CN103006689B - Antipruritic composition and application of same in preparation of antipruritics - Google Patents
Antipruritic composition and application of same in preparation of antipruritics Download PDFInfo
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- CN103006689B CN103006689B CN201210568326.5A CN201210568326A CN103006689B CN 103006689 B CN103006689 B CN 103006689B CN 201210568326 A CN201210568326 A CN 201210568326A CN 103006689 B CN103006689 B CN 103006689B
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Abstract
The invention discloses an antipruritic composition and an application of the antipruritic composition in preparation of antipruritics. The antipruritic composition comprises 0.1-0.5 parts of triclosan, 1-8 parts of sodium bicarbonate, and 0.5-2 parts of ammonia water. According to the antipruritic composition and application of the antipruritic composition in preparation of the antipruritics, provided by the invention, triclosan is used in combination with antalkalies (sodium bicarbonate and ammonia water) to achieve good antipruritic and antioncotic effects. The antipruritic composition adopts common raw materials, is low in cost, is free of skin irritation and toxic side effect, and has a wide application prospect. Moreover, the antipruritic composition is applicable to various diseases of cutaneous pruritus and skin infection, and is particular suitable for treatment of acute pruritus caused by mosquito bites, and the curative effect is effective.
Description
Technical field
The present invention relates to anti-pruritic formulation field, especially relate to a kind of antipruritic compositions and the application in preparing anti-pruritic formulation thereof.
Background technology
Summer and autumn, mosquito wreaked havoc, and to the mankind, brought many injuries, and human body is very easily caused local skin pruritus, redness, inflammation by mosquito bite, and people is constantly scratched, and then causes dermatitis, scar after even infecting.
Especially the dermatitis that mosquito bite causes is very common.The skin hypersensitivity reaction of its generation, mainly from mosquito saliva, venom and secretions, owing to wherein containing plurality of antigens composition, can produce allergy with antibody and cause inflammation after entering human body skin.As bite position in face, eyes, or the exposure portion in summer such as extremity, impact personal image, work and life.In daily life, child, particularly baby are more prone to be bit by insect, and occur redness or pain, cause that child cries and screams, and therefore, the product of effectively treating mosquito bite brings great convenience to people.
At present, although existed on the market some for antipruritic medicament, existing these medicament onsets are slow, and antipruritic effect is not good, and portioned product be not suitable for the skin that child is tender and lovely.
Summary of the invention
The object of the invention is, a kind of antipruritic compositions and the application in preparing pruritus thereof are provided, to improve the antipruritic effect of antipruritic compositions.
According to an aspect of the present invention, provide a kind of antipruritic compositions, having comprised: the triclosan of 0.1～0.5 part, the sodium bicarbonate of 1～8 part, the ammonia of 0.5～2 part.This antipruritic compositions can be equipped with acceptable adjuvant on preparation and make external use anti pruritic agent, and this pruritus can comprise 5%～100% antipruritic compositions.
The triclosan using in the antipruritic compositions of the present invention, chemical name: 2,4,4 '-tri-chloro-2 '-dihydroxy diphenyl ether (DP300) formal names used at school " triclosan ", chemical molecular formula is C
12h
7c
13o
2, having another name called " triclosan ", " Triclosan " etc., triclosan normality is white or the crystalline powder of canescence, slightly phenol stink.Water insoluble, be soluble in alkali liquor and organic solvent.The triclosan using in this antipruritic compositions is a kind of broad spectrum antimicrobicide, kills widely and inhibitory action the quick-acting and specially good effect dual function of tool to causing that infection or pathogenic bacteria, true mattress, yeast and virus etc. all have.
Inventor finds in long-term anti-pruritic formulation R&D work, and the reasonable use of triclosan also can be played antipruritic effect, but uses separately triclosan antipruritic effect not very good.In order to research and develop the desirable anti-pruritic formulation of a kind of antipruritic effect, inventor is with to skin nonirritant, suitable to child's use, further studies and prepares the antipruritic compositions that triclosan is primary raw material.Accidental chance once, inventor is used in conjunction with antalkali sodium bicarbonate and ammonia and triclosan, has significantly antipruritic and detumescence effect.The redness that small lot batch manufacture is used this antipruritic compositions that contains sodium bicarbonate, ammonia and triclosan of discovery not only mosquito bite to be caused is very itched and is had unique curative effect, and the skin infection causing due to scratching is had to obvious sterilization and bacteriostasis.
