Summary of the invention
The object of this invention is to provide a kind of compositions with Penetration enhancing effect.
The present invention also aims to the preparation method and application that said composition is provided.
In order to realize object of the present invention, the invention provides a kind of compositions with Penetration enhancing effect, it is made up by weight of following material: Herba Blumeae Balsamiferae 1 ~ 20 part and Herba Pogostemonis 1 ~ 10 part; Preferably, described compositions is made up by weight of following material: Herba Blumeae Balsamiferae 10 parts and Herba Pogostemonis 5 parts.
The present invention, in conjunction with institute of traditional Chinese medicine's traditional theory and Modern Methods, with safety, efficient, action temperature and for principle, selects Hainan Region conventional medical herbs Herba Blumeae Balsamiferae among the people to be primary raw material, by with Herba Pogostemonis compatibility, preparation derives from the permeation enhancers of natural herbal.
Herba Blumeae Balsamiferae is in Compositae Herba Blumeae Balsamiferae platymiscium Herba Blumeae Balsamiferae [Blumea balsamifera (L.) DC] herb, it is the important ethnic drug of the ethnic groups such as multitude, Seedling, not only there is expelling wind and removing dampness, warming middle-JIAO to stop diarrhea, the function of promoting blood circulation and detoxication, also has and promotes the function such as wound healing, skin regeneration.Be often used as treatment skin injury among the people, there is the effect of " superficial do not stay scar ".Herba Blumeae Balsamiferae is also unique plant material of the Blumeae preparatum Tabellae that 2010 editions " pharmacopeia " specify, the Borneolum Syntheticum that is otherwise known as ends.Herba Blumeae Balsamiferae and extract thereof have antibacterial, antiinflammatory, antioxidative effect.Oleum Blumeae Balsamiferae has heat-clearing and toxic substances removing, reducing swelling and alleviating pain, blood vessel dilating, the orthosympathetic effect of suppression, and its bactericidal anti-inflammatory effect is especially remarkable, can be used for treatment burn and scald and injures mosquito bite, be widely used at medicine and daily use chemicals industry.Blumeae preparatum Tabellae has effect of refreshment of having one's ideas straightened out, clearing away heat to alleviate pain.
Herba Pogostemonis is the herb of Labiatae gynoecium grass platymiscium Herba Pogostemonis [Pogostemon cablin (Blanco) Benth], there is effect of removing dampness by means of aromatics, stomach function regulating preventing or arresting vomiting, dispelling summer-heat from superficies of the body, cure mainly that a retention of dampness in middle-JIAO gastral cavity abdomen painful abdominal mass is vexed, inappetence, vomiting, headache, tinea manus and pedis.Take Herba Pogostemonis as the quintessence oil made of raw material and extract, there is effect that is antibacterial, antiinflammatory, can skin care, to scytitis, allergy, burn, comedo, brothers' be full of cracks, bacteriological infection, eczema has good therapeutic effect, and has the effect promoting cell metabolism.
Preferably, compositions of the present invention can make facial milk cleanser, facial film, nutritive water, essence, facial cream, spray, ointment or tincture.
In order to realize object of the present invention, the present invention also provides a kind of preparation method with the compositions of Penetration enhancing effect, and the method comprises the following steps:
A) Herba Blumeae Balsamiferae of 1 ~ 20 weight portion and the Herba Pogostemonis of 1 ~ 10 weight portion are provided;
B) volatile oil and the water extract of Herba Blumeae Balsamiferae are provided;
C) volatile oil and the water extract of Herba Pogostemonis are provided; And
D) volatile oil of described Herba Blumeae Balsamiferae and the volatile oil of water extract and described Herba Pogostemonis and water extract is mixed, with the obtained compositions with Penetration enhancing effect.
Preferably, at described step b) in, Herba Blumeae Balsamiferae is made to be soak 3 hours in the water of described Herba Blumeae Balsamiferae weight 10 ~ 15 times in weight, adopt extraction by steam distillation 8 hours, be separated the volatile oil obtaining Herba Blumeae Balsamiferae, filtration obtains aqueous extract, makes described aqueous extract centrifugal, by dry for supernatant to obtain the water extract of Herba Blumeae Balsamiferae.
Preferably, at described step c) in, Herba Pogostemonis is made to be soak 6 hours in the water of described Herba Pogostemonis weight 10 ~ 15 times in weight, adopt extraction by steam distillation 8 hours, be separated the volatile oil obtaining Herba Pogostemonis, filtration obtains aqueous extract, makes described aqueous extract centrifugal, by dry for supernatant to obtain the water extract of Herba Pogostemonis.
Preferably, described step a) in, the Herba Blumeae Balsamiferae of 10 weight portions and the Herba Pogostemonis of 5 weight portions are provided.
Preferably, at described step b) and step c) in, under the condition of 3000 ~ 5000r/min centrifugal 5 ~ 10 minutes to obtain supernatant.
