CN1222347A - Emulsion type nose spray - Google Patents
Emulsion type nose spray Download PDFInfo
- Publication number
- CN1222347A CN1222347A CN 98124406 CN98124406A CN1222347A CN 1222347 A CN1222347 A CN 1222347A CN 98124406 CN98124406 CN 98124406 CN 98124406 A CN98124406 A CN 98124406A CN 1222347 A CN1222347 A CN 1222347A
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- CN
- China
- Prior art keywords
- emulsion
- water
- nose spray
- type nose
- emulsion type
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- 239000000839 emulsion Substances 0.000 title claims abstract description 38
- 239000007921 spray Substances 0.000 title claims abstract description 18
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims abstract description 19
- 239000003270 steroid hormone Substances 0.000 claims abstract description 15
- 206010039085 Rhinitis allergic Diseases 0.000 claims abstract description 7
- 201000010105 allergic rhinitis Diseases 0.000 claims abstract description 7
- 239000002562 thickening agent Substances 0.000 claims description 9
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 claims description 7
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 claims description 7
- 229960001617 ethyl hydroxybenzoate Drugs 0.000 claims description 7
- NUVBSKCKDOMJSU-UHFFFAOYSA-N ethylparaben Chemical compound CCOC(=O)C1=CC=C(O)C=C1 NUVBSKCKDOMJSU-UHFFFAOYSA-N 0.000 claims description 7
- GYCKQBWUSACYIF-UHFFFAOYSA-N o-hydroxybenzoic acid ethyl ester Natural products CCOC(=O)C1=CC=CC=C1O GYCKQBWUSACYIF-UHFFFAOYSA-N 0.000 claims description 7
- 229940057995 liquid paraffin Drugs 0.000 claims description 6
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 6
- 229920000053 polysorbate 80 Polymers 0.000 claims description 6
- IYFATESGLOUGBX-YVNJGZBMSA-N Sorbitan monopalmitate Chemical group CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O IYFATESGLOUGBX-YVNJGZBMSA-N 0.000 claims description 5
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 5
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 5
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 5
- 239000002904 solvent Substances 0.000 claims description 5
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 4
- 229920002125 Sokalan® Polymers 0.000 claims description 4
- 229960001631 carbomer Drugs 0.000 claims description 4
- 239000002671 adjuvant Substances 0.000 claims description 3
- 239000003995 emulsifying agent Substances 0.000 claims description 3
- 239000007764 o/w emulsion Substances 0.000 claims description 3
- 239000007762 w/o emulsion Substances 0.000 claims description 3
- 210000003928 nasal cavity Anatomy 0.000 abstract description 15
- 210000001331 nose Anatomy 0.000 abstract description 8
- 230000000694 effects Effects 0.000 abstract description 5
- 239000002245 particle Substances 0.000 abstract description 4
- 239000007787 solid Substances 0.000 abstract description 4
- 239000003381 stabilizer Substances 0.000 abstract description 3
- 239000000463 material Substances 0.000 abstract 2
- 239000002260 anti-inflammatory agent Substances 0.000 abstract 1
- 230000001741 anti-phlogistic effect Effects 0.000 abstract 1
- 229960002537 betamethasone Drugs 0.000 abstract 1
- UREBDLICKHMUKA-DVTGEIKXSA-N betamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-DVTGEIKXSA-N 0.000 abstract 1
- 229940043075 fluocinolone Drugs 0.000 abstract 1
- FEBLZLNTKCEFIT-VSXGLTOVSA-N fluocinolone acetonide 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)CO)[C@@]2(C)C[C@@H]1O FEBLZLNTKCEFIT-VSXGLTOVSA-N 0.000 abstract 1
- 229940088597 hormone Drugs 0.000 abstract 1
- 239000005556 hormone Substances 0.000 abstract 1
- 230000007794 irritation Effects 0.000 abstract 1
- 239000003755 preservative agent Substances 0.000 abstract 1
- 230000002335 preservative effect Effects 0.000 abstract 1
- 229960002117 triamcinolone acetonide Drugs 0.000 abstract 1
- YNDXUCZADRHECN-JNQJZLCISA-N triamcinolone acetonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O YNDXUCZADRHECN-JNQJZLCISA-N 0.000 abstract 1
