RU2004127867A - Состав с высвобождением в толстом кишечнике - Google Patents
Состав с высвобождением в толстом кишечнике Download PDFInfo
- Publication number
- RU2004127867A RU2004127867A RU2004127867/15A RU2004127867A RU2004127867A RU 2004127867 A RU2004127867 A RU 2004127867A RU 2004127867/15 A RU2004127867/15 A RU 2004127867/15A RU 2004127867 A RU2004127867 A RU 2004127867A RU 2004127867 A RU2004127867 A RU 2004127867A
- Authority
- RU
- Russia
- Prior art keywords
- composition according
- amylose
- ethyl cellulose
- coating
- sebacate
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims 14
- 229920000856 Amylose Polymers 0.000 claims 7
- 239000001856 Ethyl cellulose Substances 0.000 claims 5
- ZZSNKZQZMQGXPY-UHFFFAOYSA-N Ethyl cellulose Chemical compound CCOCC1OC(OC)C(OCC)C(OCC)C1OC1C(O)C(O)C(OC)C(CO)O1 ZZSNKZQZMQGXPY-UHFFFAOYSA-N 0.000 claims 5
- 229920001249 ethyl cellulose Polymers 0.000 claims 5
- 235000019325 ethyl cellulose Nutrition 0.000 claims 5
- PYGXAGIECVVIOZ-UHFFFAOYSA-N Dibutyl decanedioate Chemical compound CCCCOC(=O)CCCCCCCCC(=O)OCCCC PYGXAGIECVVIOZ-UHFFFAOYSA-N 0.000 claims 4
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound 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 claims 4
- 239000011248 coating agent Substances 0.000 claims 4
- 238000000576 coating method Methods 0.000 claims 4
- 229940031954 dibutyl sebacate Drugs 0.000 claims 4
- 229910052708 sodium Inorganic materials 0.000 claims 4
- 239000011734 sodium Substances 0.000 claims 4
- 239000002775 capsule Substances 0.000 claims 3
- XOFYZVNMUHMLCC-ZPOLXVRWSA-N prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 claims 3
- 229960004618 prednisone Drugs 0.000 claims 3
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 2
- 239000000945 filler Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-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
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 1
- 108010010803 Gelatin Proteins 0.000 claims 1
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 1
- 229930195725 Mannitol Natural products 0.000 claims 1
- 229920002472 Starch Polymers 0.000 claims 1
- 241000209140 Triticum Species 0.000 claims 1
- 235000021307 Triticum Nutrition 0.000 claims 1
- 240000008042 Zea mays Species 0.000 claims 1
- 235000005824 Zea mays ssp. parviglumis Nutrition 0.000 claims 1
- 235000002017 Zea mays subsp mays Nutrition 0.000 claims 1
- 238000013270 controlled release Methods 0.000 claims 1
- 235000005822 corn Nutrition 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229960004667 ethyl cellulose Drugs 0.000 claims 1
- 238000009472 formulation Methods 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
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- 239000000594 mannitol Substances 0.000 claims 1
- 235000010355 mannitol Nutrition 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000008188 pellet Substances 0.000 claims 1
- 229960005205 prednisolone Drugs 0.000 claims 1
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 claims 1
- 239000008107 starch Substances 0.000 claims 1
- 235000019698 starch Nutrition 0.000 claims 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
- A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
- A61K31/573—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/50—Microcapsules having a gas, liquid or semi-solid filling; Solid microparticles or pellets surrounded by a distinct coating layer, e.g. coated microspheres, coated drug crystals
- A61K9/5005—Wall or coating material
- A61K9/5021—Organic macromolecular compounds
- A61K9/5036—Polysaccharides, e.g. gums, alginate; Cyclodextrin
- A61K9/5042—Cellulose; Cellulose derivatives, e.g. phthalate or acetate succinate esters of hydroxypropyl methylcellulose
- A61K9/5047—Cellulose ethers containing no ester groups, e.g. hydroxypropyl methylcellulose
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Claims (12)
1. Состав с регулируемым высвобождением, содержащий преднизолон метасульфобензоат натрия с покрытием из стекловидной амилозы, этилцеллюлозы и дибутил-себаката, в котором соотношение амилозы к этицеллюлозе в покрытии составляет от 1:3.5 до 1:4.5, а амилоза представляет собой пшеничную или кукурузную амилозу.
