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1. 发明公开

EP0857484A1 PGE 1?-CONTAINING FREEZE-DRIED PREPARATION AND PROCESS FOR THE PRODUCTION THEREOF 失效
标题翻译： PGE1 ENTHALTENDE GEFRIERGETROCKNETE ZUBEREITUNG UND VERFAHREN ZU DEREN HERSTELLUNG
公开(公告)号：EP0857484A1
公开(公告)日：1998-08-12
申请号：EP96930379.1
申请日：1996-09-12
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： YOSHIKAWA, Hirofumi , SASAKI, Hideki , SEKI, Junzo
IPC分类号： A61K31/557 , A61K9/14
CPC分类号： A61K31/5575 , A61K9/1075 , A61K9/19 , A61K31/557
摘要： A preparation relating to a PGE 1 -containing fat emulsion with excellent qualities which is superior to the conventional ones bacteriologically or in thermal or prolonged stability. The preparation is a freeze-dried one derived from a fat emulsion which contains PGE 1 , an oily component, an emulsifier and water and has a liquid nature (pH value) within the neutral region. In other words, it is a PGE 1 -containing freeze-dried preparation characterized by containing PGE 1 , an oily component and an emulsifier and having a liquid nature (pH value) falling within the neutral region immediately after the reconstitution (restoration) with distilled water of pH 7.0.
摘要翻译：一种与含有PGE1的脂肪乳剂相关的制剂，其优良品质优于传统的脂肪乳剂，在细菌学或热稳定性或长期稳定性方面优于常规的。该制剂是由含有PGE1，油性成分，乳化剂和水的脂肪乳剂得到的冷冻干燥剂，并且在中性区域内具有液体性质（pH值）。换句话说，它是一种含PGE1的冷冻干燥制品，其特征在于含有PGE1，一种油性成分和一种乳化剂，并且在用蒸馏水重构（恢复）后立即在中性区域内具有液体性质（pH值） pH 7.0。

2. 发明公开

EP0770422A1 EMULSION MANUFACTURING METHOD OF EMULSIFIER 失效
标题翻译： VERFAHREN ZUM HERSTELLEN VON EMULSIONEN AUS EINEM EMULGATOR
公开(公告)号：EP0770422A1
公开(公告)日：1997-05-02
申请号：EP95921981.7
申请日：1995-06-19
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： SAHEKI, Akira Nagaoka-ryo Nippon Shinyaku Co. Ltd , SEKI, Junzo
IPC分类号： B01F3/08 , B01F5/00 , B01J13/00 , A61K9/107
CPC分类号： B01F5/0662 , B01F3/0811 , B01F5/0256 , B01F5/0268 , B01F5/0609 , B01F5/0647 , B01F5/0648 , B01F5/0651 , B01F5/068 , Y10S514/941 , Y10S516/923 , Y10S516/928
摘要： There is provided a method of producing an emulsion by which an emulsion consisting of uniform and microfine globules can be easily obtained with a reduced energy input as compared with the conventional technology.
This method of producing an emulsion comprises applying a back pressure equal to not less than 0.2% but less than 5% of the pressure acting on the point of high-pressure emulsifying action in a high-pressure emulsification zone in the course of production of an emulsion with a high-pressure emulsification equipment. The back pressure can be obtained typically by equipping an emulsification machine with a pipeline smaller in inside diameter than the discharge line of the machine.
摘要翻译：提供了一种生产乳液的方法，与常规技术相比，能够以较少的能量输入容易地获得由均匀和微细小球组成的乳液。该制造乳液的方法包括在制造过程中施加相当于在高压乳化区域作用于高压乳化作用点的压力的0.2％以上且小于5％的背压乳液用高压乳化设备。通常，通过使乳化机具有比机器的排出管线更小的内径的管道，可以获得背压。

3. 发明授权

EP0770422B1 EMULSION MANUFACTURING METHOD OF EMULSIFIER 失效
标题翻译：用于生产乳液从乳化剂
公开(公告)号：EP0770422B1
公开(公告)日：2002-09-04
申请号：EP95921981.7
申请日：1995-06-19
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： SAHEKI, Akira Nagaoka-ryo Nippon Shinyaku Co. Ltd , SEKI, Junzo
IPC分类号： B01F3/08 , B01F5/00 , B01J13/00 , A61K9/107 , B01F5/06
CPC分类号： B01F5/0662 , B01F3/0811 , B01F5/0256 , B01F5/0268 , B01F5/0609 , B01F5/0647 , B01F5/0648 , B01F5/0651 , B01F5/068 , Y10S514/941 , Y10S516/923 , Y10S516/928
摘要： An emulsion manufacturing method capable of providing an emulsion which comprises fine emulsion particles with a lower energy supply than in the conventional method of this kind, and providing easily an emulsion comprising uniform fine emulsion particles. The method is characterized in that a back pressure which is not less than 0.2 % and less than 5 % of the pressure applied to point of high-pressure emulsification in a high-pressure emulsification unit is exerted on a raw material during the manufacturing of an emulsion in a high-pressure emulsifier. The back pressure can be obtained by providing a discharge unit with, for example, a device having a pipe the inner diameter of which is smaller than that of a pipe in the discharge unit.

