CN107519024A - A kind of alcohol-free mosquito repellent/anti-pruritic compositions and preparation method thereof - Google Patents

A kind of alcohol-free mosquito repellent/anti-pruritic compositions and preparation method thereof Download PDF

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CN107519024A
CN107519024A CN201710840403.0A CN201710840403A CN107519024A CN 107519024 A CN107519024 A CN 107519024A CN 201710840403 A CN201710840403 A CN 201710840403A CN 107519024 A CN107519024 A CN 107519024A
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water
composition
solution
based structure
oil phase
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CN107519024B (en
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刘建宁
郭奕光
陆志航
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Shanghai Jahwa United Co Ltd
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/02Cosmetics or similar toiletry preparations characterised by special physical form
    • A61K8/04Dispersions; Emulsions
    • A61K8/042Gels
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/34Alcohols
    • A61K8/342Alcohols having more than seven atoms in an unbroken chain
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/33Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing oxygen
    • A61K8/37Esters of carboxylic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/30Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
    • A61K8/49Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds
    • A61K8/4906Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom
    • A61K8/4926Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds containing heterocyclic compounds with one nitrogen as the only hetero atom having six membered rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/73Polysaccharides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K8/00Cosmetics or similar toiletry preparations
    • A61K8/18Cosmetics or similar toiletry preparations characterised by the composition
    • A61K8/72Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
    • A61K8/84Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds obtained by reactions otherwise than those involving only carbon-carbon unsaturated bonds
    • A61K8/89Polysiloxanes
    • A61K8/891Polysiloxanes saturated, e.g. dimethicone, phenyl trimethicone, C24-C28 methicone or stearyl dimethicone
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61QSPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
    • A61Q17/00Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
    • A61Q17/02Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings containing insect repellants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2800/00Properties of cosmetic compositions or active ingredients thereof or formulation aids used therein and process related aspects
    • A61K2800/20Chemical, physico-chemical or functional or structural properties of the composition as a whole
    • A61K2800/30Characterized by the absence of a particular group of ingredients

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Birds (AREA)
  • Epidemiology (AREA)
  • Emergency Medicine (AREA)
  • Pest Control & Pesticides (AREA)
  • Dermatology (AREA)
  • Plant Pathology (AREA)
  • Chemical & Material Sciences (AREA)
  • Dispersion Chemistry (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Cosmetics (AREA)

Abstract

The invention discloses a kind of alcohol-free mosquito repellent/anti-pruritic compositions, it is included:(a) the water-based structure-solution of the microgel of low viscosity, the viscosity of the water-based structure-solution are less than 200mPas, and density is 1 ± 0.01g/cm3, the water-based structure-solution includes:(i) high molecular polysaccharide polymer, and (ii) inorganic cation, and (b) oil phase, the oil phase include mosquito repellent and/or antipruritic active ingredients, and the density of the oil phase is 1 ± 0.01g/cm3

Description

A kind of alcohol-free mosquito repellent/anti-pruritic compositions and preparation method thereof
Technical field
The present invention relates to it is a kind of can stable suspersion grade oil droplet low viscosity the water-based structure-solution of microgel, and bag The mosquito expelling and/or antipruritic waterborne compositions of the water-based structure-solution of microgel containing the low viscosity.The water-based structure of the present invention The mosquito repellent and/or antipruritic waterborne compositions of solution and/or the present invention not spirituosity.It is low viscous the invention further relates to this is prepared The mosquito expelling and/or antipruritic water of the water-based structure-solution of microgel of degree and the water-based structure-solution of microgel comprising the low viscosity The method of property composition.
Background technology
Contain a certain amount of surfactant as emulsifying agent or solubilizer in conventional water phase and an oil phase emulsification system to stablize System.However, the water-based structure-solution of low viscosity can utilize the coordination cross-linked of high molecular polysaccharide polymer and inorganic cation Interaction, form tridimensional network and carry out stabilising system, the water-based structure-solution of the low viscosity need not add surfactant To reduce the surface tension of water phase and an oil phase, its microgel system formed can stable suspersion grade oil droplet, simply aqueous phase and oil The density of phase need to be controlled in 1 ± 0.01g/cm3It is interior.
