CN102319202A - Mometasone furoate gel and preparation method thereof - Google Patents
Mometasone furoate gel and preparation method thereof Download PDFInfo
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Abstract
The invention provides mometasone furoate gel and a preparation method thereof; the mometasone furoate gel is prepared by the following raw auxiliary materials by weight: 1 parts of mometasone furoate, 150 parts of glycerin, 7.5 parts of carbomer, 1 parts of sodium alginate, 5 parts of laurocapram, 10 parts of triethanolamine, 50 parts of medicinal ethanol, 2 parts of ethylparaben, and the balance of purified water which is added to allow the total weight to be 1000 parts; The advantages of the invention are that: carbomer is used as a water-soluble substrate; triethanolamine is used as a consistency regulator; the product is provided with the advantages of strong adhesion to skin surfaces, good spreading performance, prolongation of retention time of the medicament on skin surfaces; and the effect of the medicament is enhanced. The product is easy to spread and wash, is not greasy, can absorb tissue exudates, and does not interfere normal functions of skin. The product is easy to clean, does not contaminate clothes, and has good stability; the product has smooth appearance, and is transparent and fine; the product has no local irritation; the product has appropriate consistency and viscosity, and is easy to be coated for application; the product has the advantages of convenient carrying, transportation, and storage.
Description
Technical field
The present invention relates to a kind of technical field of external preparation medicine, especially a kind of external-use gel preparation medicine that contains momestasone furoate, this gel is owing to adopt the substrate combination of carbomer and triethanolamine; Carbomer is as gel-type vehicle; Triethanolamine is as consistency modifiers, and glycerol has better moisture retention and stability as wetting agent; Can not hinder the skin normal function by the absorptive tissue transudate, be specially adapted to seborrheic dermatosis.
Background technology
Momestasone furoate is the local glucocorticoid medicine of synthetic, has the low characteristics of cortex hormone function inhibition on the curative effect kidney tonifying.The momestasone furoate gel has the effect that reduces inflammation with pruritus, is applicable to effective dermatosis of glucocorticoid such as dermatitis (contact dermatitis, seborrheic dermatitis, atoipc dermatitis, neurodermatitis); Acute, subacute, chronic eczema, discoid lupus erythematosus; Lichen planus, skin amyloidosis lichen, granuloma annulare; The small size psoriasis, pretibial myxedema etc.
At present, the momestasone furoate gel of market sale, stability is generally relatively poor; And what market sale was more is cream preparation; And it is more to influence the stable factor of emulsifiable paste matrix, and lamination appears in cream preparation more easily, and gel preparation is more stable than cream preparation from stability; In addition from the convenience used, greasy feeling etc., emulsifiable paste matrix is oil phase and water composition, and oil phase is vaseline, fatty acid, aliphatic alcohol mostly, and greasy feeling is stronger during use.
The present invention is to provide the external preparation medicine that contains momestasone furoate; This gel is the substrate combination of carbomer and triethanolamine owing to what adopt, and carbomer is as gel-type vehicle, and triethanolamine is as consistency modifiers; Glycerol is as wetting agent; Have better moisture retention and stability, can not hinder the skin normal function by the absorptive tissue transudate, be specially adapted to seborrheic dermatosis.The selection of wetting agent is added can better keep not dehydration of gel, not atrophy, makes gel keep stable before the deadline.This gel also has good heat-resisting cold tolerance simultaneously.
Summary of the invention
In order to solve the deficiency that exists in the prior art, a kind of momestasone furoate gel provided by the invention and preparation method thereof, its adjuvant are selected appropriately, can be so that momestasone furoate gel moisturizes performance and stability are more outstanding.The present invention is except selecting wetting agent; Also added aqueous gel substrate carbomer in the gel; Its molding effect is superior to substrate used in the general gel; And add glycerol in the prescription and preserve moisture, make that the stability of gel is better, thereby momestasone furoate gel provided by the present invention has better stability.
The purpose of this invention is to provide a kind of momestasone furoate gel and preparation method thereof; This gel is owing to adopt the substrate combination of carbomer and triethanolamine, and wherein carbomer is as gel-type vehicle, and triethanolamine is as consistency modifiers; Glycerol is as wetting agent; Therefore have better stability, can the absorptive tissue transudate and do not hinder the skin normal function, be specially adapted to seborrheic dermatosis; Gel is more stable than emulsifiable paste with emulsifiable paste gel from stability simultaneously.
