CN1183899C - Skin protection spot-removing cream and preparation method thereof - Google Patents

Abstract

The present invention relates to skin protecting and speckle removing cream having high efficiency, and no toxic or side effects or stimulation, which is prepared from vitamin C, vitamin E, hydroquinone, titanium dioxide, ethyl dimethylamino laurate, magnesium aluminum silicate, a polyethylene glycol 400 solvent, etc. In a prescription of the skin protecting and speckle removing cream, an efficient skin penetration reinforcing agent, namely the ethyl dimethylamino laurate, is used, and therefore, biologically active materials, such as the vitamin C, the vitamin E, the hydroquinone, the titanium dioxide, etc., can rapidly penetrate sites of action. The skin protecting and speckle removing cream has the advantages of convenient preparation, favorable effects of skin penetration, rapid therapeutic effects, safe use, etc.

Description

A kind of skin protection freckle-removing cream preparation and preparation method thereof

Content of the present invention belongs to the preparing technical field of heavy chemicals, relates to a kind of technology of preparing of skin-protecting face nursing cosmetics, particularly a kind of technology of preparing that makes the bioactive substance rapid osmotic to the skin protection freckle-removing cream preparation of site of action.

The color of human skin and distribution situation thereof are mainly determined by the melanin that the melanocyte that is distributed in skin corium produces.Eumelanin and class are melanic of a great variety, but it mostly contains hydroxyl and the high sulfydryl of sulfur content.Modern medicine study thinks that the main cause of unusual melanin deposition is because the reactive oxygen free radical over-deposit in the skin causes, powerful antioxidant can be removed interior free yl effectively, the antagonism sulfydryl forms and eliminate melanin deposition, thereby plays the effect of brightening speckle removing and maintenance skin.In recent years, along with this ambit to the understanding in depth of skin texture, function and metabolic Biochemical processes, skin whitening goes the development of speckle preparation to trend towards beauty treatment and nursing is laid equal stress on, and has given prominence to safety and effectiveness more.But because human body skin and mucosal tissue have powerful barrier action, traditional skin protection goes the effect of speckle preparation transdermal penetration very limited, and medicine is difficult to infiltrate into region of interest, reaches activity, thereby has greatly influenced clinical efficacy.For this reason, about the scientific research personnel has developed and release complementary therapy and the preparation that some strengthen the percutaneous penetration of drugs effects again in succession, be wherein a kind of mode preferably as in prescription, adding skin penetration enhancer.But present skin penetration enhancer well known in the art, as dimethyl sulfoxide (Dimethyl Sulfoxide, DMSO), laurocapram (Laurocapram, Azone) etc., the actual clinical effect is all not ideal enough, they make the permeability changes of epithelial cell membrane by softening skin keratoprotein and the proteic mode of solidified structure, in the hope of strengthening the osmosis of medicine, skin, mucosal tissue are had stimulation and destruction inevitably, thereby also reduced the safety and the effectiveness of its use.

The objective of the invention is to overcome the aforementioned existing in prior technology weak point in this area, a kind of side of system science is provided and has skin protection freckle-removing cream preparation of good transdermal effect and security performance and preparation method thereof.

The material composition that constitutes skin protection freckle-removing cream preparation of the present invention comprises vitamin C, part vitamin E, hydroquinone, sodium sulfite, pharmaceutical grade titanium dioxide, N, N dimethylamine guanidine-acetic acid Laurel alcohol ester, Magnesiumaluminumsilicate (SM gel), deionized water, antiseptic and PEG400 solvent (PEG400) etc., its material composition prescription is: contain 1～3 part of vitamin C in the finished product preparation of per 100 parts of unit of weights, 0.2～1 part of vitamin E, 1～3 part of hydroquinone, 1～3 part of sodium sulfite, 2～5 parts of pharmaceutical grade titanium dioxide, 5～10 parts of N, N dimethylamine guanidine-acetic acid Laurel alcohol ester, 8～10 parts of Magnesiumaluminumsilicates, 9～11 parts of deionized waters, be not higher than 0.2 part antiseptic, all the other are the PEG400 solvent.

The actual product of this skin protection freckle-removing cream preparation obtains according to following preparation process: taking polyethylene glycol 400 solvents, and heating in water bath to 100 ℃ adds hydroquinone, vitamin C, vitamin E and titanium dioxide successively under stirring; Sodium sulfite is dissolved in the deionized water, then aqueous solution is added in the PEG400 solvent, stir; Add Magnesiumaluminumsilicate in the solution that stirs, the powerful stirring 1～1.5 hour melts gel fully; Solution is cooled under 25 ℃, adds N, N dimethylamine guanidine-acetic acid Laurel alcohol ester and antiseptic, powerful at a high speed the stirring after 30～45 minutes promptly obtains product.

