JPH08509697A - 活性物質としてジクロロメチレンジホスホン酸を含む、改良された生物利用性を有する錠剤 - Google Patents
活性物質としてジクロロメチレンジホスホン酸を含む、改良された生物利用性を有する錠剤Info
- Publication number
- JPH08509697A JPH08509697A JP6518431A JP51843194A JPH08509697A JP H08509697 A JPH08509697 A JP H08509697A JP 6518431 A JP6518431 A JP 6518431A JP 51843194 A JP51843194 A JP 51843194A JP H08509697 A JPH08509697 A JP H08509697A
- Authority
- JP
- Japan
- Prior art keywords
- tablets
- active substance
- tablet
- weight
- content
- 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.)
- Granted
Links
Classifications
-
- 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
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
- A61K47/38—Cellulose; 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
- A61K31/66—Phosphorus compounds
-
- 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
-
- 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
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Physical Education & Sports Medicine (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Description
Claims (1)
- 【特許請求の範囲】 1.活性物質クロドロン酸又は生理学的に耐性のその塩及び医薬的助剤として 微晶性セルロースの含有量を有する改良された生物利用性の錠剤。 2.錠剤の合計重量に対して5〜15重量%の微晶性セルロースの含有量を有 する請求の範囲第1項記載の錠剤。 3.200〜700mgのクロドロン酸の活性物質含有量を有する請求の範囲第1又は 2項記載の錠剤。 4.二ナトリウム塩の形で、好ましくは四水和物の形で前記活性物質を含む請 求の範囲第1〜3のいづれか1項記載の錠剤。 5.充填剤、特にコーンスターチ又はタルクをさらに含む請求の範囲第1〜4 のいづれか1項記載の錠剤。 6.滑剤及び砕解剤をさらに含む請求の範囲第1〜5のいづれか1項記載の錠 剤。 7.前記滑剤が、ステアリン酸の生理学的に耐性の塩、好ましくはステアリン 酸マグネシウムであり、そして前記砕解剤がナトリウムカルボキシメチルスター チである請求の範囲第6項記載の錠剤。 8.420〜460mgのクロドロン酸の活性物質含有量及び750〜850mg、好ましくは 790〜810mgの合計重量の錠剤を有する請求の範囲第1〜7のいづれか1項記載の 錠剤。 9.500〜530mgのクロドロン酸の活性物質含有量及び870〜970mg、好ましくは 900〜950mgの合計重量の錠剤を有する請求の範囲第1〜7のいづれか1項記載の 錠剤。 10.約200〜270mgのクロドロン酸の活性物質含有量及び350〜500mgの合計重量 の錠剤を有する請求の範囲第1〜7のいづれか1項記載の錠剤。 11.1〜3個の錠剤、好ましくは2個の錠剤の毎日の用量での投与のために請 求の範囲第8又は9項記載の錠剤30〜400個を含む医薬パック。 12.4〜8個の錠剤、好ましくは4個の錠剤の毎日の用量での投与のために請 求の範囲第10項記載の錠剤30〜400個を含む医薬パック。 13.活性物質の改良された生物利用性を有する錠剤を製造のためへの、活性物 質クロドロン酸又は生理学的に耐性のその塩及び医薬助剤としての微晶性セルロ ースの使用。 14.通常のサイズで2倍の効能を有する錠剤の製造のためへの請求の範囲第13 項記載の使用。 15.活性物質クロドロン酸又は生理学的に耐性のその塩の改良された生物利用 性を有する錠剤の製造方法であって、前記活性物質が微晶性セルロース及び所望 には、他の医薬助剤物質又はキャリヤー物質と一緒に、既知の方法に従って混合 され、そして錠剤に圧縮されることから成る方法。 16.前記活性物質が約4〜8重量%の充填剤と共に混合され、従来の結合剤と 共に顆粒化され、5〜15重量%の微晶性セルロース、3重量%までの砕解剤及び 6重量%までの滑剤が前記得られた顆粒と共に従来の混合装置で混合され、前記 顆粒が、前記混合工程の後に錠剤化され、そして所望には、その得られた錠剤コ アが活性物質の味覚を改良するために又はそれの開放性を遅延するために皮膜に より供給される請求の範囲第15項記載の方法。 17.前記活性物質が6〜7重量%の充填剤と共に顆粒化され、そして8〜12重 量%の微晶性セルロース、2重量%までの砕解剤及び3重量%までの滑剤が前記 顆粒と共に混合される請求の範囲第16項記載の方法。 18.コーンスターチ及び又はタルクが前記充填剤として使用される請求の範囲 第16又は17項記載の方法。 19.ステアリン酸マグネシウムが滑剤として使用され、そしてナトリウムカル ボキシメチルスターチが砕解剤として使用される請求の範囲第16〜18のいづれか 1項記載の方法。
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE9307393U DE9307393U1 (de) | 1993-05-15 | 1993-05-15 | Tablette mit verbesserter Bioverfügbarkeit, enthaltend Dichlormethylendiphosphonsäure als Wirkstoff |
DE4322057.6 | 1993-07-02 | ||
DE9307393.3U | 1993-07-02 | ||
DE19934322057 DE4322057A1 (de) | 1993-07-02 | 1993-07-02 | Tablette mit verbesserter Bioverfügbarkeit enthaltend Dichlormethylendiphosphonsäure als Wirkstoff |
PCT/EP1993/001967 WO1994026310A1 (de) | 1993-05-15 | 1993-07-24 | Tablette mit verbesserter bioverfügbarkeit enthaltend dichlormethylendiphosphonsäure als wirkstoff |
Publications (2)
Publication Number | Publication Date |
---|---|
JPH08509697A true JPH08509697A (ja) | 1996-10-15 |
JP3699110B2 JP3699110B2 (ja) | 2005-09-28 |
