CN1528462A - Water-soluble matrix for external transdermal paster and preparing method thereof - Google Patents
Water-soluble matrix for external transdermal paster and preparing method thereof Download PDFInfo
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- CN1528462A CN1528462A CNA2003101048781A CN200310104878A CN1528462A CN 1528462 A CN1528462 A CN 1528462A CN A2003101048781 A CNA2003101048781 A CN A2003101048781A CN 200310104878 A CN200310104878 A CN 200310104878A CN 1528462 A CN1528462 A CN 1528462A
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- aqueous solution
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Abstract
The present invention discloses a water-soluble matrix of transdermal emplastrum for external application. It is formed from the following raw materials according a certain weight ratio: olefine acids and salts copolymer; polyvinylpyrrolidone: olefinic alcohols: glycerine: hydroxide: organic acid=(3-12):(2-10):(2-10):(15-75):(0.3-2.5):(0.2-1.5). Its preparation method is characterized by that the aqueous solution of polyvinylpyrro-lidone, aqueous solution of organic acid, aqueous solution of olefinic alcohols and olefine acids and salts copolymers, glycerine and hydroxide are fully mixed and stirred uniformly so as to can obtain the invented matrix. It has high biological utilization rate of medicine, and has good compatibility with water-soluble and fat-soluble medicines.
Description
Technical field
The present invention relates to the pharmaceutical carrier substrate of a kind of water solublity capable of loading and carrying, fat-soluble Chinese and western drugs, Percutaneous absorption enhancer, relate in particular to water-soluble base of a kind of externally applied transdermal patch and preparation method thereof.
Background technology
The external used medicine patch is used for diseases such as treatment of arthritis, soft tissue injury, hyperosteogeny, neuralgia, is of long duration in China, such as the rubber cream of traditional black plaster, modern crafts, pressure sensitive adhesive etc.These traditional patch though have advantages such as convenience, part are effective fast, minimizing toxic and side effects, because of black plaster contains a large amount of lead oxide, have heavy metal toxicity; Rubber mass has skin irritation; High temperature when pressure sensitive adhesive prepares easily causes the loss of volatile medicine; Use organic solvents such as gasoline when preparing in addition, to environment, all can damage to human body.Also have pollution clothes in addition, take off and pulled pain, shortcoming such as uncomfortable, influence quite a few patient's medication.In recent years, the cataplasma of Japan, Korea S's import is though solved an above-mentioned difficult problem.But since its cost an arm and a leg and adhesion poor, make that this a kind of novel transdermal absorption formulation can not be by general popularization and use.
Summary of the invention
Technical problem to be solved by this invention is to provide water-soluble base of a kind of externally applied transdermal patch and preparation method thereof at the problems referred to above, the water-soluble base of externally applied transdermal patch of the present invention, the advantage that had both had the import cataplasma can reduce cost again, and adhesion is strong.
In order to address the above problem, the present invention is achieved in that it is to be made of by weight following raw material: olefin(e) acid class and saline copolymer: polyvinylpyrrolidone: enol class: glycerol: hydroxide: organic acid=(3-12): (2-10): (2-10): (15-75): (0.3-2.5): (0.2-1.5);
The method of above-mentioned raw materials being made the water-soluble base of externally applied transdermal patch is:
A. get polyvinylpyrrolidone and make the aqueous solution that content is 12%-16%;
B. get the enol class and make the aqueous solution that content is 10%-16%;
C. get organic acid and make the aqueous solution that content is 0.1%-0.5%;
D. the above-mentioned polyvinylpyrrolidone aqueous solution for preparing, aqueous solutions of organic acids, enol class aqueous solution and olefin(e) acid class and saline copolymer, glycerol and hydroxide are fully mixed, are stirred, place, substrate.
Above-mentioned olefin(e) acid class and saline copolymer can also be polybutene acid and polybutene sodium copolymer; The enol class can also be POLYPROPYLENE GLYCOL; Hydroxide can also be potassium hydroxide, calcium hydroxide, sodium hydroxide.