Momestasone furoate gel provided by the present invention is realized through following technical scheme:
The momestasone furoate gel, processed by the supplementary material of following weight proportioning: 1 part of momestasone furoate, 150 parts of glycerol, 7.5 parts of carbomers, 1 part of sodium alginate, 5 parts of laurocaprams, 10 parts of triethanolamine, 50 parts of medicinal alcohols, 2 parts of ethyl hydroxybenzoates, the purified water ad pond om that adds surplus are 1000 parts.
Wherein, the method for preparing of momestasone furoate gel is:
1, carbomer, sodium alginate being scattered in the emulsifying pot that 50% the purified water that is about the preparation total amount is housed, is to stir 1 hour under 60 rev/mins the situation at rotating speed, places 12-16 hour fully swelling afterwards again; Adding in glycerol, laurocapram to the above-mentioned solution, is to stir 0.5 hour under 60 rev/mins the situation at rotating speed, triethanolamine is slowly added in the above-mentioned solution again, at rotating speed is to stir 1 hour under 60 rev/mins the situation, until becoming clear gel substrate; 2, momestasone furoate, ethyl hydroxybenzoate are added in the medicinal alcohol, stir and to make dissolving, 150 mesh sieves are crossed in heating in water bath to 70～75 ℃, and are as the alcoholic solution of principal agent, subsequent use; 3, the alcoholic solution with principal agent slowly adds in the above-mentioned gel-type vehicle; Be to stir under 60 rev/mins the situation it to be evenly distributed in 0.5 hour at rotating speed; Again purified water is added to total amount; The meter reading that keeps vacuum be-0.05～-0.07MPa, at rotating speed stirring 1 hour under 60 rev/mins the situation, make the milky translucent gels at last.
Preferred version is following:
One, momestasone furoate gel, processed by the supplementary material of following weight proportioning: 1 part of momestasone furoate, 150 parts of glycerol, 7.5 parts of carbomers, 1 part of sodium alginate, 5 parts of laurocaprams, 10 parts of triethanolamine, 50 parts of medicinal alcohols, 2 parts of ethyl hydroxybenzoates, the purified water ad pond om that adds surplus are 1000 parts.
Wherein, the method for preparing of momestasone furoate gel is:
1, carbomer, sodium alginate being scattered in the emulsifying pot that 50% the purified water that is about the preparation total amount is housed, is to stir 1 hour under 60 rev/mins the situation at rotating speed, places 12 hours abundant swellings afterwards again; Adding in glycerol, laurocapram to the above-mentioned solution, is to stir 0.5 hour under 60 rev/mins the situation at rotating speed, triethanolamine is slowly added in the above-mentioned solution again, at rotating speed is to stir 1 hour under 60 rev/mins the situation, until becoming clear gel substrate; 2, momestasone furoate, ethyl hydroxybenzoate are added in the medicinal alcohol, stir and to make dissolving, heating in water bath to 70 ℃ is crossed 150 mesh sieves, and is as the alcoholic solution of principal agent, subsequent use; 3, the alcoholic solution with principal agent slowly adds in the above-mentioned gel-type vehicle; Be to stir under 60 rev/mins the situation it to be evenly distributed in 0.5 hour at rotating speed; Again purified water is added to total amount; Keeping the meter reading of vacuum be-0.05MPa, is stirring 1 hour under 60 rev/mins the situation at rotating speed, makes the milky translucent gels at last.
Two, the method for preparing of momestasone furoate gel is:
1, carbomer, sodium alginate being scattered in the emulsifying pot that 50% the purified water that is about the preparation total amount is housed, is to stir 1 hour under 60 rev/mins the situation at rotating speed, places 16 hours abundant swellings afterwards again; Adding in glycerol, laurocapram to the above-mentioned solution, is to stir 0.5 hour under 60 rev/mins the situation at rotating speed, triethanolamine is slowly added in the above-mentioned solution again, at rotating speed is to stir 1 hour under 60 rev/mins the situation, until becoming clear gel substrate; 2, momestasone furoate, ethyl hydroxybenzoate are added in the medicinal alcohol, stir and to make dissolving, heating in water bath to 75 ℃ is crossed 150 mesh sieves, and is as the alcoholic solution of principal agent, subsequent use; 3, the alcoholic solution with principal agent slowly adds in the above-mentioned gel-type vehicle; Be to stir under 60 rev/mins the situation it to be evenly distributed in 0.5 hour at rotating speed; Again purified water is added to total amount; Keeping the meter reading of vacuum be-0.07MPa, is stirring 1 hour under 60 rev/mins the situation at rotating speed, makes the milky translucent gels at last.
