JP4343693B2 - Lhrhアンタゴニストの注入溶液 - Google Patents
Lhrhアンタゴニストの注入溶液 Download PDFInfo
- Publication number
- JP4343693B2 JP4343693B2 JP2003546920A JP2003546920A JP4343693B2 JP 4343693 B2 JP4343693 B2 JP 4343693B2 JP 2003546920 A JP2003546920 A JP 2003546920A JP 2003546920 A JP2003546920 A JP 2003546920A JP 4343693 B2 JP4343693 B2 JP 4343693B2
- Authority
- JP
- Japan
- Prior art keywords
- gluconic acid
- lhrh antagonist
- solution
- tween
- mannitol
- Prior art date
- Legal status (The legal status 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 status listed.)
- Expired - Lifetime
Links
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
- A61K9/08—Solutions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K38/00—Medicinal preparations containing peptides
- A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
- A61K38/08—Peptides having 5 to 11 amino acids
- A61K38/09—Luteinising hormone-releasing hormone [LHRH], i.e. Gonadotropin-releasing hormone [GnRH]; Related peptides
-
- 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
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
- A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/10—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH
- A61P5/12—Drugs for disorders of the endocrine system of the posterior pituitary hormones, e.g. oxytocin, ADH for decreasing, blocking or antagonising the activity of the posterior pituitary hormones
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/36—Antigestagens
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Endocrinology (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Reproductive Health (AREA)
- Diabetes (AREA)
- Gastroenterology & Hepatology (AREA)
- Immunology (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Gynecology & Obstetrics (AREA)
- Pregnancy & Childbirth (AREA)
- Dermatology (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Manufacturing Of Micro-Capsules (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
Description
例1
セトロレリックス 500mg
ツイーン80 2g
グルコン酸δ−ラクトン 2.4g
マンニトール 95g
を注入用水と2リットルに混合し、均一な溶液を得た。引き続き溶液を滅菌濾過し、アンプルに分散した。アンプルの純度(HPLC)、含有量(HPLC)、pHおよび凝結(不透明度)を開始時におよび2〜8℃で6ヶ月保存後および25℃/相対湿度60%で6ヶ月保存後に検査した。
D−63153 約500mg
ツイーン80 約100mg
マンニトール 約475mg
をグルコン酸δ−ラクトン水性飽和溶液を使用してpH約2.5に調節した。約50mlの容積が得られた。透明な溶液が得られるまで混合物を攪拌した。
溶液の不透明度は最初にFTU2.4であった。24時間後FTU2.1が測定された。溶液の純度特性および含有量は変化しなかった(HPLC)。
Ac−D−Nal−pCl−D−Phe−3−D−Pal−Ser−N−Me−Tyr−D−H−Cit−Nle−Arg−Pro−D−Ala−NH2
例3
テベレリックス 約100mg
ツイーン80 約100mg
マンニトール 約475mg
をグルコン酸δ−ラクトン水性飽和溶液を使用してpH約2.5に調節した。約10mlの容積が得られた。透明な溶液が得られるまで混合物を攪拌した。
溶液の不透明度は最初にFTU6.8であった。24時間後FTU8.4が測定された。溶液の純度特性および含有量は変化しなかった(HPLC)。
Ac−D−Nal−pCl−D−Phe−3−D−Pal−Ser−Tyr−D−H−Cit−Leu−iPr−Lys−Pro−D−Ala−NH2
Claims (6)
- グルコン酸、増量剤および場合により界面活性剤を含有する、黄体形成ホルモン放出ホルモンLHRHアンタゴニストの水性注入溶液において、セトロレリックス、テベレリックス、D−63153(Ac−D−Nal−pCl−D−Phe−3−D−Pal−Ser−N−Me−Tyr−D−H−Cit−Nle−Arg−Pro−D−Ala−NH2)、ガニレリックス、アバレリックス、アンチドまたはアザリンBがLHRHアンタゴニストとして使用され、かつ、グルコン酸が、LHRHアンタゴニストの量に対して等モル量よりも多く存在し、グルコン酸がグルコン酸δ−ラクトンの形で添加され、マンニトールが増量剤として使用され、かつ、場合によりツイーン80が界面活性剤として添加されることを特徴とするLHRHアンタゴニストの水性注入溶液。
- 界面活性剤としてツイーン(Tween)80を更に含有する請求項1記載のLHRHアンタゴニストの水性注入溶液。
- 注入用水2リットル中のセトロレリックス500mg、グルコン酸δ−ラクトン2.4g、ツイーン80 2.0g、マンニトール95.0gからなる請求項1記載のLHRHアンタゴニストの水性注入溶液。
- グルコン酸δ−ラクトン飽和溶液を使用して50mlに調節したD−63153 500mg、ツイーン80 100mg、マンニトール475mgからなる請求項1記載のLHRHアンタゴニストの水性注入溶液。
- グルコン酸δ−ラクトン飽和溶液を使用して10mlに調節した、テベレリックス100mg、ツイーン80 100mg、マンニトール475mgからなる請求項1記載のLHRHアンタゴニストの水性注入溶液。
