CN107822912A

CN107822912A - Compound titanii dioxydi gel composition

Info

Publication number: CN107822912A
Application number: CN201710990319.7A
Authority: CN
Inventors: 宋宇豪; 陈有平
Original assignee: Individual
Current assignee: Individual
Priority date: 2017-10-23
Filing date: 2017-10-23
Publication date: 2018-03-23

Abstract

Compound titanii dioxydi gel composition, it is characterised in that the gel contains Muristeroid G as active component, titanium dioxide and at least one auxiliary material；The gel combination contains the Muristeroid G and 1%~2% of percentage by weight 0.2% 0.5% titanium dioxide, one or more of the auxiliary material in carbomer, NMF, solvent, preservative, surfactant, pH adjusting agent, and the water of surplus；The dosage of the carbomer is 0.5~1.5%, and the solvent load is the minimum that can dissolve Muristeroid G, and the NMF dosage is 4%~10%, and the dosage of surfactant is 0.5%~1%.

Description

Compound titanii dioxydi gel composition

Technical field：

The invention provides a kind of external-use gel composition.

Background technology：

Since industrialization, the ozone layer of the earth is destroyed, and causes earth's surface ultraviolet radiation more and more stronger, to open air The injury of the skin of movable personnel gradually increases, and common inorganic ultraviolet absorbent is mainly metal oxide, as zinc oxide, Titanium dioxide etc., although with certain preventing ultraviolet effect, the light aging caused by ultraviolet irradiates, and this can not be prevented The easy sensitization of body.How to protect the skin of outdoor activities person, prevent its by excessive UV irradiation produce it is various uncomfortable and Aging turns into urgent problem to be solved.

The content of the invention：

We have surprisingly found that under study for action, and abbreviation Muristeroid G steroidal compounds and titanium dioxide are common The outer used time, the effect for absorbing ultraviolet can be not only obviously improved, may also function as the effect of anti-light aging.

The invention provides Compound titanii dioxydi gel composition, it is characterised in that the gel contains as active component Muristeroid G, titanium dioxide and at least one auxiliary material；The gel combination contains percentage by weight 0.2%- 0.5% Muristeroid G and 1%~2% titanium dioxide, the auxiliary material are selected from carbomer, NMF, solvent, anti-corrosion One or more in agent, surfactant, pH adjusting agent, and the water of surplus；The dosage of the carbomer be 0.5~ 1.5%, the solvent load is the minimum that can dissolve Muristeroid G, and the NMF dosage is 4%~10%, The dosage of surfactant is 0.5%~1%.

The preferred Carbopol 941 of the carbomer or Acritamer 940.

The solvent is selected from one kind in ethanol, propane diols, DMF (DMF), dimethyl sulfoxide (DMSO) Or several, preferably DMSO.

Described NMF includes but are not limited to glycerine, polyethylene glycol, sorbierite, the degree of polymerization of the polyethylene glycol For 600-200, preferably 2%~3% polyethylene glycol 2000 and 0.5%~1% sorbierite.

The preferred Tween-80 of surfactant.

One or more of the described antibiotic antiseptic in methyl hydroxybenzoate, ethylparaben, propylben, it is excellent Select ethylparaben.

Described pH adjusting agent is selected from sodium hydroxide, preferably triethanolamine, triethanolamine.

Heretofore described percentage is the percentage by weight for accounting for gel combination.

Compound titanii dioxydi gel composition provided by the invention, Muristeroid G and titanium dioxide are formed into compound There is preferable assimilation effect for the ultraviolet (ultraviolet spectrogram of simulation sunlight) of different wave length afterwards.Also, pass through experiment It was also found that after Muristeroid G are added in external-use gel composition, can significantly improve in light aging animal skin The content of hydroxyproline and the light aging degree for reducing experimental animal skin, so as to realize unexpected anti-light aging Effect.Toxicity test is carried out to Muristeroid G and skin irritation test shows, as active component Muristeroid G chmice acute Oral toxicity experiment LD50 belongs to low toxicity material in 2500~4000mg, and without obvious Skin irritation and oral cumulative toxicity.Titanium dioxide or Muristeroid G is being used alone, is preventing the effect of light aging In the case of unconspicuous, external-use gel provided by the invention can significantly reduce light aging of the ultraviolet to the skin of experimental animal Effect,