Three, the method for preparing of momestasone furoate gel is:
1, carbomer, sodium alginate being scattered in the emulsifying pot that 50% the purified water that is about the preparation total amount is housed, is to stir 1 hour under 60 rev/mins the situation at rotating speed, places 14 hours abundant swellings afterwards again; Adding in glycerol, laurocapram to the above-mentioned solution, is to stir 0.5 hour under 60 rev/mins the situation at rotating speed, triethanolamine is slowly added in the above-mentioned solution again, at rotating speed is to stir 1 hour under 60 rev/mins the situation, until becoming clear gel substrate; 2, momestasone furoate, ethyl hydroxybenzoate are added in the medicinal alcohol, stir and to make dissolving, heating in water bath to 73 ℃ is crossed 150 mesh sieves, and is as the alcoholic solution of principal agent, subsequent use; 3, the alcoholic solution with principal agent slowly adds in the above-mentioned gel-type vehicle; Be to stir under 60 rev/mins the situation it to be evenly distributed in 0.5 hour at rotating speed; Again purified water is added to total amount; Keeping the meter reading of vacuum be-0.06MPa, is stirring 1 hour under 60 rev/mins the situation at rotating speed, makes the milky translucent gels at last.
Supplementary material weight proportion in above-mentioned each preferred version is identical.
Contrast from the dosage form aspect in addition and have following outstanding advantage:
No matter gel is from its stability, and the convenience of use, greasy feeling etc. all are superior to ointment; At first the main matrix of gel is a carbomer; Medicine is evenly distributed in behind dissolve with ethanol in it, and substrate must not passed through the emulsifying molding, generally speaking can layering; And the variable factor that influences emulsifiable paste matrix stability is more; Tend to cause phenomenons such as breakdown of emulsion, layering, mastic is damaged, so gel is more stable than emulsifiable paste with emulsifiable paste gel from stability; In addition from the convenience used, greasy feeling etc., emulsifiable paste matrix is oil phase and water composition, and oil phase is vaseline, fatty acid, aliphatic alcohol mostly, and panesthesia is to greasy feeling is arranged during use.Moreover gel has in the skin surface tack by force, and stretchability is good, and prolong drug has strengthened the effect of medicine in the advantage of the holdup time of skin surface; It is simple that gel also has preparation technology; Shape is attractive in appearance; Be easy to characteristics such as coating is used, is prone to clean, pollution clothes, stability be not better, aqueous gel substrate proportion in the local topical preparation of new research and development is also increasing now, receives liking and favorable comment of patient.
Gel is to be cross-linked into RF as skeleton by macromolecular material, and mostly gel-type vehicle is separately or unites the macromolecular material that uses the hydrophilic high polymer that choice of base has material impact to the rheological property and the release property of gel.
The mixed liquor of carbomer and water, when regulating its pH value with the alkaline matter triethanolamine, carbomer induces its viscosity and forms gel, and when pH value during in 7 left and right sides, its viscosity is maximum, and the most stable.Glycerol has toughness, moisture retention, skin, mucosa is had the effect of moistening.So confirm that glycerol is wetting agent.Ethyl hydroxybenzoate has stronger bacteriostasis to mycete.So confirm that ethyl hydroxybenzoate is an antiseptic.The dissolve with ethanol scope is wide, is solvent commonly used in the external preparation.Momestasone furoate dissolubility in water is less in this product, so select for use ethanol as solvent, ethanol is to dermal toxicity and stimulates minimum solvent.Sodium alginate is a kind of natural polysaccharide, has the required stability of pharmaceutical preparation adjuvant, dissolubility, viscosity and safety; It has concentrated solution, forms gel and film forming ability.Laurocapram is nonpolar transdermal enhancer, and it can make cutin softening, strengthens permeability, makes medicine see through skin barrier, improves part or whole body blood drug level, improves the preparation bioavailability.The lipotropy hydrophilic medicament all there is the transdermal facilitation.
