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1. 发明申请

WO2007012963A1 TRANSDERMAL SYSTEM FOR VARENICLINE 审中-公开
标题翻译：变幅系统VARENICLINE
公开(公告)号：WO2007012963A1
公开(公告)日：2007-02-01
申请号：PCT/IB2006/002081
申请日：2006-07-13
申请人： PFIZER PRODUCTS INC. , JOHNSON, Barbara, Alice , ZIEGLER, Carl, Bernard
发明人： JOHNSON, Barbara, Alice , ZIEGLER, Carl, Bernard
IPC分类号： A61K9/70 , A61K9/12 , A61K31/4995
CPC分类号： A61K31/4995 , A61K9/0014 , A61K9/12 , A61K9/7061 , A61K9/7084
摘要： The invention provides transdermal compositions comprising varenicline or its pharmaceutically acceptable salt or prodrug form.
摘要翻译：本发明提供了包含伐伦克林或其药学上可接受的盐或前药形式的透皮组合物。

2. 发明申请

WO2006072832A1 FAST-DISINTEGRATING DOSAGE FORMS OF 5,8,14-TRIAZATETRACYCLO[10.3.1.02,11.04,9]-HEXADECA-2(11),3,5,7,9-PENTAENE 审中-公开
标题翻译：快速消毒5,8,14-三氮杂环庚啶[10.3.1.02,11.04,9] - 十六烷基-2（11），3,5,7,9-戊二烯
公开(公告)号：WO2006072832A1
公开(公告)日：2006-07-13
申请号：PCT/IB2005/003979
申请日：2005-12-22
申请人： PFIZER PRODUCTS INC. , JOHNSON, Barbara, Alice , ZIEGLER, Carl, Bernard, Jr.
发明人： JOHNSON, Barbara, Alice , ZIEGLER, Carl, Bernard, Jr.
IPC分类号： A61K31/4985 , A61P1/00 , A61P1/04 , A61P3/04 , A61P9/00 , A61P9/10 , A61P9/12 , A61P25/00 , A61P25/02 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22
CPC分类号： A61K31/4985 , A61K9/0007 , A61K9/0056 , A61K9/2077 , A61K9/2081 , A61K9/2095 , A61K9/5047 , A61K9/7007
摘要： A fast disintegrating dosage form of varenicline comprising an effective amount of varenicline or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable excipient, wherein the dosage form disintegrates in a patient's oral cavity in less than three minutes. Also provided are a method for reducing nicotine addiction, aiding in the cessation of, or lessening of tobacco use in a subject by administering to the subject an effective amount of the fast disintegrating dosage form of varenicline or pharmaceutically acceptable salts thereof; a method of treating a disorder or condition by administering an effective amount of the fast disintegrating dosage form of varenicline; and, various methods of manufacturing or forming an immediate dosage form of varenicline.
摘要翻译：一种快速崩解的伐伦赛因剂型，其包含有效量的伐伦碱或其药学上可接受的盐和至少一种药学上可接受的赋形剂，其中所述剂型在不到三分钟的时间内在患者的口腔内崩解。还提供了一种通过向受试者施用有效量的快速崩解剂型伐木林或其药学上可接受的盐来减少尼古丁成瘾，帮助停止或减轻受试者的烟草使用的方法。通过施用有效量的快速崩解剂型的伐伦尼克来治疗病症或病症的方法; 以及制造或形成伐尼克兰立即剂型的各种方法。