Gellan gum is a kind of polysaccharide polymer with fiber trait, viscous-elastic behaviour and excellent flavor release property, and A kind of excellent gelinite.Gellan gum is by tetrose recurring unit D- (1-3) glucopyranose units, D- (1-4) glucopyra Uronic acid unit, D- (1-4) glucopyranose units, L- (1-4) rhamnopyranosyloxyhy sugar unit pass sequentially through glycosidic bond and are formed by connecting Macromolecule saccharide compound.Gellan gum product has two kinds of existence forms:One kind is that (also referred to as natural knot is cold for high acyl gellan gum Glue), another kind is low-acyl gellan gum (also referred to as deacylated gellan gum).Their host molecule structure is identical, be all on The macromolecule saccharide compound of tetrose repeat unit composition is stated, relative molecular mass is about 5 × 105Dalton.Because it has Splendid stabilization and suspension effect, the application in foods and cosmetics field become more and more extensive, wherein low acyl group knot is cold Glue formation gelling ability is stronger, is more conducive to the stability of system.
Gellan gum solution is a kind of typical pseudoplastic fluid, and its solution viscosity substantially drops with the increase of shear rate It is low, recover with the decrease of shear rate.After gellan gum is dissolved in water, it can assemble to form the double helix model automatically between molecule, Two strands form bifilar parallel spiral with right-handed spiral, and it is mainly intermolecular hydrogen to stablize double-stranded active force Key, further aggregation can form tridimensional network to double helix.Heat temperature raising or stirring can make tridimensional network and double helix Body disintegrates, therefore under high-rate of shear effect, tridimensional network will be decomposed into random ball of string structure and make solution viscosity It is rapid to reduce.And when shear rate or heat effect release, molecular structure can return to tridimensional network again.It is in addition, inorganic Cation also contributes to stablize double-spiral structure and accelerates double helix to form tridimensional network.
Xanthans also known as Xanthan Gum, be sarson Xanthomonas campestris using carbohydrate as primary raw material, through hair A kind of widely used Microbial exopolysaccharides of ferment engineering production.Xanthans is by D-Glucose, D-MANNOSE, D-Glucose " pentasaccharides repeat unit " topology convergence body of aldehydic acid, acetic acid and pyruvic acid composition, its relative molecular mass is 2 × 106-50× 106Dalton or so.
The secondary structure of xanthans be side chain around main chain backbone reverse-winding, maintain to form bar-shaped double helix knot by hydrogen bond Structure, the tertiary structure of xanthans are bar-like combining the spiral complex formed by faint non-covalent bond between double-spiral structure.By There is good thickening property, the denaturation of false creeping, water solubility, suspension, emulsion stability, acid and alkali-resistance, salt resistance and excellent in xanthans The characteristics such as good plyability, it is widely used in cosmetics, food, medicine, spices using coverage rate individual industry up to more than 20 Deng field.
Icaridin, chemical name:1- piperidine carboxylic acids -2- (2- ethoxys) -1- methyl-prop base esters, it is that a kind of efficiently micro- poison drives Mosquito agent, trade name Saltidin, colorless and odorless liquid is not soluble in water, is soluble in alcohol, vegetable oil etc., density 1.036g/ cm3.Icaridin is a kind of active ingredient for the insect repellent agent being applied on skin, has good cosmetic properties, to skin Close friend, have no toxic side effect, it is nonirritant, Metadelphene (DEET) can be substituted completely, is had good stability in formula, with a variety of synthesis Composition has good compatibility, can protect biting for a variety of arthropods.
Bisabolol is a kind of composition being present in yellow chamomile, and the antiinflammation of yellow chamomile is essentially from opopanax The monocyclic unsaturated half times of terpene alcohol of alcohol-one kind.Bisabolol not only has anti-inflammation detumescence and other effects, is also proved to have bacteriostatic activity, Anti-irritant effect, protection skin effect and repair effect, general addition be 0.2 to 1.0%, in most cases 0.2 to 0.5%;For bisabolol, an optimum concentration be present.Beyond this concentration, validity reduces that (3% compares on the contrary on the contrary 1% is weak);Bisabolol is not soluble in water and glycerine, is dissolved in fatty alcohol and paraffin etc., density 0.92g/cm3
Inventor attempts to seek the water-based structure-solution of microgel for realizing low viscosity, verifies high molecular polysaccharide polymer knot Cold glue, by Coordination interaction, forms tridimensional network, it is achieved thereby that being realized using the effect low with inorganic cation The water-based structure-solution of microgel of viscosity, it has splendid suspension stability, can stable suspersion milli under conditions of low viscosity Meter level oil droplet (such as elite oil droplet), the oil droplet can include effective active composition Icaridin or bisabolol.