Advantage of the present invention: with the gel-type vehicle that carbomer, triethanolamine, glycerol etc. are made, the transparent exquisiteness of smooth in appearance is attractive in appearance, and is easy to be applied in skin, better regulates the denseness and increase gloss of gel; Can well keep not dehydration of gel, not atrophy makes gel keep steady statue before the deadline.Use carbomer as water-soluble base, triethanolamine is as consistency modifiers, and it is strong that these article are had in the skin surface tack, and stretchability is good, and prolong drug has strengthened the effect of medicine in the advantage of the holdup time of skin surface; These article are easy to the exhibition that is coated with and washing, no greasy feeling, ability absorptive tissue transudate, do not hinder the normal function of skin.These article be prone to clean, pollution clothes good stability not; Gel of the present invention has smooth in appearance, transparent exquisiteness; Local nonirritant does not hinder the normal function of skin; Denseness, viscosity suit, and are easy to coating and use; Carry, transport, preserve advantages such as very convenient.
Describe below in conjunction with each group specific embodiment.
The specific embodiment
Embodiment 1, momestasone furoate gel, processed by the supplementary material of following weight proportioning: 1 part of momestasone furoate, 150 parts of glycerol, 7.5 parts of carbomers, 1 part of sodium alginate, 5 parts of laurocaprams, 10 parts of triethanolamine, 50 parts of medicinal alcohols, 2 parts of ethyl hydroxybenzoates, the purified water ad pond om that adds surplus are 1000 parts.
Wherein, the method for preparing of momestasone furoate gel is:
1, carbomer, sodium alginate being scattered in the emulsifying pot that 50% the purified water that is about the preparation total amount is housed, is to stir 1 hour under 60 rev/mins the situation at rotating speed, places 12 hours abundant swellings afterwards again; Adding in glycerol, laurocapram to the above-mentioned solution, is to stir 0.5 hour under 60 rev/mins the situation at rotating speed, triethanolamine is slowly added in the above-mentioned solution again, at rotating speed is to stir 1 hour under 60 rev/mins the situation, until becoming clear gel substrate; 2, momestasone furoate, ethyl hydroxybenzoate are added in the medicinal alcohol, stir and to make dissolving, heating in water bath to 70 ℃ is crossed 150 mesh sieves, and is as the alcoholic solution of principal agent, subsequent use; 3, the alcoholic solution with principal agent slowly adds in the above-mentioned gel-type vehicle; Be to stir under 60 rev/mins the situation it to be evenly distributed in 0.5 hour at rotating speed; Again purified water is added to total amount; Keeping the meter reading of vacuum be-0.05MPa, is stirring 1 hour under 60 rev/mins the situation at rotating speed, makes the milky translucent gels at last.
Embodiment 2, momestasone furoate gel, processed by the supplementary material of following weight proportioning: 1 part of momestasone furoate, 150 parts of glycerol, 7.5 parts of carbomers, 1 part of sodium alginate, 5 parts of laurocaprams, 10 parts of triethanolamine, 50 parts of medicinal alcohols, 2 parts of ethyl hydroxybenzoates, the purified water ad pond om that adds surplus are 1000 parts.
The method for preparing of momestasone furoate gel is:
1, carbomer, sodium alginate being scattered in the emulsifying pot that 50% the purified water that is about the preparation total amount is housed, is to stir 1 hour under 60 rev/mins the situation at rotating speed, places 16 hours abundant swellings afterwards again; Adding in glycerol, laurocapram to the above-mentioned solution, is to stir 0.5 hour under 60 rev/mins the situation at rotating speed, triethanolamine is slowly added in the above-mentioned solution again, at rotating speed is to stir 1 hour under 60 rev/mins the situation, until becoming clear gel substrate; 2, momestasone furoate, ethyl hydroxybenzoate are added in the medicinal alcohol, stir and to make dissolving, heating in water bath to 75 ℃ is crossed 150 mesh sieves, and is as the alcoholic solution of principal agent, subsequent use; 3, the alcoholic solution with principal agent slowly adds in the above-mentioned gel-type vehicle; Be to stir under 60 rev/mins the situation it to be evenly distributed in 0.5 hour at rotating speed; Again purified water is added to total amount; Keeping the meter reading of vacuum be-0.07MPa, is stirring 1 hour under 60 rev/mins the situation at rotating speed, makes the milky translucent gels at last.
