide of killing effect; Methyl salicylate is antiinflammatory, analgesic, and the part is used for joint or myalgia, has antiinflammatory, pain relieving, repercussive effect; Oleum Cinnamomi is the volatile oil that extracts from the cinnamomic dry bark of canella, it has bacteriostasis to gram positive bacteria and fungus, 75%～95% is cinnamic aldehyde in the middle of the Oleum Cinnamomi, cinnamic aldehyde has the effect of central and tip blood vessel dilating, and clear and definite dispersing cold for relieving pain, the effect of promoting blood circulation to remove obstruction in the collateral are arranged; Borneolum Syntheticum has the effect of the refreshment of having one's ideas straightened out, clearing away heat to alleviate pain.Safflower oil is as a kind of external oiliness liniment, absorbs by transdermal penetration, can invigorate blood circulation, antiinflammatory, analgesia, and local vascular is had dilating effect, and it is fine to be used for the arthralgia effect that articular sprain and cold-damp cause.
Yet the former dosage form of safflower oil is a liniment, and preparation technology is: add recipe quantity Oleum Ocimi Gratissimi, methyl salicylate, JIANGZHANGYOU, Oleum Cinnamomi, cinnamic aldehyde, citral, Borneolum Syntheticum, add the amount of colorant mixing, quantitative with vegetable oil, filtration forms.Its character of HONGHUAYOU CAJI is an oily liquids, in use embrocates in the affected part, and every day 4～6 times, not only easy pollution clothes, and daily requirement multiple dosing use extremely inconvenience, thereby make patient's compliance relatively poor.In addition, the volatilization of medicine in use not only influenced preparation itself stability, caused waste, the environment around also having polluted has simultaneously influenced patient's use, finally influences the therapeutic effect of medicine.
In order to reduce the drug volatilization loss, improve practicality, the convenience of pharmaceutical preparation, solve the inconvenience of multiple dosing on the one, improve the compliance of patient's medication, it is prepared into emplastrum, be one and well select.
Diseases such as normal conditions, external curing are sprained, damage, arthralgia are many with the plaster applying method.Plaster has also experienced from black plaster, plaster " need not pre-thermal softening, can the long period keep viscosity, not pollution clothes " to rubber plaster from " warm melting of time spent is affixed on the affected part " that begins to the change of rubber plaster during use in vain.But because the influence of anaphylactogen such as natural rubber and viscosifier in the rubber-type substrate, regular meeting causes red swelling of the skin, itches when patient uses, and causes interruption of the administration; Secondly, the viscosity of rubber-type substrate products made thereby is big, and it is strong to peel off pain, and the patient is difficult for accepting; In addition, when the preparation plaster, product needed causes medicine to destroy or volatilization through the drying tunnel drying, lessens the curative effect, and uses a large amount of organic solvents because of in producing, and production equipment and labor protection are had relatively high expectations, and also can pollute environment.In sum, rubber-emplastrum is not suitable for doing technology popularization widely.
Along with progress of science and technology, research worker is in order to overcome the shortcoming of above-mentioned plaster, developed novel external plaster substrate based on hydrophilic high molecular material, this type of hydrophilic matrix plaster need not use a large amount of organic solvents, not irritated, non-stimulated, sweat proof, skin followability are good, tear-off not pain, do not have the epilation phenomenon, be well suited for the more people of fine hair and use, and can take off subsides repeatedly, easy to use.This type of hydrophilic matrix plaster is early used in Japan.The Pharmacopoeia of the People's Republic of China one one of version in 2000 has also been included this substrate plaster, it is defined as cataplasma, behind the hydrophilic matrix mixing that is meant medicinal substances extract, medicine and suits, be coated with and be laid on the external preparation of making on the cloth, English name is cataplasm.
Medicine activity component in the safflower oil is made crust cloth cream as if combining with the hydrophilic matrix of subsensitivety, not only solves the inconvenience of multiple dosing on the one, improves practicality, the convenience of pharmaceutical preparation, also improves the compliance of patient's medication.As the water soluble plaster of external preparation for skin, the speed of drug release and absorption has speed with the different of substrate, and the affine degree of medicine in hypothallus is very big to the drug effect influence.One: must possess good preparation stability, this needs medicine and substrate that stronger affinity is arranged; Its two, the affinity of medicine and substrate size directly influences the Transdermal absorption effect of medicine.Usually substrate is low more to the affinity of medicine, helps the release and the absorption of medicine more.Yet the medicine of safflower oil all is oil soluble liquid, how to make itself and water-soluble base stablize coexistence, and medicine can comparatively fast be discharged from substrate, gives full play to drug effect, becomes the problem difficult point that the present invention need solve.