Preferably, above-mentioned antipruritic compositions comprises by weight: the triclosan of 0.1～0.5 part, the sodium bicarbonate of 1～8 part, the ammonia of 0.5～2 part, the tea tree oil of 0.05～0.5 part and the Mentholum of 0.1～0.5 part.
In this antipruritic compositions, triclosan, sodium bicarbonate and ammonia combine use, the redness that mosquito bite is caused is very itched unique curative effect, and the skin infection causing due to scratching is had to obvious sterilization and bacteriostasis; That the use of tea tree oil has is antibacterial, antiinflammatory, anthelmintic, the effect of killing demodicid mite, and in view of its permeability strong, can also increase the antibacterial degree of depth of this antipruritic compositions, improve fungistatic effect, and it also has characteristic perfume, can play refreshment effect; The use of Mentholum can act on skin or mucosa, has the refrigerant effect such as antipruritic.
Preferably, above-mentioned antipruritic compositions also comprises by weight: the Acritamer 940 of 0.2～1.5 part.Acritamer 940 is the matrix components that gel is conventional, and gel is a kind of conventional exterior-applied formulation, has and is coated with lubricated comfortable, good with skin coupling effect, easy cleaning, absorb fast, the features such as stable in properties.
More preferably, above-mentioned antipruritic compositions comprises: triclosan 0.2g, sodium bicarbonate 5g, ammonia 1.5g, tea tree oil 0.1g, Mentholum be 0.2g, add water to 100g.
More preferably, above-mentioned antipruritic compositions also comprises: Acritamer 940 1g.
In another aspect of the present invention, also provide the application of a kind of above-mentioned antipruritic compositions in preparing anti-pruritic formulation.Wherein, anti-pruritic formulation is preferably the medicine that is used for the treatment of skin pruritus and is used for the treatment of skin infection.More preferably, above-mentioned anti-pruritic formulation is the preparation being used for the treatment of by the caused acute skin pruritus of mosquito bite.
Preferably, in the application process of above-mentioned antipruritic compositions in preparing anti-pruritic formulation, preferably pruritus is made as to gel or liniment.And more preferably prepared gel or smear contains 2%～13% antipruritic compositions and appropriate adjuvant in agent.
Gel is a kind of conventional exterior-applied formulation, has and is coated with lubricated comfortable, good with skin coupling effect, easy cleaning, absorb fast, the features such as stable in properties.Can coordinate ballpoint bottle to use simultaneously, be more added with the advantage such as use safety, stable and durable effect, be convenient for carrying, both met people's demand, expanded again the object of clinical practice.
Beneficial effect of the present invention: antipruritic compositions provided by the present invention and the application in preparing pruritus thereof, by triclosan and antalkali sodium bicarbonate and ammonia are combined to use by a certain amount of, reach the effect of good antipruritic and detumescence.This antipruritic composition material is common and with low cost, without skin irritation, has no side effect, and is with a wide range of applications.And this antipruritic compositions is applicable to various skin pruritus and skin infection, the treatment of the acute pruritus that is particularly useful for mosquito bite to cause, and determined curative effect.
Except object described above, feature and advantage, the present invention also has other object, feature and advantage.Below with reference to the specific embodiment, the present invention is further detailed explanation.
The specific embodiment
Below in conjunction with specific embodiment, embodiments of the invention are elaborated, but following embodiment understands the present invention, and can not limit the present invention, the multitude of different ways that the present invention can be defined by the claims and cover is implemented.
Embodiment 1:
Raw material: triclosan 0.1g, sodium bicarbonate 1g, ammonia 0.5g, Acritamer 940 1.5g.
Preparation method: each raw material mixing and water adding, to 100g, is formed to gel with 15ml/ bottle subpackage after stirring 30min.
