CN106562980A - Compound fluocinonide tincture composition as well as preparation method and application thereof - Google Patents
Compound fluocinonide tincture composition as well as preparation method and application thereof Download PDFInfo
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- CN106562980A CN106562980A CN201610925705.3A CN201610925705A CN106562980A CN 106562980 A CN106562980 A CN 106562980A CN 201610925705 A CN201610925705 A CN 201610925705A CN 106562980 A CN106562980 A CN 106562980A
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- compound
- tincture composition
- potassium
- fluocinonide tincture
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- WJOHZNCJWYWUJD-IUGZLZTKSA-N Fluocinonide Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)COC(=O)C)[C@@]2(C)C[C@@H]1O WJOHZNCJWYWUJD-IUGZLZTKSA-N 0.000 title claims abstract description 72
- 229960000785 fluocinonide Drugs 0.000 title claims abstract description 71
- 229940098465 tincture Drugs 0.000 title claims abstract description 63
- 150000001875 compounds Chemical class 0.000 title claims abstract description 60
- 239000000203 mixture Substances 0.000 title claims abstract description 47
- 238000002360 preparation method Methods 0.000 title claims abstract description 29
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 claims abstract description 26
- GHMLBKRAJCXXBS-UHFFFAOYSA-N resorcinol Chemical compound OC1=CC=CC(O)=C1 GHMLBKRAJCXXBS-UHFFFAOYSA-N 0.000 claims abstract description 18
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims abstract description 15
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims abstract description 14
- 239000002253 acid Substances 0.000 claims abstract description 14
- 239000003513 alkali Substances 0.000 claims abstract description 14
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 claims abstract description 14
- 150000003839 salts Chemical class 0.000 claims abstract description 13
- DTGKSKDOIYIVQL-WEDXCCLWSA-N (+)-borneol Chemical compound C1C[C@@]2(C)[C@@H](O)C[C@@H]1C2(C)C DTGKSKDOIYIVQL-WEDXCCLWSA-N 0.000 claims abstract description 8
- REPVLJRCJUVQFA-UHFFFAOYSA-N (-)-isopinocampheol Natural products C1C(O)C(C)C2C(C)(C)C1C2 REPVLJRCJUVQFA-UHFFFAOYSA-N 0.000 claims abstract description 8
- 229940116229 borneol Drugs 0.000 claims abstract description 8
- CKDOCTFBFTVPSN-UHFFFAOYSA-N borneol Natural products C1CC2(C)C(C)CC1C2(C)C CKDOCTFBFTVPSN-UHFFFAOYSA-N 0.000 claims abstract description 8
- DTGKSKDOIYIVQL-UHFFFAOYSA-N dl-isoborneol Natural products C1CC2(C)C(O)CC1C2(C)C DTGKSKDOIYIVQL-UHFFFAOYSA-N 0.000 claims abstract description 8
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 claims abstract description 7
- 229960004889 salicylic acid Drugs 0.000 claims abstract description 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 7
- 239000008213 purified water Substances 0.000 claims abstract description 6
- KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims description 21
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims description 21
- 238000003756 stirring Methods 0.000 claims description 16
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 14
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 14
- SCVFZCLFOSHCOH-UHFFFAOYSA-M potassium acetate Chemical compound [K+].CC([O-])=O SCVFZCLFOSHCOH-UHFFFAOYSA-M 0.000 claims description 14
- BWHMMNNQKKPAPP-UHFFFAOYSA-L potassium carbonate Chemical compound [K+].[K+].[O-]C([O-])=O BWHMMNNQKKPAPP-UHFFFAOYSA-L 0.000 claims description 14
- LWIHDJKSTIGBAC-UHFFFAOYSA-K tripotassium phosphate Chemical compound [K+].[K+].[K+].[O-]P([O-])([O-])=O LWIHDJKSTIGBAC-UHFFFAOYSA-K 0.000 claims description 14
- VMHLLURERBWHNL-UHFFFAOYSA-M Sodium acetate Chemical compound [Na+].CC([O-])=O VMHLLURERBWHNL-UHFFFAOYSA-M 0.000 claims description 9
- 229940040526 anhydrous sodium acetate Drugs 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 9
- 238000010992 reflux Methods 0.000 claims description 8
- 229960001755 resorcinol Drugs 0.000 claims description 8