At present, more and more many to the basic research of hydrophilic matrix plaster both at home and abroad, but make not appearing in the newspapers as yet of plaster for the oil soluble liquid medicine is written into hydrophilic matrix.In the domestic patent, for example 02112475.2,99103062.1,98102336.3 mainly is research to novel hydrophilic substrate, does not relate to the application of concrete medicine, remains further conclusive evidence.US6485740 (methotrexate), US6355266 (indomethacin) appear in the newspapers as the hydrophilic plaster treatment rheumatism of Western medicine, arthritic patent.Now, the hydrophilic plaster is used more in Japanese Korea S, main carrying chemical drugs, nonsteroidal antiinflammatory drug for example, but this preparation is also rare in the application of the field of Chinese medicines, though the domestic research bibliographical information that has many about Chinese medicine, chemicals crust cloth cream, through State Food and Drug Administration's approval listing only have the compound recipe cercis to disappear to hinder crust cloth cream, the Moschus blood stasis dispelling clings to cloth cream.The muscles and bones king that has of approval clinical research at present clings to cloth cream, clings to cloth cream through not clinging to cloth cream, grieved crust cloth cream, the spiced crust of ten thousand spirits cloth cream, the pain that disappears bitterly.This shows in view of oil-based liquid is written into difficulty of hydrophilic matrix, how the domestic cataplasma of declaring also adds with Chinese medicine extract, Shang Weiyou prepares the open report of oil-based liquid crust cloth cream.
For the research of hydrophilic matrix, domestic patent disclosure 03111657.4---insoluble drug transdermal absorption formulation and preparation technology thereof.This patent disclosure a kind of insoluble drug at first is prepared into microemulsion, mix then and make the water-based patch with substrate, its matrix group becomes: 4～6 parts of high molecular polymers, 0.1～0.4 part of cross-linking agent, 0.1～0.5 part of organic acid, 5～40 parts of wetting agents, 30～50 parts of distilled water, 3～5 parts of penetration enhancers.After medicine activity component of the present invention was written into above-mentioned blank substrate, maximum also only can be stablized and is written into 1.8 weight portions, and is less relatively because of the carrying oil mass, is difficult to the Concentraton gradient that reaches higher, thereby limited the Transdermal absorption of medicine.
The inventor is when addressing this problem, pass through campaign, a large amount of matrix formulations is screened, from host material commonly used, filter out the specific hydrophilic matrix of a cover, this hydrophilic matrix, form stable tridimensional network by the solids strong adsorption in polyacrylic acid and salt and the filler, be aided with the gelatin figuration, pin oil content, thereby chemical crosslinking mode in addition improves the pliability of ointment, obviously improved the carrying oil mass, made that the content of medicine activity component improves on the unit are, fully, brought into play the pharmacological action of medicine activity component enduringly.Plaster of the present invention had both solved the galenic pharmacy stable problem of medicine activity component in substrate, make the suitable partition coefficient of medicine tool between substrate/skin layer again, make medicine activity component from substrate, to discharge very soon, see through skin, thereby arrive focus rapidly, and can discharge medicine with constant rate of speed for a long time, further increase the transdermal amount, lasting performance curative effect has improved bioavailability of medicament to a great extent, has reached beyond thought therapeutic effect.
[summary of the invention] the invention provides with the safflower oil Chinese medicine is the substrate composition and the preparation technology thereof of the hydrophilic matrix plaster of active component, this substrate is formed and effectively have been improved active medicine component in the safflower oil and be written into preparation stability problem in the hydrophilic matrix, and experimental studies have found that by transdermal test in vitro, this substrate has obviously strengthened the drug transdermal absorbent properties, thereby significantly improved medication effect, stick experiment by volunteer's human body, the patient uses the compliance height, drug effect is fast, the drug effect performance is lasting, and this Chinese medicine composition plaster clinical therapeutic efficacy significantly is better than the plaster of the preparation of substrate described in liniment and the documents.
Chinese medicine composition plaster of the present invention is made up of medicine activity component, hydrophilic matrix and carrier.Carrier is meant backing and isolating membrane.
This paper is described below in more detail to the present invention: plaster of the present invention is made up of three-decker:
(i) backing layer: backing can be the blended cloth or the non-woven fabrics of all cotton fabric, chemical fiber cloth, cotton and chemical fibre
(ii) ointment layer: the hydrophilic matrix layer that promptly contains the medicine active component
(iii) isolating membrane: i.e. the peel ply material that should throw off before being attached on the skin of one deck can be nontoxic polyethylene or polypropylene film, silicone oil paper.
A kind of external medicine composition plaster of the present invention, this plaster is to be medicine activity component by Oleum Ocimi Gratissimi, methyl salicylate, JIANGZHANGYOU, Oleum Cinnamomi, cinnamic aldehyde, citral, Borneolum Syntheticum, be mixed and made into behind the ointment medicament that it is applied to backing and overlay film and makes with substrate, it is to be mixed and made into by containing clinical treatment effective dose of medicine thing active component and hydrophilic matrix for wherein said ointment.
