JP2007131542A - 安定化されたカベルゴリン固形製剤 - Google Patents
安定化されたカベルゴリン固形製剤 Download PDFInfo
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- JP2007131542A JP2007131542A JP2005323402A JP2005323402A JP2007131542A JP 2007131542 A JP2007131542 A JP 2007131542A JP 2005323402 A JP2005323402 A JP 2005323402A JP 2005323402 A JP2005323402 A JP 2005323402A JP 2007131542 A JP2007131542 A JP 2007131542A
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- cabergoline
- talc
- mannitol
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- 238000002360 preparation method Methods 0.000 title claims abstract description 26
- KORNTPPJEAJQIU-KJXAQDMKSA-N Cabaser Chemical compound C1=CC([C@H]2C[C@H](CN(CC=C)[C@@H]2C2)C(=O)N(CCCN(C)C)C(=O)NCC)=C3C2=CNC3=C1 KORNTPPJEAJQIU-KJXAQDMKSA-N 0.000 title claims abstract description 22
- 229960004596 cabergoline Drugs 0.000 title claims abstract description 22
- 239000007787 solid Substances 0.000 title claims abstract description 14
- 239000000454 talc Substances 0.000 claims abstract description 21
- 229910052623 talc Inorganic materials 0.000 claims abstract description 21
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims abstract description 19
- 229930195725 Mannitol Natural products 0.000 claims abstract description 19
- 239000000594 mannitol Substances 0.000 claims abstract description 19
- 235000010355 mannitol Nutrition 0.000 claims abstract description 19
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims description 17
- 229960003136 leucine Drugs 0.000 claims description 9
- 239000004395 L-leucine Substances 0.000 claims description 8
- 235000019454 L-leucine Nutrition 0.000 claims description 8
- 239000000314 lubricant Substances 0.000 claims description 6
- 238000003860 storage Methods 0.000 abstract description 4
- 238000013329 compounding Methods 0.000 abstract 1
- 238000000354 decomposition reaction Methods 0.000 abstract 1
- 230000000052 comparative effect Effects 0.000 description 5
- 239000000546 pharmaceutical excipient Substances 0.000 description 5
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 4
- 101710150697 Inositol monophosphatase 1 Proteins 0.000 description 4
- 101710126181 Insulin-like growth factor 2 mRNA-binding protein 1 Proteins 0.000 description 4
- 102100029083 Minor histocompatibility antigen H13 Human genes 0.000 description 4
- 229960004977 anhydrous lactose Drugs 0.000 description 4
- 239000000203 mixture Substances 0.000 description 4
- 150000003797 alkaloid derivatives Chemical class 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 229960003133 ergot alkaloid Drugs 0.000 description 3
- 238000009472 formulation Methods 0.000 description 3
- 239000008187 granular material Substances 0.000 description 3
- 238000005469 granulation Methods 0.000 description 3
- 230000003179 granulation Effects 0.000 description 3
- 238000000034 method Methods 0.000 description 3
- 239000011148 porous material Substances 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 2
- 239000000654 additive Substances 0.000 description 2
- 239000007857 degradation product Substances 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000003814 drug Substances 0.000 description 2
- 239000002245 particle Substances 0.000 description 2
- 239000000047 product Substances 0.000 description 2
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- 102000015554 Dopamine receptor Human genes 0.000 description 1
- 108050004812 Dopamine receptor Proteins 0.000 description 1
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- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 description 1
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 description 1
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- 239000004472 Lysine Substances 0.000 description 1
- 208000018737 Parkinson disease Diseases 0.000 description 1
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- 239000004480 active ingredient Substances 0.000 description 1
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- 230000015556 catabolic process Effects 0.000 description 1
- 210000003169 central nervous system Anatomy 0.000 description 1
- 238000007796 conventional method Methods 0.000 description 1
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- 238000007908 dry granulation Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
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- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 239000008267 milk Substances 0.000 description 1