- RQPZNWPYLFFXCP-UHFFFAOYSA-L barium dihydroxide Chemical compound [OH-].[OH-].[Ba+2] RQPZNWPYLFFXCP-UHFFFAOYSA-L 0.000 claims description 7
- 229910001863 barium hydroxide Inorganic materials 0.000 claims description 7
- 238000000034 method Methods 0.000 claims description 7
- 235000011056 potassium acetate Nutrition 0.000 claims description 7
- 229910000027 potassium carbonate Inorganic materials 0.000 claims description 7
- 235000011181 potassium carbonates Nutrition 0.000 claims description 7
- 229910000160 potassium phosphate Inorganic materials 0.000 claims description 7
- 235000011009 potassium phosphates Nutrition 0.000 claims description 7
- 229910000029 sodium carbonate Inorganic materials 0.000 claims description 7
- 239000001488 sodium phosphate Substances 0.000 claims description 7
- 229910000162 sodium phosphate Inorganic materials 0.000 claims description 7
- 235000011008 sodium phosphates Nutrition 0.000 claims description 7
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 claims description 7
- 206010061218 Inflammation Diseases 0.000 claims description 6
- 229960005150 glycerol Drugs 0.000 claims description 6
- 235000011187 glycerol Nutrition 0.000 claims description 6
- 230000004054 inflammatory process Effects 0.000 claims description 6
- 239000002994 raw material Substances 0.000 claims description 6
- 238000006243 chemical reaction Methods 0.000 claims description 5
- 201000004624 Dermatitis Diseases 0.000 claims description 4
- 208000003251 Pruritus Diseases 0.000 claims description 4
- 206010012438 Dermatitis atopic Diseases 0.000 claims description 3
- 201000004681 Psoriasis Diseases 0.000 claims description 3
- 206010039792 Seborrhoea Diseases 0.000 claims description 3
- 201000008937 atopic dermatitis Diseases 0.000 claims description 3
- 208000010668 atopic eczema Diseases 0.000 claims description 3
- 201000010099 disease Diseases 0.000 claims description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 3
- 208000015181 infectious disease Diseases 0.000 claims description 3
- 230000002458 infectious effect Effects 0.000 claims description 3
- 238000002156 mixing Methods 0.000 claims description 3
- 230000008569 process Effects 0.000 claims description 3
- 208000008742 seborrheic dermatitis Diseases 0.000 claims description 3
- 208000017520 skin disease Diseases 0.000 claims description 3
- 206010012442 Dermatitis contact Diseases 0.000 claims description 2
- XNPAKGMQCVYQAO-UHFFFAOYSA-N [F].CC(O)=O Chemical compound [F].CC(O)=O XNPAKGMQCVYQAO-UHFFFAOYSA-N 0.000 claims description 2
- 208000010247 contact dermatitis Diseases 0.000 claims description 2
- 230000001823 pruritic effect Effects 0.000 claims description 2
- 210000005036 nerve Anatomy 0.000 claims 1
- 239000000243 solution Substances 0.000 description 16
- 239000002585 base Substances 0.000 description 4
- 239000000523 sample Substances 0.000 description 4
- -1 1- methyl ethylidene Chemical group 0.000 description 3
- 201000009053 Neurodermatitis Diseases 0.000 description 3
- 238000001514 detection method Methods 0.000 description 3
- 229940079593 drug Drugs 0.000 description 3
- 239000002075 main ingredient Substances 0.000 description 3
- 238000012360 testing method Methods 0.000 description 3
- CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- 230000001133 acceleration Effects 0.000 description 2
- 239000002131 composite material Substances 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 239000007788 liquid Substances 0.000 description 2
- WWYNJERNGUHSAO-XUDSTZEESA-N (+)-Norgestrel Chemical compound O=C1CC[C@@H]2[C@H]3CC[C@](CC)([C@](CC4)(O)C#C)[C@@H]4[C@@H]3CCC2=C1 WWYNJERNGUHSAO-XUDSTZEESA-N 0.000 description 1
- ZZZCUOFIHGPKAK-UHFFFAOYSA-N D-erythro-ascorbic acid Natural products OCC1OC(=O)C(O)=C1O ZZZCUOFIHGPKAK-UHFFFAOYSA-N 0.000 description 1
- 102000011782 Keratins Human genes 0.000 description 1
- 108010076876 Keratins Proteins 0.000 description 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 description 1
- 206010030113 Oedema Diseases 0.000 description 1
- 240000007594 Oryza sativa Species 0.000 description 1