This Chinese medicine composition plaster is characterized in that: the hydrophilic matrix in the medicated layer is to be made of polymer binder, filler, wetting agent, cross-linking agent, organic acid regulator, surfactant and water, and this plaster Chinese medicine active component is enhanced by hydrophilic matrix to the transdermal penetration and the adhesion of health.Now that each component composition and consumption division is as follows:
In the ointment layer, polymer binder described in the hydrophilic matrix is meant the mixture of acrylic homopolymer and copolymer and natural glue or itself and natural glue, vinyl-based homopolymer and copolymer, described acrylic homopolymer and copolymer are preferably polyacrylic acid and/or polyacrylate, and described natural glue is preferably the mixture of gelatin or itself and Resina persicae and/or arabic gum; Described vinyl-based homopolymer and copolymer are preferably polyvinyl alcohol and/or polyvidone.Polymer binder accounts for 1～10 part in weight portion and is advisable in whole hydrophilic matrix, wherein acrylic homopolymer and copolymer should be advisable at 0.5～5 part, be preferably 2～3.5 parts, if greater than 5 parts, Zhi Bei mastic thickness then unfavorablely is coated with exhibition, if be lower than 0.5 part, then mastic is rarer, can not form rheid, and the plaster molding effect is poor.The natural glue consumption is preferably 0.5～5 part, and wherein the gelatin consumption should be at 0.5～3.5 part, and the excipient effect of gelatin is better in this scope, surface viscosity can be regulated by 0～3.5 part plant gum consumption, because plant gum is a polysaccharide, can effectively improve the mastic surface viscosity, strengthen applicating property.Vinyl-based homopolymer and copolymer consumption are preferably 0.5～3 part.
Described in its hydrophilic matrix filler be meant water-insoluble inorganic salts, comprise Kaolin, titanium dioxide, zinc oxide, consumption is 0.2～3.0 part, is preferably 0.5～1.5 part;
Described in its hydrophilic matrix wetting agent be meant one or more mixing in the polyhydric alcohol, its described polyhydric alcohol comprises propylene glycol, glycerol, sorbitol, Polyethylene Glycol.Wetting agent accounts for 10～50 parts in weight portion and is advisable in whole hydrophilic matrix, be preferably 15～35 parts, and wetting agent is higher than 50 parts, can cause the skin surface greasy feeling or be pasted with coolness, is lower than 10 parts, and product can't keep enough moisture content.
Described in its hydrophilic matrix cross-linking agent be meant metallic aluminium salt, comprise aluminium hydroxide, aluminum glycinate, cross-linking agent accounts for 0.05～0.5 part in weight portion in whole hydrophilic matrix, be preferably 0.05～0.3 part and be advisable;
Organic acid regulator described in its hydrophilic matrix comprises tartaric acid, citric acid, and consumption is 0.1～1 part, and preferable amount is 0.1～0.6 weight portion;
Surfactant described in its hydrophilic matrix can be selected and can comprise polyoxyethylene sorbitan monoleate at the emulsifying agent of aqueous phase with oily emulsifying formation O/W, and its consumption is 0.5～8 part;
The scope of moisture is 40～75 parts, is preferably 50～65 parts; When water content during greater than 75 parts, the gained mastic easily oozes cloth, leaks cream, and when water content less than 40 parts time the, gained mastic viscosity height, stretchability is poor, and the plaster skin followability of preparation is poor, easily comes off.
Hydrophilic matrix can also comprise penetration enhancer in forming, as ethanol; Pharmaceutics field typical additives such as aromatic and antiseptic commonly used, antioxidant, coloring agent.
Externally-applied medicinal composition plaster of the present invention, its described medicine activity component can be the product of above-mentioned each medicine activity component through cyclodextrin inclusion compound or part enclose; Externally-applied medicinal composition plaster of the present invention, the mixture that its described medicine activity component can be above-mentioned each medicine activity component is through the product of lipid enclose or part enclose; Externally-applied medicinal composition plaster of the present invention, the mixture that its described medicine activity component can also be above-mentioned each medicine activity component is through the product of microencapsulation or part microencapsulation.
Illustrate the present invention in more detail by following embodiment, but the invention is not restricted to these embodiment.
Indicate: 1, in the following example each material consumption all in weight portion;
2, medicinal mixture consists of: Oleum Ocimi Gratissimi: methyl salicylate: JIANGZHANGYOU: Oleum Cinnamomi: cinnamic aldehyde: citral: Borneolum Syntheticum=56.4ml: 37.2ml: 1.07ml: 2.13ml: 2.13ml: 1.07ml: 0.23g;
3, wherein comparative example (China: the protection domain of independent claims is determined each amounts of components application number 03111657.4) according to documents.