- 210000004080 milk Anatomy 0.000 description 1
- 235000013336 milk Nutrition 0.000 description 1
- 239000011812 mixed powder Substances 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 230000001766 physiological effect Effects 0.000 description 1
- 150000003839 salts Chemical class 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 238000013112 stability test Methods 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
Landscapes
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
【解決手段】カベルゴリンにマンニトール及びタルクを配合してなる安定な経口固形製剤。
Description
更にタルクを滑沢剤としてではなく賦形剤として配合した固形製剤が湿度に対してより一層優れた安定性を示すことを見出し本発明を完成した。
実施例1
1錠中
カベルゴリン 0.25mg
マンニトール 74.58mg
タルク 1.67mg
L−ロイシン 3.5mg
合計 80mg
1錠中
カベルゴリン 0.25mg
マンニトール 76.25mg
L−ロイシン 3.5mg
合計 80mg
1錠中
カベルゴリン 0.25mg
無水乳糖 76.25mg
L−ロイシン 3.5mg
合計 80mg
得られた製剤をPTP包装とした後40℃75%RHで2週間保存し、錠剤中に含まれるカベルゴリンの分解物 1−[(6aR,9R,10aR)−7−アリル−4,6,6a,7,8,9,10,10a−オクタヒドロインドロ[4,3−fg]キノリン−9−カルボン酸(以下、IMP−1と称する)の量を高速液体クロマトグラフィーにより測定した。
Claims (3)
- カベルゴリンにマンニトール及びタルクを配合してなる安定な経口固形製剤。
- タルクの配合量が製剤1重量部に対して約0.05〜10重量%である請求項1記載の安定な経口固形製剤。
- カベルゴリンにマンニトールおよびタルクを配合し、L−ロイシンを滑沢剤として混合し、直接打錠してなる安定な経口固形製剤。
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2005323402A JP4691434B2 (ja) | 2005-11-08 | 2005-11-08 | 安定化されたカベルゴリン固形製剤 |
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2005323402A JP4691434B2 (ja) | 2005-11-08 | 2005-11-08 | 安定化されたカベルゴリン固形製剤 |
Publications (2)
Publication Number | Publication Date |
---|---|
JP2007131542A true JP2007131542A (ja) | 2007-05-31 |
JP4691434B2 JP4691434B2 (ja) | 2011-06-01 |
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Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2005323402A Expired - Fee Related JP4691434B2 (ja) | 2005-11-08 | 2005-11-08 | 安定化されたカベルゴリン固形製剤 |
Country Status (1)
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JP (1) | JP4691434B2 (ja) |
Cited By (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2014163132A1 (ja) * | 2013-04-04 | 2014-10-09 | 第一三共株式会社 | アミノカルボン酸の塩の固形組成物 |
WO2015156302A1 (ja) * | 2014-04-09 | 2015-10-15 | ゴールドクレスト医薬研究所株式会社 | 皮膚症状の改善剤、育毛剤又はスリミング剤 |
US10561628B2 (en) | 2015-03-19 | 2020-02-18 | Daiichi Sankyo Company, Limited | Solid preparation including antioxidant |
US10603285B2 (en) | 2015-03-19 | 2020-03-31 | Daiichi Sankyo Company, Limited | Solid preparation including colorant |
CN114732791A (zh) * | 2022-03-17 | 2022-07-12 | 成都倍特药业股份有限公司 | 一种含有卡麦角林的组合物及其制备方法和用途 |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH0624987A (ja) * | 1992-07-09 | 1994-02-01 | Tanabe Seiyaku Co Ltd | ニセルゴリン含有錠剤 |
WO2002049608A1 (en) * | 2000-12-21 | 2002-06-27 | Par Pharmaceutical Inc. | Cabergoline pharmaceutical compositions and methods of use thereof |
WO2007049626A1 (ja) * | 2005-10-27 | 2007-05-03 | Kissei Pharmaceutical Co., Ltd. | カベルゴリン含有経口固形製剤 |
-
2005
- 2005-11-08 JP JP2005323402A patent/JP4691434B2/ja not_active Expired - Fee Related
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPH0624987A (ja) * | 1992-07-09 | 1994-02-01 | Tanabe Seiyaku Co Ltd | ニセルゴリン含有錠剤 |
WO2002049608A1 (en) * | 2000-12-21 | 2002-06-27 | Par Pharmaceutical Inc. | Cabergoline pharmaceutical compositions and methods of use thereof |
WO2007049626A1 (ja) * | 2005-10-27 | 2007-05-03 | Kissei Pharmaceutical Co., Ltd. | カベルゴリン含有経口固形製剤 |
Cited By (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2014163132A1 (ja) * | 2013-04-04 | 2014-10-09 | 第一三共株式会社 | アミノカルボン酸の塩の固形組成物 |
JP5627062B1 (ja) * | 2013-04-04 | 2014-11-19 | 第一三共株式会社 | アミノカルボン酸の塩の固形組成物 |
US9675570B2 (en) | 2013-04-04 | 2017-06-13 | Daiichi Sanky Company, Limited | Solid compositions comprising a salt of aminocarboxylic acid |
WO2015156302A1 (ja) * | 2014-04-09 | 2015-10-15 | ゴールドクレスト医薬研究所株式会社 | 皮膚症状の改善剤、育毛剤又はスリミング剤 |
JP6026706B2 (ja) * | 2014-04-09 | 2016-11-16 | ゴールドクレスト医薬研究所株式会社 | 皮膚症状の改善剤、育毛剤又はスリミング剤 |
US10561628B2 (en) | 2015-03-19 | 2020-02-18 | Daiichi Sankyo Company, Limited | Solid preparation including antioxidant |
US10603285B2 (en) | 2015-03-19 | 2020-03-31 | Daiichi Sankyo Company, Limited | Solid preparation including colorant |
CN114732791A (zh) * | 2022-03-17 | 2022-07-12 | 成都倍特药业股份有限公司 | 一种含有卡麦角林的组合物及其制备方法和用途 |
CN114732791B (zh) * | 2022-03-17 | 2023-09-29 | 成都倍特药业股份有限公司 | 一种含有卡麦角林的组合物及其制备方法和用途 |
Also Published As
Publication number | Publication date |
---|---|
JP4691434B2 (ja) | 2011-06-01 |
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