- 235000007164 Oryza sativa Nutrition 0.000 description 1
- 241000219000 Populus Species 0.000 description 1
- BQCADISMDOOEFD-UHFFFAOYSA-N Silver Chemical compound [Ag] BQCADISMDOOEFD-UHFFFAOYSA-N 0.000 description 1
- DWAQJAXMDSEUJJ-UHFFFAOYSA-M Sodium bisulfite Chemical compound [Na+].OS([O-])=O DWAQJAXMDSEUJJ-UHFFFAOYSA-M 0.000 description 1
- 229930003268 Vitamin C Natural products 0.000 description 1
- 230000003266 anti-allergic effect Effects 0.000 description 1
- 230000000844 anti-bacterial effect Effects 0.000 description 1
- 230000003110 anti-inflammatory effect Effects 0.000 description 1
- 239000003963 antioxidant agent Substances 0.000 description 1
- 230000003078 antioxidant effect Effects 0.000 description 1
- 235000006708 antioxidants Nutrition 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 238000010009 beating Methods 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 230000000052 comparative effect Effects 0.000 description 1
- 239000013068 control sample Substances 0.000 description 1
- 238000003113 dilution method Methods 0.000 description 1
- 229960001760 dimethyl sulfoxide Drugs 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 235000013399 edible fruits Nutrition 0.000 description 1
- 239000012467 final product Substances 0.000 description 1
- 238000009472 formulation Methods 0.000 description 1
- 230000000855 fungicidal effect Effects 0.000 description 1
- 239000003862 glucocorticoid Substances 0.000 description 1
- 230000007062 hydrolysis Effects 0.000 description 1
- 238000006460 hydrolysis reaction Methods 0.000 description 1
- 238000002386 leaching Methods 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 230000003647 oxidation Effects 0.000 description 1
- 238000007254 oxidation reaction Methods 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 229920000915 polyvinyl chloride Polymers 0.000 description 1
- 239000004800 polyvinyl chloride Substances 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 235000009566 rice Nutrition 0.000 description 1
- 229910052709 silver Inorganic materials 0.000 description 1
- 239000004332 silver Substances 0.000 description 1
- JVBXVOWTABLYPX-UHFFFAOYSA-L sodium dithionite Chemical compound [Na+].[Na+].[O-]S(=O)S([O-])=O JVBXVOWTABLYPX-UHFFFAOYSA-L 0.000 description 1
- 229940079827 sodium hydrogen sulfite Drugs 0.000 description 1
- 235000010267 sodium hydrogen sulphite Nutrition 0.000 description 1
- AKHNMLFCWUSKQB-UHFFFAOYSA-L sodium thiosulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=S AKHNMLFCWUSKQB-UHFFFAOYSA-L 0.000 description 1
- 235000019345 sodium thiosulphate Nutrition 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 239000000126 substance Substances 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000000052 vinegar Substances 0.000 description 1
- 235000021419 vinegar Nutrition 0.000 description 1
- 239000011718 vitamin C Substances 0.000 description 1
- 235000019154 vitamin C Nutrition 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/60—Salicylic acid; Derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/045—Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/58—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0014—Skin, i.e. galenical aspects of topical compositions
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Inorganic Chemistry (AREA)
- Dermatology (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The invention discloses a compound fluocinonide tincture composition, which consists of the following components in percentage by weight: 0.02-0.08% of fluocinonide tincture, 3.0-10.0% of salicylic acid, 5.0-15.0% of resorcinol, 1.0-5.0% of borneol, 1.0-3.0% of dimethyl sulfoxide, 3.0-10.0% of glycerol, 60-80% of ethanol, 1.0-10.0% of purified water and 0.5-3.0% of alkali or strong alkali and weak acid salt. The invention also discloses a preparation method and an application of the composition. The compound fluocinonide tincture composition provided by the invention is significant higher in stability in comparison with the prior art.