Comparative example 1:
Sodium polyacrylate 5
Glycerol 35
Aluminium hydroxide 0.2
Tartaric acid 0.3
NMP 5
Water 48.5
Medicine activity component 1.5
Polyoxyethylene sorbitan monoleate 4
Preparation technology: aluminium hydroxide is added in the glycerol, fully disperse, add sodium polyacrylate again, mix forming gel, be the A phase; Again medicine activity component, NMP are mixed into B mutually with Tween 80; Tartaric acid is soluble in water, with tartaric aqueous solution add B mutually in, 50 ℃ are emulsified into the C phase; At last C is added to the A phase, the limit edged firmly stirs, and finally forms the ointment transparent, that viscosity is moderate, then it is coated with exhibition, 30 ℃ and is drying to obtain plaster.
Phenomenon: said preparation is more stable, the no oil droplet in mastic surface; If medicine activity component＞1.5 part, then the preparation room temperature is placed unstablely, has oil droplet to manifest.
Comparative example 2:
Sodium polyacrylate 4
Glycerol/polyethylene glycol 35/5
Aluminium hydroxide 0.3
Citric acid 0.1
Azone 5
Water 47.6
Medicine activity component 1.8
Polyoxyethylene sorbitan monoleate 4
Preparation technology: aluminium hydroxide is added in the glycerol/polyethylene glycol, fully disperse, add sodium polyacrylate again, mix forming gel, be the A phase; Again medicine activity component, Azone are mixed into B mutually with Tween 80; Citric acid is soluble in water, with the citron aqueous acid add B mutually in, 50 ℃ are emulsified into the C phase; At last C is added to the A phase, the limit edged firmly stirs, and finally forms the ointment transparent, that viscosity is moderate, then it is coated with exhibition, 30 ℃ and is drying to obtain plaster.
Phenomenon: said preparation is more stable, the no oil droplet in mastic surface, if medicine activity component＞1.8 part, then the preparation room temperature is placed instability, has oil droplet to manifest.
Comparative example 3:
Sodium polyacrylate 6
Glycerol/polyethylene glycol 35/5
Aluminium hydroxide 0.4
Citric acid 0.3
Polyoxyethylene sorbitan monoleate 5
Water 48
Medicine activity component 1.5
Preparation technology is with comparative example 2.
Phenomenon: said preparation is more stable, the no oil droplet in mastic surface, if medicine activity component＞1.5 part, then the preparation room temperature is placed instability, has oil droplet to manifest.
Embodiment 1:
Sodium polyacrylate 2
Polyacrylic acid 2
Gelatin 1.5
Glycerol 18
Sorbitol 7
Propylene glycol 10
Tartaric acid 0.5
Aluminium hydroxide 0.25
Active medicine component 2
Titanium dioxide 0.8
Polyoxyethylene sorbitan monoleate 2.5
Water 45
Ethanol 6
Preparation technology:
Polyacrylic acid and sodium salt thereof, aluminium hydroxide, titanium dioxide are uniformly dispersed with glycerol, propylene glycol, ethanol and make A mutually;
Get the recipe quantity active medicine component, add the polyoxyethylene sorbitan monoleate premix, make the B phase;
Other gets gelatin, sorbitol, tartaric acid and dissolves in 50 ℃ of suitable quantity of water, makes the C phase;
B is carried out emulsifying mutually with C, then emulsion is added the A phase, stir 2 hours promptly.Even mastic is applied on the non-woven fabrics,
30 ℃ of dryings, overlay film make water solublity Chinese medicine composition plaster.
Embodiment 2:
Polyacrylic acid 2.5
Gelatin 1.5
Resina persicae 2.5
Glycerol 22
Tartaric acid 0.3
Aluminium hydroxide 0.15
Kaolin 3
Active medicine component 8
Polyoxyethylene sorbitan monoleate 6
Water 55
Preparation technology:
Polyacrylic acid, aluminium hydroxide, Kaolin is uniformly dispersed with glycerol makes A mutually;
Get the recipe quantity active medicine component, add the polyoxyethylene sorbitan monoleate premix, make the B phase;
Other gets gelatin, Resina persicae, tartaric acid and dissolves in 50 ℃ of suitable quantity of water, makes the C phase;
B is carried out emulsifying mutually with C, then emulsion is added the A phase, stir 2 hours promptly.Even mastic is applied on the non-woven fabrics, and dry, overlay film make water solublity Chinese medicine composition plaster.