Embodiment 3, momestasone furoate gel, processed by the supplementary material of following weight proportioning: 1 part of momestasone furoate, 130 parts of glycerol, 9.5 parts of carbomers, 10 parts of triethanolamine, 50 parts of medicinal alcohols, 2 parts of ethyl hydroxybenzoates, the purified water ad pond om that adds surplus are 1000 parts.
The method for preparing of momestasone furoate gel is:
1, carbomer, sodium alginate being scattered in the emulsifying pot that 50% the purified water that is about the preparation total amount is housed, is to stir 1 hour under 60 rev/mins the situation at rotating speed, places 10 hours abundant swellings afterwards again; Adding in glycerol, laurocapram to the above-mentioned solution, is to stir 0.5 hour under 60 rev/mins the situation at rotating speed, triethanolamine is slowly added in the above-mentioned solution again, at rotating speed is to stir 1 hour under 60 rev/mins the situation, until becoming clear gel substrate; 2, momestasone furoate, ethyl hydroxybenzoate are added in the medicinal alcohol, stir and to make dissolving, heating in water bath to 85 ℃ is crossed 150 mesh sieves, and is as the alcoholic solution of principal agent, subsequent use; 3, the alcoholic solution with principal agent slowly adds in the above-mentioned gel-type vehicle; Be to stir under 60 rev/mins the situation it to be evenly distributed in 0.5 hour at rotating speed; Again purified water is added to total amount; Keeping the meter reading of vacuum be-0.09Mpa, is stirring 1 hour under 60 rev/mins the situation at rotating speed, makes the milky translucent gels at last.
The method for preparing of embodiment 4, momestasone furoate gel is:
1, carbomer, sodium alginate being scattered in the emulsifying pot that 50% the purified water that is about the preparation total amount is housed, is to stir 1 hour under 60 rev/mins the situation at rotating speed, places 10 hours abundant swellings afterwards again; Adding in glycerol, laurocapram to the above-mentioned solution, is to stir 0.5 hour under 60 rev/mins the situation at rotating speed, triethanolamine is slowly added in the above-mentioned solution again, at rotating speed is to stir 1 hour under 60 rev/mins the situation, until becoming clear gel substrate; 2, momestasone furoate, ethyl hydroxybenzoate are added in the medicinal alcohol, stir and to make dissolving, heating in water bath to 65 ℃ is crossed 150 mesh sieves, and is as the alcoholic solution of principal agent, subsequent use; 3, the alcoholic solution with principal agent slowly adds in the above-mentioned gel-type vehicle; Be to stir under 60 rev/mins the situation it to be evenly distributed in 0.5 hour at rotating speed; Again purified water is added to total amount; Keeping the meter reading of vacuum be-0.04MPa, is stirring 1 hour under 60 rev/mins the situation at rotating speed, makes the milky translucent gels at last.All the other are with embodiment 1.
The method for preparing of embodiment 5, momestasone furoate gel is:
1, carbomer, sodium alginate being scattered in the emulsifying pot that 50% the purified water that is about the preparation total amount is housed, is to stir 1 hour under 60 rev/mins the situation at rotating speed, places 17 hours abundant swellings afterwards again; Adding in glycerol, laurocapram to the above-mentioned solution, is to stir 0.5 hour under 60 rev/mins the situation at rotating speed, triethanolamine is slowly added in the above-mentioned solution again, at rotating speed is to stir 1 hour under 60 rev/mins the situation, until becoming clear gel substrate; 2, momestasone furoate, ethyl hydroxybenzoate are added in the medicinal alcohol, stir and to make dissolving, heating in water bath to 80 ℃ is crossed 150 mesh sieves, and is as the alcoholic solution of principal agent, subsequent use; 3, the alcoholic solution with principal agent slowly adds in the above-mentioned gel-type vehicle; Be to stir under 60 rev/mins the situation it to be evenly distributed in 0.5 hour at rotating speed; Again purified water is added to total amount; Keeping the meter reading of vacuum be-0.08Mpa, is stirring 1 hour under 60 rev/mins the situation at rotating speed, makes the milky translucent gels at last.All the other are with embodiment 1.