Description
Technical field
The application is a kind of medicine, belongs to field of pharmaceutical technology, and specifically, the application is related to a kind of compound fluocinonide
Tincture composition, Preparation Method And The Use.
Background technology
Fluocinonide, chemical name：The α of 11 beta-hydroxy -16,17- [(1- methyl ethylidene)-bis- (oxygen)] -21- (acetyl
Epoxide) -6,9-, bis- pregna-fluorides-Isosorbide-5-Nitrae-diene -3,20- diketone, its general external application is suitable for the effective skin of glucocorticoid
Disease, such as contact dermatitis, atopic dermatitis, seborrhea, eczema, cutaneous pruritus, psoriasis, neurodermatitis itch
Property and non-infectious inflammation dermatoses.
At present, both at home and abroad Fluocinonide is prepared into into various exterior-applied formulations, such as Fluonex, Fluocinonide
Ointment and compound fluocinonide tincture etc., especially compound fluocinonide tincture are PIYANNING DING, for neurodermatitis, to silver
Bits disease also has certain curative effect, deep to be approved by consumers in general.The component of compound fluocinonide tincture includes Fluocinonide, water
Poplar acid, borneol, resorcinol, glycerine and dimethyl sulfoxide (DMSO).Fluocinonide contained therein has stronger antiinflammatory action, can make
The vessel retraction of inflammation part, reduces the permeability of capillary, and the early stage for reducing inflammation oozes out, congested, oedema and cell leaching
Profit, alleviates the symptoms such as red and swollen heat pain, and has anti-allergic effects.Salicylic acid has dissolving skin keratin, fungicidal action.Borneol office
Portion is wiped after using pain relieving, antibacterial action.
In prior art, tincture is typically prepared with dissolution method or dilution method, and the ethanol of drug powder plus normal concentration is fitted
Amount dissolving dilutes, and stands, and obtains final product.But the compound fluocinonide tincture prepared with this preparation method, place a period of time
Afterwards it finds that preparation is highly unstable, main ingredient Fluocinonide content is substantially reduced in preparation, and is darkened.From compound vinegar
The holding conditions of sour FA tincture find that main ingredient is medicine more sensitive to temperature investigating, can only in the cool (temperature does not surpass
Cross 20 degree) preserve.Therefore, there is a kind of viewpoint to think at present, cause predominant amount to be compound fluocinonide tincture the reason for reduction
Middle resorcinol oxidation and the result decomposed.Therefore, occur in that and add antioxidant in formula (such as vitamin C, hydrochloric acid half
Cystine, sodium dithionite, sodium thiosulfate and sodium hydrogensulfite etc.) method carry out stability test, as a result show master
The content of medicine still can be reduced.
In addition, moisture is substantially free of in compound fluocinonide tincture made in prior art, therefore main ingredient therein
The hydrolysis degree of Fluocinonide is greatly reduced, though can efficiently solve that drug content in compound fluocinonide tincture declines asks
Topic.However, because prepared compound fluocinonide tincture is substantially free of moisture, therefore patient light using compound acetic acid fluorine
During loose tincture, can feel too dry so as to feel ill.
Therefore, in order to overcome prior art in the presence of compound fluocinonide tincture storage it is unstable, under drug content
Drop is very fast, the problem that drug effect is reduced and preparation method is complicated, and spy proposes this application.
The content of the invention
According to the one side of the application, there is provided a kind of compound fluocinonide tincture composition.
To achieve these goals, the application is adopted the following technical scheme that：
A kind of compound fluocinonide tincture composition, it is characterised in that the compound fluocinonide tincture composition includes
Following component：
Wherein described alkali includes one or more in NaOH, potassium hydroxide and barium hydroxide；The strong acid weak base
Salt includes the one kind in anhydrous sodium acetate, sodium carbonate, sodium acid carbonate, potassium phosphate, sodium phosphate, potassium acetate, potassium carbonate, saleratus
Or it is several.