2. Состав по п.1, отличающийся тем, что преднизолон метасульфобензоат натрия смешан с наполнителем.
3. Состав по п.1, отличающийся тем, что наполнитель представляет собой маннитол или лактозу.
4. Состав по п.1, отличающийся тем, что покрытие имеет такую толщину, при которой массовая доля покрытия составляет 15-25% от общей массы состава.
5. Состав по п.1, отличающийся тем, что он имеет форму пеллет, таблеток, мини-таб или капсул.
6. Состав по п.1, отличающийся тем, что он имеет форму размером от 0.5 до 1.5 мм в диаметре.
7. Состав по п.1, отличающийся тем, что соотношение амилозы, этилцеллюлозы и дибутил-себаката находится в пределах 1: (3.5 -4.5):(0.5-1.5).
8. Способ приготовления состава по любому из пп.1-7, включающий смешивание амилозы, этилцеллюлозы и дибутил-себаката и нанесение полученной смеси в виде покрытия на сердцевину из преднизолона метасульфобензоата натрия.
9. Состав по любому из пп.1-7 для применения с целью профилактики или лечения воспалительных заболеваний кишечника.
10. Применение стекловидной амилозы, этилцеллюлозы, дибутил-себаката и преднизолона метасульфобензоата натрия в производстве лекарственных препаратов для профилактики или лечения воспалительных заболеваний кишечника.
11. Состав по любому из пп.1-7, отличающийся тем, что он заключен в капсулу.
12. Состав по п.11, отличающийся тем, что капсула включает один или более из следующих компонентов: желатин, крахмал, гидроксопропилметилцеллюлоза.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0203421.3 | 2002-02-13 | ||
| GBGB0203421.3A GB0203421D0 (en) | 2002-02-13 | 2002-02-13 | Composition |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2004127867A true RU2004127867A (ru) | 2005-06-10 |
| RU2327446C2 RU2327446C2 (ru) | 2008-06-27 |
Family
ID=9931006
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2004127867/15A RU2327446C2 (ru) | 2002-02-13 | 2003-02-13 | Состав с высвобождением в толстом кишечнике |
Country Status (14)
| Country | Link |
|---|---|
| US (1) | US20050220861A1 (ru) |
| EP (1) | EP1474116A1 (ru) |
| JP (1) | JP2005521682A (ru) |
| CN (1) | CN100350913C (ru) |
| AR (1) | AR038426A1 (ru) |
| AU (1) | AU2003212491B2 (ru) |
| CA (1) | CA2475704C (ru) |
| GB (1) | GB0203421D0 (ru) |
| MX (1) | MXPA04007894A (ru) |
| MY (1) | MY137423A (ru) |
| RU (1) | RU2327446C2 (ru) |
| TW (1) | TWI291354B (ru) |
| WO (1) | WO2003068196A1 (ru) |
| ZA (1) | ZA200406397B (ru) |
Families Citing this family (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0607534D0 (en) | 2006-04-13 | 2006-05-24 | Univ London Pharmacy | Colonic drug delivery formulation |
| EP2046306B8 (en) * | 2006-07-27 | 2012-06-27 | University of Sunderland | Coating composition comprising starch |
| PT2079456E (pt) | 2007-04-04 | 2013-03-13 | Sigmoid Pharma Ltd | Composições farmacêuticas de ciclosporina |
| EP2179727B1 (en) * | 2008-10-27 | 2013-05-29 | Roquette Freres | Water insoluble polymer: modified starch derivative-based film coatings for colon targeting |