The method for preparing of embodiment 6, momestasone furoate gel is:
1, carbomer, sodium alginate being scattered in the emulsifying pot that 50% the purified water that is about the preparation total amount is housed, is to stir 1 hour under 60 rev/mins the situation at rotating speed, places 10 hours abundant swellings afterwards again; Adding in glycerol, laurocapram to the above-mentioned solution, is to stir 0.5 hour under 60 rev/mins the situation at rotating speed, triethanolamine is slowly added in the above-mentioned solution again, at rotating speed is to stir 1 hour under 60 rev/mins the situation, until becoming clear gel substrate; 2, momestasone furoate, ethyl hydroxybenzoate are added in the medicinal alcohol, stir and to make dissolving, heating in water bath to 85 ℃ is crossed 150 mesh sieves, and is as the alcoholic solution of principal agent, subsequent use; 3, the alcoholic solution with principal agent slowly adds in the above-mentioned gel-type vehicle; Be to stir under 60 rev/mins the situation it to be evenly distributed in 0.5 hour at rotating speed; Again purified water is added to total amount; Keeping the meter reading of vacuum be-0.09Mpa, is stirring 1 hour under 60 rev/mins the situation at rotating speed, makes the milky translucent gels at last.All the other are with embodiment 1.
Test Example:
The momestasone furoate gel that is made by the embodiment 1-6 substrate of respectively writing out a prescription is carried out stability test.
The momestasone furoate gel that embodiment 1-6 the is made substrate of respectively writing out a prescription is made as a, b, c, d, e, the f substrate experimental group of respectively writing out a prescription.
Other establishes the 7th group is matched group (wherein the 7th group of sample that provides is by certain the common momestasone furoate gel that obtains on the market).Simultaneously, the 7th group is made as the g group.
1, moisture retention test example
Extracting waste glazed paper is cut into 1cm * 2cm, 2cm * 4cm; 3cm * 6cm size after precision is heavy, evenly is coated with last layer sample (the different size sheets of each sample are respectively done 2 parts); Weigh, put into calorstat (25 ± 1) ℃ insulation 4h after, taking-up is weighed; Unit of account area water evaporates amount, 7 groups of prescription water evaporates amounts are respectively (6.8 ± 1.2) mgcm as a result
-2, (7.3 ± 1.3) mgcm
-2, (20.0 ± 2.4) mgcm
-2, (18.7 ± 1.0) mgcm
-2, (17.7 ± 1.1) mgcm
-2, (18.5 ± 1.4) mgcm
-2, (19.7 ± 1.2) mgcm
-2
Conclusion (of pressure testing): the result learns according to the moisture retention test example, and the moisture retention effect of the momestasone furoate gel that is made by embodiment 1, embodiment 2 is best, and the water evaporates area is minimum.
2, accelerated test is investigated the result
We are according to " the requirement of accelerated test in two appendix of Chinese pharmacopoeia version in 2005 " crude drug and pharmaceutical preparation stability test guideline "; Each 15g of substrate experimental group and the matched group g group of will respectively being write out a prescription by momestasone furoate gel a, b, c, d, e, the f that embodiment 1-6 makes contains in gel box; Being positioned over temperature is 30 ± 2 ℃; Relative humidity is in 65 ± 5% medicine stability test case; Respectively at sampling in 1,2,3,4,5,6 month; In " medicine stability test guideline ", each item of pharmaceutical preparation stability high spot reviews project requires these article have been carried out the investigation of character, uniformity, content, related substance, granularity, lamination, and the result sees the following form 1.
Table 1 accelerated test is investigated the result
The result: through 30 ± 2 ℃ of temperature, relative humidity can find out obviously that 65 ± 5% environment held 6 months momestasone furoate gel each item index that embodiment 1-2 makes has no significant change.Conclusion: these article are 30 ± 2 ℃ in temperature, and relative humidity is 65 ± 5% environment held 6 months, and each items such as drug content and character are investigated index not to be had significance and change, and these article are stablized.
3, the investigation result that keeps sample for a long time
We are according to " the requirement of two appendix of Chinese pharmacopoeia version in 2005 " crude drug and pharmaceutical preparation stability test guideline " long term test; Each 15g of substrate experimental group and the matched group g group of will respectively being write out a prescription by momestasone furoate gel a, b, c, d, e, the f that embodiment 1-6 makes contains in gel box; Being positioned over temperature is 18 ± 2 ℃; Relative humidity is in 60 ± 5% medicine stability test case; Respectively at sampling in 0,3,6 month; Require these article have been carried out the investigation of character, uniformity, content, related substance, granularity, lamination with each item of " crude drug and pharmaceutical preparation stability test guideline " Chinese medicine preparation stability high spot reviews project, the result sees the following form 2.