Embodiment 2:
Raw material: triclosan 0.5g, sodium bicarbonate 8g, ammonia 2g.
Preparation method: each raw material mixing and water adding, to 100g, is formed to liniment with 15ml/ bottle subpackage after stirring 30min.
Embodiment 3:
Raw material: triclosan 0.1g, sodium bicarbonate 2g, ammonia 0.5g, tea tree oil 0.05g, Mentholum are 0.1g.
Preparation method: each raw material mixing and water adding, to 100g, is formed to liniment with 15ml/ bottle subpackage after stirring 30min.
Embodiment 4:
Raw material: triclosan 0.45g, sodium bicarbonate 7g, ammonia 1.8g, tea tree oil 0.5g, Mentholum are 0.5g, Acritamer 940 1.2g.
Preparation method: each raw material mixing and water adding, to 100g, is formed to gel with 15ml/ bottle subpackage after stirring 30min.
Embodiment 5:
Raw material: triclosan 0.35g, sodium bicarbonate 5g, ammonia 1.8g, tea tree oil 0.25g, Mentholum are 0.3g, Acritamer 940 1.5g.
Preparation method: each raw material mixing and water adding, to 100g, is formed to gel with 15ml/ bottle subpackage after stirring 30min.
Embodiment 6:
Raw material: triclosan 0.2g, sodium bicarbonate 5g, ammonia 1.5g, tea tree oil 0.1g, Mentholum are 0.2g.
Preparation method: each raw material mixing and water adding, to 100g, is formed to liniment with 15ml/ bottle subpackage after stirring 30min.
Embodiment 7:
Raw material: triclosan 0.2g, sodium bicarbonate 5g, ammonia 1.5g, tea tree oil 0.1g, Mentholum are 0.2g, Acritamer 940 1g.
Preparation method: will add water to 100g after each raw material mix and blend, form gel with 15ml/ bottle subpackage after stirring 30min.
Antipruritic performance test:
Comparative example 1:
Raw material: triclosan 0.5g, tea tree oil 0.1g, Mentholum are 0.2g, Acritamer 940 1g.
Preparation method: will add water to 100g after each raw material mix and blend, form gel with 15ml/ bottle subpackage after stirring 30min.
Comparative example 2:
Raw material: triclosan 0.1g, sodium bicarbonate 15g, ammonia 4g, tea tree oil 0.1g, Mentholum are 0.2g, Acritamer 940 1g.
Preparation method: will add water to 100g after each raw material mix and blend, form gel with 15ml/ bottle subpackage after stirring 30min.
Adopt prepared drug sample in embodiment 1-7 to test as follows respectively:
Test one: antibacterial test
1, materials and methods
The mankind produce local skin pruritus, redness, inflammation after by mosquito bite, cause skin injury after scratching, and damaged skin is very easily by antibacterial and fungal infection, and then produce abscess and dermatitis.The existing clinical common infection of department of dermatologry is the fungal infection such as the antibacterial infection such as Pseudomonas aeruginosa, staphylococcus aureus, staphylococcus epidermidis and Candida albicans.The present invention is directed to clinical common bacteria and carry out antibacterial detection, evaluate the antibacterial effect of this antipruritic composite preparation.
Effective ingredient triclosan of the present invention is to skin nonirritant, and tea tree oil has characteristic perfume and antibacterial, antiinflammatory, anthelmintic, the effect of killing demodicid mite, and permeability is strong, and has refreshment effect; Mentholum acts on skin or mucosa, has the refrigerant effect such as antipruritic.And be prepared into gel and have more and be coated with by lubricated comfort, good with skin coupling effect, be easy to clean, absorb fast the features such as stable in properties.The equal temperature display of preparation constitutive property and, suitable adult and child use.
1.1 bacterial strain
(1) ATCC reference culture: (Nat'l Pharmaceutical & Biological Products Control Institute provides)
25922 escherichia colis (escherichia coli), 27853 Pseudomonas aeruginosas (bacillus pyocyaneus), 25923 staphylococcus aureuses (golden Portugal bacterium), 12228 staphylococcus epidermidiss (form staph), 90028 Candida albicans (reading in vain).
