JP2004532859A5 - - Google Patents
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- JP2004532859A5 JP2004532859A5 JP2002590955A JP2002590955A JP2004532859A5 JP 2004532859 A5 JP2004532859 A5 JP 2004532859A5 JP 2002590955 A JP2002590955 A JP 2002590955A JP 2002590955 A JP2002590955 A JP 2002590955A JP 2004532859 A5 JP2004532859 A5 JP 2004532859A5
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- 239000000443 aerosol Substances 0.000 description 33
- 230000000561 anti-psychotic Effects 0.000 description 27
- 239000000203 mixture Substances 0.000 description 17
- XJGVXQDUIWGIRW-UHFFFAOYSA-N Loxapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2OC2=CC=C(Cl)C=C12 XJGVXQDUIWGIRW-UHFFFAOYSA-N 0.000 description 12
- WIKYUJGCLQQFNW-UHFFFAOYSA-N Prochlorperazine Chemical compound C1CN(C)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 WIKYUJGCLQQFNW-UHFFFAOYSA-N 0.000 description 12
- 229960000423 loxapine Drugs 0.000 description 12
- 239000002245 particle Substances 0.000 description 12
- 229960003111 prochlorperazine Drugs 0.000 description 12
- 239000007857 degradation product Substances 0.000 description 9
- 238000010438 heat treatment Methods 0.000 description 9
- 239000007787 solid Substances 0.000 description 5
- 239000003814 drug Substances 0.000 description 4
- 229940079593 drugs Drugs 0.000 description 4
- 229940005529 ANTIPSYCHOTICS Drugs 0.000 description 3
- ZPEIMTDSQAKGNT-UHFFFAOYSA-N Chlorpromazine Chemical compound C1=C(Cl)C=C2N(CCCN(C)C)C3=CC=CC=C3SC2=C1 ZPEIMTDSQAKGNT-UHFFFAOYSA-N 0.000 description 3
- 229960001076 Chlorpromazine Drugs 0.000 description 3
- QZUDBNBUXVUHMW-UHFFFAOYSA-N Clozapine Chemical compound C1CN(C)CCN1C1=NC2=CC(Cl)=CC=C2NC2=CC=CC=C12 QZUDBNBUXVUHMW-UHFFFAOYSA-N 0.000 description 3
- RMEDXOLNCUSCGS-UHFFFAOYSA-N Droperidol Chemical compound C1=CC(F)=CC=C1C(=O)CCCN1CC=C(N2C(NC3=CC=CC=C32)=O)CC1 RMEDXOLNCUSCGS-UHFFFAOYSA-N 0.000 description 3
- 229960000394 Droperidol Drugs 0.000 description 3
- 229960002690 Fluphenazine Drugs 0.000 description 3
- PLDUPXSUYLZYBN-UHFFFAOYSA-N Fluphenazine dihydrochloride Chemical compound C1CN(CCO)CCN1CCCN1C2=CC(C(F)(F)F)=CC=C2SC2=CC=CC=C21 PLDUPXSUYLZYBN-UHFFFAOYSA-N 0.000 description 3