Preferably, the compound fluocinonide tincture composition includes following component：
Wherein described alkali includes one or more in NaOH, potassium hydroxide and barium hydroxide；The strong base weak acid
Salt includes the one kind in anhydrous sodium acetate, sodium carbonate, sodium acid carbonate, potassium phosphate, sodium phosphate, potassium acetate, potassium carbonate, saleratus
Or it is several.
Preferably, the compound fluocinonide tincture composition includes following component：
Wherein described alkali includes one or more in NaOH, potassium hydroxide and barium hydroxide；The strong base weak acid
Salt includes the one kind in anhydrous sodium acetate, sodium carbonate, sodium acid carbonate, potassium phosphate, sodium phosphate, potassium acetate, potassium carbonate, saleratus
Or it is several.
According to the another aspect of the application, there is provided a kind of preparation method of compound fluocinonide tincture composition.
To achieve these goals, the application is adopted the following technical scheme that：
A kind of preparation method of compound fluocinonide tincture composition, it is characterised in that the preparation method includes as follows
Step：
(1) raw material for standby is weighed according to formula；
(2) by the ethanol of formula ratio, glycerine, salicylic acid, borneol and resorcinol, sequentially add in reaction pot, stir, treat
Solution I is obtained after being completely dissolved；
(3) Fluocinonide of formula ratio is added into dimethyl sulfoxide (DMSO), after stirring and dissolving, is added into solution I, after
Purified water is added after continuous stirring, solution II is obtained；
(4) alkali or strong base-weak acid salt are added, adjusts the pH value of solution II to 4.5～6, be stirred for making to be well mixed obtaining
Described compound fluocinonide tincture composition.
Preferably, in step (2), while stirring, also including the process of backflow.
Preferably, in step (2), time of backflow is 1-3 hours, preferably 2 hours.
Preferably, in step (3), while continuing to stir, flowed back, the time of backflow is 20-60 minutes, preferably
30 minutes.
Preferably, in step (4), after adjusting pH value, it is further continued for being stirred at reflux, the time being stirred at reflux is 2-5 hours, excellent
Select 3 hours.
According to the another aspect of the application, there is provided a kind of purposes of compound fluocinonide tincture composition.
To achieve these goals, the application is adopted the following technical scheme that：
Compound fluocinonide tincture composition described herein and according to beating prepared by the preparation method of the application
Compound fluocinonide tincture composition is preparing treatment pruritic and non-infectious inflammation dermatoses, particularly contact skin
The purposes of the medicine in terms of inflammation, atopic dermatitis, seborrhea, eczema, cutaneous pruritus, psoriasis, neurodermatitis.
The beneficial effect that the application can be produced includes：
1) compound fluocinonide tincture composition provided herein, stability has obtained significantly carrying compared with prior art
It is high.It is demonstrated experimentally that in the compound fluocinonide tincture composite formula of prior art, add percentage by weight be 0.5%～
3.0% alkali or strong base-weak acid salt, have adjusted the pH value of the mixture to 4.5-6, and its stability is significantly improved, and studies carefully it
Reason is probably that resorcinol is not oxidizable under the conditions of the pH value range in compound fluocinonide tincture and decomposes.
2) preparation method of compound fluocinonide tincture composition provided herein, process is simple is easy to control, is suitable to
Commercial Application.Due in preparation process, adding alkali or strong base-weak acid salt to be adjusted pH value to 4.5-6, can cause made
Standby compound fluocinonide tincture composition improves compared with the prior art the stability of said composition, guarantees the quality so as to extend
Phase.
Specific embodiment
With reference to embodiment in detail the application is described in detail, but the application is not limited to these embodiments.
If no special instructions, the raw material in embodiments herein is bought by commercial sources.
According to a kind of embodiment of the application, a kind of compound fluocinonide tincture composition, including following component：
Wherein described alkali includes one or more in NaOH, potassium hydroxide and barium hydroxide；The strong base weak acid
Salt includes the one kind in anhydrous sodium acetate, sodium carbonate, sodium acid carbonate, potassium phosphate, sodium phosphate, potassium acetate, potassium carbonate, saleratus
Or it is several.
