CN101056615A - 具有稳定正ζ电势的眼用水包油型乳剂 - Google Patents
具有稳定正ζ电势的眼用水包油型乳剂 Download PDFInfo
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Abstract
Description
组分 | Z01EM042 | Z01EM043 |
CTAB(阳离子剂) | 0.05% | 0.1% |
MCT(油) | 2% | 2% |
α-生育酚(抗氧化剂) | 0.01% | 0.01% |
Lipoid E80TM(阴离子表面活性剂) | 0.32% | 0.32% |
Lutrol F68TM(非离子表面活性剂) | 0.5% | 0.5% |
甘油(张力剂) | 2.25% | 2.25% |
水 | 94.87% | 94.82% |
Z01EM042 | Z01EM043 | |
液滴大小(nm) | 126 | 128 |
ζ电势(mV) | 36.4 | 49.5 |
Z01EM042 | Z01EM043 | |||||
T(天) | 0 | 7 | 14 | 0 | 7 | 14 |
液滴大小(nm) | 126 | 143 | 155 | 128 | 140 | 151 |
ζ电势(mV) | 36.4 | 39.0 | 38.7 | 49.5 | 53.8 | 49.9 |
组分 | Z01EM042 |
BAK(阳离子剂) | 0.02% |
MCT(油) | 1% |
α-生育酚(抗氧化剂) | 0.005% |
泰洛沙泊(非离子表面活性剂) | 0.16% |
Lutrol F68(非离子表面活性剂) | 0.5% |
甘油(张力剂) | 2.25% |
水 | 96.07% |
Z01EM093 | |
ζ电势(mV) | 20.4 |
Z01EM093 | |||||||
T(天) | 0 | 2 | 5 | 7 | 9 | 12 | 14 |
ζ电势(mV) | 20.4 | 23.2 | 21.5 | 21.6 | 22.7 | 21.0 | 21.3 |
%w/w | Z01EM165 |
油胺 | 0.05 |
矿物油 | 1 |
Lutrol F68 | 0.1 |
泰洛沙泊 | 0.3 |
甘油(张力剂) | 2.25 |
水 | 至100 |
T(天) | Z01EM165 | |
液滴大小(nm) | ζ电势(mV) | |
0 | 186 | 51.3 |
3 | 184 | 47.2 |
8 | 194 | 52.1 |
13 | 163 | 48.2 |
15 | 175 | 47.9 |
%(w/w) | Z01EM092 |
CTAB | 0.005 |
MCT | 1 |
维生素E | 0.005 |
泰洛沙泊 | 0.16 |
Lutrol | 0.25 |
甘油(张力剂) | 2.25 |
水 | 至100 |
乳剂 | Z01EM092 | ||||||
T(天) | 0 | 2 | 5 | 7 | 9 | 12 | 14 |
ζ电势(mV) | 19.8 | 21.9 | 22.4 | 18.5 | 20.3 | 18.5 | 20.5 |
乳剂 | Z01EM105 | Z01EM155 | Z01EM162 | Z01EM163 |
组分 | %(w/w) | |||
BAK | 0.02 | 0.02 | 0.02 | 0.02 |
MCT | 2 | 1 | 1 | 1 |
蓖麻油 | 0 | 1 | 0 | 0 |
Cremophor | 0 | 0.25 | 0.1 | 0 |
泰洛沙泊 | 0.32 | 0 | 0.3 | 0.3 |
Montane 20 | 0 | 0 | 0 | 0.1 |
Lutrol | 0.5 | 0.1 | 0 | 0 |
Oxypol | 0 | 0.25 | 0 | 0 |
维生素E | 0.01 | 0 | 0 | 0 |
甘油 | 2.25 | 2.25 | 2.25 | 2.25 |
水 | 至100% | 至100% | 至100% | 至100% |
T(天) | Z01EM105 | Z01EM155 | Z01EM162 | Z01EM163 | |
液滴大小(nm) | 0 | nd | 288 | 243 | 249 |
7 | nd | 290 | 261 | 262 | |
14 | nd | nd | 264 | 234 | |
ζ电势(mV) | 0 | 24.9 | 19.7 | 22.3 | 18.8 |
2 | 20.7 | nd | nd | nd | |
7 | 21.3 | 14.2 | 14.7 | 16.5 | |
10 | 23.2 | nd | nd | nd | |
13 | 22.2 | nd | nd | nd | |
14 | nd | nd | 17.4 | 15.7 | |
15 | 23.2 | nd | nd | nd |
乳剂 | Z01EM170 | Z01EM171 |
组分 | %(w/w) | |
BEC | 0.02 | 0 |
BCB | 0 | 0.02 |
MCT | 2 | 2 |
泰洛沙泊 | 0.3 | 0.3 |
甘油 | 2.25 | 2.25 |
Lutrol | 0.1 | 0.1 |
水 | 至100% | 至100% |
T(天) | Z01EM170 | Z01EM171 | |
液滴大小(nm) | 0 | 210 | 239 |
7 | 232 | 250 | |
14 | 233 | nd | |
ζ电势(mV) | 0 | 23.2 | 9.1 |
7 | 22.4 | 6.4 | |
14 | 24.1 | 7.2 |
乳剂 | Z01EM151 | Z01EM152 | Z01EM153 | Z01EM164 | Z01EM173 |
组分 | %(w/w) | ||||
BAK | 0.02 | 0.02 | 0.02 | 0.02 | 0.02 |
矿物油 | 1 | 1 | 1 | 1 | 1 |
泰洛沙泊 | 0.3 | 0.3 | 0.3 | 0.3 | 0.3 |
Lutrol | 0.1 | 0.1 | 0.1 | 0.1 | 0.1 |
甘油 | 2.25 | 2.25 | 2.25 | 2.25 | 2.25 |
水 | 至100% | 至100% | 至100% | 0 | 0 |
缓冲液 | 0 | 0 | 0 | 至100% | 至100% |
T(天) | Z01EM151 | Z01EM152 | Z01EM153 | Z01EM164 | Z01EM173 | |
液滴大小(nm) | 0 | 25.8 | 26.0 | 23.4 | 16.7 | 20.7 |
3 | 22.2 | 23.0 | 26.2 | 18.3 | nd | |
5 | 23.5 | 23.8 | 24.2 | nd | nd | |
7 | nd | nd | nd | nd | 19.7 | |
8 | nd | nd | nd | 16.5 | nd | |
10 | 34.1 | 20.4 | 17.7 | nd | nd | |
12 | 23.3 | 21.7 | 23.9 | nd | nd | |
13 | nd | nd | nd | 12.7 | nd | |
14 | 23.9 | 23 | 20.3 | nd | nd | |
15 | nd | nd | nd | 13.2 | 17.8 | |
ζ电势(mV) | 0 | 174 | 220 | 185 | 209 | 200 |
3 | 178 | 215 | 184 | 200 | nd | |
5 | 170 | 213 | 182 | nd | nd | |
7 | nd | nd | nd | 213 | 200 | |
8 | nd | nd | nd | nd | nd | |
10 | 182 | 311 | 186 | nd | nd | |
12 | 176 | 221 | 224 | nd | nd | |
13 | nd | nd | nd | 218 | nd | |
14 | 168 | 216 | 188 | nd | nd | |
15 | nd | nd | nd | 203 | 216 |
乳剂 | Z06EM044 | Z06EM045 |
组成 | 0.02%BAK1.5%MCT0.24%泰洛沙泊0.01%维生素E0.375%Lutrol2.25%甘油水至100%CsA 0.1% | 0.02%BAK2%MCT0.32%泰洛沙泊0.01%维生素E0.5%Lutrol2.25%甘油水至100%CsA 0.2% |
ζ电势(mV) | T0:224T7:220T15:239 | T0:216T7:214T15:211 |
液滴大小(nm) | T0:25.3T7:22.9T15:21.8 | T0:24.8T7:22.2T15:20.8 |
乳剂 | Z06EM046 | Z06EM047 | Z06EM048 | Z06EM049 |
组成 | 0.02%BAK1%MCT0.16%泰洛沙泊0.01%维生素E2.25%甘油水至100%CsA 0.05% | 0.02%BAK0.75%MCT0.12%泰洛沙泊0.01%维生素E0.1%Lutrol2.25%甘油水至100%CsA 0.025% | 0.02%BAK2%MCT0.3%泰洛沙泊0.01%维生素E0.1%Lutrol2.25%甘油水至100%CsA 0.025% | 0.02%BAK1%MCT0.16%泰洛沙泊0.01%维生素E0.1%Lutrol2.25%甘油水至100%CsA 0.05% |
ζ电势(mV) | T0:22.7T7:20.7T15:20.7 | T0:20.9T7:18.9T15:16.9 | T0:19.6T7:19.6T15:19.4 | T0:25.0T7:24.7T15:19.2 |
液滴大小(nm) | T0:188T7:186T15:195 | T0:165T7:188T15:194 | T0:212T7:193T15:200 | T0:159T7:173T15:177 |
乳剂 | Z06EM050 | Z06EM051 | Z06EM052 | Z06EM053 |
组成 | 0.02%BAK2%MCT0.3%泰洛沙泊0.01%维生素E0.1%Lutrol2.25%甘油水至100%CsA 0.05% | 0.02%BAK2%MCT0.3%泰洛沙泊0.01%维生素E0.1%Lutrol2.25%甘油水至100%CsA0.2% | 0.02%BAK4%MCT0.3%泰洛沙泊0.01%维生素E0.1%Lutrol2.25%甘油水至100%CsA0.2% | 0.02%BAK2%MCT0.3%泰洛沙泊0.01%维生素E0.1%Lutrol2.25%甘油水至100%CsA0.1% |
ζ电势(mV) | T0:17.9T7:20.3T15:18.9 | T0:20.1T7:21.9T15:19.0 | T0:28.4T7:24.5T15:23.0 | T0:23.5T7:23.2T15:20.3 |
液滴大小(nm) | T0:224T7:212T15:221 | T0:179T7:195T15:206 | T0:176T7:201T15:195 | T0:204T7:211T15:226 |
乳剂 | Z01EM102 | Z01EM172 |
组成 | 0.05%SA1%MCT0.16%Lipoid0.005%维生素E0.25%Lutrol2.25%甘油水至100% | 0.12%SA0.01%BAK2.5%MCT0.5%Lipoid0.01%维生素E0.42%Lutrol2.25%甘油水至100% |
ζ电势(mV) | T0:60.6T2:39.1T7:10.0 | T0:55.8T7:27.8T15:4.3 |
液滴大小(nm) | T0:161T2:158T7:ND | T0:166T7:164T15:176 |
乳剂 | Z01EM186 |
组成 | 1%BAK10%豆油1.2%Lipoid2.25%甘油水至100% |
ζ电势(mV) | T0:57.5T7:55.1T15:53.9 |
液滴大小(nm) | T0:182T7:198T15:212 |
Z42EM001 | Z42EM002 | |
叶黄素 | 0.4 | 0.4 |
红花油 | 1.6 | 1.6 |
泰洛沙泊 | 0.3 | 0.3 |
Montane 20 | - | 0.1 |
BAK | 0.02 | 0.02 |
泊洛沙姆 | 0.1 | 0.1 |
甘油 | 2.25 | 2.25 |
去离子水 | qsp 100 | qsp 100 |
Z42EM001 | Z42EM002 | ||
液滴大小(nm) | T0 | 347 | 255 |
T7 | 290 | 236 | |
T14 | 285 | 321 | |
ζ电势(mV) | T0 | 15.8 | 16.0 |
T7 | 8.8 | 8.4 | |
T14 | 7.1 | 8.9 |
乳剂 | Z01EM086 | Z01EM089 |
组成 | 0.01%CTAB2%MCT0.32%Lipoid0.01%维生素E0.5%Lutrol2.25%甘油水至100% | 0.02%BAK2%MCT0.32%Lipoid0.01%维生素E0.5%Lutrol2.25%甘油水至100% |
ζ电势(mV) | T0:41.6T2:39.8T7:-15.6 | T0:33.7T7:20.4T15:-5.1 |
液滴大小(nm) | T0:155T15:167 | T0:141T15:172 |
Claims (27)
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP04292645.1 | 2004-11-09 | ||
EP04292645A EP1655021B1 (en) | 2004-11-09 | 2004-11-09 | Oil-in-water type emulsion with low concentration of cationic agent and positive zeta potential |
US10/991,346 US8298568B2 (en) | 2004-11-09 | 2004-11-18 | Oil-in-water type emulsion with low concentration of cationic agent and positive zeta potential |
US10/991,346 | 2004-11-18 | ||
PCT/EP2005/011650 WO2006050838A2 (en) | 2004-11-09 | 2005-10-10 | Ophthalmic oil-in-water type emulsion with stable positive zeta potential |
Publications (2)
Publication Number | Publication Date |
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CN101056615A true CN101056615A (zh) | 2007-10-17 |
CN101056615B CN101056615B (zh) | 2011-05-11 |
Family
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Family Applications (3)
Application Number | Title | Priority Date | Filing Date |
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CNA2005800300698A Pending CN101014317A (zh) | 2004-11-09 | 2005-10-10 | 含有免疫抑制剂的眼用乳剂 |
CN201310241506.7A Active CN103356481B (zh) | 2004-11-09 | 2005-10-10 | 含有免疫抑制剂的眼用乳剂 |
CN2005800383296A Active CN101056615B (zh) | 2004-11-09 | 2005-10-10 | 具有稳定正ζ电势的眼用水包油型乳剂 |
Family Applications Before (2)
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CNA2005800300698A Pending CN101014317A (zh) | 2004-11-09 | 2005-10-10 | 含有免疫抑制剂的眼用乳剂 |
CN201310241506.7A Active CN103356481B (zh) | 2004-11-09 | 2005-10-10 | 含有免疫抑制剂的眼用乳剂 |
Country Status (14)
Country | Link |
---|---|
US (5) | US8298568B2 (zh) |
EP (1) | EP1655021B1 (zh) |
JP (3) | JP5587936B2 (zh) |
CN (3) | CN101014317A (zh) |
AT (5) | ATE412400T1 (zh) |
DE (5) | DE602004017477D1 (zh) |
DK (1) | DK1809237T3 (zh) |
ES (4) | ES2314354T3 (zh) |
HK (2) | HK1107938A1 (zh) |
IL (3) | IL181446A (zh) |
MX (2) | MX2007005545A (zh) |
NZ (1) | NZ554929A (zh) |
PT (2) | PT1809237E (zh) |
ZA (1) | ZA200703751B (zh) |
Cited By (6)
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CN102341094A (zh) * | 2009-03-04 | 2012-02-01 | 诺瓦加利制药公司 | 含前列腺素的阳离子水包油型乳液和其用途 |
CN104546670A (zh) * | 2009-11-19 | 2015-04-29 | 参天股份公司 | 前列腺素F2α及类似物用于愈合角膜和结膜损害的用途 |
CN107249678A (zh) * | 2014-12-19 | 2017-10-13 | 凯敏工业公司 | 使用离子电渗法进行生物活性分子的眼内递送 |
CN107582605A (zh) * | 2016-07-07 | 2018-01-16 | 萨尔瓦特实验室股份有限公司 | 眼用组合物 |
CN109010268A (zh) * | 2018-09-28 | 2018-12-18 | 湖北远大天天明制药有限公司 | 一种提高氯霉素稳定性的眼用组合物及其制备方法 |
US11612658B2 (en) | 2006-07-28 | 2023-03-28 | Santen Sas | Oil-in-water emulsions comprising cetalkonium chloride and methods of making and using the same |
Families Citing this family (94)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7767216B2 (en) | 1999-04-28 | 2010-08-03 | The Regents Of The University Of Michigan | Antimicrobial compositions and methods of use |
US8232320B2 (en) | 1999-04-28 | 2012-07-31 | The Regents Of The University Of Michigan | Antimicrobial nanoemulsion compositions and methods |
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US11612658B2 (en) | 2006-07-28 | 2023-03-28 | Santen Sas | Oil-in-water emulsions comprising cetalkonium chloride and methods of making and using the same |
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CN102341094B (zh) * | 2009-03-04 | 2014-09-03 | 参天股份公司 | 含前列腺素的阳离子水包油型乳液和其用途 |
CN104546670A (zh) * | 2009-11-19 | 2015-04-29 | 参天股份公司 | 前列腺素F2α及类似物用于愈合角膜和结膜损害的用途 |
US9072750B2 (en) | 2009-11-19 | 2015-07-07 | Santen Sas | Use of prostaglandins F2Alpha and analogues for the healing of corneal and conjunctival lesions |
CN107249678A (zh) * | 2014-12-19 | 2017-10-13 | 凯敏工业公司 | 使用离子电渗法进行生物活性分子的眼内递送 |
CN107582605A (zh) * | 2016-07-07 | 2018-01-16 | 萨尔瓦特实验室股份有限公司 | 眼用组合物 |
CN109010268A (zh) * | 2018-09-28 | 2018-12-18 | 湖北远大天天明制药有限公司 | 一种提高氯霉素稳定性的眼用组合物及其制备方法 |
CN109010268B (zh) * | 2018-09-28 | 2020-07-10 | 湖北远大天天明制药有限公司 | 一种提高氯霉素稳定性的眼用组合物及其制备方法 |
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