| EP2298321A1 (en) | 2009-08-26 | 2011-03-23 | Nordic Pharma | Novel pharmaceutical compositions for treating IBD |
| US10799460B2 (en) | 2011-09-07 | 2020-10-13 | Roland SAUR-BROSCH | Formulation for the controlled release of one or several substances in the digestive tract of a mammal |
| HUE036187T2 (hu) | 2012-04-30 | 2018-06-28 | Tillotts Pharma Ag | Késleltetett leadású gyógyszerkészítmény |
| GB201304662D0 (en) | 2013-03-14 | 2013-05-01 | Sigmoid Pharma Ltd | Compositions |
| UA117260C2 (uk) | 2013-10-29 | 2018-07-10 | Тиллоттс Фарма АГ | Лікарський препарат з відстроченим вивільненням |
| EP3409688A1 (en) | 2017-05-31 | 2018-12-05 | Tillotts Pharma Ag | Topical treatment of inflammatory bowel disease using anti-tnf-alpha antibodies and fragments thereof |
| ES2938609T3 (es) | 2017-09-20 | 2023-04-13 | Tillotts Pharma Ag | Preparación de formas farmacéuticas sólidas que comprenden anticuerpos mediante estratificación de solución/suspensión |
| EP3459529A1 (en) | 2017-09-20 | 2019-03-27 | Tillotts Pharma Ag | Preparation of sustained release solid dosage forms comprising antibodies by spray drying |
| ES2938608T3 (es) | 2017-09-20 | 2023-04-13 | Tillotts Pharma Ag | Método para preparar una forma farmacéutica sólida que comprende anticuerpos mediante granulación en húmedo, extrusión y esferonización |
| EP3662900A1 (en) | 2018-12-07 | 2020-06-10 | Tillotts Pharma AG | Colonic drug delivery formulation |
| EP3662901A1 (en) | 2018-12-07 | 2020-06-10 | Tillotts Pharma AG | Delayed release drug formulation comprising an outerlayer with an enzymaticyaaly degradable polymer, its composition and its method of manufacturing |
| WO2020114616A1 (en) | 2018-12-07 | 2020-06-11 | Tillotts Pharma Ag | Topical treatment of immune checkpoint inhibitor induced diarrhoea, colitis or enterocolitis using antibodies and fragments thereof |
| EP3662902A1 (en) | 2018-12-07 | 2020-06-10 | Tillotts Pharma AG | Colonic drug delivery formulation |
| EP3662898A1 (en) | 2018-12-07 | 2020-06-10 | Tillotts Pharma AG | Solid composition comprising mesalazine |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB8926639D0 (en) * | 1989-11-24 | 1990-01-17 | Agricultural & Food Res | Delayed release formulations |
| ATE224135T1 (de) * | 1992-07-31 | 2002-10-15 | Goodman Fielder Ltd | Stärke mit hohem amylose-gehalt und resistente stärke-fraktionen |
| GB9620709D0 (en) * | 1996-10-04 | 1996-11-20 | Danbiosyst Uk | Colonic delivery of weak acid drugs |
| GB9722426D0 (en) * | 1997-10-23 | 1997-12-24 | Univ London Pharmacy | Controlled release formulations |
| GB9724186D0 (en) * | 1997-11-14 | 1998-01-14 | British Tech Group | Low temperature coatings |
| AR028253A1 (es) * | 2000-03-16 | 2003-04-30 | Pfizer Prod Inc | Inhibidores de la glucogeno fosforilasa |
-
2002
- 2002-02-13 GB GBGB0203421.3A patent/GB0203421D0/en not_active Ceased
-
2003
- 2003-02-11 TW TW092102742A patent/TWI291354B/zh not_active IP Right Cessation
- 2003-02-13 AU AU2003212491A patent/AU2003212491B2/en not_active Ceased