- LNEPOXFFQSENCJ-UHFFFAOYSA-N Haloperidol Chemical compound C1CC(O)(C=2C=CC(Cl)=CC=2)CCN1CCCC(=O)C1=CC=C(F)C=C1 LNEPOXFFQSENCJ-UHFFFAOYSA-N 0.000 description 3
- KVWDHTXUZHCGIO-UHFFFAOYSA-N Olanzapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 KVWDHTXUZHCGIO-UHFFFAOYSA-N 0.000 description 3
- ZGUGWUXLJSTTMA-UHFFFAOYSA-N Promazinum Chemical compound C1=CC=C2N(CCCN(C)C)C3=CC=CC=C3SC2=C1 ZGUGWUXLJSTTMA-UHFFFAOYSA-N 0.000 description 3
- URKOMYMAXPYINW-UHFFFAOYSA-N Quetiapine Chemical compound C1CN(CCOCCO)CCN1C1=NC2=CC=CC=C2SC2=CC=CC=C12 URKOMYMAXPYINW-UHFFFAOYSA-N 0.000 description 3
- RAPZEAPATHNIPO-UHFFFAOYSA-N Risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 description 3
- 229960001534 Risperidone Drugs 0.000 description 3
- GFBKORZTTCHDGY-UWVJOHFNSA-N Thiothixene Chemical compound C12=CC(S(=O)(=O)N(C)C)=CC=C2SC2=CC=CC=C2\C1=C\CCN1CCN(C)CC1 GFBKORZTTCHDGY-UWVJOHFNSA-N 0.000 description 3
- ZEWQUBUPAILYHI-UHFFFAOYSA-N Trifluoperazine Chemical compound C1CN(C)CCN1CCCN1C2=CC(C(F)(F)F)=CC=C2SC2=CC=CC=C21 ZEWQUBUPAILYHI-UHFFFAOYSA-N 0.000 description 3
- 229960002324 Trifluoperazine Drugs 0.000 description 3
- 239000000164 antipsychotic agent Substances 0.000 description 3
- 229960004170 clozapine Drugs 0.000 description 3
- 238000009833 condensation Methods 0.000 description 3
- 230000005494 condensation Effects 0.000 description 3
- 238000001816 cooling Methods 0.000 description 3
- 238000001704 evaporation Methods 0.000 description 3
- 229960003878 haloperidol Drugs 0.000 description 3
- 238000002664 inhalation therapy Methods 0.000 description 3
- 229960005017 olanzapine Drugs 0.000 description 3
- 229960003598 promazine Drugs 0.000 description 3
- 229960004431 quetiapine Drugs 0.000 description 3
- 229960004660 thiothixene Drugs 0.000 description 3
- 238000000354 decomposition reaction Methods 0.000 description 1
- 239000000047 product Substances 0.000 description 1
Description
【特許請求の範囲】
【請求項１】
オランザピン、トリフルオペラジン、ハロペリドール、ロクサピン、リスペリドン、クロザピン、クエチアピン、プロマジン、チオチキセン、クロルプロマジン、ドロペリドール、プロクロルペラジンおよびフルフェナジンからなる群より選ばれる抗精神病薬を含む凝縮エアロゾルであって、
ａ）１０重量％未満の前記抗精神病薬の分解生成物を含む粒子を含有し、
ｂ）５μｍ未満の空気力学的質量中位径を有する、
凝縮エアロゾル。
【請求項２】
前記抗精神病薬を蒸発させて前記抗精神病薬の蒸気を形成し、当該蒸気を凝縮して前記粒子を形成することにより得られる、請求項１記載の凝縮エアロゾル。
【請求項３】
