CN101269073A - Externally used anti-inflammatory pharmaceutical composition containing piketoprofen and preparation method thereof - Google Patents

Externally used anti-inflammatory pharmaceutical composition containing piketoprofen and preparation method thereof Download PDF

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Publication number
CN101269073A
CN101269073A CNA200710064582XA CN200710064582A CN101269073A CN 101269073 A CN101269073 A CN 101269073A CN A200710064582X A CNA200710064582X A CN A200710064582XA CN 200710064582 A CN200710064582 A CN 200710064582A CN 101269073 A CN101269073 A CN 101269073A
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China
Prior art keywords
external use
antiinflammatory agent
use according
piketoprofen
agent
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CNA200710064582XA
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Chinese (zh)
Inventor
孟凡静
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Beijing Dezhong Wanquan Medicines Technological Development Co Ltd
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Beijing Dezhong Wanquan Medicines Technological Development Co Ltd
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Priority to CNA200710064582XA priority Critical patent/CN101269073A/en
Publication of CN101269073A publication Critical patent/CN101269073A/en
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Abstract

The invention discloses an anti-inflammation drug compound for external use containing piketoprofer and the preparation method thereof. The drug compound consists of piketoprofer active ingredients and matrix components and has forms of creams, ointments or jellies. The drug compound is mainly used for treating osteoarthritis and sarcitis.

