JP2017512212A - ニコチン製剤及びその作製方法 - Google Patents
ニコチン製剤及びその作製方法 Download PDFInfo
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- JP2017512212A JP2017512212A JP2017504287A JP2017504287A JP2017512212A JP 2017512212 A JP2017512212 A JP 2017512212A JP 2017504287 A JP2017504287 A JP 2017504287A JP 2017504287 A JP2017504287 A JP 2017504287A JP 2017512212 A JP2017512212 A JP 2017512212A
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- particles
- nicotine
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- SNICXCGAKADSCV-UHFFFAOYSA-N nicotine Natural products CN1CCCC1C1=CC=CN=C1 SNICXCGAKADSCV-UHFFFAOYSA-N 0.000 title claims abstract description 170
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Abstract
Description
本出願は、2014年4月8日に出願された米国特許出願第61/976,712号の優先権を主張し、その内容全体を参照により本明細書に組み込む。
本発明は、ニコチンの乾燥粉末製剤、及び任意に他の選択された材料に関し、ニコチン成分及び任意の追加の成分が、制御された粒径範囲内に入る。例えば、一実施形態では、製剤は、粒子のMMADに基づいて、実質的に1〜10ミクロンのサイズのニコチン粒子(本明細書では、ニコチン系成分とも称される)を含む。さらに別の実施形態では、製剤は、実質的に1〜7ミクロンのサイズのニコチン粒子を含む。別の実施形態では、製剤は、実質的に2〜5ミクロンのサイズのニコチン粒子を含む。さらに別の実施形態では、製剤は、実質的に2〜3ミクロンのサイズのニコチン粒子を含む。約1ミクロンより小さいサイズ、または約2ミクロンより小さいサイズのニコチン粒子を選択的に制限または除外することによって、本発明の製剤は、ニコチンを環境に吐き戻す対象の能力を除去または少なくとも低減し、それによって副流煙に含まれるニコチンの生成を効果的に低減または除去する。さらに、非呼吸性ニコチン粒子を選択的に制限または除外することによって、本発明の製剤は、より大きい気道、咽頭、声門声帯、及び口に近位の、または口に近い他の解剖学的領域内に捕捉されたニコチン粒子によって引き起こされる望ましくない刺激を低減する。
Claims (28)
- ニコチン粒子を含む、吸入に適した乾燥粉末ニコチン製剤であって、前記ニコチン粒子が、実質的に約1〜10ミクロンのサイズである、前記乾燥粉末ニコチン製剤。
- 前記ニコチン粒子が、実質的に約2〜5ミクロンのサイズである、請求項1に記載の前記製剤。
- 前記ニコチン粒子の約10%未満が、約1ミクロン未満のサイズである、請求項1に記載の前記製剤。
- 前記ニコチン粒子の約10%未満が、約2ミクロン未満のサイズである、請求項3に記載の前記製剤。
- 前記ニコチン粒子の少なくとも約90%が、約10ミクロン未満のサイズである、請求項1に記載の前記製剤。
- 前記ニコチン粒子の少なくとも約90%が、約5ミクロン未満のサイズである、請求項5に記載の前記製剤。
- 前記ニコチン粒子の約10%未満が、約1ミクロン未満のサイズであり、前記ニコチン粒子の少なくとも約90%が、約10ミクロン未満のサイズである、請求項1に記載の前記製剤。
- 前記ニコチン粒子の約10%未満が、約2ミクロン未満のサイズであり、前記ニコチン粒子の少なくとも約90%が、約5ミクロン未満のサイズである、請求項2に記載の前記製剤。
- 吸入に適した乾燥粉末ニコチン製剤であって、
実質的に約1〜10ミクロンのサイズの粒子を有するニコチン系成分と、
実質的に約5〜10ミクロンのサイズの粒子を有する鎮咳剤成分と、を含む、前記乾燥粉末ニコチン製剤。 - 前記鎮咳剤成分が、メントールを含む、請求項9に記載の前記製剤。
- 前記ニコチン系成分粒子が、実質的に約2〜5ミクロンのサイズであり、前記鎮咳剤成分粒子が、実質的に約5〜8ミクロンのサイズである、請求項10に記載の前記製剤。
- 実質的に約10〜200ミクロンのサイズの粒子を有する鎮咳剤成分をさらに含む、請求項9に記載の前記製剤。
- 実質的に約10〜200ミクロンのサイズの粒子を有する前記鎮咳剤成分が、メントールを含む、請求項12に記載の前記製剤。
- 実質的に約10〜1000ミクロンのサイズの粒子を有する香味成分をさらに含む、請求項9に記載の前記製剤。
- 前記香味成分が、メントールを含む、請求項14に記載の前記製剤。
- 吸入に適した乾燥粉末ニコチン製剤の生成方法であって、
液体担体中にニコチン及び糖を含む流動性混合物を調製するステップと、
前記流動性混合物を噴霧乾燥させて、ニコチン及び糖を含む乾燥粉末粒子を生成するステップであって、前記乾燥粉末粒子が、実質的に約1〜10ミクロンのサイズの範囲内である、ステップと、を含む、前記方法。 - 前記糖が、ラクトースである、請求項16に記載の前記方法。
- 前記ラクトースが、球状化されていない、請求項17に記載の前記方法。
- 前記液体担体が、水である、請求項16に記載の前記方法。
- 前記液体担体が、水及びアルコールを含む、請求項16に記載の前記方法。
- 吸入に適した乾燥粉末ニコチン製剤の生成方法であって、
ニコチン粒子及び担体粒子を含む混合物を調製するステップと、
