RU2001118266A - Macrolide stabilization - Google Patents

Macrolide stabilization

Info

Publication number
RU2001118266A
RU2001118266A RU2001118266/14A RU2001118266A RU2001118266A RU 2001118266 A RU2001118266 A RU 2001118266A RU 2001118266/14 A RU2001118266/14 A RU 2001118266/14A RU 2001118266 A RU2001118266 A RU 2001118266A RU 2001118266 A RU2001118266 A RU 2001118266A
Authority
RU
Russia
Prior art keywords
macrolide
antioxidant
mixture according
hydroxy
ethylrapamycin
Prior art date
Application number
RU2001118266/14A
Other languages
Russian (ru)
Other versions
RU2243769C2 (en
Inventor
Франсуа НАВАРРО
Самюэль ПЕТИ
Гай СТОУН
Original Assignee
Новартис Аг
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from GBGB9826882.4A external-priority patent/GB9826882D0/en
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of RU2001118266A publication Critical patent/RU2001118266A/en
Application granted granted Critical
Publication of RU2243769C2 publication Critical patent/RU2243769C2/en

Links

Claims (13)

1. Смесь, содержащая полиеновый макролид и антиоксидант.1. A mixture containing polyene macrolide and antioxidant. 2. Смесь по п.1, где антиоксидант присутствует в количестве до 1% в пересчете на массу макролида.2. The mixture according to claim 1, where the antioxidant is present in an amount up to 1%, calculated on the weight of the macrolide. 3. Смесь по п.1, где антиоксидант присутствует в количестве 0,2% в пересчете на массу макролида.3. The mixture according to claim 1, where the antioxidant is present in an amount of 0.2%, calculated on the weight of the macrolide. 4. Смесь по п.1, где антиоксидант представляет собой 2,6-дитрет-бутил-4-метилфенол.4. The mixture according to claim 1, where the antioxidant is 2,6-ditret-butyl-4-methylphenol. 5. Смесь по п.1, где полиеновый макролид представляет собой рапамицин или 40-О-(2-гидрокси)этилрапамицин.5. The mixture according to claim 1, where the polyene macrolide is rapamycin or 40-O- (2-hydroxy) ethylrapamycin. 6. Смесь по п.1 в твердой форме.6. The mixture according to claim 1 in solid form. 7. Фармацевтическая композиция, содержащая в качестве действующего вещества смесь по п.1 вместе с одним или несколькими фармацевтически приемлемым (и) носителем(ями) или разбавителем(ями).7. A pharmaceutical composition comprising, as an active ingredient, a mixture according to claim 1 together with one or more pharmaceutically acceptable (s) carrier (s) or diluent (s). 8. Способ стабилизации полиенового макролида, предусматривающий добавление антиоксиданта к очищенному макролиду.8. A method for stabilizing a polyene macrolide comprising adding an antioxidant to a purified macrolide. 9. 40-О-(2-гидрокси)этилрапамицин в кристаллической форме.9. 40-O- (2-hydroxy) ethyl rapamycin in crystalline form. 10. Соединение по п.9 в кристаллической несольватированной форме.10. The compound according to claim 9 in crystalline unsolvated form. 11. Соединение по п.9, имеющее кристаллическую решетку со следующими параметрами: а=14,37A, b=11,24A, c=18,31A, объем 2805A3.11. The compound according to claim 9, having a crystal lattice with the following parameters: a = 14.37A, b = 11.24A, c = 18.31A, volume 2805A 3 . 12. Фармацевтическая композиция, содержащая соединение по п.9 или п.11 вместе с одним или несколькими фармацевтически приемлемым(и) носителем(ями) или разбавителем(ями).12. A pharmaceutical composition comprising a compound according to claim 9 or claim 11 together with one or more pharmaceutically acceptable (s) carrier (s) or diluent (s). 13. Способ очистки 40-О-(2-гидрокси)этилрапамицина, предусматривающий кристаллизацию 40-О-(2-гидрокси)этилрапамицина из среды для кристаллизации и выделение полученных таким образом кристаллов.13. A method for purifying 40-O- (2-hydroxy) ethylrapamycin, comprising crystallizing 40-O- (2-hydroxy) ethylrapamycin from a crystallization medium and isolating the crystals thus obtained.
RU2001118266/15A 1998-12-07 1999-12-06 Stabilization of macrolides RU2243769C2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GB9826882.4 1998-12-07
GBGB9826882.4A GB9826882D0 (en) 1998-12-07 1998-12-07 Organic compounds
GBGB9904934.8A GB9904934D0 (en) 1998-12-07 1999-03-04 Organic compounds
GB9904934.8 1999-03-04