- 2003-02-13 EP EP03708310A patent/EP1474116A1/en not_active Withdrawn
- 2003-02-13 RU RU2004127867/15A patent/RU2327446C2/ru not_active IP Right Cessation
- 2003-02-13 CN CNB038050137A patent/CN100350913C/zh not_active Expired - Fee Related
- 2003-02-13 MX MXPA04007894A patent/MXPA04007894A/es unknown
- 2003-02-13 US US10/504,182 patent/US20050220861A1/en not_active Abandoned
- 2003-02-13 AR ARP030100480A patent/AR038426A1/es unknown
- 2003-02-13 MY MYPI20030494A patent/MY137423A/en unknown
- 2003-02-13 WO PCT/GB2003/000651 patent/WO2003068196A1/en active Application Filing
- 2003-02-13 CA CA2475704A patent/CA2475704C/en not_active Expired - Fee Related
- 2003-02-13 JP JP2003567379A patent/JP2005521682A/ja active Pending
-
2004
- 2004-08-12 ZA ZA200406397A patent/ZA200406397B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA2475704C (en) | 2011-07-12 |
| EP1474116A1 (en) | 2004-11-10 |
| CN1638746A (zh) | 2005-07-13 |
| TW200302744A (en) | 2003-08-16 |
| CA2475704A1 (en) | 2003-08-21 |
| RU2327446C2 (ru) | 2008-06-27 |
| AU2003212491A1 (en) | 2003-09-04 |
| MXPA04007894A (es) | 2004-10-15 |
| JP2005521682A (ja) | 2005-07-21 |
| TWI291354B (en) | 2007-12-21 |
| MY137423A (en) | 2009-01-30 |
| ZA200406397B (en) | 2005-09-12 |
| AU2003212491B2 (en) | 2008-04-17 |
| WO2003068196A1 (en) | 2003-08-21 |
| AR038426A1 (es) | 2005-01-12 |
| US20050220861A1 (en) | 2005-10-06 |
| CN100350913C (zh) | 2007-11-28 |
| GB0203421D0 (en) | 2002-04-03 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2004127867A (ru) | Состав с высвобождением в толстом кишечнике | |
| JP5723289B2 (ja) | 持続放出医薬製剤 | |
| CN1195499C (zh) | 肠溶衣药用片剂及其生产方法 | |
| RU2428178C2 (ru) | Сахарные покрытия и способы их применения | |
| US4438091A (en) | Bromhexine delayed-release pharmaceutical form | |
| US4596705A (en) | Oral mopidamol preparation | |
| JP3010562B2 (ja) | 徐放性調剤単位 | |
| US20020054911A1 (en) | Novel oral dosage form for carvedilol | |
| NZ201008A (en) | Oral preparations containing dipyridamole and at least 5 molar equivalents of orally acceptable acidic excipient | |
| BG60753B2 (bg) | Indометнасin с депо излъчване | |
| JP2012144577A (ja) | トロスピウムの１日１回剤形 | |
| EP1509208A1 (en) | Hydrodynamically balancing oral drug delivery system with biphasic release | |
| AU2001249591A1 (en) | Sustained release beadlets containing stavudine | |
| CN103006612A (zh) | 一种赖诺普利迟释缓释片剂及其制备方法 | |
| AU751117B2 (en) | Novel oral dosage form for carvedilol | |
| JP2009519313A (ja) | 医薬組成物 | |
| JPH0260643B2 (ru) | ||
| WO2018228440A1 (zh) | 一种非布司他控释组合物及其制备方法 | |
| CN101658507B (zh) | 一种愈创木酚甘油醚和伪麻黄碱的复方缓释制剂 | |
| CN101756981B (zh) | 一种布洛氯雷伪麻缓释制剂及其制备方法 | |
| JP2005200399A (ja) | 塩酸タムスロシンの経口投与用徐放性ペレット組成物，経口投与用塩酸タムスロシン製剤およびその製造方法 | |
| JP4759905B2 (ja) | 糖衣錠 | |
| CN107998093A (zh) | 一种盐酸鲁拉西酮缓释片及其制备方法 | |
| CN101756987A (zh) | 一种愈创木酚甘油醚、伪麻黄碱和右美沙芬的复方缓释制剂 | |
| JP2007031380A (ja) | アジスロマイシン水和物含有製剤 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20120214 |