- 239000003814 drug Substances 0.000 description 13
- UFWIBTONFRDIAS-UHFFFAOYSA-N Naphthalene Chemical compound C1=CC=CC2=CC=CC=C21 UFWIBTONFRDIAS-UHFFFAOYSA-N 0.000 description 6
- 238000002360 preparation method Methods 0.000 description 6
- 239000012153 distilled water Substances 0.000 description 5
- MGNOVFAIHSOPMX-UHFFFAOYSA-N acetic acid naphthalene Chemical compound C1=CC=CC2=CC=CC=C12.C(C)(=O)O.C1=CC=CC2=CC=CC=C12 MGNOVFAIHSOPMX-UHFFFAOYSA-N 0.000 description 4
- 239000000546 pharmaceutical excipient Substances 0.000 description 4
- 238000003756 stirring Methods 0.000 description 3
- 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 description 2
- 229940124599 anti-inflammatory drug Drugs 0.000 description 2
- 230000002421 anti-septic effect Effects 0.000 description 2
- 229920003123 carboxymethyl cellulose sodium Polymers 0.000 description 2
- 229940063834 carboxymethylcellulose sodium Drugs 0.000 description 2
- 230000001886 ciliary effect Effects 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 239000002612 dispersion medium Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 229960000785 fluocinonide Drugs 0.000 description 2
- RZVAJINKPMORJF-UHFFFAOYSA-N Acetaminophen Chemical group CC(=O)NC1=CC=C(O)C=C1 RZVAJINKPMORJF-UHFFFAOYSA-N 0.000 description 1
- 101100232929 Caenorhabditis elegans pat-4 gene Proteins 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical group C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 240000007594 Oryza sativa Species 0.000 description 1
- 235000007164 Oryza sativa Nutrition 0.000 description 1
- 235000008331 Pinus X rigitaeda Nutrition 0.000 description 1
- 235000011613 Pinus brutia Nutrition 0.000 description 1
- 241000018646 Pinus brutia Species 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 239000004599 antimicrobial Substances 0.000 description 1
- 239000007900 aqueous suspension Substances 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 210000000481 breast Anatomy 0.000 description 1
- 230000008859 change Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000000084 colloidal system Substances 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 229960000935 dehydrated alcohol Drugs 0.000 description 1
- 238000002651 drug therapy Methods 0.000 description 1
- 238000010438 heat treatment Methods 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 238000012856 packing Methods 0.000 description 1
- 230000000704 physical effect Effects 0.000 description 1
- 229920000136 polysorbate Polymers 0.000 description 1
- 238000000518 rheometry Methods 0.000 description 1
- 235000009566 rice Nutrition 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 230000007480 spreading Effects 0.000 description 1
- 238000003892 spreading Methods 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000004094 surface-active agent Substances 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 230000008961 swelling Effects 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 238000005303 weighing Methods 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The nose spray emulsion is sprayed or dropped into nasal cavity to cure allergic rhinitis. It contains steriod hormone antiphlogistic, which is dissolved into liposoluble supplementary material mixing with water into emulsion, is Triamcinolone Acetonide typically to Fluocinolone and Betamethasone and accounts for 0.01-0.5% of total emulsion weight. It also contains other medicinal supplementary materials including stabilizer, preservative and densifier. The emulsion may be oil-in-water type or water-in-oil type. Because the steroid hormone is dissolved in liposoluble supplementary materials without solid particle, it has fast and long-time effect and no irritation to nasal cavity.
Description
The present invention is a kind of emulsion that contains the steroid hormone antiinflammatory drugs, and the emulsion type nose spray of nasal cavity treatment of allergic rhinitis is gone in spray (dripping) during use.
