CN1054529C - High performance and quick effective skin penetrating and slow releasing Chinese medical paste and preparations - Google Patents

High performance and quick effective skin penetrating and slow releasing Chinese medical paste and preparations Download PDF

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CN1054529C
CN1054529C CN96104657A CN96104657A CN1054529C CN 1054529 C CN1054529 C CN 1054529C CN 96104657 A CN96104657 A CN 96104657A CN 96104657 A CN96104657 A CN 96104657A CN 1054529 C CN1054529 C CN 1054529C
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grams
borneolum syntheticum
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pad pasting
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CN1162459A (en
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吴锦
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Abstract

The present invention discloses a diadermic slow-release skin pasting membrane used for treating coronary heart diseases and angina pectoris, which is a medical agent of external application. The present invention is prepared from the effective ingredients such as the traditional Chinese medicines of borneol and the volatile oil extracted from benzoin, santal asarum herb, grassleaf sweelflag rhizome and styrax, polyisobutylene, azone and liquid paraffin.

Description

A kind of slow release pad pasting and preparation method for the treatment of coronary heart disease
The present invention is a kind of cardiopathic topical agent that is used for the treatment of, be specifically a kind of be the transdermal slow-release skin pad pasting that effective ingredient is prepared from Chinese medicine, have treatment coronary heart disease, anginal medical function.The present invention also comprises can be prepared into any forms of pharmaceutical compositions, belongs to field of pharmaceutical preparations.
Angina pectoris is a kind of common old cardiovascular system diseases, has characteristics such as morbidity is hurried, patient's condition danger.Therefore prevention that should disease is the problem of research with treatment always.At present preparations such as oral, the buccal of treatment angina pectoris disease, injection and aerosol have been widely used in clinically, have obtained certain therapeutic effect.But these preparations are all very short action time, keep certain drug effect for a long time as need, must successive administration.This has all brought inconvenience for doctor and patient.Effective western medicine medicine nitroglycerin, though many toxic and side effects are arranged, consequently many patients can not use, but still are present common drug clinically.For the treatment of angina pectoris, still lack the advanced dosage form of efficient, long lasting Chinese medicine.Although the present domestic relevant herbal penetration therapy Study on Coronary Heart Disease of a small amount of bibliographical information that has, for example, " technology of Rhizoma Chuanxiong plaster and quality standard ", imperial ambition, " Chinese patent medicine ", 1994,16 (12), 3-4; Chinese patent CN1089833 " treatment coronary heart disease, anginal Chinese medicine external use plaster " etc.These preparations still have following deficiency: 1, dosage form is the extractum of unguentum or extraction, and its degree of absorption is lower, does not see the report of relevant treatment angina pectoris membrane agent; 2, form the Chinese medicine shortage permeability of medicament itself, directly have influence on therapeutic effect; But 3, there is not to add the pharmaceutics composition of controlled release; 4, some only limits to clinical observation, still is not prepared into medicament.Therefore, preparing a kind of easy to use and good external used medicine of curative effect has been angina pectoris patient serious hope for a long time.The topical agent that particularly needs a kind of instant effect, effective and longer duration.
The object of the invention provides a kind of externally applied transdermal slow release skin pad pasting that is used for the treatment of angina pectoris.
The object of the invention also is to provide a kind of externally applied transdermal slow release skin pad pasting preparation method for the treatment of angina pectoris.
The middle pharmaceutically active ingredient of preparation pad pasting of the present invention is that Chinese medicine component with following weight proportion is that raw material is produced:
Benzoinum 500-1000 gram
Borneolum Syntheticum 10-1000 gram
Lignum Santali Albi 200-1000 gram
Herba Asari 0.1-200 gram
Rhizoma Acori Graminei 0.1-700 gram
Styrax 50-2000 gram.
Above-mentioned Chinese medicine proportion optimization consumption is:
Benzoinum 700-800 gram
Borneolum Syntheticum 500-800 gram
Lignum Santali Albi 300-700 gram
Herba Asari 1-100 gram
Rhizoma Acori Graminei 1-500 gram
Styrax 600-800 gram.
Above-mentioned Chinese medicine proportioning consumption is more preferably:
Benzoinum 700-800 gram
Borneolum Syntheticum 500-800 gram
Lignum Santali Albi 300-700 gram
Herba Asari 50-80 gram
Rhizoma Acori Graminei 50-400 gram
Styrax 500-600 gram,
The middle pharmaceutically active ingredient of preparation pad pasting of the present invention also can be that raw material is produced with the Chinese medicine component of following weight proportion:
Borneolum Syntheticum 10-1000 gram
Herba Asari 0.1-200 gram
Rhizoma Acori Graminei 0.1-700 gram
Styrax 50-2000 gram.
Above-mentioned Chinese medicine proportion optimization consumption is:
Borneolum Syntheticum 500-800 gram
Herba Asari 1-100 gram
Rhizoma Acori Graminei 1-500 gram
Styrax 600-800 gram.
Above-mentioned Chinese medicine proportioning consumption is more preferably:
Borneolum Syntheticum 500-800 gram
Herba Asari 50-80 gram
Rhizoma Acori Graminei 50-400 gram
Styrax 500-600 gram.
Transdermal slow-release skin pad pasting of the present invention except containing above-mentioned middle pharmaceutically active ingredient, also contains polyisobutylene 300-2000 gram, nitrogen copper 10-500 milliliter, liquid paraffin 10-500 milliliter.Certainly, can be prepared into any known drug dosage form with above-mentioned pharmaceutical composition, as, peroral dosage form, spray-type etc.
The step of preparation process of transdermal slow-release skin pad pasting of the present invention is:
1, extracts father-in-law's thing effective ingredient
The medicine of above-mentioned weight proportion, except that Borneolum Syntheticum, all the other all extract volatile oil according to the extracting method of routine, and are with the Borneolum Syntheticum mixing, standby then;
2, the pastille storage storehouse of preparation pad pasting
Get polyisobutylene 300-2000 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1) in petroleum ether and the cyclohexane extraction mixed liquor 50-1000 milliliter, add above-mentioned drug volatilization oil and Borneolum Syntheticum mixture again, and 1-azone-2
The 10-500 milliliter, mix homogeneously is prepared into the pastille substrate of three kinds of different gradient concentrations; It is respectively 40-50%, 30-40% and 20-30% that these three kinds of substrate respectively contain medicine weight percent concentration scope; During preparation these three kinds of pastille substrate are coated on the shuttle backing layer, painted three layers by the order of high, medium and low concentration, every layer is coated with three times, constitutes pastille storage storehouse.Volatilize solvent then.
3, preparation viscose
Get polyisobutylene 300-1000 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1) in petroleum ether and the cyclohexane extraction 50-1000 milliliter, add liquid paraffin 10-500 milliliter and 60-5000 gram above-mentioned drug volatilization oil and Borneolum Syntheticum mixture, mix homogeneously.
4, the preparation of adhesive shell system preparation capable of permeating skin
Coating one layer thickness is the viscose of the step 3 of 0.05-0.3 millimeter on the pastille storage storehouse of step 2 preparation, and covers upward protective layer.
The mounting of transdermal slow-release skin pad pasting of the present invention is equipped with layer and can uses the material fully of mounting that is suitable on any pharmaceutics.Said protective layer can be plastic sheeting or the self-adhesive paper that is suitable on any pharmaceutics.
The Chinese medicine of above-mentioned formula ratio generally can be prepared into 1000-5000 sheet pad pasting.
The general every subsides content of dispersion of transdermal slow-release skin pad pasting of the present invention is the 0.4-8 gram.
Transdermal slow-release skin pad pasting of the present invention is compared with the other treatment treating coronary heart disease and angina pectoris, has following characteristics:
1, transdermal slow-release skin pad pasting of the present invention is a pure Chinese medicinal preparation, and therapeutical effect is not less than nitroglycerin;
2, compare with nitroglycerin.Its advantage is: (1) does not have the common toxic and side effects of nitroglycerin, as, feel sick, postural hypotension, vomiting, vascular pulsation headache etc.; (2) there is not the use contraindication of nitroglycerin, as, forbid, intracranial pressure low or increased intraocular pressure disease patient in nitroglycerin allergy, serious anemia, blood pressure; (3) patient does not produce toleration after using; (4) therapeutical effect is more lasting, patient 1/3-1/4 is arranged approximately after treatment about a course of treatment, can keep quite a while angina pectoris degree and obviously alleviate or do not show effect; (5) patient who fails to respond to any medical treatment for nitroglycerin, still effective with said preparation, for angina pectoris after the myocardial infarction, the angina pectoris of PTCA postoperative excellent curative is arranged all also;