In the present invention, described steam distillation is the method for extraction volatile oil well known to those skilled in the art, and its concrete extraction element and method can see the related contents described in Pharmacopoeia of the People's Republic of China version in 2005 annex XD.Such as, after the extraction, volatile oil evaporates and is cooled in volatile oil catcher, thus can be separated.Herbal extract in container (such as round-bottomed flask) filters to remove medicinal residues, and filtrate is extracting solution.
In order to realize object of the present invention, the present invention also provides the described compositions with Penetration enhancing effect promoting the application in drug osmotic.
Preferably, described medicine is salbutamol sulfate.
The material source with the compositions of Penetration enhancing effect provided by the invention in natural herbal, safety, gentle, not chafe.Extract obtained in preparation method provided by the invention, based on Oleum Blumeae Balsamiferae, Herba Blumeae Balsamiferae water extract, be auxiliary with patchouli oil, Herba Pogostemonis water extract, said extracted thing uses jointly, Be very effective in the osmotic absorption promoting effective ingredient, in nourishes rough skin, improves in skin quality, anti-inflammation and also has certain effect.Described compositions can make medicament together with other drug, and described medicament has the effect of skin care, anti-inflammation, whitening and speckle dispelling, while promotion drug osmotic absorbs, also has the effect of beauty treatment, treatment.
Detailed description of the invention
Below by way of the description of detailed description of the invention only for being further elaborated the present invention, protection scope of the present invention is not only confined to following examples.Those skilled in the art can according to basic ideas of the present invention, make improving and amendment all can realize object of the present invention.But only otherwise depart from basic thought of the present invention, all within protection scope of the present invention.
The preparation of embodiment 1 present composition
Get the Herba Blumeae Balsamiferae of 10kg, make Herba Blumeae Balsamiferae be soak 3 hours in the water of described Herba Blumeae Balsamiferae weight 12 times in weight, adopt extraction by steam distillation 8 hours, be separated the volatile oil 1mL obtaining Herba Blumeae Balsamiferae.Filtration obtains aqueous extract, make described aqueous extract under the condition of 4000r/min centrifugal 7 minutes to obtain supernatant, supernatant is dried to dry, obtains the water extract 1.8kg of Herba Blumeae Balsamiferae.
Get the Herba Pogostemonis of 5kg, Herba Pogostemonis is made to be soak 6 hours in the water of described Herba Pogostemonis weight 12 times in weight, adopt extraction by steam distillation 8 hours, be separated the volatile oil 0.5mL obtaining Herba Pogostemonis, filtration obtains aqueous extract, make described aqueous extract under the condition of 4000r/min centrifugal 7 minutes to obtain supernatant, supernatant is dried to dry, obtains the water extract 0.8kg of Herba Pogostemonis.
Mix the volatile oil of described Herba Blumeae Balsamiferae and the volatile oil of water extract and described Herba Pogostemonis and water extract, the obtained compositions with Penetration enhancing effect of the present invention.
The preparation of embodiment 2 present composition
Obtain the compositions with Penetration enhancing effect of the present invention according to the mode identical with embodiment 1, difference is to use the Herba Blumeae Balsamiferae of 20kg and the Herba Pogostemonis of 1kg.
The preparation of embodiment 3 present composition
Obtain the compositions with Penetration enhancing effect of the present invention according to the mode identical with embodiment 1, difference is to use the Herba Blumeae Balsamiferae of 1kg and the Herba Pogostemonis of 10kg.
Experimental example urgees osmotic effect
1 material
1.1 animal Albino guinea pigs, male and female dual-purpose, is provided by Traditional Chinese Medicine University Of Guangzhou's Experimental Animal Center, body weight 250 ~ 300g, quality certification SCXK (Guangdong)-2008-0020.
1.2 instrument UV-2450 ultraviolet-visible spectrophotometers (Japan, Shimadzu); KYC100B constant temperature gas bath (Shanghai Fuma Experiment Equipment Co., Ltd.).
1.3 medicines and reagent of sulfuric acid albuterol (Chinese pharmaceutical biological product qualification institute, lot number H00328-200502); The volatile oil of Herba Blumeae Balsamiferae of preparation in embodiment 1 and water extract, the volatile oil of Herba Pogostemonis and the volatile oil of water extract and Herba Blumeae Balsamiferae and the volatile oil of water extract and Herba Pogostemonis and the mixture of water extract; Azone (Xinxiang Gao Jin pharmaceutcal corporation, Ltd, lot number 20060710); All the other agents useful for same are analytical pure.
2 methods
The preparation of 2.1 isolated skins carefully shaves off the hair of guinea pig back, peels skin of back after execution, removes subcutaneus adipose tissue, repeatedly rinses, till without muddiness, put into 4 DEG C of refrigerators and preserve, be finished in 3 days with normal saline.
2.2 selections measuring wavelength select 275nm as the absorbing wavelength measured.