Related Child Applications (1)

Application Number Title Priority Date Filing Date
RU2003136738/04A Division RU2264405C2 (en) 1999-12-06 1999-12-06 40-o-(2-hydroxy)ethylrapamycin in crystalline nonsolvated form, pharmaceutical composition comprising such macrolide as active substance and method for its preparing

Publications (2)

Publication Number Publication Date
RU2001118266A true RU2001118266A (en) 2003-06-20
RU2243769C2 RU2243769C2 (en) 2005-01-10

Family

ID=26314797

Family Applications (1)

Application Number Title Priority Date Filing Date
RU2001118266/15A RU2243769C2 (en) 1998-12-07 1999-12-06 Stabilization of macrolides

Country Status (38)

Country Link
US (5) US6605613B2 (en)
EP (4) EP2269651A3 (en)
JP (3) JP3805625B2 (en)
KR (2) KR20060096477A (en)
CN (2) CN1876657B (en)
AR (3) AR026102A1 (en)
AT (1) ATE365051T1 (en)
AU (1) AU759219B2 (en)
BE (1) BE1012869A3 (en)
BR (1) BR9915986A (en)
CA (3) CA2651609A1 (en)
CO (1) CO4980847A1 (en)
CY (1) CY1106870T1 (en)
CZ (2) CZ303006B6 (en)
DE (1) DE69936352T3 (en)
DK (1) DK1137439T4 (en)
ES (1) ES2288033T5 (en)
FR (1) FR2786771B1 (en)
GB (2) GB9826882D0 (en)
HK (1) HK1038889B (en)
HU (2) HU230174B1 (en)
ID (1) ID29250A (en)
IL (1) IL143092A0 (en)
IT (1) IT1319701B1 (en)
MY (2) MY127579A (en)
NO (2) NO332698B1 (en)
NZ (2) NZ511936A (en)
PE (1) PE20001333A1 (en)
PL (2) PL196627B1 (en)
PT (1) PT1137439E (en)
RU (1) RU2243769C2 (en)
SG (1) SG151072A1 (en)
SI (1) SI1137439T2 (en)
SK (2) SK287325B6 (en)
TR (2) TR200101416T2 (en)
TW (2) TWI248938B (en)
WO (1) WO2000033878A2 (en)
ZA (1) ZA200104360B (en)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20070032853A1 (en) 2002-03-27 2007-02-08 Hossainy Syed F 40-O-(2-hydroxy)ethyl-rapamycin coated stent
ZA200406350B (en) 2002-02-13 2006-11-29 Teva Gyogyszergyar Reszveny Tarsasag Method for extracting a macrolide from biomatter
US7452692B2 (en) 2002-02-13 2008-11-18 Teva Gyógyszergyár Zártkörüen Müködö Részvénytársaság Method for extracting a macrolide from biomatter
NZ537829A (en) 2002-07-30 2006-09-29 Wyeth Corp Parenteral formulations containing a rapamycin hydroxyester
TW200504079A (en) * 2003-03-31 2005-02-01 Biogal Gyogyszergyar Crystallization and purification of macrolides
US20050118344A1 (en) 2003-12-01 2005-06-02 Pacetti Stephen D. Temperature controlled crimping
ATE378345T1 (en) 2003-07-24 2007-11-15 Teva Gyogyszergyar Zartkoeruee METHOD FOR PURIFYING MACROLIDS
US9114198B2 (en) * 2003-11-19 2015-08-25 Advanced Cardiovascular Systems, Inc. Biologically beneficial coatings for implantable devices containing fluorinated polymers and methods for fabricating the same
KR20060126701A (en) * 2003-12-10 2006-12-08 애크럭스 디디에스 피티와이 리미티드 Method of treatment for undesired effect following transdermal or topical drug delivery
US8551512B2 (en) 2004-03-22 2013-10-08 Advanced Cardiovascular Systems, Inc. Polyethylene glycol/poly(butylene terephthalate) copolymer coated devices including EVEROLIMUS
WO2006039237A1 (en) * 2004-09-29 2006-04-13 Cordis Corporation Pharmaceutical dosage forms of stable amorphous rapamycin like compounds
EP1848431B1 (en) 2005-02-09 2016-02-03 Santen Pharmaceutical Co., Ltd. Liquid formulations for treatment of diseases or conditions
KR20080077147A (en) * 2005-12-07 2008-08-21 와이어쓰 Methods for preparing crystalline rapamycin and for measuring crystallinity of rapamycin compounds using differential scanning calorimetry
US7700614B2 (en) * 2005-12-14 2010-04-20 Abbott Laboratories One pot synthesis of tetrazole derivatives of rapamycin
EP1962819A1 (en) * 2005-12-20 2008-09-03 Wyeth Control of cci-779 dosage form stability through control of drug substance impurities
WO2007092620A2 (en) * 2006-02-09 2007-08-16 Macusight, Inc. Stable formulations, and methods of their preparation and use
PL2001466T3 (en) 2006-03-23 2016-06-30 Santen Pharmaceutical Co Ltd Low-dose rapamycin for the treatment of vascular permeability-related diseases
AU2011260016B2 (en) 2010-06-02 2013-08-22 Fresenius Kabi Oncology Ltd. Stable pharmaceutical compositions of Rapamycin esters
EP2576590A1 (en) * 2010-06-07 2013-04-10 Telik, Inc. Crystalline ezatiostat hydrochloride ansolvate
CN103140494A (en) * 2010-08-04 2013-06-05 美利奴生命科学有限公司 Process for preparation of novel 42-0-(heteroalkoxyalkyl) rapamycin compounds with anti-proliferative properties
EP2640730B1 (en) 2010-11-19 2019-08-07 Biocon Limited Processes for preparation of everolimus and intermediates thereof
CA2838387A1 (en) 2011-06-06 2012-12-13 Chevron Phillips Chemical Company Lp Use of metallocene compounds for cancer treatment
WO2013022201A1 (en) * 2011-08-11 2013-02-14 Dong-A Pharm. Co., Ltd. Process of preparing a stabilized and solubilized formulation of sirolimus derivatives
US9610385B2 (en) 2013-03-07 2017-04-04 Abbott Cardiovascular Systems Inc. Method of fabricating an implantable medical device comprising a rapamycin derivative
IN2013MU02532A (en) 2013-07-31 2015-06-26 Sahajanand Medical Technologies Pvt Ltd
CN104721158B (en) * 2013-12-24 2018-01-30 正大天晴药业集团股份有限公司 A kind of everolimus tablet of stabilization
CN104892632B (en) * 2015-06-03 2017-12-26 道中道(菏泽)制药有限公司 A kind of everolimus of crystal form and preparation method thereof
WO2017018433A1 (en) 2015-07-28 2017-02-02 日本化薬株式会社 Pharmaceutical composition including rapamycin or derivative thereof, and production method therefor
WO2017038612A1 (en) * 2015-08-28 2017-03-09 日本化薬株式会社 Pharmaceutical composition containing rapamycin or derivative thereof
JP7020914B2 (en) * 2015-09-18 2022-02-16 日本化薬株式会社 Pharmaceutical composition containing rapamycin or a derivative thereof
WO2017129772A1 (en) 2016-01-29 2017-08-03 Xellia Phamaceuticals Aps Stable pharmaceutical compositions of temsirolimus
JP6855470B2 (en) 2016-05-27 2021-04-07 日本化薬株式会社 Pharmaceutical composition containing rapamycin or a derivative thereof
KR102051806B1 (en) * 2018-01-12 2019-12-04 주식회사 종근당 Stabilized pharmaceutical formulation comprising Everolimus
JP2023519875A (en) 2020-03-27 2023-05-15 ボストン サイエンティフィック サイムド,インコーポレイテッド Method for crystallization of drugs
JP2023028473A (en) * 2021-08-19 2023-03-03 日本マイクロバイオファーマ株式会社 Method for producing everolimus