Description

A kind of externally used antiphlogistic anti pharmaceutical composition that contains piketoprofen and preparation method thereof
Technical field
The present invention relates to a kind of externally used antiphlogistic anti pharmaceutical composition and preparation method thereof, especially relate to a kind of externally used antiphlogistic anti medicine semi-solid combination that contains piketoprofen and preparation method thereof, wherein piketoprofen is mixed in the matrix components with dispersity.This external anti-inflammatory pharmaceutical compositions is mainly used in the treatment of osteoarthritis, myositis etc.
Background technology
Piketoprofen belongs to a kind of NSAID (non-steroidal anti-inflammatory drug), is applicable to the pain relieving of motor system inflammation such as osteoarthritis, myositis; The part is used for the auxiliary treatment of periarthritis, arthrosis, rheumatoid myositis, lumbago etc.
CN03803580 discloses a kind of medicinal tablet, is applicable to that the active component of this tablet comprises piketoprofen.The shortcoming of non-steroidal anti-inflammatory preparation is that they can cause gastroenteropathy when carrying out oral administration.For avoiding these shortcomings, various researchs have been carried out with the development antiinflammatory agent for external use.
US2005004098 discloses a kind of dispersible formulation agent of antiinflammatory, and this kind preparation is mainly used in the inflammation that treatment has the liquid organ of outer opening.The medicinal active ingredient that is applicable to said preparation comprises piketoprofen.But this dispersible formulation agent can only be used to have the liquid organ of outer opening, and certain use limitation is arranged, and it mainly provides a kind of suspension, and the uniformity is bad.
The invention provides a kind of externally used antiphlogistic anti medicine that contains the piketoprofen active component,, make the semi-solid preparation outward appearance uniform and smooth, modest viscosity, the uniformity height that make by the substrate of selecting to suit.Simultaneously, because pyrrone Lip river phenol is poorly water soluble drugs, how making the particle diameter of this antiinflammatory agent for external use up to specification also is one of difficult problem, and the inventor has found a kind of suitable method, it can be distributed in the substrate uniformly, and particle diameter is very little.This externally used antiphlogistic anti preparation is mainly used in the pain relieving of motor system inflammation such as arthritis, osteitis; The part is used for the auxiliary treatment of periarthritis, arthrosis, rheumatoid myositis, lumbago etc.
Summary of the invention
The invention provides a kind of antiinflammatory agent for external use, its active component is piketoprofen or its physiologically acceptable salt, and is mixed in the substrate with dispersity, and the existence form of this antiinflammatory agent for external use is a semi-solid preparation, can be ointment, ointment or gel.
This antiinflammatory agent for external use provided by the invention, piketoprofen and physiologically acceptable salt thereof mix with the amount of 0.5%~5% percentage by weight, and preferred 1%~3%.
This antiinflammatory agent for external use provided by the invention, its matrix components contains hydrophilic polymer, oily matter, nonionic surfactant, water, antioxidant, antiseptic and penetrating agent.
This antiinflammatory agent for external use provided by the invention, its hydrophilic polymer are selected from one or more the mixture in glycerol, sorbitol, propylene glycol, the carbomer, and its percentage by weight is 50~70%.
This antiinflammatory agent for external use provided by the invention, its oily matter is selected from one or more the mixture in lanoline, octadecanol, hexadecanol, microwax, white vaseline, Cera Flava, dimethicone, liquid paraffin, the paraffin, and its percentage by weight is 30~50%.
This antiinflammatory agent for external use provided by the invention, its nonionic surfactant are selected from one or more the mixture in triolein, glyceryl monostearate, sucrose ester, spans, Tweens, the poloxamer, and its percentage by weight is 2~15%.
This antiinflammatory agent for external use provided by the invention, its penetrating agent are selected from one or more the mixture in oleic acid, menthol, dimethicone, ethanol, glycerol, liquid paraffin, dimethyl sulfoxide, the azone, and its percentage by weight is 0.01~5%.
With after the The suitable solvent heating for dissolving, redispersion is in substrate earlier for this antiinflammatory agent for external use provided by the invention, its active component piketoprofen and physiologically acceptable salt thereof.
This antiinflammatory agent for external use provided by the invention, the selected The suitable solvent of lytic activity composition are selected from a kind of in ethanol, chloroform, chloroform, the glacial acetic acid.
This antiinflammatory agent for external use provided by the invention is mainly used in the pain relieving of motor system inflammation such as osteoarthritis, myositis; The part is used for the auxiliary treatment of periarthritis, arthrosis, rheumatoid myositis, lumbago etc.
Specific embodiment
The present invention is described in further detail below in conjunction with embodiment, but be not limited to following embodiment.Wherein " % " is meant " weight % ".
Embodiment one
The existence form of this embodiment is an ointment.
Figure A20071006458200041
Figure A20071006458200051
Preparation method:
The recipe quantity sorbitol is dissolved in recipe quantity 1, in the ammediol, adds the polypropylene glycol and the PVP of recipe quantity then, stirring and dissolving gets solution 1.Recipe quantity hydrochloric acid pyrrone Lip river phenol is dissolved in the chloroform, and heating makes it to accelerate dissolving, and it is added in the solution 1, and the limit edged stirs.Mixed solution is stirred 1h at 10 ℃, get wax shape ointment.
Embodiment two
The existence form of this embodiment is an emulsifiable paste.
Figure A20071006458200052
Preparation method:
The oil phase preparation method:
1, takes by weighing recipe quantity hexadecanol, glyceryl monostearate and liquid paraffin, put into beaker, heating in water bath to 75 degree while stirring after the mixing.
2, get dissolve with ethanol hydrochloric acid piketoprofen, after the dissolving, add in the above-mentioned solution fully, stir.
Aqueous phase preparation method:
Take by weighing recipe quantity glycerol, pure water, propylene glycol, BHA and methyl hydroxybenzoate and join in the beaker, heating in water bath to 75 degree while stirring after the mixing.
The preparation of emulsifiable paste
Oil phase is put in the 75 degree water-baths,, slowly adds water simultaneously with the speed stirring oil phase of dispersing emulsification machine with 1000 rev/mins.Stir 5min, it is taken out from water-bath put into cold water, make its fast cooling, simultaneously with 100 rev/mins speed stirring.
Embodiment three
The existence form of this embodiment is a gel.
Figure A20071006458200061
Preparation method:
Card pool nurse-934, Polyethylene Glycol and PVP are dissolved in the water of recipe quantity, dissolve fully solution.Principal agent is dissolved in the glacial acetic acid, adds in the above-mentioned solution.Regulate pH value to 5~7 with triethanolamine.