(2) clinical classification strain: (Dermatosis Hospital, Chinese Academy of Medical Sciences provides)
Staphylococcus epidermidis, salmonella typhi
1.2 method of testings:
(1) preparation of culture medium
PDA culture medium: get 39gPDA powder adding distil water 1000ml, after heating for dissolving, 115 ℃, sterilizing 30min.Treat that culture medium temperature is down to 50 ℃ of left and right, pour in sterilizing culture dish and make flat board, for recovery and the cultivation of fungus.
LB culture medium: get tryptone 10g, yeast extract 5g, sodium chloride 10g; Solid medium separately adds agar powder 15-20g, and adding distil water is to 1000ml.With 5mol/L NaOH, adjust pH to 7.0,121 ℃, sterilizing 30min.Recovery, cultivation for bacterial isolates.
(2) bacteriostatic test:
1>. micropore dilution method: by by prepared 10 concentration of formulation samples doubling dilution of embodiment 1-7, the initial concentration that makes pruritus is 50%, stops concentration and is decided to be 0.1%.Each bacterium is inoculated in respectively 37 ℃ of overnight incubation in the caseinhydrolysate liquid (being purchased from Britain Oxoid company) containing blood, 0.5 Maxwell pipe colorimetric and dilute 1: 100 standby.In microwell plate, from the 1st hole to the 10 hole concentration from high to low.The 11st hole is as growth control hole, and the 12nd hole is as blank hole.Record minimum inhibitory concentration (MIC)..
2>.K-B (agar diffusion method): adopt sterilizing Oxford cup and add above-mentioned formulation samples solution, above each bacterium is carried out to drug sensitive test.Measure antibacterial circle diameter.
(5) repeated trials process of the test is completely the same, in triplicate.
2, result of the test
(1) the antibacterial result of micropore dilution method, in Table 1.
Table 1 micropore dilution method triclosan Itch Stopping Gel agent bacteriostatic test MIC testing result
(2) K-B (agar diffusion method of the paper) result of the test is in Table 2.
Table 2K-B method triclosan Itch Stopping Gel agent inhibition zone (mm) result of the test (n=3)
By table 1 and table 2 result, shown, the agent of triclosan Itch Stopping Gel all has obvious inhibitory action to each bacterial strain.Staphylococcus epidermidis clinical strain has high susceptibility to antipruritic compositions provided by the present invention, and clinical strain drug resistance is greater than type strain, and golden Portugal bacterium, Candida albicans and salmonella typhi are lower to the sensitivity of triclosan gel.Two kinds of bacteriostasis method result of the tests are consistent.And preferably the antibacterial effect of pruritus prescription 7 is obviously better than prescription 1,4,5, is more better than contrasting prescription 1,2.
To sum up result of the test shows, triclosan Itch Stopping Gel of the present invention agent is a kind of external skin anti-inflammation formulation with powerful antibacterial action.And preferably prescription antibacterial effect is best, prove that triclosan of the present invention, sodium bicarbonate, ammonia coordinate prescription bacteriostasis to be better than using separately the prescription of triclosan and the prescription beyond protection domain of the present invention simultaneously.
Test two: red and swollen, antipruritic clinical trial disappear after mosquito bite.
Process of the test: get and bitten experimenter 200 people (wherein male 96 people, women 104 people, age 15-45 year), 100 people experimenters carry out the antipruritic test of triclosan gel, and 100 people experimenters carry out the antipruritic test of triclosan liniment.Adopt ballpoint bottle directly the embodiment of the present invention 6 and the prepared sample of embodiment 7 to be applied to and to be snapped position.And record is used the service time of triclosan pruritus, onset time, persistent period and use position, affected part.
Criterion of therapeutical effect:
Fine: antipruritic, the redness that disappears fast, effect is good.
General: to alleviate the pain of itching, alleviate red swelling of the skin.
Invalid: the antipruritic red and swollen DeGrain that disappears.
