RU2004113306A - Соли-алендронаты в аморфной форме, приемлемые в фармакологолии - Google Patents
Соли-алендронаты в аморфной форме, приемлемые в фармакологолии Download PDFInfo
- Publication number
- RU2004113306A RU2004113306A RU2004113306/04A RU2004113306A RU2004113306A RU 2004113306 A RU2004113306 A RU 2004113306A RU 2004113306/04 A RU2004113306/04 A RU 2004113306/04A RU 2004113306 A RU2004113306 A RU 2004113306A RU 2004113306 A RU2004113306 A RU 2004113306A
- Authority
- RU
- Russia
- Prior art keywords
- alendronate
- monosodium
- amorphous form
- water
- form according
- Prior art date
Links
- 150000003839 salts Chemical class 0.000 title 1
- OGSPWJRAVKPPFI-UHFFFAOYSA-N Alendronic Acid Chemical class NCCCC(O)(P(O)(O)=O)P(O)(O)=O OGSPWJRAVKPPFI-UHFFFAOYSA-N 0.000 claims abstract 2
- CAKRAHQRJGUPIG-UHFFFAOYSA-M sodium;[4-azaniumyl-1-hydroxy-1-[hydroxy(oxido)phosphoryl]butyl]-hydroxyphosphinate Chemical compound [Na+].NCCCC(O)(P(O)(O)=O)P(O)([O-])=O CAKRAHQRJGUPIG-UHFFFAOYSA-M 0.000 claims 10
- 238000000034 method Methods 0.000 claims 7
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 4
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 3
- 210000000988 bone and bone Anatomy 0.000 claims 3
- 208000006386 Bone Resorption Diseases 0.000 claims 2
- 230000024279 bone resorption Effects 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000002904 solvent Substances 0.000 claims 2
- 201000009030 Carcinoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010031240 Osteodystrophy Diseases 0.000 claims 1
- 208000001132 Osteoporosis Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 238000002441 X-ray diffraction Methods 0.000 claims 1
- 230000032683 aging Effects 0.000 claims 1
- 229960004343 alendronic acid Drugs 0.000 claims 1
- 230000006378 damage Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 208000005368 osteomalacia Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 235000011121 sodium hydroxide Nutrition 0.000 claims 1
- 238000001694 spray drying Methods 0.000 claims 1
- 150000003431 steroids Chemical class 0.000 claims 1
- 238000005303 weighing Methods 0.000 claims 1
Classifications
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
- A61K31/663—Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
- C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
- C07F9/3839—Polyphosphonic acids
- C07F9/3873—Polyphosphonic acids containing nitrogen substituent, e.g. N.....H or N-hydrocarbon group which can be substituted by halogen or nitro(so), N.....O, N.....S, N.....C(=X)- (X =O, S), N.....N, N...C(=X)...N (X =O, S)
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Rheumatology (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Immunology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Claims (11)
1. Алендронат мононатрия в аморфной форме.
2. Алендронат мононатрия в аморфной форме, содержащий менее 3% воды.
3. Алендронат мононатрия в аморфной форме по п.2, содержащий менее 1% воды.
4. Алендронат мононатрия в аморфной форме, имеющий картину дифракции рентгеновских лучей, показанную на прилагаемом рисунке.
5. Способ получения алендроната мононатрия в аморфной форме по любому из пп.1-4, причем упомянутый способ содержит удаление растворителя из раствора алендроната мононатрия с помощью распылительной сушки таким образом, чтобы получить алендронат мононатрия в аморфной форме по любому из пп.1-4.
6. Способ по п.5, в котором растворитель содержит воду.
7. Способ по п.6, в котором упомянутый раствор получают путем взвешивания алендроновой кислоты в воде и регулирования рН, используя водный едкий натр.
8. Способ получения аморфного алендроната мононатрия, как он по существу описан здесь в примере 1, 2 или 3.
9. Фармацевтическая композиция, содержащая терапевтически эффективное количество алендроната мононатрия в аморфной форме по любому из пп.1-4, вместе с приемлемыми в фармакологии носителем, разбавителем или наполнителем для него.
