JP2015529215A - アゴメラチンの安定化非晶形、その調製方法及びこれを含有する医薬組成物 - Google Patents
アゴメラチンの安定化非晶形、その調製方法及びこれを含有する医薬組成物 Download PDFInfo
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- JP2015529215A JP2015529215A JP2015530452A JP2015530452A JP2015529215A JP 2015529215 A JP2015529215 A JP 2015529215A JP 2015530452 A JP2015530452 A JP 2015530452A JP 2015530452 A JP2015530452 A JP 2015530452A JP 2015529215 A JP2015529215 A JP 2015529215A
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- amorphous form
- stabilized amorphous
- agomelatin
- agomelatine
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Abstract
Description
アゴメラチン及び選択されたポリマーを、溶媒3mlと共に10mlバイアルに入れた。この混合物を、溶解が完了して均一溶液が得られるまで、40℃で30分間撹拌した。40℃で減圧下で30分間溶媒を留去した。得られた残渣を最後に周囲温度(20℃)で一晩(12時間)真空乾燥することにより、アゴメラチンの安定化非晶形を得た。各試験では、40℃及び75%RHで、40℃及び75%RHに続いて50℃で、更にまた70℃での変性条件下で非晶形の安定性を試験した。
アゴメラチン及びポリマーは、Turbula型ミキサー中で10分間プレブレンドした。得られた混合物を、HAAKE Minilab II Microcompounder型(ThermoFisher)の円錐形ローター押出機(直径5/14mm)に手作業で入れた。押出速度は100rpmとした。
得られた製剤の溶解度試験を、Crystal 16(登録商標)型装置を用いてpH6.8緩衝液中で25℃で4時間かけて700rpmの撹拌速度で実施した。種々の濃度を試験して、不溶性粒子の存在を比濁分析法の検出により監視した。参考として、このような条件下のアゴメラチンの溶解度は、0.14mg/mlであった。
実施例42
それぞれアゴメラチン25mgを含有するカプセル剤1000個の調製のための処方:
アゴメラチン 25g
Eudragit L100-55 25g
それぞれアゴメラチン25mgを含有するカプセル剤1000個の調製のための処方:
アゴメラチン 25g
Plasdone S630 58g
それぞれアゴメラチン25mgを含有する錠剤1000個の調製のための処方:
実施例36の成形品 50g
トウモロコシデンプン 10g
乳糖 20g
ステアリン酸マグネシウム 0.5g
シリカ 0.25g
ヒドロキシプロピルセルロース 2.25g
Claims (26)
- アゴメラチンが、マトリックス中に分散されていることを特徴とする、請求項1に記載のアゴメラチンの安定化非晶形。
- 使用されるマトリックスが、有機ポリマーであることを特徴とする、請求項2に記載のアゴメラチンの安定化非晶形。
- 使用されるマトリックスが、メタクリル酸化合物又はビニル若しくはセルロース系ポリマーであることを特徴とする、請求項2又は請求項3に記載のアゴメラチンの安定化非晶形。
- 使用されるマトリックスが、Eudragit L100であることを特徴とする、請求項4に記載のアゴメラチンの安定化非晶形。
- 使用されるマトリックスが、Eudragit L100-55であることを特徴とする、請求項4に記載のアゴメラチンの安定化非晶形。
- 使用されるマトリックスが、ビニルポリマーであることを特徴とする、請求項2又は請求項3に記載のアゴメラチンの安定化非晶形。
- 使用されるマトリックスが、Kollidon VA64又はSoluplusであることを特徴とする、請求項7に記載のアゴメラチンの安定化非晶形。
- 使用されるマトリックスが、ポリ酢酸フタル酸ビニルであることを特徴とする、請求項7に記載のアゴメラチンの安定化非晶形。
- 使用されるマトリックスが、Plasdone S630であることを特徴とする、請求項7に記載のアゴメラチンの安定化非晶形。
- 使用されるマトリックスが、セルロース系ポリマーであることを特徴とする、請求項2又は請求項3に記載のアゴメラチンの安定化非晶形。
- 使用されるマトリックスが、アセチルコハク酸HPMCであることを特徴とする、請求項11に記載のアゴメラチンの安定化非晶形。
- 使用されるアゴメラチンの重量百分率が、30%以上であることを特徴とする、請求項2〜12に記載のアゴメラチンの安定化非晶形。
- 使用されるアゴメラチンの重量百分率が、30%〜50%であることを特徴とする、請求項2〜12に記載のアゴメラチンの安定化非晶形。
- 使用されるアゴメラチンの重量百分率が、30%〜40%であることを特徴とする、請求項2〜12に記載のアゴメラチンの安定化非晶形。
- 任意の製造法により得られ、そして任意の結晶形、複合体、共結晶、又は薬学的に許容しうる酸若しくは塩基との付加塩として存在する、式(I)の化合物を、1種以上の溶媒中で選択されたポリマーと混合し、得られた成分を完全に溶解させ、そして次に全体として減圧下で溶媒を留去することを特徴とする、請求項1〜15のいずれか1項に記載のアゴメラチンの安定化非晶形を得るための方法。