Embodiment 3:
Polyacrylic acid 2.5
Gelatin 1.5
Resina persicae 2.5
Polyethylene Glycol 7
Propylene glycol 15
Tartaric acid 0.3
Aluminium hydroxide 0.15
Kaolin 1.5
Active medicine component 5
Polyoxyethylene sorbitan monoleate 3
Water 56
Preparation technology:
Polyacrylic acid, aluminium hydroxide, Kaolin is uniformly dispersed with Polyethylene Glycol, propylene glycol makes A mutually;
Get the recipe quantity active medicine component, add the polyoxyethylene sorbitan monoleate premix, make the B phase;
Other gets gelatin, Resina persicae, tartaric acid and dissolves in 50 ℃ of suitable quantity of water, makes the C phase;
B is carried out emulsifying mutually with C, then emulsion is added the A phase, stir 2 hours promptly.Even mastic is applied on the non-woven fabrics, and dry, overlay film make water solublity Chinese medicine composition plaster.
Embodiment 4:
Sodium polyacrylate 1.5
Gelatin 3
Polyvinyl alcohol 2
Sorbitol 15
1,3 butylene glycol 12
Tartaric acid 0.2
Aluminium hydroxide 0.1
Titanium dioxide 1.2
Active medicine component 3.5
Polyoxyethylene sorbitan monoleate 1
Water 60
Preparation technology:
Sodium polyacrylate, titanium dioxide, aluminium hydroxide be uniformly dispersed with 1,3 butylene glycol make A mutually;
Get the recipe quantity active medicine component, add the polyoxyethylene sorbitan monoleate premix, make the B phase;
Other gets gelatin, polyvinyl alcohol, sorbitol, tartaric acid and dissolves in 50 ℃ of suitable quantity of water, makes the C phase;
B is carried out emulsifying mutually with C, then emulsion is added the A phase, stir 2 hours promptly.Even mastic is applied on the non-woven fabrics, and dry, overlay film make water solublity Chinese medicine composition plaster.
Embodiment 5:
Sodium polyacrylate 1.5
Gelatin 0.6
Polyvinyl alcohol 2
Sorbitol 15
Glycerol 12
Tartaric acid 0.2
Aluminum glycinate 0.1
Titanium dioxide 0.2
Kaolin 1.3
Active medicine component 5
Polyoxyethylene sorbitan monoleate 3
Water 67
Preparation technology:
Sodium polyacrylate, titanium dioxide, Kaolin, aluminum glycinate be uniformly dispersed with glycerol make A mutually;
Get the recipe quantity active medicine component, add the polyoxyethylene sorbitan monoleate premix, make the B phase;
Other gets gelatin, polyvinyl alcohol, sorbitol, tartaric acid and dissolves in 50 ℃ of suitable quantity of water, makes the C phase;
B is carried out emulsifying mutually with C, then emulsion is added the A phase, stir 2 hours promptly.Even mastic is applied on the non-woven fabrics, and dry, overlay film make water solublity Chinese medicine composition plaster.
Preparation method is with embodiment 4.
Embodiment 6:
CBP 941 3
Polyvidone 1
Gelatin 1.4
Arabic gum 0.5
Propylene glycol 10
Sorbitol 5
Citric acid 0.6
Aluminium hydroxide 0.3
Zinc oxide 0.5
Active medicine component 3
Polyoxyethylene sorbitan monoleate 1
Water 72
Preparation technology:
CBP 941, aluminium hydroxide, zinc oxide be uniformly dispersed with propylene glycol make A mutually;
Get the recipe quantity active medicine component, add the polyoxyethylene sorbitan monoleate premix, make the B phase;
Other gets gelatin, arabic gum, polyvidone, sorbitol, citric acid and dissolves in 50 ℃ of suitable quantity of water, makes the C phase;
B is carried out emulsifying mutually with C, then emulsion is added the A phase, stir 2 hours promptly.Even mastic is applied on the non-woven fabrics, and dry, overlay film make water solublity Chinese medicine composition plaster.
Embodiment 7:
The alcohol liposome preparation: the lecithin with 2 grams is dissolved in the dehydrated alcohol of 15 grams earlier, then add the medicine of 5 grams and the mixture of 3 gram polyoxyethylene sorbitan monoleates, be stirred to evenly, under the lasting stirring of hermetic container, adding 20 gram water slowly joins in the alcoholic solution, continue to stir 5 minutes, 30 ℃ of whole process constant temperature are chilled to room temperature then and promptly get the safflower oil alcohol liposome.
Polyacrylic acid 3
Polyvidone 0.5
Gelatin 2
Glycerol 5
Sorbitol 5
Tartaric acid 0.8
Aluminium hydroxide 0.4
Water 40
Titanium dioxide 0.5
Safflower oil alcohol liposome solution 45 (being equivalent to active medicine component 5g)
Sorbic acid 0.2
Preparation technology:
Polyacrylic acid, aluminium hydroxide, titanium dioxide is uniformly dispersed with glycerol makes A mutually;
Other gets gelatin, polyvidone, sorbitol, tartaric acid and dissolves in 50 ℃ of water, makes the B phase;
B is added to the A phase, stirs, then add the alcohol liposome that has prepared, it is even to continue to be stirred to mastic, and mastic is applied on the non-woven fabrics, and cold drying, overlay film make water solublity Chinese medicine composition plaster.