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ZA737247B (en) * 1972-09-29 1975-04-30 Ayerst Mckenna & Harrison Rapamycin and process of preparation
US3996355A (en) 1975-01-02 1976-12-07 American Home Products Corporation Permanent suspension pharmaceutical dosage form
US4049128A (en) 1976-11-18 1977-09-20 Westinghouse Air Brake Company Control system for automatic railway car coupler
AU543727B2 (en) * 1980-06-02 1985-05-02 Ayerst Mckenna & Harrison Inc. Injectable composition of rapamycin
GB8803836D0 (en) 1988-02-18 1988-03-16 Glaxo Group Ltd Compositions
CA1338150C (en) 1988-02-18 1996-03-12 Edward George Howard, Jr. Ceramic/distillable binder compositions
KR0159766B1 (en) * 1989-10-16 1998-12-01 후지사와 토모키치로 Hair revitalizing agent
JPH04230389A (en) 1990-07-16 1992-08-19 American Home Prod Corp Rapamycin derivative
FI97472C (en) 1991-05-07 1996-12-27 American Home Prod Process for the preparation of therapeutically useful rapamycin derivatives as anti-inflammatory and antifungal agents
GB9221220D0 (en) * 1992-10-09 1992-11-25 Sandoz Ag Organic componds
US5302584A (en) * 1992-10-13 1994-04-12 American Home Products Corporation Carbamates of rapamycin
ES2258763T3 (en) 1992-10-13 2006-09-01 Wyeth RAPAMYCINE CARBAMATES.
HU228234B1 (en) 1995-06-09 2013-02-28 Novartis Ag Rapamycin derivatives, pharmaceutical compositions containing them and their use
BE1009856A5 (en) * 1995-07-14 1997-10-07 Sandoz Sa Pharmaceutical composition in the form of a solid release including macrolide and a vehicle.
PT1208847E (en) * 1996-07-30 2007-07-24 Novartis Ag Pharmaceutical compositions for the treatment of transplant rejection, as well as autoimmune or inflammatory conditions
US6362264B1 (en) * 1996-12-20 2002-03-26 Ck Witco Corporation Stabilizer for food contact and medical grade PVC
AU6041498A (en) 1997-02-04 1998-08-25 Abbott Laboratories Pain reducing parenteral liposome formulation