The table 2 investigation experimental result that keeps sample for a long time
The result: can find out obviously that the momestasone furoate gel that embodiment 1-2 makes kept sample 6 months for a long time, each item index was compared with 0 month and is had no significant change no significant change.
Annotate: "-" no change, "+" chap
Conclusion (of pressure testing): embodiment result learns according to stability test; Investigate in the experiment in accelerated test; The momestasone furoate gel that is made by embodiment 1-2 has better stability, can be 30 ± 2 ℃ in temperature, and relative humidity maintains a relatively stable state in 65 ± 5% environment; And in the investigation experiment that keeps sample for a long time, each organizes gel prescription substrate can be 18 ± 2 ℃ in temperature, and relative humidity maintains a relatively stable state in 60 ± 5% environment.
Comprehensive above conclusion can know that the momestasone furoate gel that is made by embodiment 1-2 is best.
Stability result shows that the content of momestasone furoate gel and related substance all do not have significant change in experimental example, shows that preparation stability is good.
Claims (4)
1. momestasone furoate gel and preparation method thereof, it is characterized in that: the supplementary material by the following weight proportioning is processed: 1 part of momestasone furoate, 150 parts of glycerol, 7.5 parts of carbomers, 1 part of sodium alginate, 5 parts of laurocaprams, 10 parts of triethanolamine, 50 parts of medicinal alcohols, 2 parts of ethyl hydroxybenzoates, the purified water ad pond om that adds surplus are 1000 parts.
2. momestasone furoate gel and preparation method thereof, processed by the supplementary material of following weight proportioning: 1 part of momestasone furoate, 150 parts of glycerol, 7.5 parts of carbomers, 1 part of sodium alginate, 5 parts of laurocaprams, 10 parts of triethanolamine, 50 parts of medicinal alcohols, 2 parts of ethyl hydroxybenzoates, the purified water ad pond om that adds surplus are 1000 parts;
The method for preparing of momestasone furoate gel is characterized in that:
The 1st step, carbomer, sodium alginate being scattered in the emulsifying pot that 50% the purified water that is about the preparation total amount is housed, is to stir 1 hour under 60 rev/mins the situation at rotating speed, places 12-16 hour fully swelling afterwards again; Adding in glycerol, laurocapram to the above-mentioned solution, is to stir 0.5 hour under 60 rev/mins the situation at rotating speed, triethanolamine is slowly added in the above-mentioned solution again, at rotating speed is to stir 1 hour under 60 rev/mins the situation, until becoming clear gel substrate; The 2nd step, momestasone furoate, ethyl hydroxybenzoate are added in the medicinal alcohol, stir and to make dissolving, 150 mesh sieves are crossed in heating in water bath to 70～75 ℃, and are as the alcoholic solution of principal agent, subsequent use; The 3rd step, the alcoholic solution of principal agent is slowly added in the above-mentioned gel-type vehicle; Be to stir under 60 rev/mins the situation it to be evenly distributed in 0.5 hour at rotating speed; Again purified water is added to total amount; The meter reading that keeps vacuum be-0.05～-0.07MPa, at rotating speed stirring 1 hour under 60 rev/mins the situation, make the milky translucent gels at last.
3. momestasone furoate gel, processed by the supplementary material of following weight proportioning: 1 part of momestasone furoate, 150 parts of glycerol, 7.5 parts of carbomers, 1 part of sodium alginate, 5 parts of laurocaprams, 10 parts of triethanolamine, 50 parts of medicinal alcohols, 2 parts of ethyl hydroxybenzoates, the purified water ad pond om that adds surplus are 1000 parts;
Wherein, the method for preparing of momestasone furoate gel is:
The 1st step, carbomer, sodium alginate being scattered in the emulsifying pot that 50% the purified water that is about the preparation total amount is housed, is to stir 1 hour under 60 rev/mins the situation at rotating speed, places 12 hours abundant swellings afterwards again; Adding in glycerol, laurocapram to the above-mentioned solution, is to stir 0.5 hour under 60 rev/mins the situation at rotating speed, triethanolamine is slowly added in the above-mentioned solution again, at rotating speed is to stir 1 hour under 60 rev/mins the situation, until becoming clear gel substrate; The 2nd step, momestasone furoate, ethyl hydroxybenzoate are added in the medicinal alcohol, stir and to make dissolving, heating in water bath to 70 ℃ is crossed 150 mesh sieves, and is as the alcoholic solution of principal agent, subsequent use; The 3rd step, the alcoholic solution of principal agent is slowly added in the above-mentioned gel-type vehicle; Be to stir under 60 rev/mins the situation it to be evenly distributed in 0.5 hour at rotating speed; Again purified water is added to total amount; Keeping the meter reading of vacuum be-0.05MPa, is stirring 1 hour under 60 rev/mins the situation at rotating speed, makes the milky translucent gels at last.