Preferred feedstock weight proportion of the present invention is: polyacrylic acid and polypropylene sodium copolymer: polyvinylpyrrolidone: polyvinyl alcohol: glycerol: aluminium hydroxide: tartaric acid=(5-10): (3-8): (3-8): (20-70): (0.5-1.5): (0.3-1.0);
The method of preferred feedstock being made the water-soluble base of externally applied transdermal patch is:
A. get polyvinylpyrrolidone and make the aqueous solution that content is 12%-16%;
B. get polyvinyl alcohol and make the aqueous solution that content is 10%-16%;
C. get tartaric acid and make the aqueous solution that content is 0.1%-0.5%;
D. the above-mentioned polyvinylpyrrolidone aqueous solution for preparing, aqueous solutions of organic acids, enol class aqueous solution and polyacrylic acid are fully mixed, stir with polypropylene sodium copolymer, glycerol and hydroxide, place, substrate.
Optimum weight proportioning of the present invention is: polyacrylic acid and polypropylene sodium copolymer: polyvinylpyrrolidone: polyvinyl alcohol: aluminium hydroxide: glycerol: tartaric acid=8: 6: 6: 50: 1: 0.5;
The method of optimum feed stock being made the water-soluble base of externally applied transdermal patch is:
A. get polyvinylpyrrolidone and make the aqueous solution that content is 12%-16%;
B. get polyvinyl alcohol and make the aqueous solution that content is 10%-16%;
C. get tartaric acid and make the aqueous solution that content is 0.1%-0.5%;
D. the above-mentioned polyvinylpyrrolidone aqueous solution for preparing, aqueous solutions of organic acids, enol class aqueous solution and polyacrylic acid are fully mixed, stir with polypropylene sodium copolymer, glycerol and hydroxide, place, substrate.
Advantage of the present invention and effect are:
The present invention had both had the advantage of import cataplasma, can reduce cost again, and adhesion was strong.Below in conjunction with experimental data advantage of the present invention and effect are elaborated.
1. drug bioavailability height can avoid that factor such as PH, enzyme reduces the individual variation that causes thus to the anaphylaxis of drug-induced degraded and liver in the gastrointestinal tract;
2. easy to use, can use at any time or stop Drug therapy, be applicable to because of a variety of causes to be difficult for oral administration or the unconspicuous disease of oral administration effect;
3. a drug can make medicine enter in the body with constant speed for a long time, plays long-acting, slow releasing function;
4. the may command medicine enters intravital speed, keeps stable blood concentration, and blood drug level " peak valley " phenomenon of avoiding other administering mode to cause reduces toxic and side effects;
5. acupuncture point meridian absorbs, but the dredging the meridian internal organs work at whole body;
6. its water-soluble base and water solublity, fat-soluble medicine intermiscibility are good, and the substrate drug loading is big, especially are fit to Chinese medicine multicomponent, heavy dose of medication characteristics;
7. the easier keratodermatitis that makes of its water-soluble base is softening, make medicine see through skin resistance and reduce, drug diffusion, absorb easier;
8. its good permeability to skin adhesion, moisture retention, skin irritation, not pollution clothes, noresidue, take off and pull aspects such as not having pain, all is better than traditional black plaster and rubber unguentum;
9. production technology is simple, does not use gasoline and other organic solvent, both safely, prevent that Chinese medicine is volatile and make the composition loss, guarantee drug effect, free from environmental pollution again.
The specific embodiment
Embodiment one
It is made by weight by following raw materials according: polyacrylic acid and polypropylene sodium copolymer: polyvinylpyrrolidone: polyvinyl alcohol: glycerol: potassium hydroxide: tartaric acid=3: 2: 2: 15: 0.3: 0.2.