Embodiment 8:
Flexible multiphasic liposomes preparation: the lecithin with 2 grams is dissolved in the acetone of 40 grams earlier, and then 50 ℃ of reduction vaporizations get phospholipid membrane; Next is got, and dispersing and dissolving gets the A phase in sodium cholate 1 gram, polyoxyethylene sorbitan monoleate 3 grams, the safflower oil 5 gram addings 10 gram dehydrated alcohol; Other get polyvidone 2 gram be dissolved in 50 ℃ of water the B phase, with A be added to 50 ℃ of B mutually in first emulsifying, then emulsion is added, established phospholipid membrane is disperseed, promptly get the safflower oil flexible lipidosome.
Polyacrylic acid 3
Gelatin 2
Glycerol 5
Sorbitol 5
Tartaric acid 0.8
Aluminium hydroxide 0.4
Water 40
Kaolin 0.8
Safflower oil flexible lipidosome solution 63 (being equivalent to active medicine component 5g)
0.2
Preparation technology:
Polyacrylic acid, aluminium hydroxide, Kaolin, sorbic acid be uniformly dispersed with glycerol make A mutually;
Other gets gelatin, tartaric acid, sorbitol and dissolves in water, makes the B phase;
B is added to the A phase, stirs, then add alcohol liposome, it is even to continue to be stirred to mastic, and mastic is applied on the non-woven fabrics, and cold drying, overlay film make water solublity Chinese medicine composition plaster.
Embodiment 9:
The preparation of cyclodextrin clathrate: adopt saturated water solution method, feed intake at 8: 1 according to cyclodextrin and medicine, carried out enclose 1.5 hours in 40 ℃ of constant temperature magnetic agitation, stop heating, continuous stirring, to be cooled to room temperature, be transferred to refrigerator (0～4 ℃) cold preservation, leave standstill 24 hours, centrifugal, 40 ℃ of dryings 1 hour promptly.The clathrate recovery rate is 83%.
Poly propenoic acid sodium acrylate 2/0.5
Gelatin 2
Ethanol 5
Sorbitol 10
Polyvidone 1.5
Tartaric acid 0.1
Aluminium hydroxide 0.05
Medicine cyclodextrin clathrate 7.5 (being equivalent to active medicine component 1g)
Titanium dioxide 1.0
Active medicine component 4
Polyoxyethylene sorbitan monoleate 0.5
Water 65
Sorbic acid 0.2
Preparation technology:
Gelatin, sorbitol, polyvidone, tartaric acid are dissolved into the A phase in suitable quantity of water; Medicine is mixed into B mutually with tween; Poly propenoic acid sodium acrylate, aluminium hydroxide, pharmaceutical pack compound, sorbic acid that other gets recipe quantity are uniformly dispersed into C mutually with glycerol; At last, with A and B emulsifying mutually, add then C mutually in, stir 2 hours promptly.Even mastic is applied on the non-woven fabrics, and dry, overlay film make.The mode that this method adopts cyclodextrin inclusion compound to combine with emulsifying is written into medicine, has not only reduced the volatilization of medicine, and rapid release is combined well with slow release, and onset is rapid, lasting medicine thereby reach, and has brought into play therapeutical effect better.
Embodiment 10:
Poly propenoic acid sodium acrylate 1/1.5
Gelatin 1.8
Glycerol 5
Sorbitol 10
Polyvidone 0.5
Tartaric acid 0.1
Aluminium hydroxide 0.05
Zinc oxide 1.5
Active medicine component 5.0
Cyclodextrin 4
Polyoxyethylene alkylphenol 2.5
Water 68
Sorbic acid 0.2
Preparation technology:
Gelatin, sorbic acid, polyvidone, tartaric acid are dissolved into the A phase in suitable quantity of water; Add A mutually with behind medicine, polyoxyethylene alkylphenol and the polyoxyethylene sorbitan monoleate premix; Poly propenoic acid sodium acrylate, aluminium hydroxide, zinc oxide, cyclodextrin, sorbic acid that other gets recipe quantity are uniformly dispersed into C mutually with glycerol, at last A, B mixed phase solution are added C mutually in, stir 2 hours promptly.Even mastic is applied on the non-woven fabrics, and dry, overlay film make.
