TW550091B - Rapamycin formulations for oral administration - Google Patents
Rapamycin formulations for oral administration Download PDFInfo
- Publication number
- TW550091B TW550091B TW087103043A TW87103043A TW550091B TW 550091 B TW550091 B TW 550091B TW 087103043 A TW087103043 A TW 087103043A TW 87103043 A TW87103043 A TW 87103043A TW 550091 B TW550091 B TW 550091B
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- rapamycin
- sugar overcoat
- sugar coating
- sugar
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- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
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- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/282—Organic compounds, e.g. fats
- A61K9/2826—Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/436—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having oxygen as a ring hetero atom, e.g. rapamycin
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- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2086—Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2806—Coating materials
- A61K9/2833—Organic macromolecular compounds
- A61K9/2853—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers, poly(lactide-co-glycolide)
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- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/28—Dragees; Coated pills or tablets, e.g. with film or compression coating
- A61K9/2893—Tablet coating processes
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- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
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- Animal Behavior & Ethology (AREA)
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- Immunology (AREA)
- Epidemiology (AREA)
- Pulmonology (AREA)
- Dermatology (AREA)
- Diabetes (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Communicable Diseases (AREA)
- Cardiology (AREA)
- Physical Education & Sports Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Emergency Medicine (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Urology & Nephrology (AREA)
- Transplantation (AREA)
- Endocrinology (AREA)
- Ophthalmology & Optometry (AREA)
- Child & Adolescent Psychology (AREA)
- Molecular Biology (AREA)
Description
550091 六、申請專利範圍 (e)蔗糖含量係占糖衣之95-99%重量比。 6. 如申請專利範圍第1項之雷帕黴素配方,其中: (a) 雷帕黴素含量爲0.5毫克, (b) 普隆尼克F68含量爲0.25毫克, (c) 普維隆含量係占糖衣之0.5%重量比, (d) 微晶纖維素係占糖衣之1%重量比,及 (e) 蔗糖含量係占糖衣之96-99%重量比。 7. 如申請專利範圍第1項之雷帕黴素配方,其中: (a) 雷帕黴素含量爲3毫克, (b) 普隆尼克F68含量爲1.5毫克, (〇普維隆含量係占糖衣之0.5%重量比, (d) 微晶纖維素係占糖衣之1%重量比,及 (e) 蔗糖含量係占糖衣之90-96^1重量比。 8. 如申請專利範圍第1項之雷帕黴素配方,其中: (a) 雷帕黴素含量爲5毫克, (b) 普隆尼克F68含量爲2.5毫克, (c) 普維隆含量係占糖衣之0.5%重量比, (d) 微晶纖維素係占糖衣之1%重量比,及 (e) 蔗糖含量係占糖衣之80-96%重量比。 9. 如申請專利範圍第1項之雷帕黴素配方,其中: (a) 雷帕黴素含量爲7.5毫克, (b) 普隆尼克F68含量爲3.75毫克, (c) 普維隆含量係占糖衣之0.5%重量比,
550091 六、申請專利範圍 (d) 微晶纖維素係占糖衣之1%重量比,及 (e) 蔗糖含量係占糖衣之75-90%重量比。 10·如申請專利範圍第1項之雷帕黴素配方,其中: (a) 雷帕黴素含量爲1〇毫克, (b) 普隆尼克F68含量爲5毫克, (c) 普維隆含量係占糖衣之0.5%重量比, (d) 微晶纖維素係占糖衣之1%重量比,及 (e) 蔗糖含量係占糖衣之65-90%重量比。 11. 一種製備口服用雷帕黴素配方之方法,該方法包含採用 下列步驟製備糖衣, (a) 製備重量比2:1之雷帕黴素:普隆尼克F68之分散 液; (b) 加入占該糖衣35-99%重量比範圍之蔗糖至分散液並 攪拌至溶解爲止; (c) 加入占該糖衣0.2-1.0%重量比範圍之普維隆,並混 合至徹底濕潤,且持續激烈混合至普維隆溶解爲止; (d) 加入占該糖衣0.1-3%重量比範圍之微晶纖維素,並 徹底混合至濕潤; (e) 加入水並徹底混合;以及 (f) 所得溶液逐份噴塗於醫藥惰性蕊上,以及於兩次噴 塗間風乾。 12. 如申請專利範圍第11項之方法,其又包含於添加糖至分 散液前或後添加一種或多種黏結劑至分散液。
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US81501597A | 1997-03-14 | 1997-03-14 |
Publications (1)