Its preparation method is:
A. getting polyvinylpyrrolidone 2kg, to make content be 12% aqueous solution;
B. getting polyvinyl alcohol 2kg, to make content be 10% aqueous solution;
C. getting tartaric acid 0.2kg, to make content be 0.1% aqueous solution;
D. the above-mentioned polyvinylpyrrolidone aqueous solution for preparing, aqueous solutions of organic acids, enol class aqueous solution and polyacrylic acid and polypropylene sodium copolymer 3kg, glycerol 15kg and potassium hydroxide 0.3kg are fully mixed, stir, place, substrate.
Embodiment two
It is made by weight by following raw materials according: polyacrylic acid and polypropylene sodium copolymer: polyvinylpyrrolidone: polyvinyl alcohol: glycerol: sodium hydroxide: tartaric acid=12: 10: 10: 75: 2.5: 1.5.
Preparation method is with embodiment one.
Embodiment three
It is made by weight by following raw materials according: polybutene acid and polybutene sodium copolymer: polyvinylpyrrolidone: polyvinyl alcohol: glycerol: potassium hydroxide: tartaric acid=8: 8: 6: 50: 1: 0.5.
Its preparation method is: a. gets polyvinylpyrrolidone 8kg, and to make content be 16% aqueous solution;
B. getting polyvinyl alcohol 6kg, to make content be 16% aqueous solution;
C. getting tartaric acid 0.5kg, to make content be 0.5% aqueous solution;
D. the above-mentioned polyvinylpyrrolidone aqueous solution for preparing, aqueous solutions of organic acids, enol class aqueous solution and polybutene acid and polybutene sodium copolymer 8kg, glycerol 50kg and potassium hydroxide 1kg are fully mixed, stir, place, substrate.
Embodiment four
It is made by weight by following raw materials according: poly-butanoic acid and polybutene sodium copolymer: polyvinylpyrrolidone: POLYPROPYLENE GLYCOL: glycerol: calcium hydroxide: tartaric acid=8: 6: 6: 50: 1: 0.4.
Preparation method is with embodiment one.
Embodiment five
It is made by weight by following raw materials according: polyacrylic acid and polypropylene sodium copolymer: polyvinylpyrrolidone: polyvinyl alcohol: glycerol: aluminium hydroxide: tartaric acid=5: 3: 3: 20: 0.5: 0.3.
Its preparation method is: a. gets polyvinylpyrrolidone 3kg, and to make content be 14% aqueous solution;
B. getting polyvinyl alcohol 3kg, to make content be 13% aqueous solution;
C. getting tartaric acid 0.5kg, to make content be 0.25% aqueous solution;
D. the above-mentioned polyvinylpyrrolidone aqueous solution for preparing, aqueous solutions of organic acids, enol class aqueous solution and polyacrylic acid are fully mixed, stir with polypropylene sodium copolymer 5kg, glycerol 20kg and aluminium hydroxide 0.5kg, place, promptly get substrate.
Embodiment six
It is made by weight by following raw materials according: polyacrylic acid and polypropylene sodium copolymer: polyvinylpyrrolidone: polyvinyl alcohol: glycerol: aluminium hydroxide: tartaric acid=8: 6: 8: 60: 1: 0.5.
Preparation method is with embodiment five.
Embodiment seven
It is made by weight by following raw materials according: polyacrylic acid and polypropylene sodium copolymer: polyvinylpyrrolidone: polyvinyl alcohol: glycerol: aluminium hydroxide: tartaric acid=10: 8: 8: 70: 1.5: 1.0.
Preparation method is with embodiment five.
Embodiment eight
It is made by weight by following raw materials according: polyacrylic acid and polypropylene sodium copolymer: polyvinylpyrrolidone: polyvinyl alcohol: glycerol: aluminium hydroxide: tartaric acid=8: 6: 8: 65: 1: 0.5.
Preparation method is with embodiment five.