10. Способ торможения резорбции костей у больного, причем этот способ содержит введение больному, страдающему резорбцией костей или восприимчивому к ней, терапевтически эффективного количества алендроната мононатрия в аморфной форме по любому из пп.1-4 или фармацевтической композиции по п.9.
11. Способ по п.10 для лечения переломов и повреждений, которые являются результатом остеопороза, остеоартрита, деформирующей остеодистрофии, остеомаляции, разрежения кости, происходящего от множественной миеломы и других форм карциномы, разрежения кости, происходящего от побочных эффектов прекращенного стероидного лечения, или потери костной массы, связанной с ревматоидными явлениями и процессом старения.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GB0125081A GB2383042A (en) | 2001-10-18 | 2001-10-18 | Amorphous alendronate sodium |
GB0125081.0 | 2001-10-18 |
Publications (2)
Publication Number | Publication Date |
---|---|
RU2004113306A true RU2004113306A (ru) | 2005-10-10 |
RU2334751C2 RU2334751C2 (ru) | 2008-09-27 |
Family
ID=9924125
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
RU2004113306/04A RU2334751C2 (ru) | 2001-10-18 | 2002-10-18 | Алендронат мононатрия в аморфной форме, способы его получения, фармацевтическая композиция на его основе и способ торможения резорбции костей у больного |
Country Status (22)
Country | Link |
---|---|
US (1) | US7112577B2 (ru) |
EP (1) | EP1436303B1 (ru) |
JP (1) | JP4490100B2 (ru) |
KR (1) | KR20040053186A (ru) |
AT (1) | ATE338761T1 (ru) |
AU (1) | AU2002334200B2 (ru) |
BR (1) | BR0213398A (ru) |
CA (1) | CA2463815C (ru) |
CL (1) | CL2004001372A1 (ru) |
DE (1) | DE60214576T2 (ru) |
EC (1) | ECSP045067A (ru) |
ES (1) | ES2271375T3 (ru) |
GB (1) | GB2383042A (ru) |
HK (1) | HK1066011A1 (ru) |
IL (1) | IL161360A0 (ru) |
MX (1) | MXPA04003549A (ru) |
NZ (1) | NZ532292A (ru) |
PT (1) | PT1436303E (ru) |
RU (1) | RU2334751C2 (ru) |
TN (1) | TNSN04067A1 (ru) |
WO (1) | WO2003033508A1 (ru) |
ZA (1) | ZA200403024B (ru) |
Families Citing this family (22)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN1620284B (zh) * | 2001-12-24 | 2010-04-28 | 特瓦制药工业有限公司 | 含有用粉末或粒状材料的压缩环状体包鞘的有效成分片芯的剂型,及其生产工艺和工具 |
US20040052843A1 (en) * | 2001-12-24 | 2004-03-18 | Lerner E. Itzhak | Controlled release dosage forms |
ITMI20020146A1 (it) * | 2002-01-29 | 2003-07-29 | Lyogen Ltd | Alendronato monosodico amorfo e processo per la sua preparazione |
UA83900C2 (en) † | 2004-02-26 | 2008-08-26 | ЗЕНТИВА, а.с. | Amorphous forms of risedronate monosodium |
DE602005001873T2 (de) | 2004-03-03 | 2008-04-24 | Chemi S.P.A., Cinisello Balsamo | Amorphe 3-Pyridyl-1-Hydroxyethyliden-1,1-Bisphosphonsäure Mononatriumsalz und Verfahren zu deren Herstellung |
CZ297262B6 (cs) * | 2004-12-28 | 2006-10-11 | Zentiva, A. S. | Trisodná sul kyseliny 4-amino-1-hydroxybutyliden-1,1-bisfosfonové |
US20090118238A1 (en) * | 2007-09-17 | 2009-05-07 | Protia, Llc | Deuterium-enriched alendronate |
RU2015113434A (ru) * | 2012-09-11 | 2016-11-10 | Др. Редди'С Лабораторис Лимитед | Полиморфные формы энзалутамида и их получение |
