CN102670624A - Patch for treating rheumatic arthritis and preparation method thereof - Google Patents
Patch for treating rheumatic arthritis and preparation method thereof Download PDFInfo
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- CN102670624A CN102670624A CN2011100613045A CN201110061304A CN102670624A CN 102670624 A CN102670624 A CN 102670624A CN 2011100613045 A CN2011100613045 A CN 2011100613045A CN 201110061304 A CN201110061304 A CN 201110061304A CN 102670624 A CN102670624 A CN 102670624A
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- rheumatoid arthritis
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- chloroform
- treating
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Abstract
The invention discloses a patch for treating rheumatic arthritis and a preparation method thereof. The patch consists of a main medicament for treating rheumatic arthritis, a medicament solvent, a substrate and a penetrating agent, wherein the main medicament consists of triptolide and lidocaine serving as a pain-relieving medicament for relieving rheumatic arthritis pain. The patch is medical controlled-release slow release preparation, has a comprehensive pharmacological action, is used for blocking major development pathologic loops of the rheumatic arthritis disease, and has high specificity and a lasting pharmacological effect; and the preparation method is simple.
Description
Technical field
The present invention relates to field of pharmaceutical preparations and formulation method, especially relate to a kind of rheumatoid arthritis of treating and have patch of topical pain relief and preparation method thereof concurrently.
Background technology
Patch is the thin slice stratiform preparation that sticks in human body skin, and its Chinese medicine percutaneous absorbs the general designation that gets into local target tissue or systemic circulation system, has comprised the patch of local skin transmission and transdermal delivery.Patch belongs to transdermal delivery system, is the pharmaceutical preparation with better usefulness row, can keep blood drug level to be stabilized in the valid density scope of treatment; Owing to avoided the first pass effect of drug oral through gastrointestinal tract and liver, more stably directly get into blood flow than oral administration, can improve medicine in vivo predictability; Improve safety; Improve patient's advantages such as compliance.
Radix Tripterygii Wilfordii lactone alcohol (triptolide) is the chemical constituent of from Celastraceae tripterygium plant Radix Tripterygii Wilfordii, extracting.From pharmacological action: (1) Radix Tripterygii Wilfordii lactone alcohol had both had non-specific antiinflammatory immunity function, and having again with the inhibition is main immunization.(2) acute and chronic inflammation all there is the obvious suppression effect, and, mainly is to cause that through hypophysis ACTH discharges the adrenal cortex reinforcing secretory function with hypophysis--system is relevant.(3) research that is applied to adjuvant arthritis shows: rat assist agent arthritis is had obvious inhibitory action, and rat assist agent arthritis is the animal model of research rheumatoid medicine, and its histopathology changes very similar with people's rheumatoid arthritis.In a word, the pharmacological action of Radix Tripterygii Wilfordii lactone alcohol is comprehensive, blocks the main pathology link of rheumatoid arthritis disease progression just, and is with strong points, evident in efficacy.It not only has the dual function of remission and state of an illness alleviation concurrently; Also have effect of parahormone appearance and immunoregulation effect; But its non-again hormone, multiple the acting on all over the body of collection multiclass medicine is that two types of resisting rheumatoid arthritis Western medicine and amcinonide are incomparable.Lignocaine is widely used clinically Bangesic, can play the symptom of rheumatoid arthritis patient pain, alleviates patient's misery.
At present, existing many about the research report of patch and patent, but do not have to the patch of Radix Tripterygii Wilfordii lactone alcohol and lignocaine specially, therefore there is not its preparation method yet.
Summary of the invention
The object of the invention is to provide a kind of treatment rheumatoid arthritis patch, and this patch is the slow releasing preparation of medicine controlled releasing, and principal agent can continue to discharge for a long time, and pharmacological effect is lasting, and prescription is simple.
A kind of patch technical scheme of treating rheumatoid arthritis is:
A kind of treatment rheumatoid arthritis patch; Wherein contain principal agent, drug solvent, binding agent, patch substrate and the Transdermal absorption penetrating agent of treating rheumatoid arthritis; The principal agent of treatment rheumatoid arthritis is the analgesic lidocaine hydrochloride of Radix Tripterygii Wilfordii lactone alcohol and rheumatoid arthritis pain, and the characteristics of this patch are the slow releasing preparation of medicine controlled releasing.
Said a kind of optimum weight proportioning of treating each composition of rheumatoid arthritis patch is: principal agent (1): principal agent (2): Transdermal absorption penetrating agent: binding agent and patch substrate and solvent=0.1～1 ‰: 2 ‰: 1～10%: 65～95%.
The present invention also provides a kind of prescription of treating the rheumatoid arthritis patch: Radix Tripterygii Wilfordii lactone alcohol (triptolide, triptolide) 481.5mg, lidocaine hydrochloride 2.4g, polyisobutylene oppanol B
10031.2g, polyisobutylene Oppanol B
1262.5g, lanoline 5.0g, liquid paraffin 15g, Borneolum Syntheticum 12g, 80% ethanol 9g, add chloroform to 1200g.
The present invention provides a kind of method for preparing of treating the rheumatoid arthritis patch simultaneously, the first step: get high molecular weight polyisobutylene oppanol B
10031.2g with low-molecular-weight polyisobutylene Oppanol B
1262.5g; Add chloroform to 1000g; Dissolve subsequent use (pressure sensitive adhesive) fully until high and low molecular weight polyisoprene isobutene.. second step: with an amount of chloroform dissolving Radix Tripterygii Wilfordii lactone alcohol; Dropwise slowly be added in the 5g lanoline, the limit edged stirs. the 3rd step: get 12g Borneolum Syntheticum and lidocaine hydrochloride 2.4g and add in the beaker, with an amount of 80% ethanol and chloroform dissolving.The 4th step: the lanoline that will contain medicine dropwise slowly is added to edged stirring in limit in the pressure sensitive adhesive.The 5th step: the solution that will contain 12g Borneolum Syntheticum and lidocaine hydrochloride dropwise slowly is added to edged stirring in limit in the pressure sensitive adhesive, and adds chloroform to 1200g.The 6th step: the pressure sensitive adhesive that will all add medicine stirs 1h with electric blender, places 12h, and the reuse electric blender stirs 1h, places 1-5h, to there not being bubble, in the impouring TB-300 type composite coating machine, is paved into the patch that thickness is 0.45mm.
Beneficial effect:
This patch:
(1) the medicine percutaneous absorbs, and directly gets into the body circulation, avoids medicine to receive the liver sausage first-pass effect;
(2) do not receive the influence of gastrointestinal tract various factors, also directly gastrointestinal tract not being caused stimulates or other adverse effect;
(3) this patch is the slow releasing preparation of medicine controlled releasing, has the slow release long-acting characteristics, can reach 24 hours, and only need be administered once every day;
(4) extremely easy to use, need not oral or injection;
(5) safety, the toxic reaction of medication as none has almost particularly been avoided the toxicity of Radix Tripterygii Wilfordii lactone alcohol;
(6) if untoward reaction in use occurs, also can wipe, stop administration immediately.
This patch method for preparing is simple, and small investment need not be purchased main equipment and adopt complicated technology.
The specific embodiment
A kind of rheumatoid arthritis patch of treating is made up of principal agent, drug solvent, binding agent, substrate and the Transdermal absorption penetrating agent of treatment rheumatoid arthritis, and principal agent is the analgesic lidocaine hydrochloride of Radix Tripterygii Wilfordii lactone alcohol and rheumatoid arthritis pain.
Drug solvent is a chloroform.
Binding agent and patch substrate are high molecular weight polyisobutylene oppanol B
100With low-molecular-weight polyisobutylene Oppanol B
12
The Transdermal absorption penetrating agent is wherein a kind or 2 kinds of lauryl alcohol, laurocapram (azone), Borneolum Syntheticum, Camphora, isopropyl myristate (IPM).
A kind of optimum weight proportioning of treating each composition of rheumatoid arthritis patch is: principal agent (1): principal agent (2): Transdermal absorption penetrating agent: binding agent and patch substrate and solvent=0.1～1 ‰: 2 ‰: 1～10%: 65～95%.
A kind of prescription of treating the rheumatoid arthritis patch is:
A kind of method for preparing of treating the rheumatoid arthritis patch is: the preparation of (1) pressure sensitive adhesive: get high molecular weight polyisobutylene oppanol B
10031.2g with low-molecular-weight polyisobutylene Oppanol B
1262.5g, add chloroform to 1000g, dissolve subsequent use fully until high and low molecular weight polyisoprene isobutene..(2) with an amount of chloroform dissolving Radix Tripterygii Wilfordii lactone alcohol, dropwise slowly be added in the 5g lanoline, the limit edged stirs.(3) get 12g Borneolum Syntheticum and lidocaine hydrochloride 2.4g and add in the beaker, with an amount of 80% ethanol and chloroform dissolving.The lanoline that (4) will contain medicine is added to slowly dropwise that the limit edged stirs in the pressure sensitive adhesive.The solution that (5) will contain 12g Borneolum Syntheticum and lidocaine hydrochloride is added to slowly dropwise that the limit edged stirs in the pressure sensitive adhesive, and adds chloroform to 1200g.The pressure sensitive adhesive that (6) will all add medicine stirs 1h with electric blender, places 12h, and the reuse electric blender stirs 1h, places 1-5h, to there not being bubble, in the impouring TB-300 type composite coating machine, is paved into the patch that thickness is 0.45mm.
Among the present invention, if necessary, can also suitably add and can be used for patch or operable additive, like PH regulators such as malic acid, phosphoric acid, citric acid, tartaric acid, lactic acid, diethanolamine, triethanolamine, diisopropanolamine (DIPA)s; Surfactants such as shrink pears sugar alcohol fatty acid ester, fatty acid glyceride, polyoxyethylene hydrogenation Semen Ricini, polyoxyethylene stearyl base ether, polyoxy ethyl lauryl ether, sodium lauryl sulfate; Lanoline, paraffin, olive are pulled oil, almond oil, polyisoprene, propylene glycol, colza wet goods softening agent; Astringent such as zinc oxide, aluminum sulfate; Antiseptic such as propyl p-hydroxybenzoate.
Patch of the present invention can adopt the method for general employing in the patch preparing technical field to prepare.
The container that among the present invention the dress patch is used has special regulation: medicinal carton or medicinal plastic bag or aluminium foil bag.
Claims (9)
1. treat the rheumatoid arthritis patch for one kind; Wherein contain principal agent, drug solvent, binding agent, patch substrate and the Transdermal absorption penetrating agent of treating rheumatoid arthritis, the principal agent that it is characterized in that treating rheumatoid arthritis is the analgesic lidocaine hydrochloride of Radix Tripterygii Wilfordii lactone alcohol and rheumatoid arthritis pain.
2. treatment rheumatoid arthritis patch according to claim 1 is characterized in that drug solvent is chloroform, dichloromethane, DMSO, acetonitrile, ethanol, methanol.
3. treatment rheumatoid arthritis patch according to claim 1 is characterized in that when drug solvent is claim 2, and binding agent and patch substrate are high molecular weight polyisobutylene oppanol B
100With low-molecular-weight polyisobutylene Oppanol B
121 kind or 2 kinds.
4. treatment rheumatoid arthritis patch according to claim 1; It is characterized in that working as drug solvent is claim 2; When binding agent and patch substrate were claim 3, the Transdermal absorption penetrating agent was wherein a kind or 2 kinds of lauryl alcohol, laurocapram (azone), Borneolum Syntheticum, Camphora, isopropyl myristate (IPM).
5. according to the patch of the described treatment rheumatoid arthritis of claim 1 to 4, it is characterized in that the optimum weight proportioning of each composition is: principal agent (1): principal agent (2): Transdermal absorption penetrating agent: binding agent and patch substrate and solvent=0.1～1 ‰: 2 ‰: 1～10%: 65～95%.
6. the patch according to the described treatment rheumatoid arthritis of claim 1 is characterized in that the prescription of this patch is: Radix Tripterygii Wilfordii lactone alcohol (triptolide, triptolide) 481.5mg, lidocaine hydrochloride 2.4g, polyisobutylene oppanol B
10031.2g, polyisobutylene Oppanol B
1262.5g, lanoline 5.0g, Borneolum Syntheticum 12g, 80% ethanol 9g, add chloroform to 1200g.
7. a method for preparing of treating the patch of rheumatoid arthritis is characterized in that: the first step: get high molecular weight polyisobutylene oppanol B
10031.2g with low-molecular-weight polyisobutylene Oppanol B
1262.5g, add chloroform to 1000g, dissolve subsequent use (pressure sensitive adhesive) fully until high and low molecular weight polyisoprene isobutene..Second step: the chloroform dissolving Radix Tripterygii Wilfordii lactone alcohol with an amount of, dropwise slowly be added in the 5g lanoline, the limit edged stirs.The 3rd step: get 12g Borneolum Syntheticum and lidocaine hydrochloride 2.4g and add in the beaker, with an amount of 80% ethanol and chloroform dissolving.The 4th step: the lanoline that will contain medicine dropwise slowly is added to edged stirring in limit in the pressure sensitive adhesive.The 5th step: the solution that will contain 12g Borneolum Syntheticum and lidocaine hydrochloride dropwise slowly is added to edged stirring in limit in the pressure sensitive adhesive, and adds chloroform to 1200g.The 6th step: the pressure sensitive adhesive that will all add medicine stirs 1h with electric blender, places 12h, and the reuse electric blender stirs 1h, places 1-5h, to there not being bubble, in the impouring TB-300 type composite coating machine, is paved into the patch that thickness is 0.45mm.
8. in the method for preparing of a patch of treating rheumatoid arthritis coating machine is not had special demands, general coating machine all is suitable for.
9. the container that among the present invention this patch is used does not have special regulation, is generally aluminium foil bag or plastic bag packaging, and outsourcing is a carton.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201110061304.5A CN102670624B (en) | 2011-03-14 | 2011-03-14 | Patch for treating rheumatic arthritis and preparation method thereof |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201110061304.5A CN102670624B (en) | 2011-03-14 | 2011-03-14 | Patch for treating rheumatic arthritis and preparation method thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN102670624A true CN102670624A (en) | 2012-09-19 |
| CN102670624B CN102670624B (en) | 2015-04-15 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201110061304.5A Expired - Fee Related CN102670624B (en) | 2011-03-14 | 2011-03-14 | Patch for treating rheumatic arthritis and preparation method thereof |
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| Country | Link |
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| CN (1) | CN102670624B (en) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109125733A (en) * | 2018-10-30 | 2019-01-04 | 成都先手生物科技有限公司 | A kind of composition for the treatment of of arthritis and its application |
| CN109908112A (en) * | 2019-04-19 | 2019-06-21 | 内蒙古科尔沁药业有限公司 | A kind of rubber paste emplastrum of not allergy and preparation method thereof |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101618030A (en) * | 2009-08-10 | 2010-01-06 | 沈阳亿灵医药科技有限公司 | Triptolide transdermal patch and preparation method thereof |
| CN102086199A (en) * | 2010-12-28 | 2011-06-08 | 广济药业（孟州）有限公司 | Method for self-extracting recycled riboflavin from liquid waste |
-
2011
- 2011-03-14 CN CN201110061304.5A patent/CN102670624B/en not_active Expired - Fee Related
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101618030A (en) * | 2009-08-10 | 2010-01-06 | 沈阳亿灵医药科技有限公司 | Triptolide transdermal patch and preparation method thereof |
| CN102086199A (en) * | 2010-12-28 | 2011-06-08 | 广济药业（孟州）有限公司 | Method for self-extracting recycled riboflavin from liquid waste |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN109125733A (en) * | 2018-10-30 | 2019-01-04 | 成都先手生物科技有限公司 | A kind of composition for the treatment of of arthritis and its application |
| CN109908112A (en) * | 2019-04-19 | 2019-06-21 | 内蒙古科尔沁药业有限公司 | A kind of rubber paste emplastrum of not allergy and preparation method thereof |
| CN109908112B (en) * | 2019-04-19 | 2022-04-19 | 内蒙古科尔沁药业有限公司 | Non-allergic rubber plaster and preparation method thereof |
Also Published As
| Publication number | Publication date |
|---|---|
| CN102670624B (en) | 2015-04-15 |
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Granted publication date: 20150415 Termination date: 20200314 |
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| CF01 | Termination of patent right due to non-payment of annual fee |