JP6205406B2 - トラニラスト組成物および共結晶 - Google Patents
トラニラスト組成物および共結晶 Download PDFInfo
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- JP6205406B2 JP6205406B2 JP2015502540A JP2015502540A JP6205406B2 JP 6205406 B2 JP6205406 B2 JP 6205406B2 JP 2015502540 A JP2015502540 A JP 2015502540A JP 2015502540 A JP2015502540 A JP 2015502540A JP 6205406 B2 JP6205406 B2 JP 6205406B2
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- Prior art keywords
- tranilast
- crystal
- pharmaceutical composition
- powder
- acid
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Description
本出願は2012年3月30日付けで出願された米国特許出願61/618,639に優先権を主張するものであり、その内容を引用によってここに組み入れる。
本発明は新規トラニラスト組成物およびトラニラスト共結晶に関する。本発明はまた、新規トラニラスト組成物または共結晶の治療における使用、ならびにこれらを含有する医薬組成物に関する。
トラニラスト(tranilast)、下記に示される(2−{[3−(3,4−ジメトキシフェニル)−1−オキソ−2−プロペニル]アミノ}安息香酸)は抗アレルギー作用を示す治療剤である。マスト細胞および好塩基球からのヒスタミンなどの炎症メディエーターの放出を抑制することが示されている(P.Zampini、Int.J.Immunopharmacol.1983;5(5):431−5)。トラニラストは日本国および南韓国において数年にわたりアレルギー性関節炎、気管支喘息、アレルギー性鼻炎およびアトピー性皮膚炎などの症状用の抗アレルギー処置剤として使用されている。
本発明は新規なトラニラスト複合体および新規なトラニラスト共結晶に関する。特に、本発明は1:1トラニラストニコチンアミド複合体、1:1トラニラストニコチンアミド共結晶、1:1トラニラストサッカリン複合体、1:1トラニラストサッカリン共結晶、1:1トラニラストゲンチジン酸複合体、1:1トラニラストゲンチジン酸共結晶、1:1トラニラストサリチル酸複合体、1:1トラニラストサリチル酸共結晶、1:1トラニラスト尿素複合体、1:1トラニラスト尿素共結晶、1:1トラニラスト4−アミノ安息香酸複合体、1:1トラニラスト4−アミノ安息香酸共結晶、1:1トラニラスト2,4−ジヒドロキシ安息香酸複合体および1:1トラニラスト2,4−ジヒドロキシ安息香酸共結晶に関する。本発明は本発明によるトラニラスト複合体または共結晶および医薬上で許容される担体を含有する医薬組成物に関する。トラニラスト複合体または共結晶はトラニラストと同一の方法で使用することができる。トラニラストは抗アレルギー性、抗線維症性、抗炎症性、抗腫瘍性、神経発生強化性および新脈管形成抑制性を有し、上記のとおりの性質を付随する疾病、傷害および症状の処置に使用することができる。
本発明は新規なトラニラスト複合体および新規なトラニラスト共結晶に関する。特に、本発明は1:1トラニラストニコチンアミド複合体、1:1トラニラストニコチンアミド共結晶、1:1トラニラストサッカリン複合体、1:1トラニラストサッカリン共結晶、1:1トラニラストゲンチジン酸複合体、1:1トラニラストゲンチジン酸共結晶、1:1トラニラストサリチル酸複合体、1:1トラニラストサリチル酸共結晶、1:1トラニラスト尿素複合体、1:1トラニラスト尿素共結晶、1:1トラニラスト4−アミノ安息香酸複合体、1:1トラニラスト4−アミノ安息香酸共結晶、1:1トラニラスト2,4−ジヒドロキシ安息香酸複合体および1:1トラニラスト2.4−ジヒドロキシ安息香酸共結晶に関する。本発明は本発明によるトラニラスト複合体または共結晶および医薬上で許容される担体を含有する医薬組成物に関する。トラニラスト複合体および共結晶、ならびにそれらの確認に使用される方法を以下で説明する。
1:1トラニラストニコチンアミド共結晶
1:1トラニラストサッカリン共結晶
1:1トラニラストサッカリン共結晶の実験的XRPDパターンを図8に示す。表4は図8の実験的XRPDパターンで同定されたピークの角度 °2θ±0.2°2θおよびd−スペーシングのリストである。ピークの全リストまたはそのサブセットは、図8と実質的に類似するXRPDパターンによるものと同様に、共結晶を確認するのに充分であることができる。一例として、本発明による1:1トラニラストサッカリン共結晶は、5.6、9.5、14.6、15.4、16.2および16.7°2θ±0.2°2θから選択される少なくとも3個のピークを有する粉末X−線回折パターンにより確認することができる。
1:1トラニラストゲンチジン酸共結晶
1:1トラニラストサリチル酸共結晶
1:1トラニラスト尿素共結晶