3. 发明申请

WO2006067577A2 STABLE NON-DIHYDRATE AZITHROMYCIN ORAL SUSPENSIONS 审中-公开
标题翻译：稳定的非二水酸阿奇霉素口服悬浮液
公开(公告)号：WO2006067577A2
公开(公告)日：2006-06-29
申请号：PCT/IB2005/003767
申请日：2005-12-09
申请人： PFIZER PRODUCTS INC. , JOHNSON, Barbara, Alice , MURPHY, Brendan, John
发明人： JOHNSON, Barbara, Alice , MURPHY, Brendan, John
CPC分类号： A61K9/0095 , A61K31/7048 , A61K47/40 , A61K47/6951 , B82Y5/00
摘要： This invention relates to a powder for oral suspension, and an oral suspension made there from, which comprises non-dihydrate azithromycin and an azithromycin conversion stabilizing excipient, wherein said excipient reduces the conversion of the form of azithromycin, when placed in suspension, to another form of azithromycin. This invention further relates to a method for reducing the conversion of a form of non-dihydrate azithromycin, in an oral suspension, by including at least one cyclodextrin in said oral suspension.
摘要翻译：本发明涉及用于口服悬浮液的粉末和由其制成的口服悬浮液，其包含非二水合阿奇霉素和阿奇霉素转化稳定赋形剂，其中所述赋形剂减少阿奇霉素形式的转化，当置于悬浮液中时，转变为另一种形式的阿奇霉素。本发明进一步涉及通过在所述口服悬浮液中包含至少一种环糊精来减少口服混悬液中非二水合阿奇霉素形式的转化的方法。

4. 发明申请

WO2005004920A1 STABLE NON-DIHYDRATE AZITHROMYCIN ORAL SUSPENSIONS 审中-公开
标题翻译：稳定的非二异丙基纤维素口服悬浮液
公开(公告)号：WO2005004920A1
公开(公告)日：2005-01-20
申请号：PCT/IB2004/001610
申请日：2004-05-12
申请人： PFIZER PRODUCTS INC. , COLLIER, Steven, William , CURATOLO, William, John , JOHNSON, Barbara, Alice , MURPHY, Brendan, John
发明人： COLLIER, Steven, William , CURATOLO, William, John , JOHNSON, Barbara, Alice , MURPHY, Brendan, John
IPC分类号： A61K47/26
CPC分类号： A61K9/0095 , A61K31/7048
摘要： This invention relates to a powder for oral suspension, and an oral suspension made there from, which comprises non-dihydrate azithromycin and an azithromycin conversion stabilizing excipient, wherein said excipient reduces the conversion of the form of azithromycin, when placed in suspension, to another form of azithromycin. This invention further relates to a method for reducing the conversion of a form of non-dihydrate azithromycin, in an oral suspension, by adding a surface tension reducing excipient that reduces the surface tension of the aqueous vehicle. Furthermore, this invention relates to a method for reducing the conversion of a non-dihydrate azithromycin, in an unflavored oral suspension, by raising the viscosity of the oral suspension, and in a flavored oral suspension by lowering the viscosity of the oral suspension.
摘要翻译：本发明涉及一种用于口服悬浮液的粉末和由其制备的口服悬浮液，其包含非二水合阿奇霉素和阿奇霉素转化稳定赋形剂，其中所述赋形剂将阿奇霉素的形式在悬浮液中降低至另一种阿奇霉素的形式。本发明还涉及通过添加降低水性载体的表面张力的表面张力降低赋形剂来降低口服悬浮液中的二水合阿奇霉素形式的转化的方法。此外，本发明涉及通过提高口腔悬浮液的粘度和通过降低口服悬浮液的粘度而在调味口服悬浮液中降低非味道口服悬浮液中非二水合阿奇霉素的转化率的方法。

5. 发明申请

WO2004110431A1 STABLE COMPOSITIONS OF ATORVASTATIN PREPARED WITH WET GRANULATION 审中-公开
标题翻译：稳定的组合物制备与湿法生成的ATORVASTATIN
公开(公告)号：WO2004110431A1
公开(公告)日：2004-12-23
申请号：PCT/IB2004/001862
申请日：2004-06-01
申请人： WARNER-LAMBERT COMPANY LLC , WATERMAN, Kenneth, Craig , FERGIONE, Michael, Bruce , JOHNSON, Barbara, Alice
发明人： WATERMAN, Kenneth, Craig , FERGIONE, Michael, Bruce , JOHNSON, Barbara, Alice
IPC分类号： A61K31/40
CPC分类号： A61K9/1623 , A61K9/1652 , A61K31/40
摘要： A wet granulated pharmaceutical composition comprising atorvastatin or a pharmaceutically acceptable salt thereof with less than about 5 weight% of an alkaline earth metal salt additive with a disintegrant which provides the atorvastatin with not more than about 3% atorvastatin lactone based on the ratio of lactone peak area compared to the total drug-related peak integrated areas, as well as said wet granulated pharmaceutical composition comprising atorvastatin or a pharmaceutically acceptable salt thereof in combination with at least one other active drug, methods for preparing said compositions, kits for containing such compositions, and a method of treating hypercholesterolemia and/or hyperlipidemia, osteoporosis, benign prostatic hyperplasia (BPH), and Alzheimer's disease using a therapeutically effective amount of the pharmaceutical compositions.
摘要翻译：一种湿颗粒状药物组合物，其包含阿托伐他汀或其药学上可接受的盐和小于约5重量％的具有崩解剂的碱土金属盐添加剂，其基于内酯峰的比例提供阿托伐他汀不超过约3％的阿托伐他汀内酯以及所述含有阿托伐他汀或其药学上可接受的盐与至少一种其它活性药物组合的湿法制粒药物组合物，所述组合物的制备方法，用于含有该组合物的试剂盒，以及使用治疗有效量的药物组合物治疗高胆固醇血症和/或高脂血症，骨质疏松症，良性前列腺增生症（BPH）和阿尔茨海默病的方法。

6. 发明申请

WO2003053399A2 METHODS FOR WET GRANULATING AZITHROMYCIN 审中-公开
标题翻译：湿法生长AZITHROMYCIN的方法
公开(公告)号：WO2003053399A2
公开(公告)日：2003-07-03
申请号：PCT/IB2002/005338
申请日：2002-12-09
申请人： PFIZER PRODUCTS INC. , FERGIONE, Michael, Bruce , JOHNSON, Barbara, Alice
发明人： FERGIONE, Michael, Bruce , JOHNSON, Barbara, Alice
IPC分类号： A61K9/00
CPC分类号： A61K31/7052 , A61K9/1611 , A61K9/1623 , A61K9/1635 , A61K9/1652 , A61K9/1688 , A61K9/1694
摘要： The present invention relates to a method of forming non-dihydrate azithromycin granules, comprising mixing non-dihydrate azithromycin particles, with a granulating amount of a granulating liquid, and, optionally, with particles of one or more excipients, to form wet granules which comprise non-dihydrate azithromycin and the granulating liquid. The granules are then dried to remove the granulating liquid. The invention further relates to a pharmaceutical composition comprising granules of a non-dihydrate azithromycin and at least one pharmaceutically acceptable excipient. The invention also relates to pharmaceutical formulations comprising granules of non-dihydrate azithromycin. The invention further relates to granules of dihydrate azitrhromycin wherein the granules comprises 98% or more dihydrate azithromycin and from about 2% to 0%, total weight, of one or more pharmaceutically acceptable excipients.
摘要翻译：本发明涉及一种形成非二水合阿奇霉素颗粒的方法，其包括将非二水合阿奇霉素颗粒与造粒量的造粒液体以及任选地与一种或多种赋形剂的颗粒混合以形成湿颗粒，其包含非二水合阿奇霉素和造粒液。然后将颗粒干燥以除去造粒液体。本发明还涉及包含非二水合阿奇霉素和至少一种药学上可接受的赋形剂的颗粒的药物组合物。本发明还涉及包含非二水合阿奇霉素颗粒的药物制剂。本发明还涉及二水合阿霉素的颗粒，其中颗粒包含98％或更多的二水合阿奇霉素和约2％至0％的总重量的一种或多种药学上可接受的赋形剂。