The content of the invention
It is an object of the invention to provide a kind of water-based structure-solution of microgel of nonalcoholic low viscosity, the water-based structure Solution being capable of the millimetre-sized oil droplet of stable suspersion.Present invention also offers a kind of water-based structure of the microgel comprising the low viscosity is molten Mosquito repellent/anti-pruritic compositions of liquid.The product such as mosquito repellent/anti-pruritic compositions of the present invention and conventional mosquito repellent/antipruritus toilet water is maximum Difference be alcohol-free, therefore milder, the oil-phase component containing anophelifuge activity composition Icaridin or stop containing anti-inflammatory The oil-phase component of itching activity composition bisabolol can stable suspersion in the water-based structure-solution of microgel of low viscosity.
On the one hand, the invention provides a kind of alcohol-free mosquito repellent/anti-pruritic compositions, it is included:
(a) the water-based structure-solution of the microgel of low viscosity, the viscosity of the water-based structure-solution is less than 200mPas, close Spend for 1 ± 0.01g/cm3, the water-based structure-solution includes:
(i) high molecular polysaccharide polymer,
(ii) inorganic cation,
(b) oil phase, the oil phase include mosquito repellent and/or antipruritic active ingredients, and the density of the oil phase is 1 ± 0.01g/ cm3
In a preferred embodiment, the high molecular polysaccharide polymer is the combination of gellan gum and xanthans.
In a preferred embodiment, it is with the gross weight meter of the composition, the total amount of the gellan gum and xanthans 0.1-0.5 weight %.
In a preferred embodiment, the inorganic cation is selected from:K+, Ca2+Or Mg2+
In a preferred embodiment, with the gross weight meter of the composition, the dosage of the inorganic cation is 0.02- 0.2 weight %.
In a preferred embodiment, the oil phase includes anophelifuge activity composition Icaridin and density is less than 1g/cm3's Grease.In a preferred embodiment, the density is less than 1g/cm3Grease be selected from:The different monooctyl ester of palmitate, palmitate Isopropyl ester, dioctyl carbonate, cetostearyl alcohol ethylhexoate and combinations thereof.
In a preferred embodiment, the oil phase includes antipruritic active ingredients bisabolol and density is more than 1g/cm3 Grease.In a preferred embodiment, the density is more than 1g/cm3Grease be selected from:Trimethyl pentaphenyltrisiloxane, The poly- trimethicone of diphenyl silicon phenyl, trimethyl silicane alcoxyl phenyl dimethicones and combinations thereof.
On the other hand, present invention also offers the preparation method of mosquito repellent/anti-pruritic compositions, methods described to include following step Suddenly:
A. the water-based structure-solution of microgel of the present invention is prepared;
B. oil phase is prepared;
C. the oil phase prepared by step B is added in the water-based structure-solution of microgel prepared by step A so that oil suspensions exist In the water-based structure-solution of microgel.
Detailed description of the invention
Inventor attempts to seek a kind of water-based structure-solution of the microgel for being adapted for carrying out low viscosity, verifies high molecular polysaccharide Polymer gellan gum, by Coordination interaction, forms tridimensional network, it is achieved thereby that utilizing the work with inorganic cation With the water-based structure-solution of the microgel for realizing low viscosity, there is splendid suspension stability, can be stable under conditions of low viscosity Suspension grade elite oil droplet, the elite oil droplet can be made up of effective active composition Icaridin or bisabolol.
Present invention firstly discovers that a kind of can be molten with the water-based structure of microgel of the low viscosity of stable suspersion grade oil droplet Liquid.The water-based structure-solution of microgel of the low viscosity includes the high molecular polysaccharide polymer being made up of gellan gum and xanthans, Viscosity is less than 200mPas, and density is 1 ± 0.01g/cm3
The gellan gum and xanthans that this water-based structure-solution of new microgel uses are caused by microbial fermentation Polysaccharide, wherein, xanthans can be that system brings viscosity, increase the rheological characteristic of system.But the ratio of xanthans need to control Below 0.2 weight %, so as to reach the present invention need low viscosity the characteristics of.
The present invention using can stable suspersion grade oil droplet low viscosity the water-based structure-solution of microgel, by adjusting water The density of phase and oil phase, oil-soluble ingredients Icaridin or bisabolol and combinations thereof stable suspersion in aqueous phase microgel system In, existing visual outward appearance, the shortcomings that avoiding using alcohol, there are good mosquito repellent and itching-relieving efficacies again.