Embodiment nine
It is made by weight by following raw materials according: polyacrylic acid and polypropylene sodium copolymer: polyvinylpyrrolidone: POLYPROPYLENE GLYCOL: glycerol: calcium hydroxide: tartaric acid=8: 6: 6: 50: 1: 0.4.
Preparation method is with embodiment two.
Embodiment ten
Optimum feed stock of the present invention is by weight: polyacrylic acid and polypropylene sodium copolymer: polyvinylpyrrolidone: polyvinyl alcohol: glycerol: aluminium hydroxide: tartaric acid=8: 6: 6: 50: 1: 0.5.
Its preparation method is: a. gets polyvinylpyrrolidone 6kg, and to make content be 14% aqueous solution;
B. getting polyvinyl alcohol 6kg, to make content be 13% aqueous solution;
C. getting tartaric acid 0.5kg, to make content be 0.25% aqueous solution;
D. the above-mentioned polyvinylpyrrolidone aqueous solution for preparing, aqueous solutions of organic acids, enol class aqueous solution and polyacrylic acid are fully mixed, stir with polypropylene sodium copolymer 8kg, glycerol 50kg and aluminium hydroxide 0.5kg, place, promptly get substrate.
Embodiment 11
The described a of preparation method, the order interchangeable in b, c step among the embodiment one to embodiment ten, other is identical.
Get this product and carry out heat resistant test: heat 110 ℃ indeformable.
The paste containing amount test: this product is no less than 4.2g for per 100 square centimeters.
Low temperature resistant test: refrigerator-5 ℃ 2 months no changes of placement.
Experimental data such as following table:
Table one: heat resistant test investigation table
Annotate: randomly draw 10 samples of each batch at every turn.
Table two: paste containing amount investigation table
Annotate: randomly draw 10 samples of each batch at every turn.
Table three: low temperature resistant test investigation table
Annotate: randomly draw 10 samples of each batch at every turn.
Claims (7)
1. the water-soluble base of an externally applied transdermal patch, it is characterized in that it is to be made of by weight following raw material, olefin(e) acid class and saline copolymer: polyvinylpyrrolidone: enol class: glycerol: hydroxide: organic acid=(3-12): (2-10): (2-10): (15-75): (0.3-2.5): (0.2-1.5).
2. the preparation method of the water-soluble base of an externally applied transdermal patch, it is characterized in that it is to be made of by weight following raw material, olefin(e) acid class and saline copolymer: polyvinylpyrrolidone: enol class: glycerol: hydroxide: organic acid=(3-12): (2-10): (2-10): (15-75): (0.3-2.5): (0.2-1.5);
The method that is made into the water-soluble base of externally applied transdermal patch is:
A. get polyvinylpyrrolidone and make the aqueous solution that content is 12%-16%;
B. get the enol class and make the aqueous solution that content is 10%-16%;
C. get organic acid and make the aqueous solution that content is 0.1%-0.5%;
D. the above-mentioned polyvinylpyrrolidone aqueous solution for preparing, aqueous solutions of organic acids, enol class aqueous solution and olefin(e) acid class and saline copolymer, glycerol and hydroxide are fully mixed, stirred, place, promptly get substrate.
3. the water-soluble base of a kind of externally applied transdermal patch according to claim 1 and 2 is characterized in that described olefin(e) acid class and saline copolymer can also be polybutene acid and polybutene sodium copolymer; The enol class can also be a POLYPROPYLENE GLYCOL; Hydroxide can also be potassium hydroxide, calcium hydroxide, sodium hydroxide.
4. the water-soluble base of a kind of externally applied transdermal patch according to claim 1 is characterized in that preferred feedstock weight proportion of the present invention is: polyacrylic acid and polypropylene sodium copolymer: polyvinylpyrrolidone: polyvinyl alcohol: glycerol: aluminium hydroxide: tartaric acid=(5-10): (3-8): (3-8): (20-70): (0.5-1.5): (0.3-1.0);
The method that is made into the water-soluble base of externally applied transdermal patch is:
A. get polyvinylpyrrolidone and make the aqueous solution that content is 12%-16%;
B. get the enol class and make the aqueous solution that content is 10%-16%;
C. get organic acid and make the aqueous solution that content is 0.1%-0.5%;
D. the above-mentioned polyvinylpyrrolidone aqueous solution for preparing, aqueous solutions of organic acids, enol class aqueous solution and polyacrylic acid are fully mixed, stir with polypropylene sodium copolymer, glycerol and hydroxide, place, promptly get substrate.