Allergic rhinitis belongs to commonly encountered diseases; the most effective medicine of this disease of treatment is exactly the steroid hormone antiinflammatory drugs at present; U.S. Pat 4; 767,612 have proposed a kind of medicine with bent peace naphthalene rule of virtue treatment allergic rhinitis, and this medicine is suspended in micronized bent peace naphthalene moral in dehydrated alcohol and the freon; be injected in the nasal cavity during use and treat; its shortcoming is to stimulate nasal cavity, does not feel like oneself, and the part patient also can be irritated sometimes.It is the song peace naphthalene moral nose agent of substrate that world patent WO98/00178 also provides water, also can reach certain therapeutical effect, because steroid hormone class medicine all is insoluble in water, to add certain suspending agent in the medicament when therefore preparing, be made into aqueous suspension, medicine also needs to make trickle solid particle, needs jolting toward contact in use, to change its physical property, the curative effect that competence exertion is certain.Two kinds of above-mentioned preparations after the solid particle medicine enters nasal cavity, can quicken the nasal cavity ciliary movement in use, are eliminated in the short time as foreign body, can not play due effect.
The object of the invention is provided for treatment of allergic rhinitis, directly acts on the medicine that contains the steroid hormone class of nasal cavity, is that a kind of drug solution is an emulsion-type, does not contain solid particle, not the emulsion type nose spray that can be eliminated from nasal cavity because of ciliary movement.
The emulsion type nose spray that the present invention adopts, the steroid hormone AID is dissolved in water and mixes in the fat-soluble adjuvant of Emulsion.
The emulsion type nose spray that the present invention adopts is that Emulsion comprises oil-in-water emulsion and water-in-oil emulsion.
The component of the emulsion type nose spray that the present invention adopts is:
Component Wt%
Steroid hormone 0.01～0.5
Solvent 20～40
Emulsifying agent 1～20
Thickening agent 0.1～1.5
Ethyl hydroxybenzoate 0.01～1
Disodiumedetate 0.01～0.5
Water adds to %
The solvent that the present invention adopts is lanoline and liquid paraffin, and thickening agent is sodium carboxymethyl cellulose or carbomer, and thickening agent is span 40 and Tween 80.
Advantage of the present invention is after making oil-in-water or water-in-oil emulsion, and steroid hormone class medicinal soluble is separated in the oiliness adjuvant, and medicament is rapid-action, long action time, can not be eliminated from nasal cavity again nasal cavity is non-stimulated, has given full play to the Drug therapy effect.
The present invention is a kind of milkiness preparation that contains the steroid hormone AID, can directly spray into or splash into the nasal cavity therapy allergic rhinitis during use.The steroid hormone class drug main that contains in the said preparation will refer to that with the bent peace of acetic acid naphthalene moral be the steroid hormone AID of some topical application of representative, can use the bent peace of acetic acid naphthalene moral, fluocinonide, its Mi Song doubly, accounts for the 0.01-0.5% of component total amount in Emulsion.Also contain some other pharmaceutic adjuvant in the Emulsion, comprising: stabilizing agent, antiseptic and thickening agent.Wherein fat-soluble pharmaceutic adjuvant comprises lanoline and liquid paraffin, is used as the solvent of steroid hormone class medicine in preparation, accounts for the 20-40% of component total amount in Emulsion; Emulsifying agent is a non-ionic surface active agent, comprises Tweens and spans, accounts for the 1-20% of component total amount in Emulsion; Stabilizing agent is a disodiumedetate, accounts for the 0.01-0.5% of component total amount in Emulsion; Antiseptic is an ethyl hydroxybenzoate, accounts for the 0.01-1% of component total amount in Emulsion.In addition, thickening agent is Sodium Tvlose or carbomer, and viscosity is the 300-800 centipoise, accounts for the 0.1-1.5% of component total amount in Emulsion.Adding thickening agent can increase the viscosity of dispersion medium, and gives this Emulsion with rheological property, purpose have two, one increases the proportion of dispersion medium, makes Emulsion be difficult for layering; Its two, when medicine sprays into nasal cavity, produce the rheology effect, viscosity increases and is difficult for flowing out, as Emulsion, the water solublity pharmaceutic adjuvant is a water, makes excipient in preparation, accounts for the 40-80% of component total amount in Emulsion.
