HRP20140811T1 - Kompozicija brimonidin gela - Google Patents
Kompozicija brimonidin gela Download PDFInfo
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- HRP20140811T1 HRP20140811T1 HRP20140811AT HRP20140811T HRP20140811T1 HR P20140811 T1 HRP20140811 T1 HR P20140811T1 HR P20140811A T HRP20140811A T HR P20140811AT HR P20140811 T HRP20140811 T HR P20140811T HR P20140811 T1 HRP20140811 T1 HR P20140811T1
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- Croatia
- Prior art keywords
- gel composition
- topical gel
- composition according
- carbomer
- receptor agonist
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- 239000000203 mixture Substances 0.000 title claims 21
- XYLJNLCSTIOKRM-UHFFFAOYSA-N Alphagan Chemical compound C1=CC2=NC=CN=C2C(Br)=C1NC1=NCCN1 XYLJNLCSTIOKRM-UHFFFAOYSA-N 0.000 title claims 3
- 229960003679 brimonidine Drugs 0.000 title claims 3
- 229940042129 topical gel Drugs 0.000 claims 15
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims 8
- 229920002125 Sokalan® Polymers 0.000 claims 7
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims 6
- 229960001631 carbomer Drugs 0.000 claims 5
- 229920005862 polyol Polymers 0.000 claims 5
- 150000003077 polyols Chemical class 0.000 claims 5
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 claims 3
- 206010015150 Erythema Diseases 0.000 claims 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 3
- 241001303601 Rosacea Species 0.000 claims 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 3
- 239000000695 adrenergic alpha-agonist Substances 0.000 claims 3
- 150000002170 ethers Chemical class 0.000 claims 3
- KUQWZSZYIQGTHT-UHFFFAOYSA-N hexa-1,5-diene-3,4-diol Chemical compound C=CC(O)C(O)C=C KUQWZSZYIQGTHT-UHFFFAOYSA-N 0.000 claims 3
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 claims 3
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 claims 3
- 229960002216 methylparaben Drugs 0.000 claims 3
- 201000004700 rosacea Diseases 0.000 claims 3
- 208000017520 skin disease Diseases 0.000 claims 3
- 229920001059 synthetic polymer Polymers 0.000 claims 3
- IWEGDQUCWQFKHS-UHFFFAOYSA-N 1-(1,3-dioxolan-2-ylmethyl)-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazole Chemical compound O1C(C)(C)C(C)(C)OB1C1=CN(CC2OCCO2)N=C1 IWEGDQUCWQFKHS-UHFFFAOYSA-N 0.000 claims 2
- CNIIGCLFLJGOGP-UHFFFAOYSA-N 2-(1-naphthalenylmethyl)-4,5-dihydro-1H-imidazole Chemical compound C=1C=CC2=CC=CC=C2C=1CC1=NCCN1 CNIIGCLFLJGOGP-UHFFFAOYSA-N 0.000 claims 2
- QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 claims 2
- 201000004624 Dermatitis Diseases 0.000 claims 2
- 206010040954 Skin wrinkling Diseases 0.000 claims 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 claims 2
- HUCJFAOMUPXHDK-UHFFFAOYSA-N Xylometazoline Chemical compound CC1=CC(C(C)(C)C)=CC(C)=C1CC1=NCCN1 HUCJFAOMUPXHDK-UHFFFAOYSA-N 0.000 claims 2
- 229960001724 brimonidine tartrate Drugs 0.000 claims 2
- 231100000321 erythema Toxicity 0.000 claims 2
- WYWIFABBXFUGLM-UHFFFAOYSA-N oxymetazoline Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C)=C1CC1=NCCN1 WYWIFABBXFUGLM-UHFFFAOYSA-N 0.000 claims 2
- 229960005323 phenoxyethanol Drugs 0.000 claims 2
- 239000003755 preservative agent Substances 0.000 claims 2
- 230000002335 preservative effect Effects 0.000 claims 2
- BYJAVTDNIXVSPW-UHFFFAOYSA-N tetryzoline Chemical compound N1CCN=C1C1C2=CC=CC=C2CCC1 BYJAVTDNIXVSPW-UHFFFAOYSA-N 0.000 claims 2
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 claims 1
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 claims 1
- 229930182837 (R)-adrenaline Natural products 0.000 claims 1
- 208000002874 Acne Vulgaris Diseases 0.000 claims 1
- GMPKIPWJBDOURN-UHFFFAOYSA-N Methoxyamine Chemical compound CON GMPKIPWJBDOURN-UHFFFAOYSA-N 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010037549 Purpura Diseases 0.000 claims 1
- 241001672981 Purpura Species 0.000 claims 1
- 206010043189 Telangiectasia Diseases 0.000 claims 1
- 206010000496 acne Diseases 0.000 claims 1
- 239000000533 adrenergic alpha-1 receptor agonist Substances 0.000 claims 1
- 239000000384 adrenergic alpha-2 receptor agonist Substances 0.000 claims 1
- 239000007864 aqueous solution Substances 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 201000010251 cutis laxa Diseases 0.000 claims 1
- 229960005139 epinephrine Drugs 0.000 claims 1
- 229960005016 naphazoline Drugs 0.000 claims 1
- 229960002748 norepinephrine Drugs 0.000 claims 1
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 claims 1
- 229960001528 oxymetazoline Drugs 0.000 claims 1
- 229960001802 phenylephrine Drugs 0.000 claims 1
- SONNWYBIRXJNDC-VIFPVBQESA-N phenylephrine Chemical compound CNC[C@H](O)C1=CC=CC(O)=C1 SONNWYBIRXJNDC-VIFPVBQESA-N 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000008213 purified water Substances 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 208000009056 telangiectasis Diseases 0.000 claims 1
- 229960000337 tetryzoline Drugs 0.000 claims 1
- 239000004408 titanium dioxide Substances 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 230000037303 wrinkles Effects 0.000 claims 1
- 229960000833 xylometazoline Drugs 0.000 claims 1
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/215—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids
- A61K31/235—Esters, e.g. nitroglycerine, selenocyanates of carboxylic acids having an aromatic ring attached to a carboxyl group
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- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
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- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
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Claims (13)
1. Kompozicija topičkog gela, koja sadrži:
od 0,05 do 0.20% (w/w) konzervansa, metilparabena;
od 0,3 do 0,5% (w/w) sljedećeg konzervansa, fenoksietanola;
od 0,80 do 1,50% (w/w) karbomera; i
od 9,0 do 13,0% (w/w) ukupnog poliola;
pri čemu kompozicija topičkog gela ima pH od 4,5 do 7,5, i
pri čemu kada je koncentracija metilparabena veća od 0,15% (w/w), onda je koncentracija karbomera manja od 1,25% (w/w).