Embodiment 11:
The preparation of medicament microcapsule: adopt complex coacervation to prepare microcapsule.The thing of getting it filled is an amount of, add to join in Arabic official's solution (4%) after a small amount of polyoxyethylene sorbitan monoleate grinds evenly and stir, the gelatin solution (4%) that adds equivalent again, be warming up to about 50 ℃, regulate pH as for 4.0～4.5 with acetic acid, stir 10min, add and use small amount of ethanol dissolved polyacrylic resin IV number, after stirring 30min, add and the isothermal 3 times of distilled water of system, microscopy is observed the sedimentation Tibetan household slave and is become situation, after the satisfaction, system naturally cools to room temperature, the reuse ice bath is cooled to rapidly below 10 ℃, with leaving standstill 24 hours behind the malonaldehyde curing 2h, makes its abundant sedimentation, filter, wash with water to no aldehyde flavor, with the microcapsule lyophilization of gained promptly, wherein, the weight ratio of medicine and glue has only elects 1: 4 as, is preferably 0.15: 1 with the weight ratio of glue polyacrylic resin IV number.This legal system is equipped with microcapsule, and to get recovery rate be 89.3%.
Poly propenoic acid sodium acrylate 2/1
Gelatin 2.5
Glycerol 15
Polyvidone 3
Tartaric acid 0.1
Aluminium hydroxide 0.05
Medicament microcapsule 11.2 (being equivalent to active medicine component 2g)
Tween65 0.3
Active medicine component 3
Water 48
Sorbic acid 0.2
Titanium dioxide 0.2
Preparation technology: gelatin, polyvidone, tartaric acid are dissolved into the A phase in suitable quantity of water; To add A mutually behind medicine and the polyoxyethylene sorbitan monoleate premix; Poly propenoic acid sodium acrylate, aluminium hydroxide, sorbic acid, medicament microcapsule, active medicine component that other gets recipe quantity are uniformly dispersed into C mutually with glycerol, at last A, B mixed phase solution are added C mutually in, stir 2 hours promptly.Even mastic is applied on the non-woven fabrics, and dry, overlay film make.
The mode that said method adopts microcapsule to combine with emulsifying is written into medicine, has not only reduced the volatilization of medicine, and rapid release is combined well with slow release, and onset is rapid, lasting medicine thereby reach, and brings into play therapeutical effect better.
Chinese medicine composition plaster of the present invention is in in-vitro percutaneous permeability experiment, compare with liniment, show tangible medicine reinforced effects, even do not add under the situation of any penetration enhancer, still obtained good transdermal effect, improved the infiltration capacity of medicine activity component more significantly than prior art, and, after adding penetration enhancer, making percutaneous absorb further increases.
The in-vitro percutaneous permeability experiment of being carried out among the present invention is as follows:
Franz diffusion cell method: content of dispersion is close, but adopt the plaster of different modes preparations such as emulsifying, cyclodextrin inclusion compound, liposome, microcapsule to carry out the transdermal test: the little Corium Mus of the processing of learning from else's experience is fixed in sample cell and accepts between the pond, the plaster of embodiment 1,3,5,7～11 is affixed on mice cornu cutaneum matter aspect respectively, acceptable solution is 30% pure normal saline solution, the fixed sample pond.Constant temperature (32 ± 0.5) ℃, respectively at sampling in 2,4,6,8,10,12,24 hours, each sampling amount is 0.5ml, and the fresh reception liquid of additional equal-volume, the drug level of eugenol and methyl salicylate in the employing HPLC method mensuration reception liquid, thereby the accumulation transmitance of the Chinese medicine of respectively writing out a prescription, the result shows as table: this experimental result shows: compare with HONGHUAYOU CAJI, the onset of Chinese medicine composition plaster is more rapid, topical remedy's penetrating concentration is higher, and its curative effect obviously is better than HONGHUAYOU CAJI.Hence one can see that, and Chinese medicine composition plaster of the present invention adopts described specific water soluble substrate, not only promotes drug transdermal to absorb, and transdermal effect significantly is better than existing preparation-HONGHUAYOU CAJI.
Table 1
Embodiment 18: clinical drug effect evaluation
For evaluating Chinese medicine composition plaster of the present invention and HONGHUAYOU CAJI in the difference aspect the curative effect, we have carried out clinical observation to 72 routine arthralgia volunteers, now the result is reported as follows: selected volunteer's age is 18 years old～65 years old, do not have the other factors that influences drug evaluation and (comprise blood, liver, cardiovascular disease or other pathological changes, do not accept other drug such as analgesic, NSAID (non-steroidal anti-inflammatory drug) and muscle relaxant treatment and naturopathy simultaneously), clear and definite arthralgia is arranged, the patient that should understand to some extent clinical verification.Employing own control research, the treatment group is the Chinese medicine composition plaster, and the treatment medicine press embodiment 1 and is prepared, and usage is to be administered once in per 12 hours, sticks in the articular surface of getting involved 1 week of the course of treatment; Matched group 1 is HONGHUAYOU CAJI (a commercial commercially available product), and usage is to be administered once in per 4 hours, embrocates in the articular surface of getting involved 1 week of the course of treatment; Matched group 2 is for press the safflower oil plaster that comparative example 2 prepares, and usage is to be administered once in per 12 hours, embrocates in getting involved articular surface, 1 week of the course of treatment.