Embodiment：

Muristeroid G preparation, according to the method disclosed in Chinese patent literature CN102250181, prepare Muristeroid G bulk drugs, content more than 98%.Muristeroid G structural formulas are：

Each obtained gel combination for antiultraviolet of embodiment is 1000g, and compound method is

Carbomer is mixed with 400ml distilled water and fully swelling obtains liquid (1), using by pH adjusting agent by liquid (1) pH Antibiotic antiseptic and Muristeroid G are dissolved in after solvent and are gradually added into liquid (1) and stir evenly to 6~7 by regulation；By titanium dioxide Add after the water of surplus to be gradually added into liquid (1) again and stir evenly with surfactant and NMF and produce gel combination.

Following (the unit of the prescription of embodiment 1~6：g)

The UV absorption contrast experiment of Pharmacological Examples 1

1. the selection of drugs compared, using cosmetics-stage nano TiO 2 (production of Shanghai Jiang Hu groups) medicine as a comparison.

2. the measure of light transmittance：Using meter successively UV A areas 400,380,360,340 and 320nm, UVB area 320, 300 and 280nm, UVC area 280,260,246,240,220 and 200nm, determine the light transmittance of each test liquid, parallel determination 3 times, Calculate average absorption ratio:A%=100%-T%.

According to national standard QB/T2410-1998 method, to sun-proof sample the 280nm, 290nm in UVB areas, 300nm, Absorbance at 320nm, 340nm, 360nm, 380nm, the 400nm in 310nm and UVA areas is measured, and tries to achieve UVB respectively Mean absorbance values under area and UVA areas wavelength.It is medical using quartz cell cuvette (1.2cm*4.5cm) and Minnesota Mining and Manufacturing Company's production Adhesive tape (3M Transpore 1527-3), using UV-5100H types it is ultraviolet/visible spectrophotometric is ultraviolet/visible spectrophotometer

Concrete operation step is as follows：

1 tape-stripping face is completely attached on the unilateral surface of cuvette printing opacity, and redundance is trimmed with scissors.

2 dual-beam ultraviolet-uisible spectrophotometers are opened, and preheat 10min, set wavelength.

3 are placed on the cuvette for posting adhesive tape in sample arm and reference light paths, school zero.

After 4 put on medical latex fingerstall, cosmetic sample is taken in the cuvette surface for posting adhesive tape, accurate weighing (8 ± 0.2) mg, sample application is uniform.Each sample horizontal survey 5 times.

Under 5 room temperature conditions, the cuvette of coated sample is placed into 30min, is put into ultraviolet instrumentation and detects its absorbance.

6 are placed in testing sample pond in sample arm, and another quartz cell for posting adhesive tape is placed in reference light paths, is surveyed respectively The ultraviolet light absorption angle value A of fixed nine wavelength, five wavelength of four, UVA areas wavelength measured value and UVB areas are asked respectively and counted Average valueWith

7 parallel samples of sequentially determining five, and five samplesWithArithmetic average is sought respectively, obtains sample The ultraviolet absorptivity A of product_UVAAnd A_UVB, A_UVAAnd A_UVBNot less than 0.5, then judge that the sample has protective action.

Gel combination and its matrix are detected according to the method described above made from Example 1~6 respectively, and will be by It is formulated according to embodiment 3, only adds titanium dioxide respectively and contrast 1 and contrast 2 is made in Muristeroid G

Result of the test is as follows

As a result show, on UVA and UVB wave bands, Muristeroid G and TiO₂Compound gel composition all significantly carry The high uv absorption property of product, especially shows more preferably in UVB areas, gel combination provided in an embodiment of the present invention Uv absorption property.

Pharmacological Examples 2

1 material

1.1 tissue hydroxyproline kits, Bioengineering Research Institute is built up purchased from Nanjing.