Emulsion of the present invention (oil-in-water) component example 1:(Wt %)
The bent peace of acetic acid naphthalene moral 0.07
Lanoline 10
Liquid paraffin 15
Span 40 4
Tween 80 6
Sodium carboxymethyl cellulose 0.2
Ethyl hydroxybenzoate 0.05
Disodiumedetate 0.1
Distilled water adds to %
Emulsion component of the present invention (oil-in-water) example 2:(Wt%)
Fluocinonide 0.1
Lanoline 15
Liquid paraffin 15
Span 40 4
Tween 80 6
Carbomer 0.5
Ethyl hydroxybenzoate 0.05
Disodiumedetate 0.1
Distilled water adds to %
Emulsion component of the present invention (Water-In-Oil) example 3:(Wt%)
Its rice pine 0.1 doubly
Lanoline 15
Liquid paraffin 15
Span 40 6
Tween 80 4
Sodium carboxymethyl cellulose 0.2
Ethyl hydroxybenzoate 0.05
Disodiumedetate 0.1
Distilled water adds to %
Emulsion prepares: take by weighing the lanoline of recipe quantity, white oil, ethyl hydroxybenzoate place and burn the bosom, heating in water bath, and after treating all to melt, the bent peace of adding acetic acid naphthalene moral stirs and makes dissolving and be heated to 70-75 ℃; Measure an amount of distilled water, add disodiumedetate and make dissolving, add Tween 80, add 1% carboxymethylcellulose sodium solution of ormal weight in the stirring, mix homogeneously is heated to 70-75 ℃, and water is mixed with oil phase, constantly stir, be cooled to room temperature, grind well packing in the impouring colloid mill.
The preparation of 1% carboxymethylcellulose sodium solution: measure distilled water 1000ml, 10 gram sodium carboxymethyl cellulose spreadings on liquid level, are treated that basic swelling is until dissolving fully.
Spray into or splash into nasal cavity during use, can directly use drop bottle to splash into chamber or working pressure pump or give compression pump and inject nasal cavity.
Claims (6)
1. the present invention is a kind of emulsion type nose spray of treatment of allergic rhinitis, contains the steroid hormone AID, it is characterized in that the steroid hormone AID is dissolved in water to be mixed in the fat-soluble adjuvant of Emulsion.
2. emulsion type nose spray according to claim 1 is characterized in that Emulsion comprises oil-in-water emulsion and water-in-oil emulsion.
3. emulsion type nose spray according to claim 1 is characterized in that the component of Emulsion is:
Component Wt%
Steroid hormone 0.07～0.5
Solvent 20～40
Emulsifying agent 1～20
Thickening agent 0.1～0.5
Ethyl hydroxybenzoate 0.01～0.1
Disodiumedetate 0.01～0.5
Water adds to %
4. emulsion type nose spray according to claim 3 is characterized in that solvent is lanoline and liquid paraffin.
5. emulsion type nose spray according to claim 3 is characterized in that thickening agent is span 40 and Tween 80.
6. emulsion type nose spray according to claim 3 is characterized in that thickening agent power sodium carboxymethyl cellulose or carbomer.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 98124406 CN1222347A (en) | 1998-10-30 | 1998-10-30 | Emulsion type nose spray |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 98124406 CN1222347A (en) | 1998-10-30 | 1998-10-30 | Emulsion type nose spray |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1222347A true CN1222347A (en) | 1999-07-14 |
Family
ID=5228624
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 98124406 Pending CN1222347A (en) | 1998-10-30 | 1998-10-30 | Emulsion type nose spray |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN1222347A (en) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR3039399A1 (en) * | 2015-07-31 | 2017-02-03 | Int Drug Licensing | CREAM FOR THE ADMINISTRATION OF STEROIDS AND PROCESS FOR PREPARING THE SAME |
-
1998
- 1998-10-30 CN CN 98124406 patent/CN1222347A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| FR3039399A1 (en) * | 2015-07-31 | 2017-02-03 | Int Drug Licensing | CREAM FOR THE ADMINISTRATION OF STEROIDS AND PROCESS FOR PREPARING THE SAME |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |