RU2013123042A - Композиции геля с бримонидином и способы применения - Google Patents
Композиции геля с бримонидином и способы применения Download PDFInfo
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- RU2013123042A RU2013123042A RU2013123042/15A RU2013123042A RU2013123042A RU 2013123042 A RU2013123042 A RU 2013123042A RU 2013123042/15 A RU2013123042/15 A RU 2013123042/15A RU 2013123042 A RU2013123042 A RU 2013123042A RU 2013123042 A RU2013123042 A RU 2013123042A
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- 239000000203 mixture Substances 0.000 title claims abstract 32
- 238000000034 method Methods 0.000 title claims 7
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims abstract 18
- 229940042129 topical gel Drugs 0.000 claims abstract 18
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims abstract 10
- 229920002125 Sokalan® Polymers 0.000 claims abstract 10
- 229960001631 carbomer Drugs 0.000 claims abstract 10
- 150000005846 sugar alcohols Polymers 0.000 claims abstract 10
- 230000000699 topical effect Effects 0.000 claims abstract 10
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 claims abstract 9
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 claims abstract 9
- 229960002216 methylparaben Drugs 0.000 claims abstract 9
- 239000000695 adrenergic alpha-agonist Substances 0.000 claims abstract 7
- 239000003755 preservative agent Substances 0.000 claims abstract 7
- 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 abstract 6
- XYLJNLCSTIOKRM-UHFFFAOYSA-N Alphagan Chemical compound C1=CC2=NC=CN=C2C(Br)=C1NC1=NCCN1 XYLJNLCSTIOKRM-UHFFFAOYSA-N 0.000 claims abstract 6
- HUCJFAOMUPXHDK-UHFFFAOYSA-N Xylometazoline Chemical compound CC1=CC(C(C)(C)C)=CC(C)=C1CC1=NCCN1 HUCJFAOMUPXHDK-UHFFFAOYSA-N 0.000 claims abstract 6
- 229960003679 brimonidine Drugs 0.000 claims abstract 6
- BYJAVTDNIXVSPW-UHFFFAOYSA-N tetryzoline Chemical compound N1CCN=C1C1C2=CC=CC=C2CCC1 BYJAVTDNIXVSPW-UHFFFAOYSA-N 0.000 claims abstract 6
- WYWIFABBXFUGLM-UHFFFAOYSA-N oxymetazoline Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C)=C1CC1=NCCN1 WYWIFABBXFUGLM-UHFFFAOYSA-N 0.000 claims abstract 5
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 claims abstract 3
- UCTWMZQNUQWSLP-VIFPVBQESA-N (R)-adrenaline Chemical compound CNC[C@H](O)C1=CC=C(O)C(O)=C1 UCTWMZQNUQWSLP-VIFPVBQESA-N 0.000 claims abstract 3
- 229930182837 (R)-adrenaline Natural products 0.000 claims abstract 3
- GMPKIPWJBDOURN-UHFFFAOYSA-N Methoxyamine Chemical compound CON GMPKIPWJBDOURN-UHFFFAOYSA-N 0.000 claims abstract 3
- 229960005139 epinephrine Drugs 0.000 claims abstract 3
- 229960005016 naphazoline Drugs 0.000 claims abstract 3
- 229960002748 norepinephrine Drugs 0.000 claims abstract 3
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 claims abstract 3
- 229960001528 oxymetazoline Drugs 0.000 claims abstract 3
- 229960001802 phenylephrine Drugs 0.000 claims abstract 3
- SONNWYBIRXJNDC-VIFPVBQESA-N phenylephrine Chemical compound CNC[C@H](O)C1=CC=CC(O)=C1 SONNWYBIRXJNDC-VIFPVBQESA-N 0.000 claims abstract 3
- 229960000337 tetryzoline Drugs 0.000 claims abstract 3
- 229960000833 xylometazoline Drugs 0.000 claims abstract 3
- 239000000533 adrenergic alpha-1 receptor agonist Substances 0.000 claims abstract 2
- 239000000384 adrenergic alpha-2 receptor agonist Substances 0.000 claims abstract 2
- 208000017520 skin disease Diseases 0.000 claims 9
- 240000005926 Hamelia patens Species 0.000 claims 8
- 201000004624 Dermatitis Diseases 0.000 claims 6
- 206010015150 Erythema Diseases 0.000 claims 6
- 231100000321 erythema Toxicity 0.000 claims 6
- 208000002874 Acne Vulgaris Diseases 0.000 claims 4
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 claims 4
- 206010000496 acne Diseases 0.000 claims 4
- QCDWFXQBSFUVSP-UHFFFAOYSA-N 2-phenoxyethanol Chemical compound OCCOC1=CC=CC=C1 QCDWFXQBSFUVSP-UHFFFAOYSA-N 0.000 claims 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 3
- 206010020565 Hyperaemia Diseases 0.000 claims 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 3
- 201000004681 Psoriasis Diseases 0.000 claims 3
- 206010037549 Purpura Diseases 0.000 claims 3
- 241001672981 Purpura Species 0.000 claims 3
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 3
- 206010043189 Telangiectasia Diseases 0.000 claims 3
- 208000010668 atopic eczema Diseases 0.000 claims 3
- 229960005323 phenoxyethanol Drugs 0.000 claims 3
- 238000007665 sagging Methods 0.000 claims 3
- 208000024891 symptom Diseases 0.000 claims 3
- 208000009056 telangiectasis Diseases 0.000 claims 3
- 230000037303 wrinkles Effects 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 group O1C(C)(C)C(C)(C)OB1C1=CN(CC2OCCO2)N=C1 IWEGDQUCWQFKHS-UHFFFAOYSA-N 0.000 claims 2
- 229960001724 brimonidine tartrate Drugs 0.000 claims 2
- SOROIESOUPGGFO-UHFFFAOYSA-N diazolidinylurea Chemical compound OCNC(=O)N(CO)C1N(CO)C(=O)N(CO)C1=O SOROIESOUPGGFO-UHFFFAOYSA-N 0.000 claims 2
- 229960001083 diazolidinylurea Drugs 0.000 claims 2
- ZCTXEAQXZGPWFG-UHFFFAOYSA-N imidurea Chemical compound O=C1NC(=O)N(CO)C1NC(=O)NCNC(=O)NC1C(=O)NC(=O)N1CO ZCTXEAQXZGPWFG-UHFFFAOYSA-N 0.000 claims 2
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 claims 2
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 claims 2
- 235000010234 sodium benzoate Nutrition 0.000 claims 2
- 239000004299 sodium benzoate Substances 0.000 claims 2
- 239000004408 titanium dioxide Substances 0.000 claims 2
- 239000007864 aqueous solution Substances 0.000 claims 1
- 230000002335 preservative effect Effects 0.000 claims 1
- 239000008213 purified water Substances 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
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Abstract
1. Композиция геля для местного применения, содержащая:от 0,05 до 0,20% (по массовой доле) метилпарабена;один или более дополнительных консервантов;от 0,80 до 1,50% (по массовой доле) карбомера;от 9,0 до 13,0% (по массовой доле) общего содержания многоатомных спиртов;где значение рН композиции геля для местного применения находится в пределах от 4,5 до 7,5, игде при концентрации метилпарабена более 0,15% (по массовой доле) концентрация карбомера составляет менее 1,25% (по массовой доле).2. Композиция геля для местного применения по п.1, где общее содержание многоатомных спиртов включает приблизительно от 4,5% до 6,5% (по массовой доле) первого многоатомного спирта.3. Композиция геля для местного применения по п.1, где композиция геля дополнительно содержит агонист альфа-адренергических рецепторов.4. Композиция геля для местного применения по п.3, где агонист альфа-адренергических рецепторов является агонистом альфа-1 или альфа-2 адренергических рецепторов.5. Композиция геля для местного применения по п.4, где агонист альфа-адренергических рецепторов выбирается из группы, включающей оксиметазолин, фенилэфрин, метоксиамин, бримонидин, тетрагидрозолин, нафазолин, ксилометазолин, эпинефрин и норэпинефрин.6. Композиция геля для местного применения, содержащая:от 0,05 до 5% (по массовой доле) бримонидина;от 0,05 до 0,20% (по массовой доле) метилпарабена;один или более дополнительных консервантов;от 0,80 до 1,50% (по массовой доле) карбомера;от 9,0 до 13,0% (по массовой доле) общего содержания многоатомных спиртов;где значение рН композиции геля для местного применения находится в пределах от 4,5 до 7,5, игде при концентрации метилпарабена более 0,15% (по массовой доле) к
Claims (20)
1. Композиция геля для местного применения, содержащая:
от 0,05 до 0,20% (по массовой доле) метилпарабена;
один или более дополнительных консервантов;
от 0,80 до 1,50% (по массовой доле) карбомера;
от 9,0 до 13,0% (по массовой доле) общего содержания многоатомных спиртов;
где значение рН композиции геля для местного применения находится в пределах от 4,5 до 7,5, и
где при концентрации метилпарабена более 0,15% (по массовой доле) концентрация карбомера составляет менее 1,25% (по массовой доле).
2. Композиция геля для местного применения по п.1, где общее содержание многоатомных спиртов включает приблизительно от 4,5% до 6,5% (по массовой доле) первого многоатомного спирта.
3. Композиция геля для местного применения по п.1, где композиция геля дополнительно содержит агонист альфа-адренергических рецепторов.
4. Композиция геля для местного применения по п.3, где агонист альфа-адренергических рецепторов является агонистом альфа-1 или альфа-2 адренергических рецепторов.
5. Композиция геля для местного применения по п.4, где агонист альфа-адренергических рецепторов выбирается из группы, включающей оксиметазолин, фенилэфрин, метоксиамин, бримонидин, тетрагидрозолин, нафазолин, ксилометазолин, эпинефрин и норэпинефрин.
6. Композиция геля для местного применения, содержащая:
от 0,05 до 5% (по массовой доле) бримонидина;
от 0,05 до 0,20% (по массовой доле) метилпарабена;
один или более дополнительных консервантов;
от 0,80 до 1,50% (по массовой доле) карбомера;
от 9,0 до 13,0% (по массовой доле) общего содержания многоатомных спиртов;
где значение рН композиции геля для местного применения находится в пределах от 4,5 до 7,5, и
где при концентрации метилпарабена более 0,15% (по массовой доле) концентрация карбомера составляет менее 1,25% (по массовой доле).
7. Композиция геля для местного применения по п.6, где общее содержание многоатомных спиртов включает приблизительно от 4,5% до 6,5% (по массовой доле) первого многоатомного спирта.
8. Композиция геля для местного применения по п.6, дополнительно содержащая от 0,04 до 0,08% (по массовой доле) водорастворимой формы диоксида титана.
9. Композиция геля для местного применения по п.6, где карбомер выбирается из группы, включающей карбомер 934Р, Карбопол®974Р или Карбопол®980.
10. Композиция геля для местного применения по п.6, где бримонидин является бримонидин тартратом.
11. Композиция геля для местного применения по п.6, где один или более дополнительных консервантов выбирается из группы, включающей бензоат натрия, феноксиэтанол, бензиловый спирт, имидазолидинилмочевину и диазолидинилмочевину.
12. Композиция геля для местного применения, содержащая:
от 0,1 до 0,6% (по массовой доле) бримонидин тартрата;
от 0,05 до 0,15% (по массовой доле) метилпарабена;
один или более дополнительных консервантов, выбранных из группы, включающей бензоат натрия, феноксиэтанол, бензиловый спирт, имидазолидинилмочевину и диазолидинилмочевину;
от 0,80 до 1,50% (по массовой доле) карбомера;
от 4,5 до 6,5% (по массовой доле) пропиленгликоля;
от 4,5 до 6,5% (по массовой доле) глицерина; и
очищенной воды;
где значение рН композиции геля для местного применения доводится до 5-6,5 достаточным количеством водного раствора гидроксида натрия.
13. Композиция геля для местного применения по п.12, содержащая более 0,3 (по массовой доле) феноксиэтанола в качестве дополнительного консерванта.
14. Композиция геля для местного применения по п.13, дополнительно содержащая от 0,04 до 0,08% (по массовой доле) водорастворимой формы диоксида титана.
15. Способ лечения или предотвращения заболевания кожи у пациента, включающий местное нанесение на участок кожи пациента композиции геля для местного применения по п.6, где участок кожи подвержен или склонен к заболеванию кожи.
16. Способ по п.15, где заболевание кожи представляет собой красные угри, эритему, вызванную красными угрями, телеангиэктазию, псориаз, пурпуру, эритему угревой сыпи, экзему, не ассоциированное с красными угрями воспаление кожи, гиперемию, обвисание кожи, образование складок и/или морщин, или связанный с ним симптом.
17. Способ лечения или предотвращения заболевания кожи у пациента, включающий местное нанесение на участок кожи пациента композиции геля для местного применения по п.12, где участок кожи подвержен или склонен к заболеванию кожи.
18. Способ по п.17, где заболевание кожи представляет собой красные угри, эритему, вызванную красными угрями, телеангиэктазию, псориаз, пурпуру, эритему угревой сыпи, экзему, не ассоциированное с красными угрями воспаление кожи, гиперемию, обвисание кожи, образование складок и/или морщин, или связанный с ним симптом.
19. Способ лечения или предотвращения заболевания кожи у пациента, включающий местное нанесение на участок кожи пациента композиции геля для местного применения по п.1, где композиция геля дополнительно содержит агонист альфа-адренергических рецепторов, выбранный из группы, включающей оксиметазолин, фенилэфрин, метоксиамин, бримонидин, тетрагидрозолин, нафазолин, ксилометазолин, эпинефрин и норэпинефрин, и где участок кожи подвержен или склонен к заболеванию кожи.
20. Способ по п.19, где заболевание кожи представляет собой красные угри, эритему, вызванную красными угрями, телеангиэктазию, псориаз, пурпуру, эритему угревой сыпи, экзему, не ассоциированное с красными угрями воспаление кожи, гиперемию, обвисание кожи, образование складок и/или морщин, или связанный с ним симптом.
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