CN102793660B - Etofesalamide ointment and preparation technology thereof - Google Patents
Etofesalamide ointment and preparation technology thereof Download PDFInfo
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- CN102793660B CN102793660B CN201210273702.8A CN201210273702A CN102793660B CN 102793660 B CN102793660 B CN 102793660B CN 201210273702 A CN201210273702 A CN 201210273702A CN 102793660 B CN102793660 B CN 102793660B
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Abstract
The invention relates to an ointment for the treatment of eczema and neurodermatitis, and concretely relates to an etofesalamide ointment. The ointment comprises a therapeutically effective amount of the etofesalamide ointment, and pharmaceutically acceptable excipients; and the ointment further comprises a hydrophilic gel material and a skin penetration enhancer. The hydrophilic gel material is carbomer resin, and the skin penetration enhancer is macrogolglyceride. Compared with the prior art, the technology improves penetration rate of the drug through skin. The ointment prepared by the technology has the characteristics of being not greasy and easy to clean, and does not affect the normal function of the skin, can promote the excretion of eczema secretion, and thereby significantly improves compliance of patients. The technology is simple and feasible, and easy to realize.
Description
Technical field
The present invention relates to a kind of emulsifiable paste for the treatment of eczema and neurodermatitis, be specifically related to a kind of Trial of Etofesalamide emulsifiable paste and preparation technology thereof.
Background technology
Eczema and neurodermatitis are common dermatosiss.
The cause of disease complexity of eczema, environmental stimuli, animality, vegetalitas factor, various reinforcing stimuluss all can bring out primary disease.Eczema is generally divided into acute, subacute and chronic three kinds, can occur in any age, asexuality difference, and any position of health all can occur, and has the advantages that repeatability is strong, the acute pruritus healing cycle is long.
Neurodermatitis is common a kind of chronic skin delayed ischemic neurological deficits disease, accounts for department of dermatologry first visit patient's 5% left and right, becomes feature with violent pruritus and the fresh sample of skin limitation tongue, and the course of disease is long, and refractory more.For the pathogenesis of neurodermatitis, there is no at present final conclusion, but there are some researches show that psychentonia, irascible temperament, fatigue, insomnia, melancholy can cause aggravation.
The sickness rate showed increased of eczema and neurodermatitis in recent years, there are some researches show to use frequent with environmental pollution, cosmetics and rhythm of life is too fast relevant, medicine is taking glucocorticoids as main clinically.
Trial of Etofesalamide, its chemical name: N-(4-ethoxyphenyl)-2-Hydroxylbenzamide, structural formula is as follows:
For non-steroidal anti-inflammatory, Claritin, former name benefit skin phthalein amine, efuamide, it is first class national new drug, this medicine can effectively be avoided because life-time service hormone medicine causes atrophoderma, color lake, hirsutism, bounces, brings out the untoward reaction such as infection and drug dependence, become the novel medicine that is used for the treatment of neurodermatitis and eczema, have market potential.External preparation for skin type Trial of Etofesalamide Ointment is in Discussion on Chinese Listed, and trade name is Ai Dite.
But we find under study for action, the Trial of Etofesalamide Ointment (Ai Dite) of listing exists that medicine skin transmitance is low, appearance property is poor, the shortcoming of greasy not easy cleaning, thereby has greatly affected clinical practice and the effect of this product.
Summary of the invention
The object of the present invention is to provide a kind of Trial of Etofesalamide emulsifiable paste and preparation technology thereof, this emulsifiable paste has the feature of non-greasy, easy cleaning, and not cutaneous normal function, and eczema secretions is had to absorption function, can promote the excretion of eczema secretions, greatly improve patient's compliance.
Trial of Etofesalamide emulsifiable paste of the present invention, comprises the pharmaceutically acceptable adjuvant of Trial of Etofesalamide for the treatment of effective dose, and this emulsifiable paste also includes hydrophilic gel material and Percutaneous absorption enhancer.
Described hydrophilic gel material is carbomer resin series, preferably Carbomer974,0.1 ~ 2.0wt.% that Carbomer974 consumption is whole recipe quantity, preferably 0.6 ~ 1.0wt.%.
Described Percutaneous absorption enhancer is polyethylene glycol glycerol lipid, preferably octanoic acid capric acid polyethyleneglycol glyceride and/or pegoxol 7 stearate, 2.0 ~ 20.0wt.% that Labraso consumption is whole recipe quantity, preferably 5.0 ~ 10.0wt.%; Pegoxol 7 stearate consumption is 2.0 ~ 20.0wt.% of whole recipe quantity, preferably 5.0 ~ 7.0%wt.%.
Described pharmaceutically acceptable adjuvant is emollient, antiseptic, stabilizing agent and diluent.
Described emollient is liquid paraffin, 5.0 ~ 30.0wt.% that consumption is whole recipe quantity, preferably 6.0 ~ 10.0wt.%.
Described antiseptic is mud moor gold ester class, preferably one or more in methyl hydroxybenzoate, ethyl hydroxybenzoate, propylparaben, butoben, preferably ethyl hydroxybenzoate, 0.01 ~ 0.5wt.% that antiseptic consumption is whole recipe quantity.