前記混合物を粉砕して、実質的に約1〜10ミクロンのサイズの範囲内の粒子を有する乾燥粉末ニコチン製剤を生成するステップと、を含む、前記方法。 - 前記ニコチン粒子が、酒石酸ニコチンを含む、請求項21に記載の前記方法。
- 前記担体粒子が、ラクトース含む、請求項21に記載の前記方法。
- 前記乾燥粉末ニコチン製剤が、約1.5〜7%ニコチンである、請求項21に記載の前記方法。
- 粉砕した後、追加の担体粒子を添加することをさらに含む、請求項21に記載の前記方法。
- 粉砕した後、5〜10ミクロンの粒径範囲を有する鎮咳剤成分を添加することをさらに含む、請求項21に記載の前記方法。
- 粉砕した後、5〜200ミクロンの粒径範囲を有する鎮咳剤成分を添加することをさらに含む、請求項21に記載の前記方法。
- 粉砕した後、10〜1000ミクロンの粒径範囲を有する香味成分を添加することをさらに含む、請求項21に記載の前記方法。
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2020527377A (ja) * | 2017-06-28 | 2020-09-10 | フィリップ・モーリス・プロダクツ・ソシエテ・アノニム | 吸入器と併用するための粒子を含む容器 |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP3102185B1 (en) * | 2014-02-03 | 2021-07-14 | Apurano Pharmaceuticals GmbH | Nanosuspension of natural materials and preparation method thereof |
GB201411526D0 (en) * | 2014-06-27 | 2014-08-13 | British American Tobacco Co | Powder |
US20170071248A1 (en) * | 2015-09-16 | 2017-03-16 | Sansa Corporation (Barbados) Inc. | System and Method for Controlling the Harshness of Nicotine-Based Dry Powder Formulations |
US10149844B2 (en) | 2015-09-16 | 2018-12-11 | Philip Morris Products S.A. | Inhalable nicotine formulations, and methods of making and using thereof |
US9585835B1 (en) * | 2015-09-16 | 2017-03-07 | Sansa Corporation (Barbados) Inc. | Inhalable nicotine formulations and methods of making and using the same |
US11224594B2 (en) * | 2015-09-16 | 2022-01-18 | Philip Morris Products S.A. | Nicotine formulations and methods of making and using the same |
CN108289841A (zh) | 2015-12-24 | 2018-07-17 | 菲利普莫里斯生产公司 | 带香味尼古丁粉末 |
RU2767064C2 (ru) * | 2016-06-30 | 2022-03-16 | Филип Моррис Продактс С.А. | Никотиносодержащие частицы и композиции |
BR112018075017A2 (pt) * | 2016-06-30 | 2019-03-19 | Philip Morris Products S.A. | partículas de nicotina |
WO2018163085A1 (en) * | 2017-03-07 | 2018-09-13 | Philip Morris Products S.A. | Inhalable nicotine formulations, and methods of making and using thereof |
GB2604314A (en) | 2017-09-22 | 2022-09-07 | Nerudia Ltd | Device, system and method |
CN112273713A (zh) * | 2019-07-10 | 2021-01-29 | 云南巴菰生物科技有限公司 | 一种水溶性物质爆珠及其制备方法 |
WO2022056173A1 (en) * | 2020-09-09 | 2022-03-17 | Inhale Health Llc | Nicotine-free formulations, devices and methods thereof for cessation of smoking or nicotine replacement |
US20220312830A1 (en) * | 2021-04-06 | 2022-10-06 | Altria Client Services Llc | Nicotine-containing agglomerates and methods of forming the same |
CN113367375B (zh) * | 2021-05-12 | 2022-11-04 | 云南中烟工业有限责任公司 | 一种基于等酸碱比外消旋扁桃酸尼古丁盐胶凝剂的载香超分子凝胶 |
GB2620956A (en) * | 2022-07-27 | 2024-01-31 | Air Ip Holdings Ltd | Smoking product |
WO2024090890A1 (ko) * | 2022-10-27 | 2024-05-02 | 주식회사 케이티앤지 | 흡입용 저용량 니코틴 건조 분말 조성물 |