1.2 animal Kunming mouses, female mice, body weight 20-25g, 7-8 week old, by Shanghai Univ. of Traditional Chinese Medicine experimental animal The heart provides, every group 10, and the gel combination of the making of embodiment 1~6 is respectively adopted in experimental group.Control group uses Pharmacological Examples Contrast 1 and contrast 2 in 1, model group use, and packet is as follows with being administered：

2 methods

2.1 animal packets and model preparation are shaved mouse back skin only with electric hair clipper, about 2cm × 2cm, exposed skin Skin, random point 3 groups.Normal group, skin smears a matrix of embodiment 3 (0.5g) daily, without other any processing.Model group, Skin smears 1%8- Medadinines (8-MOP) 1 time again after smearing the matrix of embodiment 3 daily, gives 190w's after 1.5-2h UVA irradiates, cumulative exposure 138h (integrated intensity 95J/cm²), irradiation terminates to take skin in rear 24h；Other each experimental groups and right It is Experimental agents and control drug 0.5g to smear concentration daily according to 1,2 group of animal skin, and 1%8-MOP, 1.5- are smeared again after slightly dry After 2h, 190w UVA irradiations, cumulative exposure 138h (integrated intensity 95J/cm2) are given, irradiation terminates to take skin in rear 24h；Enter Row hydroxyproline content determines, while determines skin histology thickness (using model group thickness as 100), and skin histology is carried out old Change degree scores, and selects Bissett scorings i.e., remembers 0 point without thick wrinkle, occur less table it is shallow, it is thick cross back, wrinkle Line remembers 2 points, shallow compared with multilist, the thick wrinkle for crossing back occurs and remembers 4 points, the deep and long wrinkle for crossing back note 6 occurs Point.

2.2 tissue hydroxyproline content measure assay methods operate according to kit, while detect histone, calculate hydroxyl Proline/total protein ratio, t check analysis results,The mean skin tissue relative thick of each group is recorded simultaneously Degree and degree of aging score data see the table below.

In the prior art, the content of hydroxyproline is usually utilized to characterize the degree of aging of skin, such as prior art " Chinese medicine Influence of the anti aging effect agent to mouse skin hydroxyproline content " (Li Zhen etc., Shandong Traditional Chinese Medicine University's journal, in March, 1997 The 2nd phase of volume 21,142-143)

Test result indicates that model group is decreased obviously as positive control its hydroxyproline/total protein ratio.Control Group 1,2 is compared with model group, and hydroxyproline/total protein ratio does not significantly improve, and embodiment 1-6 is compared with control group 1,2, hydroxyl The raising of the content ratio of proline is obvious.Hydroxyproline/total protein ratio in the skin of experimental group 1-6 experimental animal Higher and closer normal group.Hydroxyproline/total protein ratio is higher and closer in the skin of experimental group 1-6 experimental animal Normal group, in the test of skin histology thickness and skin aging scoring, the skin histology thickness and degree of aging of experimental group 1~6 Significantly lower than 1,2 group of model group and control.

Claims

1. Compound titanii dioxydi gel composition, it is characterised in that the gel contains the Muristeroid as active component G, titanium dioxide and at least one auxiliary material；The gel combination contains percentage by weight 0.2%-0.5% Muristeroid G and 1%~2% titanium dioxide, the auxiliary material are selected from carbomer, NMF, solvent, preservative, surfactant, pH regulations One or more in agent, and the water of surplus；The dosage of the carbomer is 0.5~1.5%, and the solvent load is can Muristeroid G minimum is dissolved, the NMF dosage is 4%~10%, and the dosage of surfactant is 0.5% ~1%.

2. Compound titanii dioxydi gel composition as claimed in claim 1, it is characterised in that the preferred carbomer of carbomer 941 or Acritamer 940；The solvent is selected from ethanol, propane diols, DMF (DMF), dimethyl sulfoxide (DMSO) One or more, described NMF is selected from glycerine, polyethylene glycol, sorbierite, and the degree of polymerization of the polyethylene glycol is 600-200, the preferred Tween-80 of surfactant, described antibiotic antiseptic be selected from methyl hydroxybenzoate, ethylparaben, One or more in propylben, described pH adjusting agent are selected from sodium hydroxide, triethanolamine.

3. Compound titanii dioxydi gel composition as claimed in claim 2, it is characterised in that described pH adjusting agent is selected from excellent Select triethanolamine, the preferred DMSO of solvent, the polyethylene glycol 2000 and 0.5%~1% of the NMF preferably 2%~3% Sorbierite, the preferred ethylparaben of antibiotic antiseptic.