前記抗精神病薬の蒸発が、前記抗精神病薬を含む組成物により表面が被覆された固体サポートを加熱し、前記組成物から前記抗精神病薬を蒸発させることにより行われる、請求項２記載の凝縮エアロゾル。
【請求項４】
前記蒸気の凝縮が、前記蒸気を冷却することにより行われる、請求項２または３に記載の凝縮エアロゾル。
【請求項５】
前記粒子が、５重量％未満の抗精神病薬の分解生成物を含む、請求項１〜４のいずれか一項に記載の凝縮エアロゾル。
【請求項６】
前記粒子が、２．５重量％未満の抗精神病薬の分解生成物を含む、請求項１〜４のいずれか一項に記載の凝縮エアロゾル。
【請求項７】
少なくとも５重量％の前記抗精神病薬を含む、請求項１〜６のいずれか一項に記載の凝縮エアロゾル。
【請求項８】
少なくとも９０重量％の前記抗精神病薬を含む、請求項１〜６のいずれか一項に記載の凝縮エアロゾル。
【請求項９】
３μｍ未満の空気力学的質量中位径を有する、請求項１〜８のいずれか一項に記載の凝縮エアロゾル。
【請求項１０】
吸入療法に使用される、請求項１〜９のいずれか一項に記載の凝縮エアロゾル。
【請求項１１】
請求項１〜１０のいずれか一項に記載の凝縮エアロゾルを含む、前記抗精神病薬を送出するための組成物。
【請求項１２】
抗精神病薬含有エアロゾルを形成する方法であって、
ａ）少なくとも５重量％のオランザピン、トリフルオペラジン、ハロペリドール、ロクサピン、リスペリドン、クロザピン、クエチアピン、プロマジン、チオチキセン、クロルプロマジン、ドロペリドール、プロクロルペラジンおよびフルフェナジンからなる群より選ばれる抗精神病薬を含む組成物を加熱し、前記抗精神病薬を蒸発させて前記抗精神病薬の蒸気を形成する工程と、
ｂ）前記蒸気を凝縮させることにより、１０重量％未満の抗精神病薬の分解生成物を含む粒子を含有し、５μｍ未満の空気力学的質量中位径を有する凝縮エアロゾルを形成する工程と、
を含む方法。
【請求項１３】
前記工程ａ）が、前記抗精神病薬を含む組成物により表面が被覆された固体サポートを加熱し、前記抗精神病薬を前記組成物から蒸発させることを含む、請求項１２記載の方法。
【請求項１４】
前記工程ａ）が、前記抗精神病薬を含む組成物が上に置かれた固体サポートを加熱し、前記抗精神病薬を前記組成物から蒸発させることを含む、請求項１２記載の方法。
【請求項１５】
前記工程ｂ）が、前記蒸気を冷却して前記凝縮エアロゾルを形成することを含む、請求項１２〜１４のいずれか一項に記載の方法。
【請求項１６】
前記粒子が、５重量％未満の抗精神病薬の分解生成物を含む、請求項１２〜１５のいずれか一項に記載の方法。
【請求項１７】
前記粒子が、２．５重量％未満の抗精神病薬の分解生成物を含む、請求項１２〜１５のいずれか一項に記載の方法。
【請求項１８】
前記凝縮エアロゾルが、少なくとも９０重量％の前記抗精神病薬を含む、請求項１２〜１７のいずれか一項に記載の方法。
【請求項１９】
前記粒子が、０．５ｍｇ／秒より大きい速度で形成される、請求項１２〜１８のいずれか一項に記載の方法。
【請求項２０】
前記粒子が、１ｍｇ／秒より大きい速度で形成される、請求項１２〜１８のいずれか一項に記載の方法。
【請求項２１】
前記凝縮エアロゾルが、３μｍ未満の空気力学的質量中位径を有する、請求項１２〜２０のいずれか一項に記載の方法。
【請求項２２】
前記凝縮エアロゾルが吸入療法に使用される、請求項１２〜２１のいずれか一項に記載の方法。
【請求項２３】
抗精神病薬を送出するためのキットであって、
ａ）少なくとも５重量％のオランザピン、トリフルオペラジン、ハロペリドール、ロクサピン、リスペリドン、クロザピン、クエチアピン、プロマジン、チオチキセン、クロルプロマジン、ドロペリドール、プロクロルペラジンおよびフルフェナジンからなる群より選ばれる抗精神病薬を含む組成物と、
ｂ）前記組成物から、前記抗精神病薬を含む凝縮エアロゾルを形成する装置と、
を具備し、
前記装置が、
１）前記組成物を加熱して蒸気を形成する要素と、
２）前記蒸気を冷却して凝縮エアロゾルを形成する要素と、
３）前記エアロゾルを吸入するのを可能にする要素と、
を具備するキット。
【請求項２４】
前記凝縮エアロゾルが、吸入療法に使用される、請求項２３記載のキット。
【請求項２５】
前記凝縮エアロゾルが、請求項１〜１０のいずれか一項に記載の凝縮エアロゾルである、請求項２３または２４に記載のキット。
【請求項２６】
ロクサピンを含む凝縮エアロゾルであって、
ａ）１０重量％未満のロクサピンの分解生成物を含む粒子を含有し、
ｂ）５μｍ未満の空気力学的質量中位径を有する、
凝縮エアロゾル。
【請求項２７】
ロクサピン含有エアロゾルを形成する方法であって、
ａ）少なくとも５重量％のロクサピンを含む組成物を加熱し、前記ロクサピンを蒸発させて前記ロクサピンの蒸気を形成する工程と、
ｂ）前記蒸気を凝縮させることにより、１０重量％未満のロクサピンの分解生成物を含む粒子を含有し、５μｍ未満の空気力学的質量中位径を有する凝縮エアロゾルを形成する工程と、
を含む方法。
【請求項２８】
前記工程ａ）が、ロクサピンを含む組成物により表面が被覆された固体サポートを加熱し、前記ロクサピンを前記組成物から蒸発させることを含む、請求項２７記載の方法。