A kind of preparation method of compound fluocinonide tincture composition, it is characterised in that methods described comprises the steps：
(1) raw material for standby is weighed according to formula；
(2) by the ethanol of formula ratio, glycerine, salicylic acid, borneol and resorcinol, sequentially add in reaction pot, stir, treat
Solution I is obtained after being completely dissolved；
(3) Fluocinonide of formula ratio is added into dimethyl sulfoxide (DMSO), after stirring and dissolving, is added into solution I, after
Purified water is added after continuous stirring, solution II is obtained；
(4) alkali or strong base-weak acid salt are added, adjusts the pH value of solution II to 4.5～6, be stirred for making to be well mixed obtaining
Described compound fluocinonide tincture composition.
Embodiment 1
The present embodiment is related to compound fluocinonide tincture composite formula.
Table 1
Embodiment 2
The present embodiment is related to a kind of preparation method of compound fluocinonide tincture composition.
A kind of preparation method of compound fluocinonide tincture composition, it is characterised in that methods described comprises the steps：
(1) raw material for standby is weighed according to formula 1；
(2) by the ethanol of formula ratio, glycerine, salicylic acid, borneol and resorcinol, sequentially add in reaction pot, stir back
Stream 3 hours, obtains until completely dissolved solution I；
(3) Fluocinonide of formula ratio is added into dimethyl sulfoxide (DMSO), after stirring and dissolving, is added into solution I, after
Continue and add purified water after being stirred at reflux 60 minutes, obtain solution II；
(4) anhydrous sodium acetate is added, adjusts the pH value of solution II to 4.5～5.5, be stirred at reflux 5 hours, make mixing equal
It is even to obtain described compound fluocinonide tincture composition.
The nature examination result of prepared compound fluocinonide tincture composition is as shown in table 2 below：
Table 2
| Detection project | Testing result | Check conclusion |
| Proterties | Light brown red clear liquid | Meet regulation |
| pH | 5.0 | Meet regulation |
| Content | 98.9% | Meet regulation |
Embodiment 3
The present embodiment is related to a kind of preparation method of compound fluocinonide tincture composition.
A kind of preparation method of compound fluocinonide tincture composition, it is characterised in that methods described comprises the steps：
(1) raw material for standby is weighed according to formula 2；
(2) by the ethanol of formula ratio, glycerine, salicylic acid, borneol and resorcinol, sequentially add in reaction pot, stir back
Stream 2 hours, obtains until completely dissolved solution I；
(3) Fluocinonide of formula ratio is added into dimethyl sulfoxide (DMSO), after stirring and dissolving, is added into solution I, after
Continue and add purified water after being stirred at reflux 30 minutes, obtain solution II；
(4) anhydrous sodium acetate is added, adjusts the pH value of solution II to 5～6, be further continued for being stirred at reflux 3 hours, make mixing equal
It is even to obtain described compound fluocinonide tincture composition.
The nature examination result of prepared compound fluocinonide tincture composition is as shown in table 3 below：
Table 3
| Detection project | Testing result | Check conclusion |
| Proterties | Light brown red clear liquid | Meet regulation |
| PH | 5.5 | Meet regulation |
| Content | 99.8% | Meet regulation |
Comparative example 1
It is difficult to understand with Zhejiang after being packed using polyvinyl chloride medicine bottle according to the sample that the preparation method in embodiment 2 is prepared
Auspicious special compound fluocinonide tincture sample contrast, in 40 DEG C ± 2 DEG C of temperature, 75% ± 5%RH of humidity accelerated test 2 is carried out
Month, the every quality index of detection compared with 0 month, had no significant change, and met the pertinent regulations in quality standard.Main knot
Fruit is shown in Table 4 and table 5：
The self-control sample of table 4 is positioned over the acceleration environment stability data of lower 2 months：
The Zhejiang Ovrette compound fluocinonide tincture sample acceleration environment stability data of lower 2 months of table 5：
The compound fluocinonide tincture and wash rice river Ovrette compound of the present invention are can be seen that from the experimental result of table 4 and table 5
Fluocinonide tincture sample folk prescription is comparatively, relevant material raises slower, and quality is more stable.