Result of the test is as shown in Table 3-5:
Table 3 triclosan Itch Stopping Gel agent detumescence, antipruritic effect detect
The detumescence of table 4 triclosan antipruritic application agent, antipruritic effect detect
Table 5 triclosan pruritus onset time and persistent period record
To be used for mosquito bite by the prepared formulation samples of antipruritic compositions provided by the present invention, use in latter 5 minutes, 100% experimenter's pruritus disappears, and average onset time is 5 minutes, 2 hours experimenters of gel continuous action reach 95%, and 1 hour experimenter of liniment continuous action reaches 93%.Result of the test shows, triclosan cooperation sodium bicarbonate and ammonia use, and very itching that mosquito bite is caused has unique curative effect, and to the red swelling of the skin causing due to scratching and infection determined curative effect.
These are only the preferred embodiments of the present invention, be not limited to the present invention, for a person skilled in the art, the present invention can have various modifications and variations.Within the spirit and principles in the present invention all, any modification of doing, be equal to replacement, improvement etc., within all should being included in protection scope of the present invention.
Claims (9)
1. an antipruritic compositions, is characterized in that, described antipruritic compositions comprises by weight: the triclosan of 0.1～0.5 part, the sodium bicarbonate of 1～8 part, the ammonia of 0.5～2 part, the tea tree oil of 0.05～0.5 part and the Mentholum of 0.1～0.5 part.
2. antipruritic compositions according to claim 1, is characterized in that, described antipruritic compositions comprises: triclosan 0.2g, sodium bicarbonate 5g, ammonia 1.5g, tea tree oil 0.1g, Mentholum be 0.2g, add water to 100g.
3. antipruritic compositions according to claim 1, is characterized in that, described antipruritic compositions also comprises: the Acritamer 940 of 0.2～1.5 part.
4. antipruritic compositions according to claim 2, is characterized in that, described antipruritic compositions also comprises: Acritamer 940 1g.
5. an external use anti pruritic agent, it comprises according to acceptable adjuvant on the antipruritic compositions of claim 1-4 any one and its preparation.
6. according to the external use anti pruritic agent of claim 5, the antipruritic compositions that it comprises 5%-100%, described pruritus is gel or liniment.
7. the application of the antipruritic compositions described in any one in preparing pruritus in a claim 1-4.
8. application according to claim 7, is characterized in that, described pruritus is the preparation that is used for the treatment of skin pruritus and is used for the treatment of skin infection.
9. application according to claim 8, is characterized in that, described pruritus is the preparation being used for the treatment of by the caused acute skin pruritus of mosquito bite.
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| CN103735494B (en) * | 2014-01-14 | 2015-07-01 | 山东司邦得制药有限公司 | External antipruritic ointment for treating mosquito bite and preparation method of external antipruritic ointment |
| CN104606095A (en) * | 2015-01-07 | 2015-05-13 | 青岛明药堂医疗股份有限公司 | Marine flower dew gel and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1237420A (en) * | 1998-11-30 | 1999-12-08 | 王长虹 | Compound beriberi powder |
| CN1411857A (en) * | 2002-10-08 | 2003-04-23 | 重庆康尔威药业股份有限公司 | Tea oil ointment and suppository |
| CN1647804A (en) * | 2004-01-20 | 2005-08-03 | 北京东方凯恩医药科技有限公司 | External medicine spray |
| CN102755255A (en) * | 2012-07-10 | 2012-10-31 | 北京同仁堂麦尔海生物技术有限公司 | Nanoscale liposome external preparation for relieving itching |
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2012
- 2012-12-25 CN CN201210568326.5A patent/CN103006689B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1237420A (en) * | 1998-11-30 | 1999-12-08 | 王长虹 | Compound beriberi powder |
| CN1411857A (en) * | 2002-10-08 | 2003-04-23 | 重庆康尔威药业股份有限公司 | Tea oil ointment and suppository |
| CN1647804A (en) * | 2004-01-20 | 2005-08-03 | 北京东方凯恩医药科技有限公司 | External medicine spray |
| CN102755255A (en) * | 2012-07-10 | 2012-10-31 | 北京同仁堂麦尔海生物技术有限公司 | Nanoscale liposome external preparation for relieving itching |
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