【請求項２９】
プロクロルペラジンを含む凝縮エアロゾルであって、
ａ）１０重量％未満のプロクロルペラジンの分解生成物を含む粒子を含有し、
ｂ）５μｍ未満の空気力学的質量中位径を有する、
凝縮エアロゾル。
【請求項３０】
プロクロルペラジン含有エアロゾルを形成する方法であって、
ａ）少なくとも５重量％のプロクロルペラジンを含む組成物を加熱し、前記プロクロルペラジンを蒸発させて前記プロクロルペラジンの蒸気を形成する工程と、
ｂ）前記蒸気を凝縮させることにより、１０重量％未満のプロクロルペラジンの分解生成物を含む粒子を含有し、５μｍ未満の空気力学的質量中位径を有する凝縮エアロゾルを形成する工程と、
を含む方法。
【請求項３１】
前記工程ａ）が、プロクロルペラジンを含む組成物により表面が被覆された固体サポートを加熱し、前記プロクロルペラジンを前記組成物から蒸発させることを含む、請求項３０記載の方法。
【請求項１】
オランザピン、トリフルオペラジン、ハロペリドール、ロクサピン、リスペリドン、クロザピン、クエチアピン、プロマジン、チオチキセン、クロルプロマジン、ドロペリドール、プロクロルペラジンおよびフルフェナジンからなる群より選ばれる抗精神病薬を含む凝縮エアロゾルであって、
ａ）１０重量％未満の前記抗精神病薬の分解生成物を含む粒子を含有し、
ｂ）５μｍ未満の空気力学的質量中位径を有する、
凝縮エアロゾル。
【請求項２】
前記抗精神病薬を蒸発させて前記抗精神病薬の蒸気を形成し、当該蒸気を凝縮して前記粒子を形成することにより得られる、請求項１記載の凝縮エアロゾル。
【請求項３】
前記抗精神病薬の蒸発が、前記抗精神病薬を含む組成物により表面が被覆された固体サポートを加熱し、前記組成物から前記抗精神病薬を蒸発させることにより行われる、請求項２記載の凝縮エアロゾル。
【請求項４】
前記蒸気の凝縮が、前記蒸気を冷却することにより行われる、請求項２または３に記載の凝縮エアロゾル。
【請求項５】
前記粒子が、５重量％未満の抗精神病薬の分解生成物を含む、請求項１〜４のいずれか一項に記載の凝縮エアロゾル。
【請求項６】
前記粒子が、２．５重量％未満の抗精神病薬の分解生成物を含む、請求項１〜４のいずれか一項に記載の凝縮エアロゾル。
【請求項７】
少なくとも５重量％の前記抗精神病薬を含む、請求項１〜６のいずれか一項に記載の凝縮エアロゾル。
【請求項８】
少なくとも９０重量％の前記抗精神病薬を含む、請求項１〜６のいずれか一項に記載の凝縮エアロゾル。
【請求項９】
３μｍ未満の空気力学的質量中位径を有する、請求項１〜８のいずれか一項に記載の凝縮エアロゾル。
【請求項１０】
吸入療法に使用される、請求項１〜９のいずれか一項に記載の凝縮エアロゾル。
【請求項１１】
請求項１〜１０のいずれか一項に記載の凝縮エアロゾルを含む、前記抗精神病薬を送出するための組成物。
【請求項１２】
抗精神病薬含有エアロゾルを形成する方法であって、
ａ）少なくとも５重量％のオランザピン、トリフルオペラジン、ハロペリドール、ロクサピン、リスペリドン、クロザピン、クエチアピン、プロマジン、チオチキセン、クロルプロマジン、ドロペリドール、プロクロルペラジンおよびフルフェナジンからなる群より選ばれる抗精神病薬を含む組成物を加熱し、前記抗精神病薬を蒸発させて前記抗精神病薬の蒸気を形成する工程と、
ｂ）前記蒸気を凝縮させることにより、１０重量％未満の抗精神病薬の分解生成物を含む粒子を含有し、５μｍ未満の空気力学的質量中位径を有する凝縮エアロゾルを形成する工程と、
を含む方法。
【請求項１３】
前記工程ａ）が、前記抗精神病薬を含む組成物により表面が被覆された固体サポートを加熱し、前記抗精神病薬を前記組成物から蒸発させることを含む、請求項１２記載の方法。
【請求項１４】
前記工程ａ）が、前記抗精神病薬を含む組成物が上に置かれた固体サポートを加熱し、前記抗精神病薬を前記組成物から蒸発させることを含む、請求項１２記載の方法。
【請求項１５】
前記工程ｂ）が、前記蒸気を冷却して前記凝縮エアロゾルを形成することを含む、請求項１２〜１４のいずれか一項に記載の方法。
【請求項１６】
前記粒子が、５重量％未満の抗精神病薬の分解生成物を含む、請求項１２〜１５のいずれか一項に記載の方法。
【請求項１７】
前記粒子が、２．５重量％未満の抗精神病薬の分解生成物を含む、請求項１２〜１５のいずれか一項に記載の方法。
【請求項１８】
前記凝縮エアロゾルが、少なくとも９０重量％の前記抗精神病薬を含む、請求項１２〜１７のいずれか一項に記載の方法。
【請求項１９】
前記粒子が、０．５ｍｇ／秒より大きい速度で形成される、請求項１２〜１８のいずれか一項に記載の方法。
【請求項２０】
前記粒子が、１ｍｇ／秒より大きい速度で形成される、請求項１２〜１８のいずれか一項に記載の方法。
【請求項２１】
前記凝縮エアロゾルが、３μｍ未満の空気力学的質量中位径を有する、請求項１２〜２０のいずれか一項に記載の方法。
【請求項２２】
前記凝縮エアロゾルが吸入療法に使用される、請求項１２〜２１のいずれか一項に記載の方法。
【請求項２３】
抗精神病薬を送出するためのキットであって、