- 任意の製造法により得られ、そして任意の結晶形、複合体、共結晶、又は薬学的に許容しうる酸若しくは塩基との付加塩として存在する、式(I)の化合物を、選択されたポリマーと混合及びプレブレンドし、そして次にこの混合物を、押出機(そのスクリューピッチ及び温度は、この混合物の粘度の関数として選択される)に導入することにより、成形品が得られ、次にこれを所望のサイズに切り出し、次いで場合により粉砕することを特徴とする、請求項1〜15のいずれか1項に記載のアゴメラチンの安定化非晶形を得るための方法。
- アゴメラチンの重量百分率が、30%以上であることを特徴とする、請求項16又は請求項17に記載のアゴメラチンの安定化非晶形を得るための方法。
- アゴメラチンの重量百分率が、30%〜50%であることを特徴とする、請求項16又は請求項17に記載のアゴメラチンの安定化非晶形を得るための方法。
- アゴメラチンの重量百分率が、30%〜40%であることを特徴とする、請求項16又は請求項17に記載のアゴメラチンの安定化非晶形を得るための方法。
- 活性成分として請求項1〜15のいずれか1項に記載のアゴメラチンの安定化非晶形を、そのままで、又は1種以上の不活性で非毒性かつ薬学的に許容しうる担体と組合せて含む、医薬組成物。
- 製剤の総重量に対してアゴメラチンの重量百分率が、25%以上であることを特徴とする、請求項21に記載の医薬組成物。
- メラトニン作動系の障害を処置するための医薬品の製造において使用するための、請求項21又は22に記載の医薬組成物。
- 睡眠障害、ストレス、不安、季節性情動障害又は大鬱病、心血管病態、消化器系病態、ジェットラグによって起こる不眠症及び疲労、統合失調症、パニック発作、鬱病、食欲障害、肥満症、不眠症、疼痛、精神病、てんかん、糖尿病、パーキンソン病、老年性認知症、正常又は病的加齢に伴う種々の障害、片頭痛、記憶喪失、アルツハイマー病、脳循環障害の処置のための、及びまた性機能障害における、そして排卵抑制剤及び免疫調節剤としての、及び癌の処置における医薬品の製造において使用するための、請求項21又は22に記載の医薬組成物。
- メラトニン作動系の障害の処置のための、請求項1〜15のいずれか1項に記載のアゴメラチンの安定化非晶形。
- 睡眠障害、ストレス、不安、季節性情動障害又は大鬱病、心血管病態、消化器系病態、ジェットラグによって起こる不眠症及び疲労、統合失調症、パニック発作、鬱病、食欲障害、肥満症、不眠症、疼痛、精神病、てんかん、糖尿病、パーキンソン病、老年性認知症、正常又は病的加齢に伴う種々の障害、片頭痛、記憶喪失、アルツハイマー病、脳循環障害の処置のための、及びまた性機能障害における、そして排卵抑制剤及び免疫調節剤としての、及び癌の処置における、請求項1〜15のいずれか1項に記載のアゴメラチンの安定化非晶形。
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PCT/CN2012/081250 WO2014040228A1 (en) | 2012-09-11 | 2012-09-11 | Stabilised amorphous form of agomelatine, a process for its preparation and pharmaceutical compositions containing it |
CNPCT/CN2012/081250 | 2012-09-11 | ||
FR12/59064 | 2012-09-26 | ||
FR1259064A FR2995896B1 (fr) | 2012-09-26 | 2012-09-26 | Forme amorphe stabilisee de l'agomelatine, son procede de preparation et les compositions pharmaceutiques qui la contiennent. |
PCT/EP2013/068792 WO2014041015A1 (en) | 2012-09-11 | 2013-09-11 | Stabilised amorphous form of agomelatine, a process for its preparation and pharmaceutical compositions containing it. |
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WO2015153971A1 (en) * | 2014-04-03 | 2015-10-08 | Ovid Therapeutics Inc. | Methods of treating sleep disorders associated with neurodegenerative diseases |
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Cited By (1)
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US11708463B2 (en) | 2018-04-06 | 2023-07-25 | Capsugel Belgium Nv | Spray drying process for low aspect ratio particles comprising poly[(methyl methacrylate)-co-(methacrylic acid)] |
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