3, transdermal slow-release skin pad pasting of the present invention can play slow release, controlled-release function owing to be to adopt advanced technology to make, and makes lasting medicine, stable, pastes with once, can keep bacterium reason effect 24-48 hour, and easy to use, has efficient, long lasting characteristics;
4, research to the hematoblastic function of angina pectoris patient, and myocardial ultrastructure and different Chinese and western drugs show that to the result of study of the different protective effects of cardiac muscle transdermal slow-release skin pad pasting of the present invention has good protective action to myocardial ischemia when the animal coronary vasospasm caused myocardial ischemia; And the cardiac hemodynamic of improvement is arranged, reduce good actions such as myocardial oxygen consumption.
Embodiment 1
Get Benzoinum 600 grams, Lignum Santali Albi 500 grams, Herba Asari 100 grams, Rhizoma Acori Graminei 100 grams, Styrax 800 grams add in the multi-function extractor, extract respectively and collect volatile oil, and are standby;
Get polyisobutylene 800 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1) in 150 milliliters of petroleum ether and the cyclohexane extraction, add above-mentioned drug volatilization oil and Borneolum Syntheticum 500 grams again, and 1-azone-2 50-500 milliliter, mix homogeneously is prepared into and contains the pastille substrate that medicine weight percent concentration scope is respectively three kinds of different gradient concentrations of 40-50%, 30-40% and 20-30%; These three kinds of pastille substrate are coated mount on the backing layer, paint three layers by the order of high, medium and low concentration, every layer of coating three times constitutes nine layers of pastille and stores storehouses.Volatilize solvent then;
Get polyisobutylene 800 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1) in 150 milliliters of petroleum ether and the cyclohexane extraction, add 100 milliliters of liquid paraffin and above-mentioned drug volatilization oil and the Borneolum Syntheticum of 200 grams, mix homogeneously is made viscose, and is standby;
Coating one layer thickness is the viscose of 0.2 millimeter above-mentioned preparation on the pastille storage storehouse of above-mentioned preparation, and covers upward protective layer, makes 2000 pad pastings.
Embodiment 2
Get Benzoinum 800 grams, Lignum Santali Albi 300 grams, Herba Asari 150 grams, Rhizoma Acori Graminei 500 grams, Styrax 600 grams add in the multi-function extractor, extract respectively and collect volatile oil, and are standby;
Get polyisobutylene 700 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1) in 200 milliliters of petroleum ether and the cyclohexane extraction, add above-mentioned drug volatilization oil and Borneolum Syntheticum 800 grams again, and 1-azone-2 100 milliliter, mix homogeneously, be prepared into that to contain medicine weight percent concentration scope be respectively 40-50%, the pastille substrate of three kinds of different gradient concentrations of 30-40% and 20-30%; These three kinds of pastille substrate are coated mount on the backing layer, paint three layers by the order of high, medium and low concentration, every layer of coating three times constitutes nine layers of pastille and stores storehouses.Volatilize solvent then;
Get polyisobutylene 700 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1) in 200 milliliters of petroleum ether and the cyclohexane extraction, add 200 milliliters of liquid paraffin and above-mentioned drug volatilization oil and the Borneolum Syntheticum of 400 grams, mix homogeneously is made sticking clear and bright liquid, and is standby;
Coating one layer thickness is the viscose of 0.1 millimeter above-mentioned preparation on the pastille storage storehouse of above-mentioned preparation, and covers upward protective layer, makes 200 pad pastings.
Embodiment 3.
Get Benzoinum 900 grams, Lignum Santali Albi 200 grams, Herba Asari 50 grams, Rhizoma Acori Graminei 400 grams, Styrax 500 grams add in the multi-function extractor, extract and collect volatile oil, and are standby;
Get polyisobutylene 600 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1) in 250 milliliters of petroleum ether and the cyclohexane extraction, add above-mentioned drug volatilization oil and Borneolum Syntheticum 800 grams again, and 1-azone-250 milliliter, mix homogeneously is prepared into and contains the pastille substrate that medicine weight percent concentration scope is respectively three kinds of different gradient concentrations of 40-50%, 30-40% and 20-30%; These three kinds of pastille substrate are coated mount on the backing layer, paint three layers by the order of high, medium and low concentration, every layer of coating three times constitutes nine layers of pastille and stores storehouses.Volatilize solvent then;