WO2024090892A1 (ko) * | 2022-10-27 | 2024-05-02 | 주식회사 케이티앤지 | 흡입용 니코틴 건조 분말의 제조 방법 |
Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2001026630A1 (fr) * | 1999-10-12 | 2001-04-19 | Kaken Pharmaceutical Co., Ltd. | Preparations pour inhalation en poudre et leur procede de production |
JP2009520545A (ja) * | 2005-12-22 | 2009-05-28 | フィリップ・モーリス・プロダクツ・ソシエテ・アノニム | 吸入器具 |
JP2011506589A (ja) * | 2007-12-21 | 2011-03-03 | ウェイ,エドワード,タク | 気道疾患を治療するためのp−メンタン−3−カルボン酸エステル |
JP2011231124A (ja) * | 1998-11-13 | 2011-11-17 | Jagotec Ag | 吸入用の乾燥粉末 |
JP2013082660A (ja) * | 2011-10-11 | 2013-05-09 | Nico Puff Corp | ニコチン薬の製造法およびその方法により製造される医薬 |
WO2013128283A2 (en) * | 2012-02-28 | 2013-09-06 | Iceutica Holdings Inc. Bvi | Inhalable pharmaceutical compositions |
WO2014047569A2 (en) * | 2012-09-21 | 2014-03-27 | Basil Rigas | Product comprising a nicotine-containing material and an anti-cancer agent |
Family Cites Families (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AUPN862596A0 (en) * | 1996-03-12 | 1996-04-04 | F.H. Faulding & Co. Limited | Pharmaceutical compositions |
CN1110271C (zh) * | 1997-09-22 | 2003-06-04 | 株式会社大城 | 烟草调味剂及其烟草 |
SE9703458D0 (sv) * | 1997-09-25 | 1997-09-25 | Pharmacia & Upjohn Ab | Nicotine compositions and methods of formulation thereof |
CA2231968A1 (en) * | 1998-03-11 | 1999-09-11 | Smoke-Stop, A Partnership Consisting Of Art Slutsky | Method of producing a nicotine medicament |
US20120042886A1 (en) * | 1998-03-11 | 2012-02-23 | Hanna Piskorz | Method of producing a nicotine medicament and a medicament made by the method |
US20080138399A1 (en) * | 1999-07-16 | 2008-06-12 | Aradigm Corporation | Dual release nicotine formulations, and systems and methods for their use |
GB0010709D0 (en) * | 2000-05-03 | 2000-06-28 | Vectura Ltd | Powders for use a in dry powder inhaler |
US20030087937A1 (en) * | 2001-10-15 | 2003-05-08 | Nils-Olof Lindberg | Nicotine and cocoa powder compositions |
US6886557B2 (en) * | 2002-10-31 | 2005-05-03 | Hewlett-Packard Development Company, L.P. | Inhalation device and method for delivering variable amounts of different components |
SE528121C2 (sv) * | 2004-03-29 | 2006-09-05 | Mederio Ag | Preparering av torrpulver för på förhand uppmätt DPI |
US7838532B2 (en) * | 2005-05-18 | 2010-11-23 | Mpex Pharmaceuticals, Inc. | Aerosolized fluoroquinolones and uses thereof |
WO2008066810A2 (en) * | 2006-11-27 | 2008-06-05 | Novartis Ag | Pleasant tasting dry powder compositions suitable for pulmonary delivery |
US20080286340A1 (en) * | 2007-05-16 | 2008-11-20 | Sven-Borje Andersson | Buffered nicotine containing products |
GB0709811D0 (en) * | 2007-05-22 | 2007-07-04 | Vectura Group Plc | Pharmaceutical compositions |