- 請求項1から5までのいずれか1項記載のLHRHアンタゴニストの水性注入溶液を製造する方法において、選択的に
LHRHアンタゴニスト、グルコン酸δ−ラクトンの形のグルコン酸(グルコン酸は、LHRHアンタゴニストの量に対して等モル量よりも多く存在する)、増量剤としてのマンニトールおよび場合により界面活性剤としてのツイーン80を注入用水に溶解し、均一化し、注入目的のために処理するか、または
LHRHアンタゴニスト、増量剤としてのマンニトールおよび場合により界面活性剤としてのツイーン80をグルコン酸δ−ラクトンの飽和水溶液を使用して溶解し、均一化し、注入目的のために処理する
ことを特徴とする請求項1から5までのいずれか1項記載のLHRHアンタゴニストの水性注入溶液を製造する方法。
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE10157628A DE10157628A1 (de) | 2001-11-26 | 2001-11-26 | Injektionslösung eines LHRH-Antagonisten |
PCT/EP2002/012798 WO2003045419A1 (de) | 2001-11-26 | 2002-11-15 | Injektionslösung eines lhrh-antagonisten |
Publications (3)
Publication Number | Publication Date |
---|---|
JP2005510544A JP2005510544A (ja) | 2005-04-21 |
JP2005510544A5 JP2005510544A5 (ja) | 2005-12-22 |
JP4343693B2 true JP4343693B2 (ja) | 2009-10-14 |
Family
ID=7706799
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2003546920A Expired - Lifetime JP4343693B2 (ja) | 2001-11-26 | 2002-11-15 | Lhrhアンタゴニストの注入溶液 |
Country Status (33)
Country | Link |
---|---|
EP (1) | EP1448221B1 (ja) |
JP (1) | JP4343693B2 (ja) |
KR (1) | KR100936636B1 (ja) |
CN (1) | CN100404068C (ja) |
AR (1) | AR037424A1 (ja) |
AT (1) | ATE350050T1 (ja) |
AU (1) | AU2002365504B2 (ja) |
BR (1) | BRPI0214412B8 (ja) |
CO (1) | CO5580793A2 (ja) |
CY (1) | CY1106401T1 (ja) |
DE (2) | DE10157628A1 (ja) |
DK (1) | DK1448221T3 (ja) |
EA (1) | EA010787B1 (ja) |
ES (1) | ES2276970T3 (ja) |
GE (1) | GEP20063861B (ja) |
HK (1) | HK1073078A1 (ja) |
HR (1) | HRP20040587B1 (ja) |
HU (1) | HU230992B1 (ja) |
IL (2) | IL161894A0 (ja) |
IS (1) | IS2725B (ja) |
ME (1) | ME00499B (ja) |
MX (1) | MXPA04005018A (ja) |
NO (1) | NO333364B1 (ja) |
NZ (1) | NZ533712A (ja) |
PL (1) | PL206199B1 (ja) |
PT (1) | PT1448221E (ja) |
RS (1) | RS51408B (ja) |
RU (1) | RU2322969C2 (ja) |
SI (1) | SI1448221T1 (ja) |
TW (1) | TWI312283B (ja) |
UA (1) | UA81612C2 (ja) |
WO (1) | WO2003045419A1 (ja) |
ZA (1) | ZA200404051B (ja) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7658938B2 (en) | 1999-02-22 | 2010-02-09 | Merrion Reasearch III Limited | Solid oral dosage form containing an enhancer |
US8119159B2 (en) | 1999-02-22 | 2012-02-21 | Merrion Research Iii Limited | Solid oral dosage form containing an enhancer |
ES2426445T3 (es) | 2006-04-07 | 2013-10-23 | Merrion Research Iii Limited | Forma de dosificación oral sólida que contiene un potenciador |
US8999383B2 (en) * | 2008-05-07 | 2015-04-07 | Merrion Research Iii Limited | Compositions of GnRH related compounds and processes of preparation |
US9089484B2 (en) | 2010-03-26 | 2015-07-28 | Merrion Research Iii Limited | Pharmaceutical compositions of selective factor Xa inhibitors for oral administration |
WO2012094598A2 (en) | 2011-01-07 | 2012-07-12 | Merrion Research Iii Limited | Pharmaceutical compositions of iron for oral administration |
CN103690560B (zh) * | 2013-12-17 | 2016-08-17 | 辽宁海思科制药有限公司 | 一种转化糖电解质注射液药物组合物及其制备方法 |
US10265384B2 (en) | 2015-01-29 | 2019-04-23 | Novo Nordisk A/S | Tablets comprising GLP-1 agonist and enteric coating |
RU2614234C2 (ru) * | 2015-03-31 | 2017-03-23 | Федеральное государственное бюджетное учреждение науки Институт общей генетики им. Н.И. Вавилова Российской академии наук (ИОГЕН РАН) | Фармацевтическая композиция на основе 3-(4-Метилимидазол-1-ил)имидазо[1,2-b][1,2,4,5]тетразина в качестве противоопухолевого средства |
