公开(公告)号：WO1997024114A1

公开(公告)日：1997-07-10

申请号：PCT/IB1996001461

申请日：1996-12-23

Applicant: DOMPE' S.P.A. ,  GENTILE, Marco ,  BOLTRI, Luigi ,  CLAVENNA, Gaetano

Inventor： DOMPE' S.P.A.

IPC: A61K31/19

CPC classification number: A61K31/192 ,  A61K9/08

Abstract: A pharmaceutical composition for parenteral administration having anti-inflammatory and analgesic properties which contain, as active principle, alkylammonium salts of 2-arylpropionic acids.

Abstract translation: 作为活性成分含有2-芳基丙酸的烷基铵盐的具有抗炎和止痛特性的肠胃外给药用药物组合物。

公开(公告)号：WO2009000473A2

公开(公告)日：2008-12-31

申请号：PCT/EP2008/004993

申请日：2008-06-20

Applicant: DOMPE PHA.R.MA S.P.A. ,  GENTILE, Marco ,  CANTARINI, Marco

Inventor： GENTILE, Marco ,  CANTARINI, Marco

IPC: A61K31/573 ,  A61K9/46 ,  A61K9/72

CPC classification number: A61K31/573 ,  A61K9/0007 ,  A61K9/0078 ,  A61K9/2009

Abstract: The present invention relates to the use of effervescent tablets containing insoluble active principles for the preparation of a suspension for inhalatory use that retain the primary particle size of the drug substance. The tablets dissolve in the solution until a fine suspension is obtained. The suspension maintains the initial particle size distribution of the drug substance, ensuring the achievement of the therapeutic window of the aspired fraction.

Abstract translation: 本发明涉及含有不溶性活性成分的泡腾片剂用于制备保留药物物质一次粒径的吸入用悬浮液。 片剂溶于溶液中直到获得细小的悬浮液。 悬浮液维持药物物质的初始粒度分布，确保达到预期成分的治疗窗口。

公开(公告)号：WO2004078102A2

公开(公告)日：2004-09-16

申请号：PCT/EP2004/050235

申请日：2004-03-02

Applicant: DOMPE S.p.A. ,  GENTILE, Marco ,  DRAGANI, Maria, Concetta ,  DELL'UOMO, Marco

Inventor： GENTILE, Marco ,  DRAGANI, Maria, Concetta ,  DELL'UOMO, Marco

IPC: A61K

CPC classification number: C07J7/00 ,  A61K9/0078 ,  A61K31/56 ,  A61K31/57 ,  A61K31/573 ,  A61L2/0005 ,  A61L2/0011 ,  A61L2/0023 ,  A61L2/04 ,  A61L2/07 ,  C07J5/0015 ,  C07J5/0061 ,  C07J51/00 ,  C07J75/00

Abstract: A process for the sterilization of water insoluble solid medicinal substances is described.The process provides the sterilization of drug substances, which are suitable for pulmonary administration. In particular, the process is used in industrial plants for the production of formulations of sterile glucocorticoids for inhalation delivery, so as to avoid any modifications in particle size distribution and in the impurities profile of the drug. the process is carried out by heating a mixture of micronized glucocorticoid and purified water only, preferably at a temperature of about 120° C for 20 minutes. The process is particularly efficient and economic for the steam sterilization of beclomethasone dipropionate in formulations for pulmonary delivery.

Abstract translation: 描述了对水不溶性固体药物进行灭菌的方法。该方法提供适用于肺部给药的药物灭菌。 特别地，该方法用于生产用于吸入递送的无菌糖皮质激素制剂的工业装置中，以避免药物的粒度分布和杂质分布的任何修改。 该方法仅通过加热微粉化糖皮质激素和纯化水的混合物进行，优选在约120℃的温度下加热20分钟。 该方法对于用于肺部输送的制剂中的丙酸倍氯米松的蒸汽灭菌是特别有效和经济的。

公开(公告)号：WO2008110351A3

公开(公告)日：2008-09-18

申请号：PCT/EP2008/001965

申请日：2008-03-12

Applicant: DOMPE' PHA.R.MA S.P.A. ,  CANTARINI, Marco ,  GENTILE, Marco

Inventor： CANTARINI, Marco ,  GENTILE, Marco

IPC: A61K31/165 ,  A61K31/167 ,  A61K31/40 ,  A61K31/4453 ,  A61P31/00

Abstract: The present invention relates to the use of amides of (R) and (S)-2-aryl- propionic acids as antiseptic agents. The present invention also provides a pharmaceutical preparation including compounds of formula (I), having antiseptic properties for the treatment of gastrointestinal, muco-epidermal and epidermal infections. The present invention is related to pharmaceutical compositions containing an antiseptic agent carried in a suitable vehicle to provide mouthwashes, tablets, solutions, gels, creams and others. The formulations are applied topically to sites of gastrointestinal, muco-epidermal or epidermal infections. Compounds of present invention can be useful in the treatment of nausea, vomiting, bloating, diarrhea, constipation and oropharyngeal, esophageal, vaginal, rectal, nasal and other mucosal infections.

公开(公告)号：WO2008110351A2

公开(公告)日：2008-09-18

申请号：PCT/EP2008001965

申请日：2008-03-12

Applicant: DOMPE PHA R MA SPA RES & MFG ,  CANTARINI MARCO ,  GENTILE MARCO

Inventor： CANTARINI MARCO ,  GENTILE MARCO

IPC: A61K31/165 ,  A61K31/167 ,  A61K31/40 ,  A61K31/4453 ,  A61P31/00

CPC classification number: A61K31/165 ,  A61K31/167 ,  A61K31/40 ,  A61K31/4453

Abstract: The present invention relates to the use of amides of (R) and (S)-2-aryl- propionic acids as antiseptic agents. The present invention also provides a pharmaceutical preparation including compounds of formula (I), having antiseptic properties for the treatment of gastrointestinal, muco-epidermal and epidermal infections. The present invention is related to pharmaceutical compositions containing an antiseptic agent carried in a suitable vehicle to provide mouthwashes, tablets, solutions, gels, creams and others. The formulations are applied topically to sites of gastrointestinal, muco-epidermal or epidermal infections. Compounds of present invention can be useful in the treatment of nausea, vomiting, bloating, diarrhea, constipation and oropharyngeal, esophageal, vaginal, rectal, nasal and other mucosal infections.

Abstract translation: 本发明涉及（R）和（S）-2-芳基 - 丙酸的酰胺作为防腐剂的用途。 本发明还提供了包含式（I）化合物的药物制剂，其具有用于治疗胃肠道，粘膜表皮和表皮感染的防腐性质。 本发明涉及含有在合适的载体中携带的防腐剂以提供漱口剂，片剂，溶液，凝胶，霜剂等的药物组合物。 将制剂局部施用于胃肠道，粘膜表皮或表皮感染的部位。 本发明化合物可用于治疗恶心，呕吐，腹胀，腹泻，便秘和口咽，食管，阴道，直肠，鼻和其他粘膜感染。

公开(公告)号：WO03035673A9

公开(公告)日：2003-11-13

申请号：PCT/EP0211761

申请日：2002-10-21

Applicant: DOMPE SPA ,  GENTILE MARCO ,  DI PALMA CESARE ,  CESTA MARIA CANDIDA

Inventor： GENTILE MARCO ,  DI PALMA CESARE ,  CESTA MARIA CANDIDA

IPC: C12N9/96 ,  C07K1/30 ,  C07K1/32

CPC classification number: C07K1/30 ,  Y02P20/544

Abstract: A process for the co-precipitation of a substance with a stabiliser therefor, by a gas anti solvent process comprising introducing into a particle formation vessel a supercritical fluid pure or mixed with a modifier; and a solution comprising said substance and said stabiliser dissolved in a solvent; so as said solvent is extracted from the solution by said supercritical fluid and co-precipitation of the substance and stabiliser occurs. The process may be carried out using an apparatus comprising a particle formation vessel (22) and a nozzle (27) having a central orifice (39) serving to introduce a solution of the substance and a plurality of outer orifices (41) serving to carry a flow of supercritical fluid into the particle formation vessel (22), such that the solvent is extracted from the solution by the supercritical fluid and precipitation of micron sized particles of the substance/stabilizer occurs. The substance is preferably a protein of pharmaceutical interest, which is highly stabilized for storage by this process.