Get polyisobutylene 600 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1), add 50 milliliters of liquid paraffin and 400 and restrain above-mentioned drug volatilization oil and Borneolum Syntheticum, mix homogeneously is made viscose, and is standby in 250 milliliters of petroleum ether and the cyclohexane extraction;
Coating one layer thickness is the viscose of 0.1 millimeter above-mentioned preparation on the pastille storage storehouse of above-mentioned preparation, and covers upward protective layer, makes 2000 pad pastings.
Embodiment 4
Get Herba Asari 100 grams, Rhizoma Acori Graminei 100 grams, Styrax 800 grams add in the multi-function extractor, extract respectively and collect volatile oil, and are standby;
Get polyisobutylene 800 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1) in 150 milliliters of petroleum ether and the cyclohexane extraction, add above-mentioned drug volatilization oil and Borneolum Syntheticum 500 grams again, and 1-azone-2 50-500 milliliter, mix homogeneously is prepared into and contains the pastille substrate that medicine weight percent concentration scope is respectively three kinds of different gradient concentrations of 40-50%, 30-40% and 20-30%; These three kinds of pastille substrate are coated mount on the backing layer, paint three layers by the order of high, medium and low concentration, every layer of coating three times constitutes nine layers of pastille and stores storehouses.Volatilize solvent then;
Get polyisobutylene 800 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1) in 150 milliliters of petroleum ether and the cyclohexane extraction, add 100 milliliters of liquid paraffin and above-mentioned drug volatilization oil and the Borneolum Syntheticum of 200 grams, mix homogeneously is made viscose, and is standby;
Coating one layer thickness is the viscose of 0.2 millimeter above-mentioned preparation on the pastille storage storehouse of above-mentioned preparation, and covers upward protective layer, makes 2000 pad pastings.
Embodiment 5
Get Herba Asari 150 grams, Rhizoma Acori Graminei 500 grams, Styrax 600 grams add in the multi-function extractor, extract respectively and collect volatile oil, and are standby;
Get polyisobutylene 700 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1) in 200 milliliters of petroleum ether and the cyclohexane extraction, add above-mentioned drug volatilization oil and Borneolum Syntheticum 800 grams again, and 1-azone-2 100 milliliter, mix homogeneously is prepared into and contains the pastille substrate that medicine weight percent concentration scope is respectively three kinds of different gradient concentrations of 40-50%, 30-40% and 20-30%; These three kinds of pastille substrate are coated mount on the backing layer, paint three layers by the order of high, medium and low concentration, every layer of coating three times constitutes nine layers of pastille and stores storehouses.Volatilize solvent then;
Get polyisobutylene 700 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1), add 200 milliliters of liquid paraffin and 400 and restrain above-mentioned drug volatilization oil and Borneolum Syntheticum, mix homogeneously is made glue, and is standby in 200 milliliters of petroleum ether and the cyclohexane extraction;
Coating one layer thickness is the viscose of 0.1 millimeter above-mentioned preparation on the pastille storage storehouse of above-mentioned preparation, and covers upward protective layer, makes 2000 pad pastings.
Embodiment 6
Get Herba Asari 50 grams, Rhizoma Acori Graminei 400 grams, Styrax 500 grams add in the multi-function extractor, extract and collect volatile oil, and are standby;
Get polyisobutylene 600 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1) in 250 milliliters of petroleum ether and the cyclohexane extraction, add above-mentioned drug volatilization oil and Borneolum Syntheticum 400 grams again, and 1-azone-2 50 milliliter, mix homogeneously is prepared into and contains the pastille substrate that medicine weight percent concentration scope is respectively three kinds of different gradient concentrations of 40-50%, 30-40% and 20-30%; These three kinds of pastille substrate are coated mount on the backing layer, paint three layers by the order of high, medium and low concentration, every layer of coating three times constitutes nine layers of pastille and stores storehouses.Volatilize solvent then;
Get polyisobutylene 600 gram and be dissolved in that (wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1), add 50 milliliters of liquid paraffin and 100 and restrain above-mentioned drug volatilization oil and Borneolum Syntheticum, mix homogeneously is made viscose, and is standby in 250 milliliters of petroleum ether and the cyclohexane extraction;
Coating one layer thickness is the viscose of 0.1 millimeter above-mentioned preparation on the pastille storage storehouse of above-mentioned preparation, and covers upward protective layer, makes 1500 pad pastings.