After treatment, the doctor has clear improvement to the evaluation of three groups of patient's articular pains and movable pain, before treating with after treating utmost point significant difference (P＜0.001) is arranged more all, Chinese medicine composition plaster group result is better than the HONGHUAYOU CAJI group, and the safflower oil plaster therapeutic effect for preparing by comparative example 2 is lower than HONGHUAYOU CAJI.Three groups the total effective rate toatl proportion of produce effects (effectively and) is respectively 87.50%, 79.17%, 65.28%, and the general curative effect optimum of the made Chinese medicine composition plaster of the present invention is described.
Observe proof by above animal transdermal experiment and volunteer's medication: the described Chinese medicine composition plaster of patent of the present invention is on the convenience of lasting performance curative effect of medication and use, obviously be better than existing preparation, greatly improved the transdermal efficient of external transdermal drug-supplying system, strengthen drug effect, and the compliance of medication improves a lot, and feeds back fabulous.
Claims (2)
1. the Chinese medicine composition plaster of an externally applied wind-expelling, this plaster is formed medicine activity component by Oleum Ocimi Gratissimi 56.4ml, methyl salicylate 37.2ml, JIANGZHANGYOU 1.07ml, Oleum Cinnamomi 2.13ml, cinnamic aldehyde 2.13ml, citral 1.07ml, Borneolum Syntheticum 0.23g, be mixed and made into behind the ointment medicament of it being coated backing and overlay film and making with hydrophilic matrix, it is characterized in that each composition is as follows by weight in the described ointment:
22 parts of 2.5 parts of glycerol of 1.5 parts of Resina persicaes of 2.5 parts of gelatin of 8 parts of polyacrylic acid of medicine activity component
55 parts in 6 parts of water of 3 parts of polyoxyethylene sorbitan monoleates of 0.15 part of Kaolin of 0.3 part of aluminium hydroxide of tartaric acid.
2. the Chinese medicine composition plaster of an externally applied wind-expelling, this plaster is formed medicine activity component by Oleum Ocimi Gratissimi 56.4ml, methyl salicylate 37.2ml, JIANGZHANGYOU 1.07ml, Oleum Cinnamomi 2.13ml, cinnamic aldehyde 2.13ml, citral 1.07ml, Borneolum Syntheticum 0.23g, be mixed and made into behind the ointment medicament of it being coated backing and overlay film and making with hydrophilic matrix, it is characterized in that each composition is as follows by weight in the described ointment:
7 parts of 2.5 parts of Polyethylene Glycol of 1.5 parts of Resina persicaes of 2.5 parts of gelatin of 5 parts of polyacrylic acid of medicine activity component
3 parts of 1.5 parts of polyoxyethylene sorbitan monoleates of 0.15 part of Kaolin of 0.3 part of aluminium hydroxide of 15 parts of tartaric acid of propylene glycol
56 parts in water.
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200510002460 CN1806823B (en) | 2005-01-21 | 2005-01-21 | Externally applied wind-expelling Chinese medicinal composition plaster |
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| CN 200510002460 CN1806823B (en) | 2005-01-21 | 2005-01-21 | Externally applied wind-expelling Chinese medicinal composition plaster |
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| CN1806823B true CN1806823B (en) | 2010-12-22 |
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| CN102293829B (en) * | 2011-08-31 | 2014-04-16 | 曾爱忠 | Externally applying medicine for relieving pain and preparation method thereof |
| CN103356508A (en) * | 2012-03-27 | 2013-10-23 | 上海卫生材料厂有限公司 | Centella total glycoside cataplasm and preparation method thereof |
| CN103405488B (en) * | 2013-08-13 | 2015-12-09 | 上海美宝生命科技有限公司 | One treats skin scar cataplasma and preparation method thereof |
| CN104887755A (en) * | 2015-05-08 | 2015-09-09 | 寿根其 | Method for preparing lumbar disc herniation therapeutic agent |
| CN108578586A (en) * | 2018-06-22 | 2018-09-28 | 陕西杨凌陕特农业发展有限公司 | A kind of externally used detumescence anodyne and preparation method thereof |
| CN111493723A (en) * | 2020-06-19 | 2020-08-07 | 广东轻工职业技术学院 | Bacteriostatic facial tissue containing natural bactericidal components and preparation method and application thereof |
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