7. 发明申请

WO2006067577A3 STABLE NON-DIHYDRATE AZITHROMYCIN ORAL SUSPENSIONS 审中-公开
标题翻译：稳定的非二异丙基纤维素口服悬浮液
公开(公告)号：WO2006067577A3
公开(公告)日：2006-12-28
申请号：PCT/IB2005003767
申请日：2005-12-09
申请人： PFIZER PROD INC , JOHNSON BARBARA ALICE , MURPHY BRENDAN JOHN
发明人： JOHNSON BARBARA ALICE , MURPHY BRENDAN JOHN
IPC分类号： A61K31/7048 , A61K9/00 , A61K47/40 , A61K47/48
CPC分类号： A61K9/0095 , A61K31/7048 , A61K47/40 , A61K47/6951 , B82Y5/00
摘要： This invention relates to a powder for oral suspension, and an oral suspension made there from, which comprises non-dihydrate azithromycin and an azithromycin conversion stabilizing excipient, wherein said excipient reduces the conversion of the form of azithromycin, when placed in suspension, to another form of azithromycin. This invention further relates to a method for reducing the conversion of a form of non-dihydrate azithromycin, in an oral suspension, by including at least one cyclodextrin in said oral suspension.
摘要翻译：本发明涉及用于口服悬浮液的粉末和由其制备的口服悬浮液，其包含非二水合阿奇霉素和阿奇霉素转化稳定赋形剂，其中所述赋形剂将阿奇霉素的形式在悬浮液中降低至另一种阿奇霉素的形式。本发明还涉及通过在所述口服悬浮液中包含至少一种环糊精来减少口服悬浮液中的一种形式的二水合阿奇霉素的转化的方法。

8. 发明申请

WO2006040680A1 COMPOSITIONS AND METHODS FOR INTRANASAL, BUCCAL, SUBLINGUAL AND PULMONARY DELIVERY OF VARENICLINE 审中-公开
标题翻译：内脏，膀胱，子宫颈和肺动脉分布的组成和方法
公开(公告)号：WO2006040680A1
公开(公告)日：2006-04-20
申请号：PCT/IB2005/003236
申请日：2005-10-06
申请人： PFIZER PRODUCTS INC. , ZIEGLER, Carl, Bernard, Jr. , JOHNSON, Barbara, Alice
发明人： ZIEGLER, Carl, Bernard, Jr. , JOHNSON, Barbara, Alice
IPC分类号： A61K9/08 , A61K9/12 , A61K9/20 , A61K31/55 , A61P25/34
CPC分类号： A61K9/0075 , A61K9/0043 , A61K9/0056 , A61K9/006 , A61K9/146 , A61K9/1611 , A61K9/1617 , A61K9/2013 , A61K9/2068 , A61K9/2095 , A61K31/55 , A61K47/12 , A61K47/36 , A61K47/38
摘要： A composition for nasal administration comprising varenicline or its pharmaceutically acceptable salt and at least one excipient. The invention also provides a composition for buccal administration comprising varenicline or its pharmaceutically acceptable salt and at least one excipient to form a solid dosage form, wherein the solid dosage form disintegrates in an oral cavity at body temperature and may adhere to body tissue of the oral cavity; a composition for pulmonary administration comprising varenicline or its pharmaceutically acceptable salt and at least one excipient; and, a method for reducing nicotine addiction, aiding in the cessation of, or lessening of tobacco use in a subject.
摘要翻译：一种用于鼻内给药的组合物，其包含伐伦克林或其药学上可接受的盐和至少一种赋形剂。本发明还提供了一种用于口腔给药的组合物，其包含伐伦克林或其药学上可接受的盐和至少一种赋形剂以形成固体剂型，其中固体剂型在体温下在口腔中崩解并且可能粘附于口腔的身体组织腔; 用于肺部施用的组合物，其包含伐伦克林或其药学上可接受的盐和至少一种赋形剂; 以及减少尼古丁成瘾，帮助停止或减轻受试者中烟草使用的方法。