The present invention also aims to provide a kind of alcohol-free water aqua type mosquito-repellent water or antipruritic water of low viscosity, the mosquito repellent Water or antipruritic water and the difference of the mosquito-expelling and antipruritic floral water maximum of routine are alcohol-free, milder, will contain mosquito repellent and live Property the oil-phase component of composition Icaridin or the oil-phase component stable suspersion containing inflammation-resisting itch-stopping active component bisabolol in low viscous In the water-based structure-solution of microgel of degree.
The present invention specifically provides a kind of alcohol-free mosquito repellent/anti-pruritic compositions, and it includes the micro- solidifying of described low viscosity Glue structure-solution and oil phase.The water-based structure-solution includes high molecular polysaccharide polymer and inorganic cation.Institute State oil phase and include mosquito repellent and/or antipruritic active ingredients.It is water-based for alcohol-free mosquito repellent/anti-pruritic compositions of the present invention The density of structure-solution and oil phase is 1 ± 0.01g/cm3
The present invention provides a kind of low viscosity alcohol-free novel form mosquito-repellent water or antipruritic water, the mosquito-expelling and antipruritic liquid distilled from honeysuckle flowers or lotus leaves with routine Water is different, and spirituosity, the effective mosquito component used are not efficient micro- malicious culicifuge Icaridin to the mosquito-expelling and antipruritic water, Icaridin Chemical name is 1- piperidine carboxylic acids -2- (2- ethoxys) -1- methyl-prop base esters, and the antipruritic composition of effective antiinflammatory used is opopanax Alcohol.
In some specific embodiments of the invention, the molecular weight ranges of the high molecular polysaccharide polymer used is 2 ×105-50×106Dalton.
In some preferred embodiments, the high molecular polysaccharide polymer of use is the group of gellan gum and xanthans Close.In other words, the present invention is surprised to find that gellan gum and xanthans being applied in combination that can be formed can be with stable suspersion grade The water-based structure-solution of microgel of oil droplet.
Applicant also attempts to replace Huang using high molecular PEG-240/HDI copolymers pair-ether of decyl tetradecyl alcohol polyethers -20 Virgin rubber is arranged in pairs or groups with gellan gum, it would be desirable to forms the water-based structure-solution of microgel of more stable low viscosity.But PEG-240/ HDI copolymers are double-and the addition of the ether of decyl tetradecyl alcohol polyethers -20 causes the suspension of gellan gum to die down, occurs on oil droplet during high temperature Floating phenomenon.
The aqueous phase microgel suspension system of the present invention has the low viscosity less than 200mPas, can Effective Suspension grade The long-time stability of Icaridin mixing oil phase and bisabolol mixing oil phase, the mosquito-repellent water and antipruritic water are good;It is easy to use, can Effectively it is sprayed at skin surface.
Aqueous phase microgel suspension system in the present invention is mutual using high molecular polysaccharide polymer and ionomer coordination Effect is formed, and macromolecule polysaccharide includes gellan gum and xanthans, and ion includes sodium ion or calcium ion.Gellan gum solution is a kind of Typical pseudoplastic fluid, its solution viscosity are substantially reduced with the increase of shear rate, recovered with the decrease of shear rate. After gellan gum is dissolved in water, it can assemble to form the double helix model automatically between molecule, two strands form double with right-handed spiral The parallel spiral of stock, it is mainly intermolecular hydrogen bonding to stablize double-stranded active force, and further aggregation can form three to double helix Tie up network structure.
The oil-phase component of the present invention uses efficient micro- malicious culicifuge Icaridin (1.036g/cm3) with other density be less than 1g/ cm3Grease mixing composition, by the different monooctyl ester of palmitate, palmitate isopropyl ester, dioctyl carbonate and cetostearyl alcohol second The one or more greases such as base capronate mixing composition, can dissolve each other and appearance transparent.
Another oil-phase component of the present invention is more than 1g/ using inflammation-resisting itch-stopping functional component bisabolol with other density cm3Grease mixing composition, by trimethyl pentaphenyltrisiloxane, the poly- trimethicone of diphenyl silicon phenyl, Or the one or more greases such as trimethyl silicane alcoxyl phenyl dimethicones mixing composition, it can dissolve each other and appearance transparent.
In the cosmetic composition of the present invention, relative to the gross weight of composition, include 0.1 weight %-0.5 weight %'s Macromolecule polysaccharide gellan gum and xanthans, when its content is less than 0.1 weight %, suspension stability is weaker;Its content is more than 0.5 weight When measuring %, gel is formed, the low viscosity characteristics of the present invention can not be met.