In above-mentioned material formula, vitamin C (having another name called ascorbic acid) is a kind of biology cofactor and antioxidant altogether, it plays an important role in biological oxidation and Cellular respiration, matter is synthetic between participation amino acid metabolism, collagen protein and histiocyte, is used for the injury of protectiving ultraviolet radiation to skin.In the present invention's prescription, except that using vitamin C, also can use its derivant, comprise ascorbyl stearate, ascorbic palmitate, two ascorbic palmitate, magnesium ascorbyl phosphate ester etc., wherein ascorbic palmitate and magnesium ascorbyl phosphate ester are that the percutaneous assimilation effect is good, the choice drug of stable performance.Vitamin E has another name called tocopherol, and it not only has the function of free radical scavenger, also can capture the oxygen atom of excited state, prevents that cell membrane from damaging because of oxidation.Vitamin E can be stablized human body endoperoxides dismutase, prevents the damage that ultraviolet radiation causes skin, and simultaneously, it also can directly act on the skin corium blood vessel wall, improves skin microcirculation to lasting stability, prevents and delaying decrepitude of skin.Vitamin E and vitamin C compatibility use, and can bring into play clinical effectiveness better, prevent pachylosis, chap and unusual melanin pigmentation treatment senile plaque, freckle, macula lutea, hair follicle keratinization, chloasma hepaticum and melanosis etc.Hydroquinone is safety skin whitener commonly used, and it can organize melanic formation effectively, is equipped with in preparation and the fractional sulfurous hydracid of its equal in quality sodium, can be used for preventing that hydroquinone oxidation from decomposing.Titanium dioxide is the skin whitener safely and effectively that the present U.S., Japan and EU member country are all approved, its effect is to be used for skin whitening by its covering, and the titanium dioxide of sodium meter level can also the protectiving ultraviolet radiation; In addition.Titanium dioxide also is a kind of reliable catalyst, and compatibility uses and can make vitamin C, vitamin E and hydroquinone bring into play biological activity better.

Generally, above-mentioned four kinds of biological activities in the prescription are difficult to be dissolved in the same solution system, because vitamin E is an oil soluble material, be difficult to be used with water-soluble vitamin c and hydroquinone, titanium dioxide was both water insoluble, also be insoluble to most of known cosmetics solvents, for this reason, select the thickening stabilizing agent of suitable solvent and solution just to become a key technology of prescription success or not of the present invention.The present invention fills a prescription and adopts PEG400 is solvent, makes the thickening and the stabilizing agent of solution with Magnesiumaluminumsilicate.Polyethylene Glycol is that PEG400 is by oxirane and water or ethylene glycol progressively addition and a kind of water solublity straight chain polymer of making, and according to varying in size of relative molecular mass, its physical aspect can be from the mucus of white until hard waxy solid.The molecular weight of PEG400 is 380～420, is colourless heavy-gravity liquid at normal temperatures, and it can fully dissolve vitamin C, vitamin E and hydroquinone, can dissolve titanium dioxide fully under 100 ℃ high temperature.Therefore in addition, PEG400 is the nonionic atent solvent, and is under general condition highly stable, can not react with transdermal agent isoreactivity material and has influence on clinical effectiveness.The U.S., Japan and the European Community are listed Polyethylene Glycol in the food additive in, and its prescription has mildness, use back skin wet, softness, the joyful aftersensation of using is arranged.The SM gel is by the refining natural inorganic stick that forms of the Ore that contains Magnesiumaluminumsilicate, be odorless, slightly astringent taste, do not fire, the white powder of the soft cunning of quality, its safety non-toxic, the solution dispersion does not have sticking tower and greasy feeling, in PEG400 after long-time high-speed stirred high degree of dispersion, be overlapped to form network structure, make multiple free solution system change constraint solution in the network structure into, form the thixotropy gel of non-newtonian fluid type, have the thixotropy of suspension and unlimited reversibleization of gel under external force; The chemical stability of this gelatinous mass is good, compatibility is good, and not oxidation, azymic have thickening property, diffusibility, suspension and water holding performance of keeping humidity preferably, and have certain heat resistance and heat stability.