Described stabilizing agent is triethanolamine, disodiumedetate or sodium sulfite, 0.05% ~ 1.5wt.% that triethanolamine consumption is whole recipe quantity; 0.05% ~ 0.5wt.% that disodiumedetate or sodium sulfite consumption are whole recipe quantity.
Described diluent is water, 40 ~ 80wt.% that consumption is whole recipe quantity, preferably 52 ~ 73wt.%.
The preparation technology of described Trial of Etofesalamide emulsifiable paste, comprises the steps:
(1) oil phase preparation: take Percutaneous absorption enhancer, emollient and antiseptic in container, heating in water bath to 75 ~ 80 DEG C, all meltings after mixing, then add Trial of Etofesalamide, 75 ~ 80 DEG C of insulations, as oil phase;
(2) water preparation:
Take carbomer resin in container, add the diluent of recipe quantity 80 ~ 90% to soak at least 24 hours, heating in water bath to 75 ~ 80 DEG C, after carbomer resin dissolves, then add stabilizing agent, after all dissolving in 75 ~ 80 DEG C of insulations, as water;
(3) cream processed:
Water is added in oil phase, and 75 ~ 80 DEG C of insulation emulsifyings are after 20 ~ 30 minutes, and water-bath is cooled to below 40 DEG C, adds the diluent of stabilizing agent and surplus, and homogenizing, the even breast of vacuum, make Trial of Etofesalamide emulsifiable paste.
The present invention has following beneficial effect:
Compared with prior art, the present invention has improved medicine skin transmitance; There is the feature of non-greasy, easy cleaning, and the not cutaneous normal function of emulsifiable paste of the present invention, eczema secretions is had to absorption function, can promote the excretion of eczema secretions, thereby greatly improved patient's compliance, preparation is simple for it, be easy to realize.
Detailed description of the invention
Below in conjunction with embodiment, the present invention is described further.
Embodiment 1
Preparation technology:
(1) oil phase preparation: take recipe quantity pegoxol 7 stearate, Labraso, liquid paraffin and ethyl hydroxybenzoate in a container, heating in water bath to 75 ~ 80 DEG C, be uniformly mixed and make whole meltings, add Trial of Etofesalamide rapid stirring 30 minutes, 75 ~ 80 DEG C of insulations, as oil phase.
(2) water preparation:
Take the Carbomer974 of recipe quantity in a container, add the purified water of recipe quantity 90% to soak 24 hours, for subsequent use; By above-mentioned Carbomer974 soak heating in water bath to 75 ~ 80 DEG C, stir and make, after all dissolvings, to add disodiumedetate, to stir and make whole dissolvings, 75 ~ 80 DEG C of insulations, as water.
(3) cream processed:
Water is slowly added in oil phase, and limit edged stirs, 75 ~ 80 DEG C of insulation rapid stirrings emulsifying 30 minutes, then water-bath is cooled to below 40 DEG C, adds the purified water of triethanolamine and surplus, rapid stirring 30 minutes, homogenizing 5 minutes, even newborn 30 minutes of vacuum, obtains emulsifiable paste.
Embodiment 2
Preparation process is with embodiment 1.
Embodiment 3
Preparation process is with embodiment 1.
Embodiment 4
Preparation process is with embodiment 1.
Embodiment 5
Preparation process is with embodiment 1.
Embodiment 6
Preparation process is with embodiment 1.
Embodiment 7
The emulsifiable paste that above-described embodiment 1 ~ 6 is prepared is tested as follows:
Centrefuge experiment: get respectively by the emulsifiable paste 5g of each embodiment formula preparation in 10ml centrifuge tube, under rotating speed 4000rpm centrifugal 30 minutes, all do not find lamination.
Uniformity: get respectively by each embodiment formula preparation emulsifiable paste and be coated in right amount skim on glass plate, observe mastic all without granule existence separately, and micro-Microscopic observation drop size is even, particle rounding.
Granularity: microscopic examination method, get respectively by the emulsifiable paste of each embodiment formula preparation in right amount, be placed on microscope slide, under 100 power microscopes, observe and all do not observe the particle that is greater than 100um, also all without coacervation.
High temperature breaking test: get respectively by the emulsifiable paste of each embodiment formula preparation in right amount, be placed in after glass tubing sealing, put in 50 ± 2 DEG C of baking ovens, take out for 24 hours, return to room temperature, observe the situations of change such as emulsifiable paste outward appearance, uniformity, granularity, the results are shown in following table 1.
Table 1 high temperature breaking test result table
As shown in Table 1, the emulsifiable paste of preparing has good thermostability.
Low temperature damage experiment: the emulsifiable paste of getting respectively preparation is appropriate, is placed in after glass tubing sealing, puts in-15 ± 2 DEG C of refrigerators, places taking-up in 24 hours, returns to room temperature, observes the situations of change such as emulsifiable paste outward appearance, uniformity, granularity, and result of the test sees the following form 2.