Family
ID=25927331
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP51843194A Expired - Fee Related JP3699110B2 (ja) | 1993-05-15 | 1993-07-24 | 活性物質としてジクロロメチレンジホスホン酸を含む、改良された生物利用性を有する錠剤 |
Country Status (25)
Country | Link |
---|---|
US (1) | US5650168A (ja) |
EP (2) | EP0697890A1 (ja) |
JP (1) | JP3699110B2 (ja) |
KR (1) | KR100263284B1 (ja) |
CN (1) | CN1041797C (ja) |
AT (2) | ATE128363T1 (ja) |
AU (1) | AU687744B2 (ja) |
BR (1) | BR9307859A (ja) |
CA (1) | CA2162470C (ja) |
CZ (1) | CZ287984B6 (ja) |
DE (1) | DE59300688D1 (ja) |
DK (1) | DK0625355T5 (ja) |
ES (1) | ES2065313T5 (ja) |
FI (1) | FI111519B (ja) |
GR (2) | GR940300095T1 (ja) |
HU (1) | HU220872B1 (ja) |
IL (1) | IL106743A (ja) |
NO (1) | NO307548B1 (ja) |
NZ (1) | NZ254765A (ja) |
PL (1) | PL173026B1 (ja) |
RU (1) | RU2134103C1 (ja) |
SK (1) | SK281193B6 (ja) |
TW (1) | TW350772B (ja) |
UA (1) | UA39884C2 (ja) |
WO (1) | WO1994026310A1 (ja) |
Families Citing this family (14)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
FI94926C (fi) | 1993-11-12 | 1995-11-27 | Leiras Oy | Menetelmä klodronaattivalmisteen valmistamiseksi |
DE19615812A1 (de) * | 1996-04-20 | 1997-10-23 | Boehringer Mannheim Gmbh | Pharmazeutische Zubereitung enthaltend Diphosphonsäuren zur oralen Applikation |
DE19719680A1 (de) | 1997-05-09 | 1998-11-19 | Boehringer Mannheim Gmbh | Verwendung von Diphosphonsäuren zur präventiven Behandlung von Spätfolgen bei Harnblasenerweiterung oder Harnblasenersatz |
FI109088B (fi) * | 1997-09-19 | 2002-05-31 | Leiras Oy | Tabletti ja menetelmä sen valmistamiseksi |
EP0998932A1 (de) | 1998-10-09 | 2000-05-10 | Boehringer Mannheim Gmbh | Feste pharmazeutische Darreichungsform enthaltend Diphosphonsäure oder deren Salze und Verfahren zu ihrer Herstellung |
SE9901272D0 (sv) * | 1999-04-09 | 1999-04-09 | Astra Ab | New improved formulation |
CZ289261B6 (cs) * | 2000-07-11 | 2001-12-12 | Léčiva, A.S. | Tableta vyrobitelná přímým tabletováním, obsahující aktivní látku kyselinu 4-amino-1-hydroxybutyliden-1,1-bisfosfonovou, a způsob její výroby |
US8163306B2 (en) * | 2003-09-19 | 2012-04-24 | Sun Pharma Advanced Research Company | Oral drug delivery system |
US10213387B2 (en) | 2003-09-19 | 2019-02-26 | Sun Pharma Advanced Research Company Ltd. | Oral drug delivery system |
US10226428B2 (en) | 2003-09-19 | 2019-03-12 | Sun Pharma Advanced Research Company Ltd. | Oral drug delivery system |
US7151400B2 (en) * | 2004-07-13 | 2006-12-19 | Taiwan Semiconductor Manufacturing Company, Ltd. | Boost-biased level shifter |
CN100370972C (zh) * | 2006-01-10 | 2008-02-27 | 北京申科联华科技有限公司 | 一种具有益气养阴、活血复脉功效的片剂及制备方法 |
CA2694638A1 (en) * | 2007-08-02 | 2009-02-05 | Teijin Pharma Limited | Preventive or therapeutic agent for diseases caused by abnormal bone metbolism |
WO2009122431A2 (en) * | 2008-02-15 | 2009-10-08 | Sun Pharma Advanced Research Company Ltd., | Oral controlled release tablet |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE2813121A1 (de) * | 1977-03-29 | 1978-10-12 | Procter & Gamble | Verwendung von dichlormethan-diphosphonatverbindungen bei der bekaempfung von collagen-erkrankungen und zur wundheilung |
US4634691A (en) * | 1980-10-07 | 1987-01-06 | The Procter & Gamble Company | Method for inhibiting tumor metastasis |
US4517179A (en) * | 1983-04-29 | 1985-05-14 | Pennwalt Corporation | Rapid dissolving, uniform drug compositions and their preparation |