In material formula of the present invention, as the N of skin penetration enhancer, N dimethylamine guanidine-acetic acid Laurel alcohol ester is that a kind of molecular structural formula by long chain alkanol and aminoacid be combined into is CH ₃(CH ₂) ₁₀CH ₂OOCCH ₂N (CH ₃) ₂The two methylamino acetate preparations of long chain alkanol.N, N dimethylamine guanidine-acetic acid Laurel alcohol ester can dissolve the lipomicron in skin and mucosal tissue epithelial cell gap under 0.5%～40% concentration, make medicine pass through the iuntercellular effusion to linked groups, because it is not to keratodermatitis and epithelial cell generation effect, therefore can injured skin and mucous epithelium.Long chain alkanol and aminoacid are decomposed in reinforcing agent can be organized emiocytosis immediately after entering tissue esterase (esterases) cutting, absorb thereby further be organized institute's metabolism.After removing this acting factor of dermal penetration enhancer, the lipomicron in epithelial cell gap can solidify again automatically, thereby can not produce stimulation and harm to skin and mucosal tissue, and after using, the patient allergic phenomena can not take place yet, have no side effect and untoward reaction.This dermal penetration enhancer is compared with the like product laurocapram, and the speed that bioactive substance can be higher than 5～6 times of laurocaprams arrives site of action by epithelium and mucosal barrier, thereby has greatly strengthened the curative effect of medicine.In addition, this skin penetration enhancer also can with the hydroxyl combination in eumelanin and the class melanin, produce the speckle removing effect thereby drive melanin to the deep skin infiltration.

The antiseptic that uses in the preparation by Buddhist nun's ripple tortoise beetle ester, Ni Bojin ethyl ester, Ni Bojin propyl ester and Ni Bojin butyl ester by 70: 10: 10: 10 mixed is formulated.

Compared with prior art, novelty of the present invention is to use N, N dimethylamine guanidine-acetic acid Laurel alcohol ester cooperates with biological activities such as vitamin C, vitamin E, hydroquinone and titanium dioxide, form novel skin protection and removed the speckle preparation, it can be higher than tradition and pass through epithelium barrier arrival site of action with the speed of 5～6 times of agent, its pharmaceutical formulation is safe and convenient to use, effect obvious, have no side effect, do not have skin irritation and allergic phenomena takes place, be easy to be accepted, thereby its product has boundless market prospect by the patient.

Application Example

1, preparation technology: get mass fraction and be 67.3% PEG400, heating in water bath to 100 ℃ dissolves in mass fraction and is 2% hydroquinone, 2% vitamin C, 0.5% vitamin E and 3% titanium dioxide successively under stirring; Get mass fraction and be 10% deionized water, dissolve in 2% sodium sulfite, then aqueous solution is added in the PEG400 solution, stir; Add mass fraction again and be 8% SM gel in solution, the powerful stirring 1～1.5 hour melts gel fully; Solution is cooled under 25 ℃ of temperature, and the adding mass fraction is 5% N, and N dimethylamine guanidine-acetic acid Laurel alcohol ester and mass fraction are 0.2% antiseptic, and powerful at a high speed the stirring after 0.5 hour promptly obtains product.

2, using method: the skin protection freckle-removing cream that takes a morsel is applied in the affected part, fully rubs, and makes the local skin heating, after 0.5 hour, smears once every day 3～4 times again.The careful usefulness of child.

3, observation of curative effect: the pilot scale stage is used skin protection freckle-removing cream of the present invention to 35 routine patients, can eliminate general skin splash within 48 hours, for example chloasma, sunburn, senile plaque, butterfly spot, cyasma etc.; After using 7 days, also very obvious for the colour killing effect of cicatrix after birthmark, freckle, the operation; After using 24 hours, skin begins to bleach, exquisiteness is soft and moist.

Claims (1)

1, a kind of skin protection freckle-removing cream preparation, it is characterized in that in the finished product preparation of per 100 parts of unit of weights, containing 1～3 part of vitamin C, 0.2～1 part of vitamin E, 1～3 part of hydroquinone, 1～3 part of sodium sulfite, 2～5 parts of pharmaceutical grade titanium dioxide, 5～10 parts of N, N dimethylamine guanidine-acetic acid Laurel alcohol ester, 8～10 parts of Magnesiumaluminumsilicates, 9～11 parts of deionized waters, be not higher than 0.2 part antiseptic, all the other are the PEG400 solvent.2, be exclusively used in the method for preparing the described skin protection freckle-removing cream of claim 1 preparation, it is characterized in that comprising following preparation process: taking polyethylene glycol 400 solvents, heating in water bath to 100 ℃ adds hydroquinone, vitamin C, vitamin E and titanium dioxide successively under stirring; Sodium sulfite is dissolved in the deionized water, then aqueous solution is added in the PEG400 solvent, stir; Add Magnesiumaluminumsilicate in the solution that stirs, the powerful stirring 1～1.5 hour melts gel fully; Solution is cooled under 25 ℃, adds N, N dimethylamine guanidine-acetic acid Laurel alcohol ester and antiseptic, powerful at a high speed the stirring 30～45 minutes.