EP3725778B1 (en) | 2012-09-11 | 2021-08-18 | Medivation Prostate Therapeutics LLC | Formulations of enzalutamide |
US11447506B2 (en) | 2016-05-09 | 2022-09-20 | Anacor Pharmaceuticals, Inc. | Crystal forms of crisaborole in free form and preparation method and use thereof |
MX2018013742A (es) * | 2016-05-09 | 2019-08-01 | Anacor Pharmaceuticals Inc | Formas cristalinas de crisaborol en forma libre, metodo de preparacion y uso de las mismas. |
CA3026885A1 (en) * | 2016-06-16 | 2017-12-21 | Xenon Pharmaceuticals Inc. | Solid state forms of spiro-oxindole compounds |
JP2019526637A (ja) * | 2016-09-06 | 2019-09-19 | インデナ・ソチエタ・ペル・アチオニ | 固体形態のインゲノール 3−(3,5−ジエチルイソオキサゾール−4−カルボキシラート)及びその調製方法 |
EA037868B1 (ru) | 2016-09-07 | 2021-05-28 | Атеа Фармасьютикалс, Инк. | 2'-замещенные-n6-замещенные пуриновые нуклеотиды для лечения вызванных рнк-вирусом заболеваний |
US10336679B2 (en) * | 2016-10-24 | 2019-07-02 | Syneurx International (Taiwan) Corp. | Polymorphic forms of sodium benzoate and uses thereof |
US11369579B2 (en) | 2016-10-24 | 2022-06-28 | Syneurx International (Taiwan) Corp. | Polymorphic forms of sodium benzoate and uses thereof |
JP7066728B2 (ja) | 2017-02-01 | 2022-05-13 | アテア ファーマシューティカルズ, インコーポレイテッド | C型肝炎ウイルスの治療のためのヌクレオチドヘミ硫酸塩 |
CN110446705B (zh) * | 2017-03-30 | 2023-04-14 | 默克专利股份公司 | (s)-[2-氯-4-氟-5-(7-吗啉-4-基喹唑啉-4-基)苯基]-(6-甲氧基-哒嗪-3-基)甲醇的固体形式 |
MX2020005348A (es) * | 2017-11-22 | 2020-08-13 | Agios Pharmaceuticals Inc | Formas cristalinas de la n-(4-(4-(ciclopropilmetil)piperazin-1-car bonil)fenil)quinolin-8-sulfonamida. |
CN112351799A (zh) | 2018-04-10 | 2021-02-09 | 阿堤亚制药公司 | 具有硬化的hcv感染患者的治疗 |
US10874687B1 (en) | 2020-02-27 | 2020-12-29 | Atea Pharmaceuticals, Inc. | Highly active compounds against COVID-19 |
WO2022176017A1 (ja) * | 2021-02-16 | 2022-08-25 | 大塚製薬株式会社 | 非晶質体及び当該非晶質体を含む組成物 |
Family Cites Families (8)
Publication number | Priority date | Publication date | Assignee | Title |
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US4304734A (en) * | 1980-10-16 | 1981-12-08 | Vysoka Skola Chemicko-Technologicka | 6-Amino-1-hydroxyhexylidene diphosphonic acid, salts and a process for production thereof |
US4922007A (en) | 1989-06-09 | 1990-05-01 | Merck & Co., Inc. | Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid or salts thereof |
ES2236737T3 (es) * | 1995-06-06 | 2005-07-16 | MERCK & CO., INC. | Formulaciones de sal de alendronato monosodico anhidro y su uso en el tratamiento de enfermedades oseas. |
US5853759A (en) * | 1996-05-17 | 1998-12-29 | Merck & Co.. Inc. | Effervescent alendronate formulation |
WO2000012517A1 (en) * | 1998-08-27 | 2000-03-09 | Teva Pharmaceutical Industries Ltd. | Novel hydrate forms of alendronate sodium, processes for manufacture thereof, and pharmaceutical compositions thereof |
US6160165A (en) * | 1998-12-10 | 2000-12-12 | Aesgen, Inc. | Method for preparation of disodium pamidronate |
WO2000034293A1 (en) | 1998-12-10 | 2000-06-15 | Aesgen, Inc. | Method for preparation of disodium pamidronate |