Claims (7)

1, a kind of transdermal slow-release skin pad pasting that is used for the treatment of angina pectoris is characterized in that the volatile oil that it contains Borneolum Syntheticum and extracts from Benzoinum, Lignum Santali Albi, Herba Asari, Rhizoma Acori Graminei, Styrax, and the weight proportion of said raw material of Chinese medicine is
Benzoinum 500-1000 gram
Borneolum Syntheticum 10-1000 gram
Lignum Santali Albi 200-1000 gram
Herba Asari 0.1-200 gram
Rhizoma Acori Graminei 0.1-700 gram
Styrax 50-2000 gram.
2, according to the pad pasting of claim 1, the weight proportion of said raw material of Chinese medicine is
Benzoinum 700-800 gram
Borneolum Syntheticum 500-800 gram
Lignum Santali Albi 300-700 gram
Herba Asari 1-100 gram
Rhizoma Acori Graminei 1-500 gram
Styrax 600-800 gram.
3, according to the pad pasting of claim 1, the weight proportion of said raw material of Chinese medicine is
Benzoinum 800 grams
Borneolum Syntheticum 800 grams
Lignum Santali Albi 300 grams
Herba Asari 150 grams
Rhizoma Acori Graminei 500 grams
Styrax 600 grams.
4,, it is characterized in that it also contains following substrate according to the pad pasting of claim 1:
Polyisobutylene 300-2000 gram
1-azone-2 10-500 milliliter
Liquid paraffin 10-500 milliliter.
5, the preparation technology of the said pad pasting of claim 1 comprises the steps:
A, extraction effective ingredient
By the medicine of described weight proportion, except that Borneolum Syntheticum, all the other all extract volatile oil according to the extracting method of routine, and are with the Borneolum Syntheticum mixing, standby then;
The pastille storage storehouse of b, preparation pad pasting
Getting polyisobutylene 300-2000 gram is dissolved in petroleum ether and the cyclohexane extraction mixed liquor 50-1000 milliliter, wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1, add above-mentioned drug volatilization oil and Borneolum Syntheticum mixture again, and 1-azone-210-500 milliliter, mix homogeneously is prepared into the pastille substrate of three kinds of different gradient concentrations; It is respectively 40-50%, 30-40% and 20-30% that these three kinds of substrate respectively contain medicine weight percent concentration scope; During preparation these three kinds of pastille substrate are coated and mount on the backing layer, paint three layers by the order of high, medium and low concentration, every layer of coating three times constitutes pastille storage storehouse.Volatilize solvent then;
C, preparation viscose
Getting polyisobutylene 300-1000 gram is dissolved in petroleum ether and the cyclohexane extraction 50-1000 milliliter, wherein the ratio of petroleum ether and cyclohexane extraction is 1: 100-100: 1, add liquid paraffin 10-500 milliliter and 60-5000 gram above-mentioned drug volatilization oil and Borneolum Syntheticum mixture again, mix homogeneously, glue mucus;
The preparation of d, adhesive shell system preparation capable of permeating skin
Coating one layer thickness is the viscose of the step c of 0.50-0.3 millimeter on the pastille storage storehouse of step b preparation, and covers upward protective layer, promptly.
6, according to the technology of claim 5, wherein said pad pasting mount backing layer can use on any pharmaceutics be suitable for mount the backing material.
7, according to the technology of claim 5, wherein said protective layer can be plastic sheeting or the self-adhesive paper that is suitable on any pharmaceutics.
CN96104657A 1996-04-16 1996-04-16 High performance and quick effective skin penetrating and slow releasing Chinese medical paste and preparations Expired - Fee Related CN1054529C (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN96104657A CN1054529C (en) 1996-04-16 1996-04-16 High performance and quick effective skin penetrating and slow releasing Chinese medical paste and preparations

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN96104657A CN1054529C (en) 1996-04-16 1996-04-16 High performance and quick effective skin penetrating and slow releasing Chinese medical paste and preparations

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CN1162459A CN1162459A (en) 1997-10-22
CN1054529C true CN1054529C (en) 2000-07-19

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Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1061252C (en) * 1997-12-02 2001-01-31 牛永杰 Preparation of Chinese medicine for curing cardiac and cerebral diseases atomized by oxygen and its preparation process
CN102397311A (en) * 2011-11-28 2012-04-04 成都盛尔嘉科技有限公司 Coronary heart disease preparation and preparation method thereof
CN104547287A (en) * 2014-12-30 2015-04-29 范靖 Slow-release medicine patch for stenocardia
CN104840449B (en) * 2015-04-22 2018-05-18 崔建平 A kind of medicine patch and preparation method thereof

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1089833A (en) * 1993-01-18 1994-07-27 贵州三力技术发展有限公司 Treatment coronary heart disease, anginal Chinese medicine external use plaster

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1089833A (en) * 1993-01-18 1994-07-27 贵州三力技术发展有限公司 Treatment coronary heart disease, anginal Chinese medicine external use plaster

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