CN103655523A - Tapentadol composition - Google Patents
Tapentadol composition Download PDFInfo
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- CN103655523A CN103655523A CN201310722266.2A CN201310722266A CN103655523A CN 103655523 A CN103655523 A CN 103655523A CN 201310722266 A CN201310722266 A CN 201310722266A CN 103655523 A CN103655523 A CN 103655523A
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- tapentadol
- preparation
- tapentadol hydrochloride
- present
- sodium acetate
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- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention discloses a tapentadol transdermal agent which contains tapentadol hydrochloride, an adhesive and sodium acetate. The tapentadol transdermal agent disclosed by the invention has the advantages that the little skin irritation is caused, the skin permeability of the tapentadol hydrochloride is excellent, and the tapentadol transdermal agent still has high stability after being used for a long time.
Description
Technical field
The present invention relates to contain tapentadol hydrochloride (chemical name: 3-[(1R, 2R)-3-(dimethylamino)-1-ethyl-methyl-propyl] phenol) or the tape preparation of the transdermal administration of its hydrochlorate, said preparation has fabulous percutaneous permeability and has low skin irritation.The tape preparation of the transdermal administration containing tapentadol hydrochloride of the present invention is supposed to as Lente anesthetic agent or analgesic.
Background technology
The chemical name of tapentadol hydrochloride is 3-[(1R, 2R)-3-(dimethylamino)-1-ethyl-methyl-propyl] phenolate hydrochlorate, molecular formula is C
14h
23nOHCl, molecular weight is 257.8.The central analgesics of a kind of novel double action mechanism of this medicine, it is opium μ receptor (MOR) agonist, again norepinephrine (norepinephrine, NE) cell reabsorption inhibitor, it all has good analgesic activity to acute, inflammatory and chronic neuropathic pain model.
In the U.S., the slow releasing preparation that contains tapentadol hydrochloride goes on the market.But, there are no preparation capable of permeating skin list marketing.
Therefore, the object of the invention is to solve above-mentioned problems of the prior art, provide a kind of little to skin irritation, permeability is fabulous, the preparation capable of permeating skin of long-time stable hydrochloric tapentadol hydrochloride.
Inventor of the present invention, for achieving the above object, through further investigation, find to there is fabulous percutaneous permeability and the preparation capable of permeating skin low to skin irritation by adding sodium acetate to prepare in the binding agent to containing tapentadol hydrochloride or its salt, thereby completed the present invention.
Because tapentadol hydrochloride has good clinical value and application prospect, institute both domestic and external and medicine enterprise all attach great importance to the research and development of this medicine and production.At present, not yet there is open source literature report this product to be prepared as preparation capable of permeating skin, this product is prepared as to preparation capable of permeating skin, can more be widely used in ache in late cancer, Postoperative analgesia and other are not suitable with oral patient.
Summary of the invention
Preferably tapentadol hydrochloride accounts for the 1-20% of adhesive phase gross weight of the present invention.If be less than 1%, as the tape preparation of transdermal administration, can not obtain enough infiltration capacities, if its content surpasses 20%, the physical property of preparation itself is had to bad influence, so not preferred.
The binding agent that in fentanyl transdermal administration tape preparation of the present invention, adhesive phase contains, without particular limitation.Can use preferred example to comprise polyisobutylene (PIB), styrene isoprene styrene block copolymer (SIS), isoprene rubber, styrene butadiene styrene block copolymer (SBS) (SIS), silicon gel binding agent (SGA), acrylic acid polymer.These polymer can be used alone or use mixture two or more in them.In them, preferably use 2 kinds of components that contain PIB and SIS.In this case, the weight ratio of PIB used and SIS is preferably 1:1 to 1:4.
Binding agent preferably accounts for the 1-98% of adhesive phase gross weight of the present invention, more preferably 1-70%, particularly preferably 1-50%.If the amount of binding agent is less than 1%, the physical property of preparation itself can be poor, therefore not preferred.If its content surpasses 98%, can not obtain the satisfied bonding effect of application on human skin, therefore not preferred.
If add sodium acetate in the adhesive phase of tapentadol hydrochloride transdermal administration tape preparation of the present invention, the percutaneous permeability of tapentadol hydrochloride or its salt can improve greatly.Preferably containing the amount of sodium acetate, account for the 1-15% of adhesive phase total amount, more preferably 1-10%, particularly preferably 1-5%.If the amount of sodium acetate is less than 1%, can not obtain the effect that increases significantly percutaneous permeability; If its content surpasses 15%, the thorn of skin is become silted up and wins and will increase, therefore not preferred.
When tapentadol hydrochloride salt is tapentadol hydrochloride, the weight ratio of tapentadol hydrochloride and sodium acetate is at (2-4): (0.5-2.5), preferably (3-3.5): (1.0-2.0), particularly preferably during 3:1, aspect physical property and percutaneous permeability, can reach maximum effect.If the weight of allocating into of sodium acetate is less than aforementioned proportion, percutaneous permeability obviously reduces, and if the weight of allocating into of sodium acetate is greater than aforementioned proportion, tape preparation is by inhomogeneous, and physical property is as very poor in bond property, therefore, not preferred.
In addition, because the cohesive of binding agent is low, in order to increase the cohesive of preparation, can in the adhesive phase of preparation of the present invention, add viscosifier, viscosifier can be polyterpene resin classes.