AU7902800A (en) * | 1999-10-26 | 2001-05-08 | A/S Gea Farmaceutisk Fabrik | Novel salts of 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid, their preparation and use |
-
2001
- 2001-10-18 GB GB0125081A patent/GB2383042A/en not_active Withdrawn
-
2002
- 2002-10-18 RU RU2004113306/04A patent/RU2334751C2/ru not_active IP Right Cessation
- 2002-10-18 MX MXPA04003549A patent/MXPA04003549A/es active IP Right Grant
- 2002-10-18 AT AT02801429T patent/ATE338761T1/de not_active IP Right Cessation
- 2002-10-18 BR BR0213398-9A patent/BR0213398A/pt not_active Withdrawn
- 2002-10-18 PT PT02801429T patent/PT1436303E/pt unknown
- 2002-10-18 AU AU2002334200A patent/AU2002334200B2/en not_active Ceased
- 2002-10-18 IL IL16136002A patent/IL161360A0/xx not_active IP Right Cessation
- 2002-10-18 NZ NZ532292A patent/NZ532292A/en not_active IP Right Cessation
- 2002-10-18 US US10/492,977 patent/US7112577B2/en not_active Expired - Fee Related
- 2002-10-18 WO PCT/GB2002/004730 patent/WO2003033508A1/en active IP Right Grant
- 2002-10-18 DE DE60214576T patent/DE60214576T2/de not_active Expired - Lifetime
- 2002-10-18 ES ES02801429T patent/ES2271375T3/es not_active Expired - Lifetime
- 2002-10-18 KR KR10-2004-7005768A patent/KR20040053186A/ko not_active Application Discontinuation
- 2002-10-18 CA CA002463815A patent/CA2463815C/en not_active Expired - Fee Related
- 2002-10-18 EP EP02801429A patent/EP1436303B1/en not_active Expired - Lifetime
- 2002-10-18 JP JP2003536247A patent/JP4490100B2/ja not_active Expired - Fee Related
-
2004
- 2004-04-16 EC EC2004005067A patent/ECSP045067A/es unknown
- 2004-04-16 TN TNP2004000067A patent/TNSN04067A1/en unknown
- 2004-04-21 ZA ZA200403024A patent/ZA200403024B/xx unknown
- 2004-06-04 CL CL200401372A patent/CL2004001372A1/es unknown
- 2004-11-09 HK HK04108787A patent/HK1066011A1/xx not_active IP Right Cessation
Also Published As
Publication number | Publication date |
---|---|
RU2334751C2 (ru) | 2008-09-27 |
TNSN04067A1 (en) | 2006-06-01 |
ECSP045067A (es) | 2004-07-23 |
CA2463815C (en) | 2009-04-07 |
US7112577B2 (en) | 2006-09-26 |
ES2271375T3 (es) | 2007-04-16 |
DE60214576T2 (de) | 2007-08-30 |
ZA200403024B (en) | 2005-03-30 |
JP4490100B2 (ja) | 2010-06-23 |
KR20040053186A (ko) | 2004-06-23 |
HK1066011A1 (en) | 2005-03-11 |
GB0125081D0 (en) | 2001-12-12 |
DE60214576D1 (de) | 2006-10-19 |
EP1436303A1 (en) | 2004-07-14 |
EP1436303B1 (en) | 2006-09-06 |
JP2005521636A (ja) | 2005-07-21 |
BR0213398A (pt) | 2005-01-11 |
WO2003033508A1 (en) | 2003-04-24 |
GB2383042A (en) | 2003-06-18 |
CA2463815A1 (en) | 2003-04-24 |
CL2004001372A1 (es) | 2005-05-06 |
NZ532292A (en) | 2005-07-29 |
PT1436303E (pt) | 2006-12-29 |
MXPA04003549A (es) | 2004-07-22 |
AU2002334200B2 (en) | 2008-04-03 |
IL161360A0 (en) | 2004-09-27 |
ATE338761T1 (de) | 2006-09-15 |
US20040259846A1 (en) | 2004-12-23 |
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Legal Events
Date | Code | Title | Description |
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MM4A | The patent is invalid due to non-payment of fees |
Effective date: 20121019 |