0.02 weight %-0.2 weight % cation Na is included in the composition of the present invention+, K+, Ca2+Or Mg2+, wherein Bivalent ions neutralization efficiency is higher.In some preferred embodiments, control high molecular polysaccharide polymer and inorganic sun The ratio of ion is 5:2.In some especially preferred embodiments, it is 5 to control the ratio of gellan gum and inorganic cation:2.
The content of effectively mosquito component Icaridin is 5 weight %-20 weight % in the composition of the present invention, and effective antiinflammatory stops The content of composition bisabolol of itching is 0.2 weight %-1.0 weight %, and the content of oil-phase component includes 1.0 weight %-25.
Embodiment
Unless otherwise defined, all technologies used herein and scientific terminology have art ordinary skill people of the present invention The identical meanings that member is commonly understood by.Although it can be used for implementing or testing with similar or equivalent any method described herein and material The present invention, but described herein is preferable method and material.
The present invention is expanded on further with reference to specific embodiment.It should be appreciated, however, that these embodiments are only used for It is bright the present invention and be not meant to limit the scope of the invention.The test method of unreceipted actual conditions in the following example, generally According to normal condition, or according to the condition proposed by manufacturer.Unless otherwise indicated, all percentage and number be by weight Meter.
The gellan gum and xanthans used in embodiment is polysaccharide caused by microbial fermentation, and gellan gum of the present invention is derived from CP Kelco companies of the U.S., trade nameCG-LA;Xanthans is derived from DANISCO companies of Denmark;The knot used Cold glue is low-acyl gellan gum.
Embodiment 1-8:The preparation of the water-based structure-solution of microgel of low viscosity
Embodiment 1-8 investigates inorganic cation in the water-based structure-solution system of microgel of low viscosity in gellan gum With the selection of degree.
Table 1
Each composition is weighed by raw material addition shown in table 1, is mixed, dissolves and is dispersed with stirring completely under the conditions of 80 DEG C Afterwards, stirring is cooled to room temperature, and the water-based structure-solution of microgel that low viscosity is made is standby.Fly (Brookfield) public affairs using rich strangle The viscosimeter (Brookfield RVDV-C) of department carries out viscosity test, and embodiment 1-8 viscosity is respectively less than 200mPas, profit The density that aqueous phase system is measured with densitometer is 1.0000 ± 0.01g/cm3, can form the water-based structure of microgel of low viscosity Solution.
Embodiment 9-12:The preparation of the water-based structure-solution of microgel of low viscosity
Influence of the addition of embodiment 9-12 investigation gellan gums to the water-based structure-solution of microgel of low viscosity.
Table 2
Each composition is weighed by raw material addition shown in table 2, is mixed, dissolves and is dispersed with stirring completely under the conditions of 80 DEG C Afterwards, stirring is cooled to room temperature, and the water-based structure-solution of microgel that low viscosity is made is standby.Fly (Brookfield) public affairs using rich strangle The viscosimeter (Brookfield RVDV-C) of department carries out viscosity test, and embodiment 9-12 viscosity is respectively less than 200mPas, profit The density that aqueous phase system is measured with densitometer is 1.0000 ± 0.01g/cm3, can form the water-based structure of microgel of low viscosity Solution.
Embodiment 13-16:Mix the preparation of oil phase
Embodiment 13-16 is prepared for the various mixing oil phases of the present invention.
Table 3
By raw material addition shown in table 3, embodiment 13-16 is different by Icaridin and isopropyl palmitate, palmitic acid respectively Four kinds of monooctyl ester, dioctyl carbonate and cetostearyl alcohol ethylhexoate ester oils are mixed in above ratio, are dispersed with stirring Even, it is good to be made intersolubility, transparent mixing oil phase, and density is adjusted in 1.0000 ± 0.01g/cm3.Comparative example 1-2 is respectively by hydroxyl Piperazine ester mixes in proportion with octyl group polymethyl siloxane, ring five dimethyl silicone polymer, is dispersed with stirring uniformly, low temperature becomes after standing It is mixed, it is impossible to transparent mixing oil phase is made.
Embodiment 17-20:Mix the preparation of oil phase
Embodiment 17-20 is prepared for the various mixing oil phases of the present invention.