5. the water-soluble base of a kind of externally applied transdermal patch according to claim 1 is characterized in that its raw material optimum weight proportioning is: polyacrylic acid and polypropylene sodium copolymer: polyvinylpyrrolidone: polyvinyl alcohol: aluminium hydroxide: glycerol: tartaric acid=8: 6: 6: 50: 1: 0.5;
The method that is made into the water-soluble base of externally applied transdermal patch is:
A. get polyvinylpyrrolidone and make the aqueous solution that content is 12%-16%;
B. get the enol class and make the aqueous solution that content is 10%-16%;
C. get organic acid and make the aqueous solution that content is 0.1%-0.5%;
D. the above-mentioned polyvinylpyrrolidone aqueous solution for preparing, aqueous solutions of organic acids, enol class aqueous solution and polyacrylic acid are fully mixed, stir with polypropylene sodium copolymer, glycerol and hydroxide, place, promptly get substrate.
6. the preparation method of the water-soluble base of a kind of externally applied transdermal patch according to claim 2 is characterized in that the order in described a, b, c step can be changed.
7. according to the water-soluble base of claim 4 or 5 described a kind of externally applied transdermal patches, it is characterized in that a, b, the order in c step in the method for the described water-soluble base of making the externally applied transdermal patch can be changed.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200310104878 CN1215880C (en) | 2003-10-21 | 2003-10-21 | Water-soluble matrix for external transdermal paster and preparing method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200310104878 CN1215880C (en) | 2003-10-21 | 2003-10-21 | Water-soluble matrix for external transdermal paster and preparing method thereof |
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| Publication Number | Publication Date |
|---|---|
| CN1528462A true CN1528462A (en) | 2004-09-15 |
| CN1215880C CN1215880C (en) | 2005-08-24 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN 200310104878 Expired - Fee Related CN1215880C (en) | 2003-10-21 | 2003-10-21 | Water-soluble matrix for external transdermal paster and preparing method thereof |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101254214B (en) * | 2007-02-26 | 2010-10-06 | 江苏七O七天然制药有限公司 | Chinese medicine catablasm base material |
| CN105078645A (en) * | 2014-05-12 | 2015-11-25 | 天津卓普医疗器械有限公司 | Cold-compression patch with hydrogel as substrate and method for manufacturing cold-compression patch |
-
2003
- 2003-10-21 CN CN 200310104878 patent/CN1215880C/en not_active Expired - Fee Related
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101254214B (en) * | 2007-02-26 | 2010-10-06 | 江苏七O七天然制药有限公司 | Chinese medicine catablasm base material |
| CN105078645A (en) * | 2014-05-12 | 2015-11-25 | 天津卓普医疗器械有限公司 | Cold-compression patch with hydrogel as substrate and method for manufacturing cold-compression patch |
Also Published As
| Publication number | Publication date |
|---|---|
| CN1215880C (en) | 2005-08-24 |
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Owner name: MA TIANTIAN Free format text: FORMER OWNER: DONGLING PHARMACEUTICAL CO., LTD., SHENYANG Effective date: 20060616 |
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Effective date of registration: 20060616 Address after: 110042, D-20-10, 100 Binhe Road, Shenhe District, Liaoning, Shenyang Patentee after: Ma Tiantian Address before: 110161, Dongling Road, Dongling District, Liaoning, Shenyang, 111 Patentee before: Dongling Pharmaceutical Co., Ltd., Shenyang |
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