Table 2 low temperature damage experimental result
As shown in Table 2, the emulsifiable paste of preparing has good tolerance to cold.
Can obviously improve the hold-up of medicine in skin in order to further illustrate Trial of Etofesalamide emulsifiable paste medicine of the present invention, select the large Corium Mus of firm processing as material, with 40% ethanol/PH7.4 phosphoric acid solution, as receiver media, the emulsifiable paste of preparing with the embodiment of the present invention 2 and commercially available Trial of Etofesalamide Ointment (Ai Dite) have carried out in-vitro percutaneous infiltration comparative experiments.Result of the test is as following table 3:
Table 3 body place transdermal result of the test table
Trial of Etofesalamide emulsifiable paste percutaneous rate of the present invention and drug transdermal cumulant are all 3.1 times of Ai Dite ointment from the above results, show Trial of Etofesalamide emulsifiable paste of the present invention all former Trial of Etofesalamide Ointment (Ai Dite ointment) skin permeation rate be significantly improved.
In order to further illustrate Trial of Etofesalamide emulsifiable paste steady quality of the present invention, the fill a prescription Trial of Etofesalamide emulsifiable paste of preparation of the present invention has been carried out to accelerated test, formulation Example 2 of the present invention is prepared after emulsifiable paste aluminum pipe filling in temperature: 30 ± 2 DEG C; Under the condition of relative humidity 65 ± 5%, place 6 months, detect respectively at sampling at the the the 0th, 1,2,3,6 the end of month, emphasis test item is content, related substance, character, granularity, uniformity and lamination (centrefuge experiment), result shows that above-mentioned indices is without significant change, show Trial of Etofesalamide emulsifiable paste steady quality of the present invention, be applicable to long-term storage and use.
Claims (3)
1. a Trial of Etofesalamide emulsifiable paste, comprise the pharmaceutically acceptable adjuvant of Trial of Etofesalamide for the treatment of effective dose, described pharmaceutically acceptable adjuvant is emollient, antiseptic, stabilizing agent and diluent, it is characterized in that this emulsifiable paste also includes hydrophilic gel material and Percutaneous absorption enhancer;
Described hydrophilic gel material is carbomer resin 974; 0.1～2.0wt.% that described Carbomer974 consumption is whole recipe quantity;
Described Percutaneous absorption enhancer is Labraso and pegoxol 7 stearate; 2.0～20.0wt.% that described Percutaneous absorption enhancer consumption is whole recipe quantity;
The preparation technology of described Trial of Etofesalamide emulsifiable paste, comprises the steps:
(1) oil phase preparation: take Percutaneous absorption enhancer, emollient and antiseptic in container, heating in water bath to 75～80 DEG C, all meltings after mixing, then add Trial of Etofesalamide, 75～80 DEG C of insulations, as oil phase;
Described emollient is liquid paraffin, 5.0～30.0wt.% that consumption is whole recipe quantity;
Described antiseptic is parabens;
(2) water preparation:
Take carbomer resin in container, add the diluent of recipe quantity 80～90% to soak at least 24 hours, heating in water bath to 75～80 DEG C, after carbomer resin dissolves, then add stabilizing agent, after all dissolving in 75～80 DEG C of insulations, as water;
Described stabilizing agent is the combination of triethanolamine and disodiumedetate, 0.05%～1.5wt.% that triethanolamine consumption is whole recipe quantity; Disodiumedetate consumption is 0.05%～0.5wt.% of whole recipe quantity;
(3) cream processed:
Water is added in oil phase, and 75～80 DEG C of insulation emulsifyings are after 20～30 minutes, and water-bath is cooled to below 40 DEG C, adds the diluent of stabilizing agent and surplus, and homogenizing, the even breast of vacuum, make Trial of Etofesalamide emulsifiable paste.
2. Trial of Etofesalamide emulsifiable paste according to claim 1, is characterized in that described antiseptic is one or more in methyl hydroxybenzoate, ethyl hydroxybenzoate, propylparaben, butoben, 0.01～0.5wt.% that antiseptic consumption is whole recipe quantity.
3. Trial of Etofesalamide emulsifiable paste according to claim 1, is characterized in that described diluent is water, 40～80wt.% that consumption is whole recipe quantity.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210273702.8A CN102793660B (en) | 2012-08-02 | 2012-08-02 | Etofesalamide ointment and preparation technology thereof |
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| CN201210273702.8A CN102793660B (en) | 2012-08-02 | 2012-08-02 | Etofesalamide ointment and preparation technology thereof |
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| CN102793660A CN102793660A (en) | 2012-11-28 |
| CN102793660B true CN102793660B (en) | 2014-07-02 |
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2012
- 2012-08-02 CN CN201210273702.8A patent/CN102793660B/en active Active
Non-Patent Citations (1)
| Title |
|---|
| 关玉晶.自乳化基质乙氧苯柳胺乳膏的研究.《中国优秀硕博士学位论文全文数据库（硕士） 医药生物科技辑（月刊）》.2007,(第01期), * |
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