Table 4
By raw material addition shown in table 3, respectively by bisabolol and trimethyl pentaphenyltrisiloxane, diphenylmethyl silicon The poly- trimethicone of alkoxyl phenyl and trimethyl silicane alcoxyl phenyl dimethicones mix in proportion, are dispersed with stirring It is even, transparent mixing oil phase can be made, adjustment density is in 1.0000 ± 0.01g/cm3
Embodiment 21-24:The system of the mosquito repellent composition of the water-based structure-solution of microgel comprising low viscosity of the present invention It is standby
The mosquito repellent that the water-based structure-solution of microgel comprising low viscosity of the present invention is prepared according to formula table 5 Suo Shi combines Thing.
Table 5
Gellan gum, xanthans, calcium chloride, PEG-240/HDI copolymers pair-decyl ten are weighed by addition shown in table 5 The ether of tetrol polyethers -20, methyl hydroxybenzoate and deionized water, dissolve and be dispersed with stirring completely under the conditions of 80 DEG C, stirring is cooled to room Temperature, adds Phenoxyethanol, and the water-based structure-solution of microgel for preparing low viscosity is standby.
It is respectively that Icaridin and isopropyl palmitate, isobutyl palmitate, dioctyl carbonate and spermaceti is hard at room temperature Lipidol ethylhexoate mixes in proportion, is dispersed with stirring uniformly, transparent mixing oil phase is made.
Transparent miscella is added in the water-based structure-solution of microgel of low viscosity again so that transparent mixing oil phase 0.5-2 millimeter oil droplets are dispersed into the water-based structure-solution of microgel of low viscosity, are made comprising low viscosity of the present invention The mosquito repellent composition of the water-based structure-solution of microgel.
Embodiment 25-28:The system of the anti-pruritic compositions of the water-based structure-solution of microgel comprising low viscosity of the present invention It is standby
The antipruritic combination of the water-based structure-solution of microgel comprising low viscosity of the present invention is prepared according to formula table 6 Suo Shi Thing.
Table 6
Gellan gum, xanthans, calcium chloride, PEG-240/HDI copolymers pair-decyl ten are weighed by addition shown in table 6 The ether of tetrol polyethers -20, methyl hydroxybenzoate and deionized water, dissolve and be dispersed with stirring completely under the conditions of 80 DEG C, stirring is cooled to room Temperature, adds Phenoxyethanol, and the water-based structure-solution of microgel for preparing low viscosity is standby.
At room temperature respectively by bisabolol, trimethyl pentaphenyltrisiloxane, diphenyl silicon phenyl poly- three Methylsiloxane, pigment and colouring agent mix in proportion, are dispersed with stirring uniformly, transparent mixing oil phase is made.
Transparent miscella is added in the water-based structure-solution of microgel of low viscosity again so that transparent mixing oil phase exists 0.5-2 millimeter oil droplets are dispersed into the water-based structure-solution of microgel of low viscosity, are made micro- comprising low viscosity of the present invention The anti-pruritic compositions of the water-based structure-solution of gel.
Test case 1:Study on the stability
Embodiment 21-24 includes mosquito repellent composition and the implementation of the water-based structure-solution of microgel of low viscosity of the present invention Example 25-28 includes the study on the stability of the anti-pruritic compositions of the water-based structure-solution of microgel of low viscosity of the present invention
Table 7
4℃ 25℃ 40℃ 48℃ -15℃ Circulation Illumination
Time 3 months 3 months 3 months 3 months 3 months 1 month 3 months
Embodiment 21 It is good It is good It is good It is good It is good It is good It is good
Embodiment 22 It is good It is good It is good It is good It is good It is good It is good
Embodiment 23 It is good It is good It is good It is good It is good It is good It is good
Embodiment 24 It is good It is good It is good It is good It is good It is good It is good
Comparative example 3 It is good It is good Layering Layering It is good Layering Layering
Embodiment 25 It is good It is good It is good It is good It is good It is good It is good
Embodiment 26 It is good It is good It is good It is good It is good It is good It is good
Embodiment 27 It is good It is good It is good It is good It is good It is good It is good
Embodiment 28 It is good It is good It is good It is good It is good It is good It is good
Comparative example 4 It is good It is good Layering Layering It is good Layering Layering
As can be seen from Table 7, embodiment 21-28 is in high temperature (40 DEG C and 48 DEG C), low temperature (4 DEG C and -15 DEG C), room temperature (25 DEG C), the stability under illumination and cycling condition is good, does not occur oil droplet floating or sinkage in system;Wherein, Under the conditions of centrefuge experiment (rotating speed 1000,30 minutes time), do not occur oil droplet floating or sinkage yet, have good stability. Experiment proves that the water-based structure-solution of the low viscosity of the present invention has good suspension stability, is controlling water phase and an oil phase density Under conditions of, can suspend grade oil droplet well, obtain the stable water-based knot of microgel comprising low viscosity of the present invention Mosquito repellent/anti-pruritic compositions of structure solution
Lamination occurs in high temperature circulation and illumination in comparative example 3 and 4.