1:1トラニラスト4−アミノ安息香酸共結晶
1:1トラニラスト2,4−ジヒドロキシ安息香酸共結晶
固体状態光安定性試験
溶液光安定性試験
溶解度試験
Claims (16)
- 粉末X−線回折パターンが6.0、8.0、12.0、15.0および15.6°2θ±0.2°2θから選択される少なくとも3個のピークを有することを特徴とする1:1トラニラストニコチンアミド共結晶。
- 粉末X−線回折パターンが5.6、9.5、14.6、15.4、16.2および16.7°2θ±0.2°2θから選択される少なくとも3個のピークを有することを特徴とする1:1トラニラストサッカリン共結晶。
- 粉末X−線回折パターンが7.4、10.5、12.2、14.8、15.7および26.4°2θ±0.2°2θから選択される少なくとも3個のピークを有することを特徴とする1:1トラニラストゲンチジン酸共結晶。
- 粉末X−線回折パターンが4.4、10.4、13.1、16.9および18.5°2θ±0.2°2θから選択される少なくとも3個のピークを有することを特徴とする1:1トラニラストサリチル酸共結晶。
- 粉末X−線回折パターンが8.2、11.3、13.8、15.0、16.3および25.3°2θ±0.2°2θから選択される少なくとも3個のピークを有することを特徴とする1:1トラニラスト尿素共結晶。
- 粉末X−線回折パターンが5.4、6.7、11.5、12.0、16.4および17.9°2θ±0.2°2θから選択される少なくとも3個のピークを有することを特徴とする1:1トラニラスト4−アミノ安息香酸共結晶。
- 粉末X−線回折パターンが3.9、7.9、11.8、12.6および15.4°2θ±0.2°2θから選択される少なくとも3個のピークを有することを特徴とする1:1トラニラスト2,4−ジヒドロキシ安息香酸共結晶。
- 請求項1〜7のいずれか一項に記載のトラニラスト共結晶および医薬上で許容される担体を含む医薬組成物。
- 組成物が局所用製剤である、請求項8に記載の医薬組成物。
- 組成物が吸入可能な製剤である、請求項8に記載の医薬組成物。
- 治療有効量の請求項1〜7のいずれか一項に記載のトラニラスト共結晶を含む、アレルギー性障害、線維性障害または炎症性障害の治療のための医薬組成物。
- 治療有効量の請求項1〜7のいずれか一項に記載のトラニラスト共結晶または請求項8に記載の医薬組成物を含む、腫瘍増殖および転移を阻止する、神経発生を強化する、または新脈管形成を阻止するための医薬組成物。
- 溶解によって液体医薬組成物を調製するための請求項1〜7のいずれか一項に記載のトラニラスト共結晶の使用。
- 液体医薬組成物の調製方法であって、請求項1〜7のいずれか一項に記載のトラニラスト共結晶を医薬上で許容される溶媒に溶解する工程を含む調製方法。
- 組成物は、経口製剤である、請求項8に記載の医薬組成物。
- 組成物は、注射用製剤である、請求項8に記載の医薬組成物。
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- 2013-03-29 WO PCT/IB2013/052545 patent/WO2013144916A1/en active Application Filing
- 2013-03-29 KR KR1020147030137A patent/KR102093863B1/ko active IP Right Grant
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EP2830590A1 (en) | 2015-02-04 |
CA2908440A1 (en) | 2013-10-03 |
EP2830590B1 (en) | 2017-06-28 |
CA2908440C (en) | 2021-04-20 |
ES2634993T3 (es) | 2017-10-02 |
CN104379130B (zh) | 2018-01-02 |
HK1206619A1 (en) | 2016-01-15 |
WO2013144916A1 (en) | 2013-10-03 |
US20180118662A1 (en) | 2018-05-03 |
BR112014024276A2 (pt) | 2017-08-08 |
US20170158618A1 (en) | 2017-06-08 |
KR20140139100A (ko) | 2014-12-04 |
AU2013239114A1 (en) | 2014-10-30 |
US9512064B2 (en) | 2016-12-06 |
JP2015516951A (ja) | 2015-06-18 |
US20150119428A1 (en) | 2015-04-30 |
IN2014DN09031A (ja) | 2015-05-22 |
KR102093863B1 (ko) | 2020-03-26 |
AU2013239114B2 (en) | 2017-07-20 |
US10150729B2 (en) | 2018-12-11 |
CN104379130A (zh) | 2015-02-25 |
US9822066B2 (en) | 2017-11-21 |
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