2. Kompozicija topičkog gela prema zahtjevu 1, pri čemu ukupni poliol sadrži oko 4,5% do 6,5% (w/w) prvog poliola.
3. Kompozicija topičkog gela prema zahtjevu 1, pri čemu kompozicija gela dalje sadrži agonist alfa adrenergijskog receptora ili njegovu farmaceutski prihvatljivu sol.
4. Kompozicija topičkog gela prema zahtjevu 3, pri čemu agonist alfa adrenergijskog receptora je agonist alfa-1 ili alfa-2 adrenergijskog receptora.
5. Kompozicija topičkog gela prema zahtjevu 4, pri čemu je agonist alfa adrenergijskog receptora izabran iz grupe koja se sastoji od oksimetazolina, fenilefrina, metoksiamina, brimonidina, tetrahidrozolina, nafazolina, ksilometazolina, epinefrina, i norepinefrina.
6. Kompozicija topičkog gela prema zahtjevu 5, pri čemu kompozicija sadrži: od 0,05 do 5% (w/w) brimonidina ili brimonidin tartrata.
7. Kompozicija topičkog gela prema zahtjevu 6, pri čemu ukupni poliol sadrži od oko 4,5% do 6,5% (w/w) prvog poliola.
8. Kompozicija topičkog gela prema zahtjevu 6, pri čemu je karbomer izabran iz grupe koja se sastoji od Carbomer® 934P (sintetički polimer akrilne kiseline umrežene sa polialkenil etrima ili divinil glikolom), Carbopol® 974P (sintetički polimer akrilne kiseline umrežen sa polialkenil etrima ili divinil glikolom), i Carbopol® 980 (sintetički polimer akrilne kiseline umrežen sa polialkenil etrima ili divinil glikolom).
9. Kompozicija topičkog gela prema zahtjevu 6, pri čemu ta kompozicija sadrži:
od 0,1 do 0,6% (w/w) brimonidin tartrata;
od 0,05 do 0,15% (w/w) metilparabena;
od 0,80 do 1,50% (w/w) karbomera;
od 4,5 do 6,5% (w/w) propilen glikola;
od 4,5 do 6,5% (w/w) glicerola; i
prečišćenu vodu;
pri čemu je pH kompozicije topičkog gela podešen na 5,0 do 6,5 adekvatnom količinom vodene otopine natrijum hidroksida.
10. Kompozicija topičkog gela prema zahtjevu 9, pri čemu ta kompozicija sadrži više od 0,3 (w/w) fenoksietanola.
11. Kompozicija topičkog gela prema zahtjevu 6 ili zahtjevu 10, koja dalje sadrži od 0,04 do 0,08% (w/w) vodorastvornog oblika titanijum dioksida.
12. Kompozicija topičkog gela prema bilo kojem od zahtjeva 5-11 za primjenu u lječenju ili prevenciji poremećaja kože kod subjekta, pri čemu se kompozicija primjenjuje topički na površini kože subjekta koji je pogođen poremećajem kože ili mu je podložan.
13. Kompozicija topičkog gela za primjenu prema zahtjevu 12, pri čemu kožni poremećaj je rozacea, eritem od rozacee, telangiektazija, psorijaza, purpura, eritem od akni, ekcem, zapaljenje kože koje nije povezano sa rozaceom, crvenilo, opuštanje kože, stvaranje nabora i/ili bora, ili simptom koji je povezan sa njima.
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US40538810P | 2010-10-21 | 2010-10-21 | |
FR1058612A FR2966366B1 (fr) | 2010-10-21 | 2010-10-21 | Composition de gel de brimonidine |
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CN104666239A (zh) * | 2013-11-27 | 2015-06-03 | 杭州赛利药物研究所有限公司 | 酒石酸溴莫尼定凝胶及其制备方法 |
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CN108126186B (zh) * | 2017-12-28 | 2021-10-29 | 未名生物医药有限公司 | 一种含神经生长因子的水凝胶及其制备方法 |
EP3927319A1 (en) * | 2019-02-20 | 2021-12-29 | AI Therapeutics, Inc. | Topical rapamycin formulations and their use in treating facial angiofibromas and other skin disorders |
CN113543773B (zh) | 2019-03-08 | 2023-07-14 | 塔罗制药工业有限公司 | 稳定的局部用非诺多泮组合物 |
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