Viscosifier preferably account for the 1-60% of adhesive phase total amount, more preferably 5-40%, particularly preferably 10-35% in preparation of the present invention.
In addition, in order to improve the processing characteristics of transdermal administration tape preparation of the present invention and to control its cohesive, can in adhesive phase, add oil as softening agent.As oil, liquid paraffin preferably and particularly preferably.The content of oil preferably accounts for the 1-70% of preparation adhesive phase total amount of the present invention, more preferably 5-50%, and 20-50% particularly preferably.
In addition, as required, can in the adhesive phase of preparation of the present invention, add Percutaneous absorption enhancer.As Percutaneous absorption enhancer, can use any known compound that increases percutaneous permeability, particularly preferably lauryl alcohol.
In addition, for absorb that skin produces as the hydrous matter of antiperspirant etc., can as required, in preparation of the present invention, add hydrophilic polymer.As hydrophilic polymer, preferred hydroxypropyl cellulose.
Also can add cross-linking agent, antiseptic, antioxidant in addition, and in the adhesive phase of other components preparation of the present invention.
The adhesive phase of tape preparation of the present invention is preferably made with non-aqueous substrate, uses non-aqueous substrate can effectively bring into play effect of the present invention.
The adhesive phase with above-mentioned composition can be used the preparation of any conventional method.For example, when using solvent method to prepare, can then stir by adding other components in the organic solution to polymer, be applied in bottom dry, make preparation of the present invention.In addition, when used polymer will be used with hot melt, can then add other components by dissolve polymer component when high temperature, stir, be applied in basal layer and make preparation of the present invention.
Embodiment
The object of the present invention is achieved like this:
| Sodium acetate | 2.0% |
| Silicon gel binding agent (SGA) | 88.5% |
| Epoxy resin (cross-linking agent) | 3.0% |
| Antioxidant (BHT) | 0.5% |
| Tapentadol hydrochloride | 6.0% |
| Total amount | 100% |
By sodium acetate, epoxy resin and tapentadol hydrochloride add in ethanol, in stirring at room, dissolve.Then, in mixture, add solution and BHT the stirring of silicon gel binding agent in ethyl acetate.Mixture is applied on polyethylene terephthalate vinegar film, 80 ℃ of heat cross-linkings 20 minutes, obtains the thick adhesive phase of 50 μ m.Use this adhesive phase to make transdermal administration tape preparation of the present invention by conventional method.
Claims (5)
1. a preparation capable of permeating skin for pharmaceutical composition, comprises tapentadol hydrochloride.
2. preparation capable of permeating skin according to claim 1, is characterized in that, tapentadol hydrochloride is hydrochlorate.
3. the preparation capable of permeating skin of claim 2, wherein the weight ratio of tapentadol hydrochloride and sodium acetate is 2-4:0.5-2.5.
4. the preparation capable of permeating skin of claim 2, wherein the weight ratio of tapentadol hydrochloride and sodium acetate is 3-3.5:1.0-2.0.
5. the preparation capable of permeating skin of claim 2, wherein the weight ratio of tapentadol hydrochloride and sodium acetate is 3:1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310722266.2A CN103655523A (en) | 2013-12-24 | 2013-12-24 | Tapentadol composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310722266.2A CN103655523A (en) | 2013-12-24 | 2013-12-24 | Tapentadol composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN103655523A true CN103655523A (en) | 2014-03-26 |
Family
ID=50295087
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201310722266.2A Pending CN103655523A (en) | 2013-12-24 | 2013-12-24 | Tapentadol composition |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN103655523A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111346077A (en) * | 2018-12-21 | 2020-06-30 | 宜昌人福药业有限责任公司 | Tapentadol transdermal drug delivery pharmaceutical composition, preparation method and application thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1193275A (en) * | 1996-05-13 | 1998-09-16 | 久光制药株式会社 | Percutaneous tap preparation containing fentanyl |
| CN102159284A (en) * | 2008-09-05 | 2011-08-17 | 格吕伦塔尔有限公司 | Pharmaceutical combination of 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol and antiepileptic |
| CN102281876A (en) * | 2008-10-30 | 2011-12-14 | 格吕伦塔尔有限公司 | Novel and potent tapentadol dosage forms |
| CN103108631A (en) * | 2010-06-15 | 2013-05-15 | 格吕伦塔尔有限公司 | Pharmaceutical combination for the treatment of pain |
-
2013
- 2013-12-24 CN CN201310722266.2A patent/CN103655523A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1193275A (en) * | 1996-05-13 | 1998-09-16 | 久光制药株式会社 | Percutaneous tap preparation containing fentanyl |
| CN102159284A (en) * | 2008-09-05 | 2011-08-17 | 格吕伦塔尔有限公司 | Pharmaceutical combination of 3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol and antiepileptic |
| CN102281876A (en) * | 2008-10-30 | 2011-12-14 | 格吕伦塔尔有限公司 | Novel and potent tapentadol dosage forms |
| CN103108631A (en) * | 2010-06-15 | 2013-05-15 | 格吕伦塔尔有限公司 | Pharmaceutical combination for the treatment of pain |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111346077A (en) * | 2018-12-21 | 2020-06-30 | 宜昌人福药业有限责任公司 | Tapentadol transdermal drug delivery pharmaceutical composition, preparation method and application thereof |
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| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20140326 |
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| WD01 | Invention patent application deemed withdrawn after publication |