Publication Number | Publication Date |
---|---|
TW550091B true TW550091B (en) | 2003-09-01 |
Family
ID=25216622
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
TW087103043A TW550091B (en) | 1997-03-14 | 1998-03-03 | Rapamycin formulations for oral administration |
Country Status (25)
Country | Link |
---|---|
EP (1) | EP0868911B1 (zh) |
JP (2) | JP4616426B2 (zh) |
KR (1) | KR100513919B1 (zh) |
CN (1) | CN1140268C (zh) |
AR (1) | AR012069A1 (zh) |
AT (1) | ATE223705T1 (zh) |
AU (1) | AU723943B2 (zh) |
BR (1) | BR9801120B1 (zh) |
CA (1) | CA2230748C (zh) |
CY (1) | CY2313B1 (zh) |
CZ (1) | CZ292949B6 (zh) |
DE (1) | DE69807768T2 (zh) |
DK (1) | DK0868911T3 (zh) |
ES (1) | ES2183287T3 (zh) |
HK (1) | HK1015677A1 (zh) |
HU (1) | HU224701B1 (zh) |
IL (1) | IL123525A (zh) |
NZ (1) | NZ329976A (zh) |
PT (1) | PT868911E (zh) |
RU (1) | RU2220714C2 (zh) |
SG (1) | SG63824A1 (zh) |
SI (1) | SI0868911T1 (zh) |
TW (1) | TW550091B (zh) |
UA (1) | UA56143C2 (zh) |
ZA (1) | ZA982112B (zh) |
Cited By (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US10441584B2 (en) | 2016-11-23 | 2019-10-15 | Novartis Ag | Methods of enhancing immune response |
US10576076B2 (en) | 2015-05-20 | 2020-03-03 | Novartis Ag | Pharmaceutical combination of everolimus with dactolisib |
US10596165B2 (en) | 2018-02-12 | 2020-03-24 | resTORbio, Inc. | Combination therapies |
Families Citing this family (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CH686761A5 (de) | 1993-05-27 | 1996-06-28 | Sandoz Ag | Galenische Formulierungen. |
ZA985095B (en) * | 1997-06-13 | 1999-12-13 | American Home Prod | Rapamycin formulations for oral administration. |
JP4969747B2 (ja) * | 2001-01-19 | 2012-07-04 | 武田薬品工業株式会社 | 錠剤フィルムコーティング用組成物 |
PT1635830E (pt) * | 2002-09-17 | 2008-12-31 | Wyeth Corp | Formulação granulada do éster de rapamicina cci-779 |
BRPI0608573A2 (pt) * | 2005-03-08 | 2017-07-25 | Lifecycle Pharma As | Composição farmacêutica, e, método para a preparação de uma composição farmacêutica. |
EP2086514A2 (en) * | 2006-09-26 | 2009-08-12 | Novartis Ag | Pharmaceutical compositions comprising an s1p modulator |
MX2009004960A (es) * | 2006-11-07 | 2009-06-05 | Wyeth Corp | Revestimientos de azucar y metodos para los mismos. |
US20080138405A1 (en) * | 2006-12-06 | 2008-06-12 | Raheja Praveen | Sirolimus nanodispersion |
EP1952807A1 (en) * | 2007-01-24 | 2008-08-06 | LEK Pharmaceuticals D.D. | Sirolimus formulation |
FR2943539B1 (fr) | 2009-03-31 | 2011-07-22 | Ethypharm Sa | Composition pharmaceutique comprenant un macrolide immunosuppresseur de la famille des limus. |
US8912215B2 (en) * | 2011-12-13 | 2014-12-16 | Everon Biosciences, Inc. | Rapamycin composition |
HUP1400075A2 (hu) | 2014-02-14 | 2015-08-28 | Druggability Technologies Ip Holdco Jersey Ltd | Sirolimus és származékainak komplexei, elõállítása és gyógyszerészeti kompozíciói |
CN110585159B (zh) * | 2019-09-12 | 2021-11-02 | 杭州华东医药集团新药研究院有限公司 | 一种含有西罗莫司的片剂 |
Family Cites Families (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH04234812A (ja) * | 1990-03-16 | 1992-08-24 | Yamanouchi Pharmaceut Co Ltd | 持続性製剤用顆粒 |
US5223268A (en) * | 1991-05-16 | 1993-06-29 | Sterling Drug, Inc. | Low solubility drug-coated bead compositions |
DE69209183T2 (de) * | 1991-06-18 | 1996-08-08 | American Home Prod | Verwendung von Rapamycin zur Behandlung von T-Zellen Lymphom/Leukämie bei Erwachsenen |