KR20210157482A (ko) * | 2017-01-30 | 2021-12-28 | 안테브 리미티드 | 적어도 하나의 gnrh 길항제를 포함하는 조성물 |
DK3811927T3 (da) | 2019-10-24 | 2021-12-13 | Sun Pharmaceutical Ind Ltd | Stabil, parenteral doseringsform af cetrorelixacetat |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4800191A (en) * | 1987-07-17 | 1989-01-24 | Schally Andrew Victor | LHRH antagonists |
US5300492A (en) * | 1988-02-10 | 1994-04-05 | Tap Pharmaceuticals | LHRH analogs |
US5140009A (en) * | 1988-02-10 | 1992-08-18 | Tap Pharmaceuticals, Inc. | Octapeptide LHRH antagonists |
KR100772852B1 (ko) * | 1999-09-23 | 2007-11-02 | 젠타리스 게엠베하 | 자궁내막증 치료용 약제학적 조성물 |
DE10024451A1 (de) * | 2000-05-18 | 2001-11-29 | Asta Medica Ag | Pharmazeutische Darreichungsform für Peptide, Verfahren zu deren Herstellung und Verwendung |
-
2001
- 2001-11-26 DE DE10157628A patent/DE10157628A1/de not_active Withdrawn
-
2002
- 2002-11-15 EP EP02790384A patent/EP1448221B1/de not_active Expired - Lifetime
- 2002-11-15 IL IL16189402A patent/IL161894A0/xx unknown
- 2002-11-15 UA UA20040503816A patent/UA81612C2/ru unknown
- 2002-11-15 GE GE5568A patent/GEP20063861B/en unknown
- 2002-11-15 WO PCT/EP2002/012798 patent/WO2003045419A1/de active IP Right Grant
- 2002-11-15 ME MEP-2008-800A patent/ME00499B/me unknown
- 2002-11-15 JP JP2003546920A patent/JP4343693B2/ja not_active Expired - Lifetime
- 2002-11-15 RU RU2004119821/15A patent/RU2322969C2/ru active
- 2002-11-15 DE DE50209193T patent/DE50209193D1/de not_active Expired - Lifetime
- 2002-11-15 RS YUP-449/04A patent/RS51408B/sr unknown
- 2002-11-15 PL PL369548A patent/PL206199B1/pl unknown
- 2002-11-15 KR KR1020047007807A patent/KR100936636B1/ko active IP Right Grant
- 2002-11-15 CN CNB028234901A patent/CN100404068C/zh not_active Expired - Lifetime
- 2002-11-15 MX MXPA04005018A patent/MXPA04005018A/es active IP Right Grant
- 2002-11-15 NZ NZ533712A patent/NZ533712A/en not_active IP Right Cessation
- 2002-11-15 BR BRPI0214412A patent/BRPI0214412B8/pt not_active IP Right Cessation
- 2002-11-15 EA EA200400742A patent/EA010787B1/ru unknown
- 2002-11-15 ES ES02790384T patent/ES2276970T3/es not_active Expired - Lifetime
- 2002-11-15 HU HU0401986A patent/HU230992B1/hu unknown
- 2002-11-15 AT AT02790384T patent/ATE350050T1/de active
- 2002-11-15 PT PT02790384T patent/PT1448221E/pt unknown
- 2002-11-15 DK DK02790384T patent/DK1448221T3/da active
- 2002-11-15 SI SI200230505T patent/SI1448221T1/sl unknown
- 2002-11-15 AU AU2002365504A patent/AU2002365504B2/en not_active Expired
- 2002-11-20 TW TW091133846A patent/TWI312283B/zh not_active IP Right Cessation
- 2002-11-25 AR ARP020104523A patent/AR037424A1/es not_active Application Discontinuation
-
2004
- 2004-05-06 IS IS7251A patent/IS2725B/is unknown
- 2004-05-10 IL IL161894A patent/IL161894A/en active IP Right Grant
- 2004-05-14 CO CO04044748A patent/CO5580793A2/es not_active Application Discontinuation
- 2004-05-25 ZA ZA2004/04051A patent/ZA200404051B/en unknown
- 2004-06-11 NO NO20042449A patent/NO333364B1/no not_active IP Right Cessation
- 2004-06-24 HR HR20040587A patent/HRP20040587B1/xx not_active IP Right Cessation
-
2005
- 2005-07-11 HK HK05105809.5A patent/HK1073078A1/xx not_active IP Right Cessation
-
2007
- 2007-03-20 CY CY20071100391T patent/CY1106401T1/el unknown
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