Claims (10)

1. antiinflammatory agent for external use, its active component is piketoprofen or its physiologically acceptable salt, wherein said piketoprofen is mixed in the substrate with dispersity, and the existence form of this antiinflammatory agent for external use is a semi-solid preparation, can be ointment, ointment or gel.
2. antiinflammatory agent for external use according to claim 1 is characterized in that piketoprofen and physiologically acceptable salt thereof mix preferred 1%~3% with the amount of 0.5%~5% percentage by weight.
3. antiinflammatory agent for external use according to claim 1 is characterized in that the pH value scope is between 6~8.
4. antiinflammatory agent for external use according to claim 1, wherein said matrix components contain hydrophilic polymer, oily matter, nonionic surfactant, water, antioxidant, antiseptic, pH regulator agent and penetrating agent.
5. antiinflammatory agent for external use according to claim 3 is characterized in that hydrophilic polymer is selected from one or more the mixture in glycerol, sorbitol, propylene glycol, the carbomer, and its percentage by weight is 50~70%.
6. antiinflammatory agent for external use according to claim 3, it is characterized in that oily matter is selected from one or more the mixture in lanoline, 16 octadecanol, hexadecanol, microwax, white vaseline, Cera Flava, dimethicone, liquid paraffin, the paraffin, its percentage by weight is 30~50%.
7. antiinflammatory agent for external use according to claim 3, it is characterized in that nonionic surfactant is selected from one or more the mixture in triolein, glyceryl monostearate, sucrose ester, spans, Tweens, the poloxamer, its percentage by weight is 2~15%.
8. antiinflammatory agent for external use according to claim 3, it is characterized in that penetrating agent is selected from one or more the mixture in oleic acid, menthol, dimethicone, ethanol, glycerol, liquid paraffin, dimethyl sulfoxide, the azone, its percentage by weight is 0.01~5%.
9. according to claim 1 described antiinflammatory agent for external use, it is characterized in that active component piketoprofen and physiologically acceptable salt thereof earlier with after the The suitable solvent heating for dissolving, redispersion is in substrate.
10. antiinflammatory agent for external use according to claim 8, wherein said The suitable solvent are selected from a kind of in ethanol, chloroform, chloroform, the glacial acetic acid.
CNA200710064582XA 2007-03-21 2007-03-21 Externally used anti-inflammatory pharmaceutical composition containing piketoprofen and preparation method thereof Pending CN101269073A (en)

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CNA200710064582XA CN101269073A (en) 2007-03-21 2007-03-21 Externally used anti-inflammatory pharmaceutical composition containing piketoprofen and preparation method thereof

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Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102068405A (en) * 2010-12-16 2011-05-25 天津工业大学 Ketoprofen gel and preparation method thereof
CN102258568A (en) * 2010-05-27 2011-11-30 迪特克(济源)绿色生物科技有限公司 Method for preparing external rabdosia rubescens antibacterial cream
CN103446044A (en) * 2013-09-05 2013-12-18 江苏中丹制药有限公司 Liranaftate ointment and preparation method thereof

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102258568A (en) * 2010-05-27 2011-11-30 迪特克(济源)绿色生物科技有限公司 Method for preparing external rabdosia rubescens antibacterial cream
CN102258568B (en) * 2010-05-27 2012-11-21 迪特克(济源)绿色生物科技有限公司 Method for preparing external rabdosia rubescens antibacterial cream
CN102068405A (en) * 2010-12-16 2011-05-25 天津工业大学 Ketoprofen gel and preparation method thereof
CN103446044A (en) * 2013-09-05 2013-12-18 江苏中丹制药有限公司 Liranaftate ointment and preparation method thereof

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Application publication date: 20080924