Similar Documents

Publication Publication Date Title
RU2001118266A (en) Macrolide stabilization
CA2351580A1 (en) Stabilization of macrolides
SU1430392A1 (en) Laevo-rotatory enathiomer (s)-alpha-ethyl-2-oxo-1-pyrroliddine acetamide displaying antihypoxic and antiischemic activity
CN1040746C (en) New crystalline form of a vitamin D analogue
CA2192418C (en) New crystal modification of cdch, a process for its preparation and pharmaceutical formulations comprising this modification
US20050209451A1 (en) Crystalline form of cefdinir
CA2467285A1 (en) Crystals of non-natural-type stereoisomer salt of monatin and use thereof
RU2002134764A (en) STABILIZED PHARMACEUTICALLY EFFECTIVE COMPOSITION AND PHARMACEUTICAL DRUG CONTAINING IT
CA2275166A1 (en) Novel benzopyran derivatives
RU94041836A (en) Derivatives of amidine, mixture of their isomers or individual isomers and their salts, pharmaceutical composition exhibiting antagonistic activity with respect to leukotriene b4 activity
CA2415447A1 (en) Novel .gamma. crystalline form of perindopril tert-butylamine salt, preparation method, and pharmaceutical compositions containing same
HUP0104330A2 (en) Crystalline forms of eto2c-ch2-(r)cgl-aze-pab-oh, method for their preparation, pharmaceutical compositions comprising thereof and their use
HUP0202536A2 (en) Crystals of the sodium salt of pravastatin
CA2415442A1 (en) Novel .beta. crystalline form of perindopril tert-butylamine salt, preparation method, and pharmaceutical compositions containing same
JPS55104253A (en) Stereoisomer of more active carboxylic ester, method of obtaining it, insecticide and acaricide comprising it
RU2004127981A (en) METHOD FOR PRODUCING SODIUM SALT OF PRAVASTATIN IN CRYSTAL FORM AND SODIUM SALT OF PRAVASTATIN OBTAINED BY THIS METHOD
RO112295B1 (en) Solid lactulose preparation process
RU96101800A (en) AMIDA DERIVATIVES OF PHENYLCYCLOGAXYLICARBONIC ACID, MIXTURE OF THEIR ISOMERS OR SEPARATE ISOMERES AND THEIR SALT, PHARMACEUTICAL COMPOSITION WITH ANTI-ARTERIOCLEROTIC AND ANTI-RETENCY
RU2006105481A (en) STABLE MODIFICATIONS OF TEGASEROD HYDROMALATE
US11926583B2 (en) Stabilized 1, 25-dihydroxyvitamin D2 and method of making same
RU2003136738A (en) 40-O- (2-HYDROXY) ETHYLRAPAMICIN IN A CRYSTALLIC NONSOLVATED FORM, PHARMACEUTICAL COMPOSITION CONTAINING THIS MACROLIDE AS AN ACTIVE SUBSTANCE AND METHOD FOR PRODUCING IT
CA2204734A1 (en) Process for the crystallization from water of (s)-n,n'-bis[2-hydroxy-1-(hydroxymethyl)ethyl]-5-[(2-hydroxy-1-oxopropyl)amino]-2,4,6-triiodo-1,3-benzendicarboxamide
UA66832C2 (en) (r)-3-[ [(4-fluorophenyl) sulfonyl] amino] -1,2,3,4-tetrahydro-9н-carbazole-9-propanoic acid of thermodynamic solid form (rematroban)
CA1240329A (en) 5-oxo-2-pyrrolidinepropanoic acid and derivatives as cognition activators
SK19002001A3 (en) Method for separating the diastereomer bases of 2-[(dimethylamino)methyl]-1-(3-methoxyphenyl)-cyclohexanol