GB2278780B (en) * | 1993-05-27 | 1998-10-14 | Sandoz Ltd | Macrolide formulations |
CH686761A5 (de) * | 1993-05-27 | 1996-06-28 | Sandoz Ag | Galenische Formulierungen. |
US5352783A (en) * | 1993-06-09 | 1994-10-04 | Merck & Co., Inc. | Microbial transformation product having immunosuppressive activity |
IL111004A (en) * | 1993-09-30 | 1998-06-15 | American Home Prod | Oral formulations of rapamycin |
SE9402422D0 (sv) * | 1994-07-08 | 1994-07-08 | Astra Ab | New beads for controlled release and a pharmaceutical preparation containing the same |
US5547948A (en) * | 1995-01-17 | 1996-08-20 | American Home Products Corporation | Controlled release of steroids from sugar coatings |
FR2736550B1 (fr) * | 1995-07-14 | 1998-07-24 | Sandoz Sa | Composition pharmaceutique sous la forme d'une dispersion solide comprenant un macrolide et un vehicule |
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1998
- 1998-03-02 CA CA2230748A patent/CA2230748C/en not_active Expired - Lifetime
- 1998-03-03 IL IL12352598A patent/IL123525A/en not_active IP Right Cessation
- 1998-03-03 TW TW087103043A patent/TW550091B/zh not_active IP Right Cessation
- 1998-03-09 SI SI9830250T patent/SI0868911T1/xx unknown
- 1998-03-09 DE DE69807768T patent/DE69807768T2/de not_active Expired - Lifetime
- 1998-03-09 ES ES98301716T patent/ES2183287T3/es not_active Expired - Lifetime
- 1998-03-09 AT AT98301716T patent/ATE223705T1/de active
- 1998-03-09 EP EP98301716A patent/EP0868911B1/en not_active Expired - Lifetime
- 1998-03-09 PT PT98301716T patent/PT868911E/pt unknown
- 1998-03-09 DK DK98301716T patent/DK0868911T3/da active
- 1998-03-12 ZA ZA9802112A patent/ZA982112B/xx unknown
- 1998-03-12 SG SG1998000512A patent/SG63824A1/en unknown
- 1998-03-13 BR BRPI9801120-0A patent/BR9801120B1/pt not_active IP Right Cessation
- 1998-03-13 AU AU58383/98A patent/AU723943B2/en not_active Expired
- 1998-03-13 AR ARP980101154A patent/AR012069A1/es active IP Right Grant
- 1998-03-13 KR KR1019980008439A patent/KR100513919B1/ko not_active IP Right Cessation
- 1998-03-13 UA UA98031295A patent/UA56143C2/uk unknown
- 1998-03-13 CN CNB981082440A patent/CN1140268C/zh not_active Expired - Lifetime
- 1998-03-13 HU HU9800573A patent/HU224701B1/hu active IP Right Grant
- 1998-03-13 JP JP06288598A patent/JP4616426B2/ja not_active Expired - Lifetime
- 1998-03-13 RU RU98104946/15A patent/RU2220714C2/ru active
- 1998-03-13 CZ CZ1998771A patent/CZ292949B6/cs not_active IP Right Cessation
- 1998-03-17 NZ NZ329976A patent/NZ329976A/en not_active IP Right Cessation
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1999
- 1999-02-12 HK HK99100627A patent/HK1015677A1/xx not_active IP Right Cessation
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Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
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US10576076B2 (en) | 2015-05-20 | 2020-03-03 | Novartis Ag | Pharmaceutical combination of everolimus with dactolisib |
US10441584B2 (en) | 2016-11-23 | 2019-10-15 | Novartis Ag | Methods of enhancing immune response |
US10993940B2 (en) | 2016-11-23 | 2021-05-04 | Novartis Ag | Methods of enhancing immune response |
US11045463B2 (en) | 2016-11-23 | 2021-06-29 | Novartis Ag | Methods of enhancing immune response |
US10596165B2 (en) | 2018-02-12 | 2020-03-24 | resTORbio, Inc. | Combination therapies |
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