Test case 2:The mosquito repellent test of pesticide effectiveness
Method of testing:GB/T13917.9-2009
Test sample:Embodiment 21-24 mosquito repellent compositions
Subjects:Sensitive aedes albopictus (Aedes albopictus), the female insect that emergence is not sucked blood for 3-5 days;Come Source:The sensitive strain of Shanghai plant physiological ecology research institute of Chinese Academy of Sciences laboratory Long-term breeding.
Temperature:26 ± 1 DEG C, relative humidity 65 ± 10%
Mosquito cage:The high 300mm of the long wide 300mmX of 400mmX
Attack is tested:300 test worms, tester's the back of the hand exposure 40mmX 40mm skins, its remaining part are put into mosquito cage Divide tight masking.Hand is stretched into mosquito cage and stopped 2 minutes, close observation, it is found that mosquito stops falling, before its mouthpart will be pierced into skin Shake arm is expelled, and is designated as 1 test worm and is stopped falling.Tester and the test worm that the test worm for coming to stop falling is more than 30 are attack Power is qualified, and this person and this cage mosquito can carry out repellent experiment.
Repellent is tested:Selecting the qualified tester of 5-7 name attacks, (men and women half and half, and before testing and during experiment not Drink, tea or coffee, the product of the class containing essence should not be used), 50mmX 50mm skin area is respectively drawn in its both hands the back of the hand, A wherein hand smears culicifuge to be measured by 1.5 μ L/cm2 dose uniformity, exposes 40mmX 40mm skins therein, tightly Remainder is covered, another hand is blank control.Smear culicifuge 2 hours, hand is stretched into the qualified mosquito cage of attack 2 points Clock, observation, which whether there is mosquito, is come to stop to fall to suck blood.Afterwards at interval of test in 1 hour once, as long as there is a mosquito to come to suck blood i.e. Sentence and make repellant failure.Record the effective protecting time (hour) of repellant.Control hand first does check experiment every time, and attack closes The test worm of lattice can continue to test, and test worm attack is unqualified, need to change qualified test worm and tested.
Result of the test
Test sample Effective repellent time (hour)
The mosquito repellent composition of embodiment 21 6.33
The mosquito repellent composition of embodiment 22 6.14
The mosquito repellent composition of embodiment 23 6.28
The mosquito repellent composition of embodiment 24 6.17
Effective repellent time of embodiment 21-24 mosquito repellent compositions is all higher than 6 hours, with reference to GB/T13917.9-2009 《Agriculture chemical registration hygienic insecticide indoor pharmacodynamic test method》The evaluation criterion of middle pharmacodynamics index, effective repellent time >=6 are small When be A levels, it is possible to determine that the preparation-obtained mosquito repellent compositions of 21-24 of the embodiment of the present invention have reached A level product, can reach Effective repelling effect.Test case 3:Antipruritic experiment
Test material:
Animal:Cavy 110 (every group 10) body weight:300g or so is female/the limited public affairs of the male dry biotechnology of half and half Shanghai first Department
Histamine phosphate:National Institute for Food and Drugs Control
Positive control:Dexamethasone (30g:22.5mg) three nine-day periods after the winter solstice pharmaceutical sector
Sample:Embodiment 25-28 anti-pruritic compositions
Experimental condition:Laboratory temperature:20-25 DEG C of relative humidity:60-70%
Test method:
Cavy is randomly divided into 8 groups, every group 10.Divide blank control group, positive controls, three groups of sample.Before experiment One day, to instep behind each group cavy right side, apply sample once.Experimental day, at instep shaving behind the coarse sandpaper scratch animal right side, about 1 square centimeter of scope or so, then smear sample once in this place, blank control group gives equivalent distilled water.After waiing upon 10 minutes, open Begin in the histamine phosphate 0.05ml/ of wound face Chu Di 0.01% only, hereafter to press 0.01%, 0.02%, 0.03% every 3 minutes, 0.04%...... progressive concentration, it is 0.05ml/ every time.Until cavy occur later licks right metapedes, finally to there is globefish It is itch-threshold that mouse, which turns one's head to lick the histamine phosphate total amount given during right metapedes,.Record and compare the itch-threshold of each group.