SE457326B (sv) * | 1986-02-14 | 1988-12-19 | Lejus Medical Ab | Foerfarande foer framstaellning av en snabbt soenderfallande kaerna innehaallande bl a mikrokristallin cellulosa |
ATE60711T1 (de) * | 1986-12-20 | 1991-02-15 | Boehringer Mannheim Gmbh | Clodronat-haltige arzneimittel und verfahren zur herstellung derselben. |
DE3804686A1 (de) * | 1988-02-15 | 1989-08-24 | Henkel Kgaa | Arzneimittel mit einer kombination von cytostatika bzw. hormontherapeutika und phosphonoderivaten |
FR2629716B1 (fr) * | 1988-04-07 | 1991-07-19 | Sanofi Sa | Composition pharmaceutique pour administration orale a base d'un derive d'acide diphosphonique |
FI83421C (fi) † | 1989-06-21 | 1991-07-10 | Huhtamaeki Oy | Foerfarande foer framstaellning av farmakologiskt anvaendbara metylenbisfosfonsyraderivat. |
DK0573604T3 (da) * | 1991-02-26 | 1995-05-29 | Procter & Gamble Pharma | Fremgangsmåde til behandling af osteoporosis |
SE501389C2 (sv) * | 1992-04-24 | 1995-01-30 | Leiras Oy | Farmaceutiskt preparat och förfarande för dess framställning |
AU5953894A (en) * | 1992-12-23 | 1994-07-19 | Merck & Co., Inc. | Bisphosphonate/estrogen therapy for treating and preventing bone loss |
-
1993
- 1993-07-24 AU AU47020/93A patent/AU687744B2/en not_active Expired
- 1993-07-24 DK DK93111827T patent/DK0625355T5/da active
- 1993-07-24 EP EP93917636A patent/EP0697890A1/de not_active Withdrawn
- 1993-07-24 ES ES93111827T patent/ES2065313T5/es not_active Expired - Lifetime
- 1993-07-24 JP JP51843194A patent/JP3699110B2/ja not_active Expired - Fee Related
- 1993-07-24 UA UA95114854A patent/UA39884C2/uk unknown
- 1993-07-24 DE DE59300688T patent/DE59300688D1/de not_active Expired - Lifetime
- 1993-07-24 HU HU9403160A patent/HU220872B1/hu unknown
- 1993-07-24 RU RU95121748A patent/RU2134103C1/ru active
- 1993-07-24 KR KR1019950705094A patent/KR100263284B1/ko not_active IP Right Cessation
- 1993-07-24 BR BR9307859A patent/BR9307859A/pt not_active Application Discontinuation
- 1993-07-24 US US08/537,853 patent/US5650168A/en not_active Expired - Lifetime
- 1993-07-24 SK SK48-95A patent/SK281193B6/sk not_active IP Right Cessation
- 1993-07-24 PL PL93307133A patent/PL173026B1/pl unknown
- 1993-07-24 NZ NZ254765A patent/NZ254765A/en not_active IP Right Cessation
- 1993-07-24 EP EP93111827A patent/EP0625355B2/de not_active Expired - Lifetime
- 1993-07-24 AT AT93111827T patent/ATE128363T1/de active
- 1993-07-24 WO PCT/EP1993/001967 patent/WO1994026310A1/de not_active Application Discontinuation
- 1993-07-24 CZ CZ1995100A patent/CZ287984B6/cs not_active IP Right Cessation
- 1993-07-24 CA CA002162470A patent/CA2162470C/en not_active Expired - Lifetime
- 1993-08-19 IL IL10674393A patent/IL106743A/en not_active IP Right Cessation
- 1993-09-10 TW TW082106635A patent/TW350772B/zh not_active IP Right Cessation
- 1993-09-23 CN CN93118149A patent/CN1041797C/zh not_active Expired - Lifetime
-
1994
- 1994-05-13 AT AT0007494U patent/AT128U1/de not_active IP Right Cessation
- 1994-11-11 FI FI945313A patent/FI111519B/fi not_active IP Right Cessation
- 1994-11-17 NO NO944405A patent/NO307548B1/no not_active IP Right Cessation
-
1995
- 1995-01-31 GR GR940300095T patent/GR940300095T1/el unknown
- 1995-09-28 GR GR950402574T patent/GR3017547T3/el unknown
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