Salbutamol sulfate is got in the preparation of 2.3 standard curves, and accurately weighed 20.00mg, is made into 200mgL with normal saline
-1stock solution, with normal saline be diluted to 200.00 successively, 100.00,50.00,20.00,10.00mgL
-1serial solution, get this serial solution, measure its luminosity at 275nm respectively.Take absorbance as vertical coordinate, mass concentration is that abscissa carries out linear regression, obtains standard curve equation and is: Y=0.0057X+0.0091 (R
2=0.9999), the range of linearity is 10 ~ 200mgL
-1.
2.4 precision and the response rate get 101.11,49.58,18.92mgL
-13 mass concentration salbutamol sulfate solution measure 5 times, continuous measurement 3d every day.Record withinday precision RSD 0.15%, 0.39%, 0.59%, day to day precision RSD 0.69%, 1.00%, 1.69%.Get 101.11,49.58,18.92mgL
-13 mass concentration salbutamol sulfate solution 2mL, each mass concentration gets 3 samples, add 49.58 respectively, 48.83,49.58mgL
-1solution 2mL, measures its absorbance (A).RSD is respectively 1.78%, 2.16%, 2.83%.In table 1.
Table 1 response rate is tested
The preparation of 2.5 release liquid and acceptable solution
Release liquid A to H adopts the ethanol water of 70 volume % to be solvent.
A group is that it is the salbutamol sulfate solution of 1.0 % by weight not containing the matched group of permeation enhancers;
B group adopts the volatile oil of Herba Blumeae Balsamiferae obtained in embodiment 1 and the volatile oil of water extract and Herba Pogostemonis and the mixture of water extract, and it is the composition solution of 0.5 % by weight, and wherein the concentration of salbutamol sulfate is 1.0 % by weight;
C group adopts the volatile oil of Herba Blumeae Balsamiferae obtained in embodiment 1 and the volatile oil of water extract and Herba Pogostemonis and the mixture of water extract, and it is the composition solution of 1.0 % by weight, and wherein the concentration of salbutamol sulfate is 1.0 % by weight;
D group adopts the volatile oil of Herba Blumeae Balsamiferae obtained in embodiment 1 and the volatile oil of water extract and Herba Pogostemonis and the mixture of water extract, and it is the composition solution of 2.0 % by weight, and wherein the concentration of salbutamol sulfate is 1.0 % by weight;
E group adopts azone, and it is the azone solution of 1.0 % by weight, and wherein the concentration of salbutamol sulfate is 1.0 % by weight;
F group adopts the volatile oil of Herba Blumeae Balsamiferae obtained in embodiment 1 and the volatile oil of water extract and Herba Pogostemonis and the mixture of water extract and azone, the concentration of wherein said compositions is 1.0 % by weight, the concentration of described azone is 1.0 % by weight, and the concentration of salbutamol sulfate is 1.0 % by weight;
G group adopts the volatile oil of Herba Blumeae Balsamiferae obtained in embodiment 1 and the mixture of water extract, and it is the mixture solution of 1.0 % by weight, and wherein the concentration of salbutamol sulfate is 1.0 % by weight;
H group adopts the volatile oil of Herba Pogostemonis obtained in embodiment 1 and the mixture of water extract, and it is the mixture solution of 1.0 % by weight, and wherein the concentration of salbutamol sulfate is 1.0 % by weight;
Receiving liquid is normal saline.
2.6 penetrating absorption carry out Transdermal Absorption experiment at two rooms transdermal disperser, and release room uses the release liquid of A to H respectively, and consumption is 0.1mL, and the receiving liquid of receiving chamber is the normal saline of 5mL, and temperature is (32.0 ± 0.5) DEG C, and vibration velocity is 120rmin
-1, diffusion area is 0.502cm
2.2,4,8,12,24h gets 4.0mL receiving liquid respectively, adds the receiving liquid of equivalent simultaneously.Measure absorbance, and substitute into regression equation, calculating concentration, after the continuous transdermal 24h of above-mentioned skin, remove the release liquid in release room, skin physiological saline cleans repeatedly, and blots with filter paper bar.
2.7 result treatment bring formula below into by recording concentration at every turn, calculate accumulative transit dose Q(list of references: Zhu Qianyun, Li Xiaoqing, Lee becomes net. and azone is on the impact [J] of Ruyi Jinhuang emulsifiable paste Transdermal Absorption. Chinese experimental pharmacology of Chinese medical formulae magazine, 2011 (20): 246).
Wherein, Cn is the drug level (μ g/mL) of the n-th sample point, and Ci is the drug level (mgL of i-th sample point
-1), A is diffusion area.Carry out linear regression with Percutaneous permeability (Q) to time t, the slope of gained Q-t linear equation is infiltration rate P (μ gcm
-2h
-1).
2.8 interference tests, by 2.6 method operations, are got transdermal receiving liquid during 12h, and are scanned in 200nm ~ 300nm wave-length coverage, near 275nm, do not occur Interference Peaks.
The all statistics of 2.9 statistical method complete on DAS1.0 software, and measurement data adopts
represent.
3 results
Different permeation enhancers is on the impact of salbutamol sulfate percutaneous permeation