US20090004248A1 (en) * | 2007-06-29 | 2009-01-01 | Frank Bunick | Dual portion dosage lozenge form |
US20140171511A1 (en) * | 2011-07-07 | 2014-06-19 | Eva Millqvist | Cough Reducing Product |
WO2013034910A1 (en) * | 2011-09-06 | 2013-03-14 | Verona Pharma Plc | Inhalable compositions |
US20130177646A1 (en) * | 2012-01-05 | 2013-07-11 | Mcneil Ab | Solid Nicotine-Comprising Dosage Form with Reduced Organoleptic Disturbance |
GB201215273D0 (en) * | 2012-08-28 | 2012-10-10 | Kind Consumer Ltd | Nicotine composition |
US20140261474A1 (en) * | 2013-03-15 | 2014-09-18 | Aradigm Corporation | Methods for inhalation of smoke-free nicotine |
-
2015
- 2015-04-08 KR KR1020167031075A patent/KR20170003926A/ko not_active Application Discontinuation
- 2015-04-08 WO PCT/IB2015/001327 patent/WO2015173648A2/en active Application Filing
- 2015-04-08 CA CA2944471A patent/CA2944471C/en not_active Expired - Fee Related
- 2015-04-08 AU AU2015260870A patent/AU2015260870B2/en not_active Ceased
- 2015-04-08 CN CN201580000663.6A patent/CN105828819A/zh active Pending
- 2015-04-08 US US14/681,859 patent/US20150283070A1/en not_active Abandoned
- 2015-04-08 KR KR1020197017739A patent/KR20190075168A/ko not_active Application Discontinuation
- 2015-04-08 EP EP15792688.2A patent/EP3129024A4/en not_active Ceased
- 2015-04-08 JP JP2017504287A patent/JP6672258B2/ja not_active Expired - Fee Related
Patent Citations (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2011231124A (ja) * | 1998-11-13 | 2011-11-17 | Jagotec Ag | 吸入用の乾燥粉末 |
WO2001026630A1 (fr) * | 1999-10-12 | 2001-04-19 | Kaken Pharmaceutical Co., Ltd. | Preparations pour inhalation en poudre et leur procede de production |
JP2009520545A (ja) * | 2005-12-22 | 2009-05-28 | フィリップ・モーリス・プロダクツ・ソシエテ・アノニム | 吸入器具 |
JP2011506589A (ja) * | 2007-12-21 | 2011-03-03 | ウェイ,エドワード,タク | 気道疾患を治療するためのp−メンタン−3−カルボン酸エステル |
JP2013082660A (ja) * | 2011-10-11 | 2013-05-09 | Nico Puff Corp | ニコチン薬の製造法およびその方法により製造される医薬 |
WO2013128283A2 (en) * | 2012-02-28 | 2013-09-06 | Iceutica Holdings Inc. Bvi | Inhalable pharmaceutical compositions |
WO2014047569A2 (en) * | 2012-09-21 | 2014-03-27 | Basil Rigas | Product comprising a nicotine-containing material and an anti-cancer agent |
Non-Patent Citations (1)
Title |
---|
製剤の達人による製剤技術の伝承 下巻 非経口投与製剤の製剤設計と製造方法, 2013/5,P.239-240, JPN6018051969, ISSN: 0004069097 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2020527377A (ja) * | 2017-06-28 | 2020-09-10 | フィリップ・モーリス・プロダクツ・ソシエテ・アノニム | 吸入器と併用するための粒子を含む容器 |
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AU2015260870B2 (en) | 2018-02-08 |
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