ａ）少なくとも５重量％のオランザピン、トリフルオペラジン、ハロペリドール、ロクサピン、リスペリドン、クロザピン、クエチアピン、プロマジン、チオチキセン、クロルプロマジン、ドロペリドール、プロクロルペラジンおよびフルフェナジンからなる群より選ばれる抗精神病薬を含む組成物と、
ｂ）前記組成物から、前記抗精神病薬を含む凝縮エアロゾルを形成する装置と、
を具備し、
前記装置が、
１）前記組成物を加熱して蒸気を形成する要素と、
２）前記蒸気を冷却して凝縮エアロゾルを形成する要素と、
３）前記エアロゾルを吸入するのを可能にする要素と、
を具備するキット。
【請求項２４】
前記凝縮エアロゾルが、吸入療法に使用される、請求項２３記載のキット。
【請求項２５】
前記凝縮エアロゾルが、請求項１〜１０のいずれか一項に記載の凝縮エアロゾルである、請求項２３または２４に記載のキット。
【請求項２６】
ロクサピンを含む凝縮エアロゾルであって、
ａ）１０重量％未満のロクサピンの分解生成物を含む粒子を含有し、
ｂ）５μｍ未満の空気力学的質量中位径を有する、
凝縮エアロゾル。
【請求項２７】
ロクサピン含有エアロゾルを形成する方法であって、
ａ）少なくとも５重量％のロクサピンを含む組成物を加熱し、前記ロクサピンを蒸発させて前記ロクサピンの蒸気を形成する工程と、
ｂ）前記蒸気を凝縮させることにより、１０重量％未満のロクサピンの分解生成物を含む粒子を含有し、５μｍ未満の空気力学的質量中位径を有する凝縮エアロゾルを形成する工程と、
を含む方法。
【請求項２８】
前記工程ａ）が、ロクサピンを含む組成物により表面が被覆された固体サポートを加熱し、前記ロクサピンを前記組成物から蒸発させることを含む、請求項２７記載の方法。
【請求項２９】
プロクロルペラジンを含む凝縮エアロゾルであって、
ａ）１０重量％未満のプロクロルペラジンの分解生成物を含む粒子を含有し、
ｂ）５μｍ未満の空気力学的質量中位径を有する、
凝縮エアロゾル。
【請求項３０】
プロクロルペラジン含有エアロゾルを形成する方法であって、
ａ）少なくとも５重量％のプロクロルペラジンを含む組成物を加熱し、前記プロクロルペラジンを蒸発させて前記プロクロルペラジンの蒸気を形成する工程と、
ｂ）前記蒸気を凝縮させることにより、１０重量％未満のプロクロルペラジンの分解生成物を含む粒子を含有し、５μｍ未満の空気力学的質量中位径を有する凝縮エアロゾルを形成する工程と、
を含む方法。
【請求項３１】
前記工程ａ）が、プロクロルペラジンを含む組成物により表面が被覆された固体サポートを加熱し、前記プロクロルペラジンを前記組成物から蒸発させることを含む、請求項３０記載の方法。
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2002
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2004
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2006
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- 2006-07-18 US US11/488,943 patent/US20060257329A1/en not_active Abandoned
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2007
- 2007-01-09 US US11/621,397 patent/US7468179B2/en not_active Expired - Fee Related
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2008
- 2008-03-27 US US12/057,330 patent/US7988952B2/en not_active Expired - Fee Related
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2009
- 2009-03-27 US US12/413,339 patent/US8173107B2/en not_active Expired - Fee Related
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2010
- 2010-07-23 JP JP2010165688A patent/JP5629151B2/ja not_active Expired - Lifetime
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2013
- 2013-08-19 FR FR13C0051C patent/FR13C0051I1/fr active Active
- 2013-08-19 BE BE2013C054C patent/BE2013C054I2/nl unknown
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