Abstract translation: 一种通过气体反溶剂方法使物质与稳定剂共沉淀的方法，该方法包括向颗粒形成容器中引入纯净的或与改性剂混合的超临界流体; 以及包含溶解在溶剂中的所述物质和所述稳定剂的溶液; 从而通过所述超临界流体从溶液中提取所述溶剂并且发生物质和稳定剂的共沉淀。 该过程可以使用包括颗粒形成容器（22）和喷嘴（27）的装置来实施，所述喷嘴具有用于引入所述物质的溶液的中心孔口（39）和用于承载所述物质的多个外部孔口（41） 超临界流体流入颗粒形成容器（22）中，使得通过超临界流体从溶液中提取溶剂并且发生物质/稳定剂的微米尺寸颗粒的沉淀。 该物质优选是药物感兴趣的蛋白质，其通过该过程高度稳定以用于储存。

公开(公告)号：WO2004078102A3

公开(公告)日：2004-11-18

申请号：PCT/EP2004050235

申请日：2004-03-02

Applicant: DOMPE SPA ,  GENTILE MARCO ,  DRAGANI MARIA CONCETTA ,  DELL UOMO MARCO

Inventor： GENTILE MARCO ,  DRAGANI MARIA CONCETTA ,  DELL UOMO MARCO

IPC: A61K9/00 ,  A61K31/56 ,  A61K31/57 ,  A61K31/573 ,  A61L2/00 ,  A61L2/04 ,  A61L2/07 ,  C07J5/00 ,  C07J7/00 ,  C07J51/00 ,  C07J75/00

CPC classification number: C07J7/00 ,  A61K9/0078 ,  A61K31/56 ,  A61K31/57 ,  A61K31/573 ,  A61L2/0005 ,  A61L2/0011 ,  A61L2/0023 ,  A61L2/04 ,  A61L2/07 ,  C07J5/0015 ,  C07J5/0061 ,  C07J51/00 ,  C07J75/00

Abstract: A process for the sterilization of water insoluble solid medicinal substances is described.The process provides the sterilization of beclomethasone, which is suitable for pulmonary administration. In particular, the process is used in industrial plants for the production of formulations of sterile beclomethasone for inhalation delivery, so as to avoid any modifications in particle size distribution and in the impurities profile of the drug. The process is carried out by heating a mixture of micronized beclomethasone and purified water only, preferably at a temperature of about 120° C for 20 minutes. The process is particularly efficient and economic for the steam sterilization of beclomethasone dipropionate in formulations for pulmonary delivery.

Abstract translation: 描述了对水不溶性固体药物灭菌的方法。该方法提供了适用于肺部给药的倍氯米松的灭菌方法。 特别地，该方法用于生产用于吸入输送的无菌倍氯米松配方的工业装置中，以避免药物的粒度分布和杂质分布的任何修改。 该方法通过仅加热微粉化的倍氯米松和纯化水的混合物，优选在约120℃的温度下加热20分钟来进行。 该方法对于用于肺部输送的制剂中的丙酸倍氯米松的蒸汽灭菌是特别有效和经济的。

公开(公告)号：WO2009000473A3

公开(公告)日：2009-07-30

申请号：PCT/EP2008004993

申请日：2008-06-20

Applicant: DOMPE PHA R MA SPA RES & MFG ,  GENTILE MARCO ,  CANTARINI MARCO

Inventor： GENTILE MARCO ,  CANTARINI MARCO

IPC: A61K9/46 ,  A61K9/72 ,  A61K31/573

CPC classification number: A61K31/573 ,  A61K9/0007 ,  A61K9/0078 ,  A61K9/2009

Abstract: The present invention relates to the use of effervescent tablets containing insoluble active principles for the preparation of a suspension for inhalatory use that retain the primary particle size of the drug substance. The tablets dissolve in the solution until a fine suspension is obtained. The suspension maintains the initial particle size distribution of the drug substance, ensuring the achievement of the therapeutic window of the aspired fraction.