4. momestasone furoate gel, processed by the supplementary material of following weight proportioning: 1 part of momestasone furoate, 130 parts of glycerol, 9.5 parts of carbomers, 1 part of sodium alginate, 5 parts of laurocaprams, 10 parts of triethanolamine, 50 parts of medicinal alcohols, 2 parts of ethyl hydroxybenzoates, the purified water ad pond om that adds surplus are 1000 parts;
The method for preparing of momestasone furoate gel is:
The 1st step, carbomer, sodium alginate being scattered in the emulsifying pot that 50% the purified water that is about the preparation total amount is housed, is to stir 1 hour under 60 rev/mins the situation at rotating speed, places 14 hours abundant swellings afterwards again; Adding in glycerol, laurocapram to the above-mentioned solution, is to stir 0.5 hour under 60 rev/mins the situation at rotating speed, triethanolamine is slowly added in the above-mentioned solution again, at rotating speed is to stir 1 hour under 60 rev/mins the situation, until becoming clear gel substrate; The 2nd step, momestasone furoate, ethyl hydroxybenzoate are added in the medicinal alcohol, stir and to make dissolving, heating in water bath to 73 ℃ is crossed 150 mesh sieves, and is as the alcoholic solution of principal agent, subsequent use; The 3rd step, the alcoholic solution of principal agent is slowly added in the above-mentioned gel-type vehicle; Be to stir under 60 rev/mins the situation it to be evenly distributed in 0.5 hour at rotating speed; Again purified water is added to total amount; Keeping the meter reading of vacuum be-0.06MPa, is stirring 1 hour under 60 rev/mins the situation at rotating speed, makes the milky translucent gels at last.
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| CN109602693A (en) * | 2018-11-13 | 2019-04-12 | 华润三九（南昌）药业有限公司 | Mometasone furoate gel and preparation method thereof |
| CN112754990A (en) * | 2020-11-12 | 2021-05-07 | 广州白云山医药集团股份有限公司白云山何济公制药厂 | Mometasone furoate cream and preparation method thereof |
| CN113230203A (en) * | 2021-05-18 | 2021-08-10 | 广州白云山医药集团股份有限公司白云山何济公制药厂 | Mometasone furoate gel and preparation method thereof |
| CN114306180A (en) * | 2021-12-18 | 2022-04-12 | 中国人民解放军空军军医大学 | Ultraviolet sunburn repairing agent capable of being placed for long time and preparation method thereof |
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| CN112754990A (en) * | 2020-11-12 | 2021-05-07 | 广州白云山医药集团股份有限公司白云山何济公制药厂 | Mometasone furoate cream and preparation method thereof |
| CN112754990B (en) * | 2020-11-12 | 2023-08-29 | 广州白云山医药集团股份有限公司白云山何济公制药厂 | Mometasone furoate emulsifiable paste and preparation method thereof |
| CN113230203A (en) * | 2021-05-18 | 2021-08-10 | 广州白云山医药集团股份有限公司白云山何济公制药厂 | Mometasone furoate gel and preparation method thereof |
| CN114306180A (en) * | 2021-12-18 | 2022-04-12 | 中国人民解放军空军军医大学 | Ultraviolet sunburn repairing agent capable of being placed for long time and preparation method thereof |
| CN114306180B (en) * | 2021-12-18 | 2023-08-29 | 中国人民解放军空军军医大学 | Ultraviolet sunburn repairing agent capable of being placed for long time and preparation method thereof |
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| CN102319202B (en) | 2012-12-12 |
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