9. 发明申请

WO2003063838A1 DRY GRANULATED FORMULATIONS OF AZITHROMYCIN 审中-公开
标题翻译：阿霉素的干燥制粒剂
公开(公告)号：WO2003063838A1
公开(公告)日：2003-08-07
申请号：PCT/IB2003/000212
申请日：2003-01-20
申请人： PFIZER PRODUCTS INC. , JOHNSON, Barbara, Alice , QUAN, Ernest, Shing
发明人： JOHNSON, Barbara, Alice , QUAN, Ernest, Shing
IPC分类号： A61K9/20
CPC分类号： A61K31/70 , A61K9/2009 , A61K9/2054 , A61K9/2095
摘要： This invention relates to a pharmaceutical formulation, in the form of a tablet, sachet or powder for suspension dosage form, which comprises dry granulated particles of a non-dihydrate form of azithromycin and, optionally, one or more pharmaceutically acceptable excipients. Preferably, the pharmaceutical formulation is a tablet containing between about 40%, by weight, to about 85% , by weight, non-dihydrate azithromycin. More preferably, the pharmaceutical formulation contains non-dihydrate azithromycin selected from the forms B, D, E, F, G, H, J, M, N, 0, P, Q, R, or mixtures thereof. Even more preferably, the invention relates to a pharmaceutical formulation wherein the dosage of azithromycin is 250 mgA, 500 mgA, 600 mgA or 1000 mgA. The present invention further relates to a dry granulated azithromycin particle, comprising a form of azithromycin, selected from forms D, E, F, G, H, J, M, N, 0, P, Q, R and mixtures of non-dihydrate forms, and at least one pharmaceutically acceptable excipient.
摘要翻译：本发明涉及一种片剂形式的药物制剂，用于悬浮剂型的小药囊或粉剂，其包含非二水合形式的阿奇霉素和任选的一种或多种药学上可接受的赋形剂的干燥造粒颗粒。优选地，药物制剂是含有约40重量％至约85重量％的非二水合阿奇霉素的片剂。更优选地，药物制剂含有选自形式B，D，E，F，G，H，J，M，N，O，P，Q，R或其混合物的非二水合阿奇霉素。更优选地，本发明涉及药物制剂，其中阿奇霉素的剂量为250mgA，500mgA，600mgA或1000mgA。本发明还涉及一种包含形式D，E，F，G，H，J，M，N，O，P，Q，R和非二水合物混合物的阿奇霉素形式的干燥粒状阿奇霉素颗粒形式和至少一种药学上可接受的赋形剂。

10. 发明申请

WO2003053416A1 DIRECTLY COMPRESSIBLE FORMULATIONS OF AZITHROMYCIN 审中-公开
标题翻译：直接强制制备AZITHROMYCIN
公开(公告)号：WO2003053416A1
公开(公告)日：2003-07-03
申请号：PCT/IB2002/005222
申请日：2002-12-09
申请人： PFIZER PRODUCTS INC. , MURPHY, Brendn, John , COLLIER, Steven, William , QUAN, Ernest, Shing , JOHNSON, Barbara, Alice
发明人： MURPHY, Brendn, John , COLLIER, Steven, William , QUAN, Ernest, Shing , JOHNSON, Barbara, Alice
IPC分类号： A61K9/20
CPC分类号： A61K31/7052 , A61K9/2018 , A61K9/2054 , A61K9/2095
摘要： The present invention relates to a dry blend, used for forming azithromycin tablets by direct compression, comprising non-dihydrate azithromycin and at least one pharmaceutically acceptable excipient. This invention also relates to an azithromycin tablet comprising non-dihydrate azithromycin and at least one pharmaceutically acceptable excipient. Preferably, the azithromycin tablet is formed by direct compressing the dry blend, of the present invention, to form said azithromycin tablet. Preferably, the azithromycin tablet, of the present invention, contains a dosage of 250 mgA, 500 mgA or 600 mgA of azithromycin. This invention further relates to an azithromycin tablet which is produced by forming a dry blend of a non-granulated azithromycin form A and at least one pharmaceutically acceptable excipient. The azithromycin tablet is then formed by formed by direct compressing the dry blend.
摘要翻译：本发明涉及用于通过直接压制形成阿奇霉素片剂的干混物，其包含非二水合阿奇霉素和至少一种药学上可接受的赋形剂。本发明还涉及包含非二水合阿奇霉素和至少一种药学上可接受的赋形剂的阿奇霉素片剂。优选地，阿奇霉素片剂通过直接压制本发明的干混物形成，以形成所述阿奇霉素片剂。优选地，本发明的阿奇霉素片剂含有250mgA，500mgA或600mgA阿奇霉素的剂量。本发明还涉及阿奇霉素片剂，其通过形成无颗粒状阿奇霉素A型和至少一种药学上可接受的赋形剂的干混合物而制备。然后通过直接压缩干混合物形成阿奇霉素片剂。

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