Result of the test:
Embodiment 25-28 anti-pruritic compositions cause the influence of reaction of itching to histamine phosphate
*:P values are test group compared with blank control group
Compared with blank control, embodiment 25-28 anti-pruritic compositions be improved cavy itch-threshold effect (P<0.01), have Obvious antipruritic effect.
Although having been given and describing typical embodiment, those skilled in the art will be understood that, not depart from , can be to the various changes in its form and details in the case of the scope of the invention defined by the claims.

Claims (10)

1. a kind of alcohol-free mosquito repellent/anti-pruritic compositions, it is included:
(a) the water-based structure-solution of the microgel of low viscosity, the viscosity of the water-based structure-solution are less than 200mPas, density 1 ±0.01g/cm3, the water-based structure-solution includes:
(i) high molecular polysaccharide polymer,
(ii) inorganic cation,
(b) oil phase, the oil phase include mosquito repellent and/or antipruritic active ingredients, and the density of the oil phase is 1 ± 0.01g/cm3
2. composition as claimed in claim 1, it is characterised in that the high molecular polysaccharide polymer is gellan gum and xanthan The combination of glue.
3. composition as claimed in claim 2, it is characterised in that with the gross weight meter of the composition, the gellan gum with The total amount of xanthans is 0.1-0.5 weight %.
4. composition as claimed in claim 1, it is characterised in that the inorganic cation is selected from:K+, Ca2+Or Mg2+
5. composition as claimed in claim 1, it is characterised in that with the gross weight meter of the composition, it is described it is inorganic sun from The dosage of son is 0.02-0.2 weight %.
6. composition as claimed in claim 1, it is characterised in that the oil phase includes anophelifuge activity composition Icaridin and close Degree is less than 1g/cm3Grease.
7. composition as claimed in claim 6, it is characterised in that the density is less than 1g/cm3Grease be selected from:Palmitate Different monooctyl ester, palmitate isopropyl ester, dioctyl carbonate, cetostearyl alcohol ethylhexoate and combinations thereof.
8. composition as claimed in claim 1, it is characterised in that the oil phase include antipruritic active ingredients bisabolol and Density is more than 1g/cm3Grease.
9. composition as claimed in claim 8, it is characterised in that the density is more than 1g/cm3Grease be selected from:Trimethyl five Phenyl trisiloxanes, the poly- trimethicone of diphenyl silicon phenyl, trimethyl silicane alcoxyl phenyl polydimethylsiloxanes Alkane and combinations thereof.
10. the preparation method of mosquito repellent/anti-pruritic compositions as claimed in claim 1, the described method comprises the following steps:
A. the water-based structure-solution of the microgel is prepared;
B. oil phase is prepared;
C. the oil phase prepared by step B is added in the water-based structure-solution of microgel prepared by step A so that oil suspensions are micro- solidifying In glue structure-solution.
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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111758723A (en) * 2020-07-20 2020-10-13 成都彩虹电器(集团)股份有限公司 Synergist for electric heating mosquito-repellent incense tablet and electric heating mosquito-repellent incense tablet
CN116211731A (en) * 2023-03-15 2023-06-06 广州市圣莎拉化妆品有限公司 Wheat protein repairing and hair care composition and hair conditioner

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CN104027255A (en) * 2014-06-20 2014-09-10 广州立白企业集团有限公司 Water-based insect expelling aerosol composition
CN105456052A (en) * 2015-12-25 2016-04-06 肇庆迪彩日化科技有限公司 Skin care composition

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Publication number Priority date Publication date Assignee Title
CN104027255A (en) * 2014-06-20 2014-09-10 广州立白企业集团有限公司 Water-based insect expelling aerosol composition
CN105456052A (en) * 2015-12-25 2016-04-06 肇庆迪彩日化科技有限公司 Skin care composition

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111758723A (en) * 2020-07-20 2020-10-13 成都彩虹电器(集团)股份有限公司 Synergist for electric heating mosquito-repellent incense tablet and electric heating mosquito-repellent incense tablet
CN116211731A (en) * 2023-03-15 2023-06-06 广州市圣莎拉化妆品有限公司 Wheat protein repairing and hair care composition and hair conditioner

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