The above, is only several embodiments of the application, any type of restriction is not done to the application, although this Shen
Please disclosed as above with preferred embodiment, but and be not used to limit the application, any those skilled in the art are not taking off
In the range of technical scheme, make a little variation using the technology contents of the disclosure above or modification is equal to
Effect case study on implementation, belongs in the range of technical scheme.
Claims (10)
1. a kind of compound fluocinonide tincture composition, it is characterised in that the compound fluocinonide tincture composition include as
The component of lower weight percentage：
Wherein described alkali includes one or more in NaOH, potassium hydroxide and barium hydroxide；The strong base-weak acid salt bag
Include the one kind or several in anhydrous sodium acetate, sodium carbonate, sodium acid carbonate, potassium phosphate, sodium phosphate, potassium acetate, potassium carbonate, saleratus
Kind.
2. compound fluocinonide tincture composition according to claim 1, it is characterised in that the compound fluocinonide
Tincture composition includes the component of following weight percentage：
Wherein described alkali includes one or more in NaOH, potassium hydroxide and barium hydroxide；The strong base-weak acid salt bag
Include the one kind or several in anhydrous sodium acetate, sodium carbonate, sodium acid carbonate, potassium phosphate, sodium phosphate, potassium acetate, potassium carbonate, saleratus
Kind.
3. compound fluocinonide tincture composition according to claim 1 and 2, it is characterised in that the compound acetic acid fluorine
Easily tincture composition includes the component of following weight percentage：
Wherein described alkali includes one or more in NaOH, potassium hydroxide and barium hydroxide；The strong base-weak acid salt bag
Include the one kind or several in anhydrous sodium acetate, sodium carbonate, sodium acid carbonate, potassium phosphate, sodium phosphate, potassium acetate, potassium carbonate, saleratus
Kind.
4. a kind of preparation method of the compound fluocinonide tincture composition as described in any one in claim 1-3, it is special
Levy and be, the preparation method comprises the steps：
(1) raw material for standby is weighed according to formula；
(2) by the ethanol of formula ratio, glycerine, salicylic acid, borneol and resorcinol, sequentially add in reaction pot, stir, treat completely
Solution I is obtained after dissolving；
(3) Fluocinonide of formula ratio is added into dimethyl sulfoxide (DMSO), after stirring and dissolving, is added into solution I, continue to stir
Purified water is added after mixing, solution II is obtained；
(4) alkali or strong base-weak acid salt are added, adjust the pH value of solution II to 4.5～6, be stirred for making to be well mixed obtain it is described
Compound fluocinonide tincture composition.
5. the preparation method of compound fluocinonide tincture composition according to claim 4, it is characterised in that step (2)
In, while stirring, also including the process of backflow.
6. the preparation method of the compound fluocinonide tincture composition according to claim 4 or 5, it is characterised in that step
(2) in, the time of the backflow is 1-3 hours.
7. the preparation method of the compound fluocinonide tincture composition according to any one in claim 4-6, its feature
It is that in step (2), the time of the backflow is 2 hours.
8. the preparation method according to any one in claim 4-7, it is characterised in that in step (3), continues what is stirred
Meanwhile, flowed back；The time of backflow be 20-60 minutes, preferably 30 minutes.
9. the preparation method according to any one in claim 4-8, it is characterised in that in step (4), adjusts pH value
Afterwards, be further continued for being stirred at reflux, the time being stirred at reflux be 2-5 hours, preferably 3 hours.
10. compound fluocinonide tincture composition described in claim 1-3 any one and appoint according in claim 4-9
Compound fluocinonide tincture composition prepared by the preparation method described in meaning one treats pruritic and non-infectious inflammation in preparation
Disease dermatoses, particularly contact dermatitis, atopic dermatitis, seborrhea, eczema, cutaneous pruritus, psoriasis, nerve
The purposes in medicine in terms of property dermatitis.
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| CN112022805A (en) * | 2020-10-20 | 2020-12-04 | 内蒙古盛唐国际蒙医药研究院有限公司 | High-stability compound fluocinonide tincture and preparation method thereof |
| CN116807983A (en) * | 2023-05-15 | 2023-09-29 | 浏阳津兰药业有限公司 | Preparation method of a highly stable composition containing fluocinonide acetate |
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Application publication date: 20170419 |