CN105288582A - Preparation for inhibiting protease activated receptor 2 - Google Patents
Preparation for inhibiting protease activated receptor 2 Download PDFInfo
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- CN105288582A CN105288582A CN201410365869.6A CN201410365869A CN105288582A CN 105288582 A CN105288582 A CN 105288582A CN 201410365869 A CN201410365869 A CN 201410365869A CN 105288582 A CN105288582 A CN 105288582A
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- preparation
- activated receptor
- protease activated
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- par
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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Abstract
The invention provides a preparation for inhibiting a protease activated receptor 2. The preparation is composed of 1%-10% of acetyl hexapeptide-46 and 0.1%-2% of nicotinamide. The preparation is capable of effectively inhibiting PAR-2 (protease activated receptor 2) to treat skin inflammation.
Description
Technical field
The present invention relates to field of medicine preparations, relate to a kind of preparation of protease inhibition activated receptor 2 specifically.
Background technology
Proteinase activated receptors (proteaseactivatedreceptors, PARS) belongs to g protein coupled receptor family member, and PARs has 4, and wherein PAR-2 is the receptor of trypsin and mastocyte pancreatin.PAR-2 molecule is present in polytype cell of different system, widely distributed, all there is PAR-2, have the effect of its uniqueness in skin metabolism in the multiple organ of human body.First, PAR-2 is the key receptor participating in neurogenic inflammation and pruritis, and PAR-2 activation can improve the release of the inflammatory factor such as interleukin-6, interleukin-8.Meanwhile, PAR-2 transports at the melanin of skin, also play important regulative in cutaneous pigmentation after ultraviolet radiation and inflammation, suppresses the melanin pigmentation of its active skin capable of blocking.Therefore, the skin pruritus, the pigmentation that suppress the preparation of PAR-2 activity to can be used for treating inflammation and inflammation to cause.
Summary of the invention
The object of the present invention is to provide a kind of preparation of protease inhibition activated receptor 2, said preparation is containing, for example the component of lower weight percent content:
1% ~ 10% acetyl group six peptide-46;
0.1% ~ 2% nicotiamide.
The preparation of a kind of protease inhibition activated receptor 2 of the present invention is also containing medically acceptable carrier.
The content of wherein said acetyl group six peptide-46 is preferably 2% ~ 5%, is preferably 3%;
The content of wherein said nicotiamide, preferably for being 0.2% ~ 0.8%, is preferably 0.5%.
The preparation of a kind of protease inhibition activated receptor 2 of the present invention, gel, unguentum, liquid preparation (as drop) etc. can be mixed with, can by the mode such as embrocating, for diseases such as prevention or treatment neurogenic dermatitis, skin pruritus, pigment anomaly are calm.
Positive progressive effect of the present invention is: different from other anti-inflammatory composition, and this compositions selects PAR-2 as its action target spot, and be for scytitis, the approach that especially neurogenic inflammation is more novel, this approach can affect the links of inflammation.Experiment in vitro proves, preparation of the present invention effectively can suppress PAR-2, thus reaches the effect for the treatment of scytitis.
Detailed description of the invention
The compound source used in example is as shown in table 1:
Table 1: the title of the compound used in embodiment and source
Embodiment 1 prepares antipruritic dermatitis plaster
Antipruritic dermatitis plaster raw material and content as shown in table 2:
Table 2: antipruritic dermatitis plaster raw material and content
Preparation technology comprises the steps:
The preparation technology of antipruritic dermatitis plaster comprises the steps, A group, B group raw material are mixed respectively, are heated to 80 C, B group raw material is added in A group raw material, homogenizing 2 minutes, the temperature of homogenizing is 80-90 C, and homogenization pressure is normal pressure, then adds C group raw material continuation homogenizing, the temperature of homogenizing is 80-90 C, and homogenization pressure is normal pressure.200-600RPM stirs cooling, and add D group raw material after being cooled to 40 DEG C, 500-1000RPM stirs, and obtains antipruritic dermatitis plaster.
The antipruritic dermatitis gel of embodiment 2
Raw material and the content of antipruritic dermatitis gel are as shown in table 3:
Table 3: antipruritic dermatitis gel material and content
Preparation technology comprises the steps:
C group sodium polyacrylate is swollen in water, temperature 50-60 C, stir 10min with 600-800PRM speed.Then be cooled to 38-40 C, stir with 800-1000PRM speed, while add acetyl group six peptide-46 and nicotiamide, continue to stir 20min; Add A group, B group raw material, 600-800RPM stirs, and obtains antipruritic dermatitis gel.
Experiment in vitro proves, the preparation of embodiment 1 and embodiment 2 to the suppression ratio of protease-activated receptor-2 more than 50%.
The foregoing is only better embodiment of the present invention; protection scope of the present invention is not limited with above-mentioned embodiment; in every case those of ordinary skill in the art modify or change according to the equivalence that disclosed content is done, and all should include in the protection domain recorded in claims.
Claims (3)
1. a preparation for protease inhibition activated receptor 2, is characterized in that the component of said preparation containing, for example lower weight percent content:
1% ~ 10% acetyl group six peptide-46;
0.1% ~ 2% nicotiamide.
2. the preparation of protease inhibition activated receptor 2 according to claim 1, is characterized in that the content of wherein said acetyl group six peptide-46 is 2% ~ 5%.
3. the preparation of protease inhibition activated receptor 2 according to claim 1, is characterized in that the content of wherein said nicotiamide is 0.2% ~ 0.8%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410365869.6A CN105288582A (en) | 2014-07-29 | 2014-07-29 | Preparation for inhibiting protease activated receptor 2 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201410365869.6A CN105288582A (en) | 2014-07-29 | 2014-07-29 | Preparation for inhibiting protease activated receptor 2 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN105288582A true CN105288582A (en) | 2016-02-03 |
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ID=55186857
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201410365869.6A Pending CN105288582A (en) | 2014-07-29 | 2014-07-29 | Preparation for inhibiting protease activated receptor 2 |
Country Status (1)
| Country | Link |
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| CN (1) | CN105288582A (en) |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013139965A2 (en) * | 2012-03-22 | 2013-09-26 | Lipotec, S.A. | Exopolysaccharide for the treatment and/or care of the skin, mucous membranes and/or nails |
| CN103619415A (en) * | 2010-11-30 | 2014-03-05 | 利普泰股份公司 | Exopolysaccharide for the treatment and/or care of the skin, mucous membranes, hair and/or nails |
-
2014
- 2014-07-29 CN CN201410365869.6A patent/CN105288582A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103619415A (en) * | 2010-11-30 | 2014-03-05 | 利普泰股份公司 | Exopolysaccharide for the treatment and/or care of the skin, mucous membranes, hair and/or nails |
| WO2013139965A2 (en) * | 2012-03-22 | 2013-09-26 | Lipotec, S.A. | Exopolysaccharide for the treatment and/or care of the skin, mucous membranes and/or nails |
Non-Patent Citations (2)
| Title |
|---|
| 张景云: "《实用美容药物学》", 31 July 2006 * |
| 魏保生: "《皮肤湿疹与荨麻疹》", 31 March 2014 * |
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| PB01 | Publication | ||
| C10 | Entry into substantive examination | ||
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| WD01 | Invention patent application deemed withdrawn after publication |
Application publication date: 20160203 |
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| WD01 | Invention patent application deemed withdrawn after publication |