RU2001116719A - Диспергируемые стабилизированные фосфолипидом микрочастицы - Google Patents
Диспергируемые стабилизированные фосфолипидом микрочастицыInfo
- Publication number
- RU2001116719A RU2001116719A RU2001116719/14A RU2001116719A RU2001116719A RU 2001116719 A RU2001116719 A RU 2001116719A RU 2001116719/14 A RU2001116719/14 A RU 2001116719/14A RU 2001116719 A RU2001116719 A RU 2001116719A RU 2001116719 A RU2001116719 A RU 2001116719A
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- Prior art keywords
- dosage form
- form according
- rapidly dispersible
- solid dosage
- dispersible solid
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- 150000003904 phospholipids Chemical class 0.000 title claims 3
- 239000011859 microparticle Substances 0.000 title 1
- 239000007909 solid dosage form Substances 0.000 claims 9
- 239000002245 particle Substances 0.000 claims 6
- 239000007787 solid Substances 0.000 claims 5
- 239000000126 substance Substances 0.000 claims 4
- 239000002552 dosage form Substances 0.000 claims 3
- 239000011159 matrix material Substances 0.000 claims 3
- GUBGYTABKSRVRQ-YOLKTULGSA-N Maltose Natural products O([C@@H]1[C@H](O)[C@@H](O)[C@H](O)O[C@H]1CO)[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 GUBGYTABKSRVRQ-YOLKTULGSA-N 0.000 claims 2
- 239000000654 additive Substances 0.000 claims 2
- 150000001720 carbohydrates Chemical group 0.000 claims 2
- 229920003174 cellulose-based polymer Polymers 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 150000004676 glycans Polymers 0.000 claims 2
- 239000003906 humectant Substances 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 229920005615 natural polymer Polymers 0.000 claims 2
- 229920001282 polysaccharide Polymers 0.000 claims 2
- 239000005017 polysaccharide Substances 0.000 claims 2
- 150000004804 polysaccharides Polymers 0.000 claims 2
- DNIAPMSPPWPWGF-UHFFFAOYSA-N propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 claims 2
- 229920001059 synthetic polymer Polymers 0.000 claims 2
- VUKAUDKDFVSVFT-UHFFFAOYSA-N 2-[6-[4,5-bis(2-hydroxypropoxy)-2-(2-hydroxypropoxymethyl)-6-methoxyoxan-3-yl]oxy-4,5-dimethoxy-2-(methoxymethyl)oxan-3-yl]oxy-6-(hydroxymethyl)-5-methoxyoxane-3,4-diol Chemical compound COC1C(OC)C(OC2C(C(O)C(OC)C(CO)O2)O)C(COC)OC1OC1C(COCC(C)O)OC(OC)C(OCC(C)O)C1OCC(C)O VUKAUDKDFVSVFT-UHFFFAOYSA-N 0.000 claims 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims 1
- FBPFZTCFMRRESA-KAZBKCHUSA-N D-Mannitol Natural products OC[C@@H](O)[C@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KAZBKCHUSA-N 0.000 claims 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N D-sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 1
- 229920002307 Dextran Polymers 0.000 claims 1
- 108010010803 Gelatin Proteins 0.000 claims 1
- 229940031574 HYDROXYMETHYL CELLULOSE Drugs 0.000 claims 1
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims 1
- GUBGYTABKSRVRQ-UUNJERMWSA-N Lactose Natural products O([C@@H]1[C@H](O)[C@H](O)[C@H](O)O[C@@H]1CO)[C@H]1[C@@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1 GUBGYTABKSRVRQ-UUNJERMWSA-N 0.000 claims 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 1
- XAPRFLSJBSXESP-UHFFFAOYSA-N Oxycinchophen Chemical compound N=1C2=CC=CC=C2C(C(=O)O)=C(O)C=1C1=CC=CC=C1 XAPRFLSJBSXESP-UHFFFAOYSA-N 0.000 claims 1
- 229960000502 Poloxamer Drugs 0.000 claims 1
- 239000002202 Polyethylene glycol Substances 0.000 claims 1
- 229920002472 Starch Polymers 0.000 claims 1
- CZMRCDWAGMRECN-GDQSFJPYSA-N Sucrose Natural products O([C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1)[C@@]1(CO)[C@H](O)[C@@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-GDQSFJPYSA-N 0.000 claims 1
- HDTRYLNUVZCQOY-LIZSDCNHSA-N Trehalose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-LIZSDCNHSA-N 0.000 claims 1
- HDTRYLNUVZCQOY-WSWWMNSNSA-N Trehalose Natural products O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 HDTRYLNUVZCQOY-WSWWMNSNSA-N 0.000 claims 1
- QORWJWZARLRLPR-UHFFFAOYSA-H Tricalcium phosphate Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O QORWJWZARLRLPR-UHFFFAOYSA-H 0.000 claims 1
- NIXOWILDQLNWCW-UHFFFAOYSA-M acrylate Chemical compound [O-]C(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-M 0.000 claims 1
- 230000000996 additive Effects 0.000 claims 1
- 125000000129 anionic group Chemical group 0.000 claims 1
- 239000011230 binding agent Substances 0.000 claims 1
- 125000002091 cationic group Chemical group 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 239000011248 coating agent Substances 0.000 claims 1
- 238000000576 coating method Methods 0.000 claims 1
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims 1
- 239000003086 colorant Substances 0.000 claims 1
- 239000000796 flavoring agent Substances 0.000 claims 1
- 235000013355 food flavoring agent Nutrition 0.000 claims 1
- 229920000159 gelatin Polymers 0.000 claims 1
- 239000008273 gelatin Substances 0.000 claims 1
- 235000019322 gelatine Nutrition 0.000 claims 1
- 235000011852 gelatine desserts Nutrition 0.000 claims 1
- 235000011187 glycerol Nutrition 0.000 claims 1
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerol group Chemical group OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 1
- 229920003063 hydroxymethyl cellulose Polymers 0.000 claims 1
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims 1
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 229940071676 hydroxypropylcellulose Drugs 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 1
- 239000008108 microcrystalline cellulose Substances 0.000 claims 1
- 239000003607 modifier Substances 0.000 claims 1
- 229920001983 poloxamer Polymers 0.000 claims 1
- 229920001223 polyethylene glycol Polymers 0.000 claims 1
- 229920000642 polymer Polymers 0.000 claims 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N silicium dioxide Chemical group O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 1
- 239000000600 sorbitol Substances 0.000 claims 1
- 239000008107 starch Substances 0.000 claims 1
- 235000019698 starch Nutrition 0.000 claims 1
- 239000005720 sucrose Substances 0.000 claims 1
- 239000004094 surface-active agent Substances 0.000 claims 1
- 230000001225 therapeutic Effects 0.000 claims 1
- 235000019731 tricalcium phosphate Nutrition 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Claims (10)
1. Быстро диспергируемая твердая терапевтическая дозированная форма, состоящая из нерастворимого в воде соединения, существующего в виде наномерных или микромерных твердых частиц, поверхность которых стабилизирована одним или несколькими поверхностными модификаторами, из которых, по меньшей мере, один может быть фосфолипидом, частицы твердого вещества диспергированы в создающей объем матрице, также необязательно включающей высвобождающее вещество, образующей дозированную терапевтическую форму при сушке, у которой, когда дозированную форму вводят в водную среду, образующая объем, высвобождающая матрица по существу полностью дезинтегрируется в течение менее чем 2 мин, высвобождая тем самым частицы нерастворимого в воде твердого вещества в неагрегированном и/или неагломерированном состоянии.
2. Быстро диспергируемая твердая дозированная форма по п. 1, в которой частицы нерастворимого в воде твердого компонента, состоящие по существу из композиции нерастворимого в воде вещества, включающего частицы терапевтически полезного нерастворимого в воде или плохо растворимого в воде соединения, фосфолипид и также, необязательно, по меньшей мере, одно неионное, анионное, катионное или амфипатическое поверхностно-активное вещество, в которой объемно-весовой средний размер частиц нерастворимого в воде вещества составляет 5 микрометров или менее.
3. Быстро диспергируемая твердая дозированная форма по п. 1, в которой компонент образующей объем, высвобождающей матрицы выбирается из сахаридов, полисахаридов, увлажнителей, природных или синтетических полимеров, неорганических добавок или полимеров на основе целлюлозы.
4. Быстро диспергируемая твердая дозированная форма по п. 3, в которой сахаридом или полисахаридом является маннит, трегалоза, лактоза, сахароза, сорбит или мальтоза.
5. Быстро диспергируемая твердая дозированная форма по п. 3, в которой увлажнителем является глицерин, пропиленгликоль или полиэтиленгликоль.
6. Быстро диспергируемая твердая дозированная форма по п. 3, в которой природным или синтетическим полимером является желатин, декстран, крахмал, поливинилпирролидон, полоксамер или акрилат.
7. Быстро диспергируемая твердая дозированная форма по п. 3, в которой неорганической добавкой является коллоидный диоксид кремния или трехосновной фосфат кальция.
8. Быстро диспергируемая твердая дозированная форма по п. 3, в которой полимером на основе целлюлозы является микрокристаллическая целлюлоза, гидроксиметилцеллюлоза, гидроксипропилцеллюлоза или метилцеллюлоза.
9. Быстро диспергируемая твердая дозированная форма по п. 1, для которой время дезинтеграции в водной среде составляет менее 2 мин и, предпочтительно, менее 60 с, более предпочтительно менее 30 с, и наиболее предпочтительно, менее 10 с.
10. Быстро диспергируемая твердая дозированная форма по п. 1, дополнительно содержащая шипучее средство, связывающее средство, вкусовую добавку, полимерное покрытие на наружной поверхности дозированной формы, красящее вещество или их сочетание.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US10920298P | 1998-11-20 | 1998-11-20 | |
US60/109,202 | 1998-11-20 |
Publications (2)
Publication Number | Publication Date |
---|---|
RU2001116719A true RU2001116719A (ru) | 2003-03-20 |
RU2233654C2 RU2233654C2 (ru) | 2004-08-10 |
Family
ID=22326353
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2001116719/15A RU2233654C2 (ru) | 1998-11-20 | 1999-11-19 | Диспергируемые стабилизированные фосфолипидом микрочастицы |
Country Status (24)
Country | Link |
---|---|
US (3) | US7939105B2 (ru) |
EP (1) | EP1133281A1 (ru) |
JP (2) | JP4809533B2 (ru) |
KR (1) | KR20010073232A (ru) |
CN (1) | CN1287769C (ru) |
AU (1) | AU767154B2 (ru) |
BG (1) | BG65254B1 (ru) |
BR (1) | BR9915738A (ru) |
CA (1) | CA2349203C (ru) |
CZ (1) | CZ20011739A3 (ru) |
EE (1) | EE05190B1 (ru) |
HK (1) | HK1042856B (ru) |
HU (1) | HUP0105089A3 (ru) |
ID (1) | ID29270A (ru) |
IL (2) | IL143197A0 (ru) |
IS (1) | IS5945A (ru) |
NO (1) | NO331819B1 (ru) |
NZ (1) | NZ511792A (ru) |
PL (1) | PL201578B1 (ru) |
RU (1) | RU2233654C2 (ru) |
SK (1) | SK288117B6 (ru) |
UA (1) | UA80652C2 (ru) |
WO (1) | WO2000030616A1 (ru) |
ZA (1) | ZA200104069B (ru) |
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-
1999
- 1999-11-19 SK SK685-2001A patent/SK288117B6/sk not_active IP Right Cessation
- 1999-11-19 KR KR1020017006364A patent/KR20010073232A/ko not_active Application Discontinuation
- 1999-11-19 JP JP2000583500A patent/JP4809533B2/ja not_active Expired - Fee Related
- 1999-11-19 CN CNB998156450A patent/CN1287769C/zh not_active Expired - Fee Related
- 1999-11-19 NZ NZ511792A patent/NZ511792A/en not_active IP Right Cessation
- 1999-11-19 ID IDW00200101323A patent/ID29270A/id unknown
- 1999-11-19 HU HU0105089A patent/HUP0105089A3/hu not_active Application Discontinuation
- 1999-11-19 CZ CZ20011739A patent/CZ20011739A3/cs unknown
- 1999-11-19 PL PL348868A patent/PL201578B1/pl unknown
- 1999-11-19 WO PCT/US1999/027436 patent/WO2000030616A1/en active IP Right Grant
- 1999-11-19 IL IL14319799A patent/IL143197A0/xx unknown
- 1999-11-19 BR BR9915738-1A patent/BR9915738A/pt not_active Application Discontinuation
- 1999-11-19 RU RU2001116719/15A patent/RU2233654C2/ru not_active IP Right Cessation
- 1999-11-19 EP EP99960498A patent/EP1133281A1/en not_active Withdrawn
- 1999-11-19 CA CA2349203A patent/CA2349203C/en not_active Expired - Fee Related
- 1999-11-19 US US09/443,863 patent/US7939105B2/en not_active Expired - Lifetime
- 1999-11-19 AU AU17375/00A patent/AU767154B2/en not_active Ceased
- 1999-11-19 EE EEP200100269A patent/EE05190B1/xx not_active IP Right Cessation
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2001
- 2001-05-17 IL IL143197A patent/IL143197A/en not_active IP Right Cessation
- 2001-05-18 ZA ZA200104069A patent/ZA200104069B/en unknown
- 2001-05-18 IS IS5945A patent/IS5945A/is unknown
- 2001-05-18 NO NO20012467A patent/NO331819B1/no not_active IP Right Cessation
- 2001-06-07 BG BG105573A patent/BG65254B1/bg unknown
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2002
- 2002-06-25 HK HK02104730.5A patent/HK1042856B/zh not_active IP Right Cessation
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2003
- 2003-05-23 US US10/443,772 patent/US7939106B2/en not_active Expired - Lifetime
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2006
- 2006-08-19 UA UAA200609196A patent/UA80652C2/ru unknown
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2011
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- 2011-05-10 US US13/104,094 patent/US20110244032A1/en not_active Abandoned
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