Abstract translation: 本发明涉及含有不溶性活性成分的泡腾片剂用于制备保留药物物质一次粒径的吸入用悬浮液。 片剂溶于溶液中直到获得细小的悬浮液。 悬浮液维持药物物质的初始粒度分布，确保达到预期成分的治疗窗口。

公开(公告)号：WO2004037242A1

公开(公告)日：2004-05-06

申请号：PCT/EP2003/011689

申请日：2003-10-22

Applicant: DOMPE S.P.A. ,  GENTILE, Marco, Maria ,  DRAGANI, Maria, Concetta

Inventor： GENTILE, Marco, Maria ,  DRAGANI, Maria, Concetta

IPC: A61K31/192

CPC classification number: A61K31/192

Abstract: Pharmaceutical compositions are described, containing an alkylammonium salt of a 2-arylpropionic acid, which are suitable for parenteral administration and do not generate pain upon injection. The compositions contain preferably ketoprofen, ibuprofen, naproxen or tiaprofenic acid in aqueous solution at pH in the range between 8 and 9. The alkylammonium salt is preferably a L-lysine salt. Compositions at pH=8,5 have shown to cause less pain upon injection than other known compositions.

Abstract translation: 描述了含有2-芳基丙酸的烷基铵盐的药物组合物，其适用于肠胃外给药，并且在注射时不产生疼痛。 所述组合物优选在pH为8至9的范围内，在水溶液中含有酮洛芬，布洛芬，萘普生或噻吗啡。烷基铵盐优选为L-赖氨酸盐。 pH = 8,5的组合物已显示注射时疼痛少于其他已知组合物。

公开(公告)号：WO2003035673A1

公开(公告)日：2003-05-01

申请号：PCT/EP2002/011761

申请日：2002-10-21

Applicant: DOMPE S.P.A. ,  GENTILE, Marco ,  DI PALMA, Cesare ,  CESTA, Maria, Candida

Inventor： GENTILE, Marco ,  DI PALMA, Cesare ,  CESTA, Maria, Candida

IPC: C07K1/32

CPC classification number: C07K1/30 ,  Y02P20/544

Abstract: A process for the co-precipitation of a substance with a stabiliser therefor, by a gas anti solvent process comprising introducing into a particle formation vessel a supercritical fluid pure or mixed with a modifier; and a solution comprising said substance and said stabiliser dissolved in a solvent; so as said solvent is extracted from the solution by said supercritical fluid and co-precipitation of the substance and stabiliser occurs. The process may be carried out using an apparatus comprising a particle formation vessel (22) and a nozzle (27) having a central orifice (39) serving to introduce a solution of the substance and a plurality of outer orifices (41) serving to carry a flow of supercritical fluid into the particle formation vessel (22), such that the solvent is extracted from the solution by the supercritical fluid and precipitation of micron sized particles of the substance/stabilizer occurs. The substance is preferably a protein of pharmaceutical interest, which is highly stabilized for storage by this process.

Abstract translation: 通过气体反溶剂法将物质与其稳定剂共沉淀的方法包括将纯的或与改性剂混合的超临界流体引入颗粒形成容器中; 和包含所述物质和所述稳定剂溶于溶剂中的溶液; 因为所述溶剂是通过所述超临界流体从溶液中提取的，并且发生物质和稳定剂的共沉淀。 该方法可以使用包括颗粒形成容器（22）和具有用于引入物质溶液的中心孔（39）和用于携带的多个外孔（41）的喷嘴（27）的装置来进行 将超临界流体流入颗粒形成容器（22），使得通过超临界流体从溶液中提取溶剂，并发生物质/稳定剂的微米级颗粒的沉淀。 该物质优选是药物感兴趣的蛋白质，其通过该方法高度稳定以储存。