4. 发明授权

EP0598116B1 FAT EMULSION 失效
标题翻译： FETTEMULSION
公开(公告)号：EP0598116B1
公开(公告)日：1996-07-24
申请号：EP90917270.2
申请日：1990-11-26
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： SEKI, Junzo , USHIMARU, Kouichi , SUGIYAMA, Makoto
IPC分类号： A61K9/107 , A61K31/71
CPC分类号： A61K9/1075 , A61K31/7048
摘要： A fat emulsion developed to solve the problems of polyene antifungal antibiotics that they have such a severe toxicity as to limit the administration range thereof by suitably designing the administration form, thereby reducing the hemolytic toxicity and nephrotoxicity and facilitating the migration of a drug toward infected parts without adversely affecting the pharmacological action (antifungal action) on a molecular level. The emulsion comprises 0.005 to 5 % of a polyene antifungal antibiotic, 0.5 to 30 % of a simple lipid, and a phospholipid in an amount 0.15 to 2 times as large as that of the simple lipid, wherein the relative proportion of each ingredient is controlled to give a fine microemulsion of a mean particle diameter of at least 10 nm up to 100 nm. This emulsion can remarkably enhance the efficacy of polyene antifungal antibiotics such as Amphotericin B and is very useful for the development of medicines.

5. 发明公开

EP0598116A1 FAT EMULSION 失效
标题翻译： FETTEMULSION。
公开(公告)号：EP0598116A1
公开(公告)日：1994-05-25
申请号：EP90917270.2
申请日：1990-11-26
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： SEKI, Junzo , USHIMARU, Kouichi , SUGIYAMA, Makoto
IPC分类号： A61K9/107 , A61K31/71
CPC分类号： A61K9/1075 , A61K31/7048
摘要： A fat emulsion developed to solve the problems of polyene antifungal antibiotics that they have such a severe toxicity as to limit the administration range thereof by suitably designing the administration form, thereby reducing the hemolytic toxicity and nephrotoxicity and facilitating the migration of a drug toward infected parts without adversely affecting the pharmacological action (antifungal action) on a molecular level. The emulsion comprises 0.005 to 5 % of a polyene antifungal antibiotic, 0.5 to 30 % of a simple lipid, and a phospholipid in an amount 0.15 to 2 times as large as that of the simple lipid, wherein the relative proportion of each ingredient is controlled to give a fine microemulsion of a mean particle diameter of at least 10 nm up to 100 nm. This emulsion can remarkably enhance the efficacy of polyene antifungal antibiotics such as Amphotericin B and is very useful for the development of medicines.
摘要翻译：为了解决多烯抗真菌抗生素的问题，开发了一种脂肪乳剂，它们具有如此严重的毒性，通过适当地设计给药形式来限制其给药范围，从而降低溶血毒性和肾毒性并促进药物向感染部位的迁移而不会对分子水平的药理作用（抗真菌作用）产生不利影响。乳液含有0.005〜5％的多烯抗真菌抗生素，0.5〜30％的单一脂质，磷脂的量为单质脂质量的0.15〜2倍，其中各成分的相对比例被控制得到至少10nm至100nm的平均粒径的微细微乳液。该乳液可以显着提高多烯抗真菌抗生素如两性霉素B的功效，对于药物的开发是非常有用的。

6. 发明公开

EP0510197A1 FAT EMULSION 失效
公开(公告)号：EP0510197A1
公开(公告)日：1992-10-28
申请号：EP91901901.8
申请日：1991-01-09
申请人： NIPPON SHINYAKU COMPANY, LIMITED
发明人： SEKI, Junzo , USHIMARU, Kouichi , SUGIYAMA, Makoto
IPC分类号： A61K31/40 , A61K31/58 , A61K9/107 , A61K47/24
CPC分类号： A61K9/1075 , A61K31/40
摘要： A fat emulsion mainly comprising 0.001 to 10 % (w/v) of a mitomycin C derivative of general formula (I), 0.5 to 30 % (w/v) of a simple lipid, a phospholipid in an amount of 0.05 to 2 times by weight as large as the simple lipid, and an appropriate amount of water: (I) wherein X represents -(CH₂) n -O- or -(CH₂) n -NHCOO-; n represents an integer of 0 to 4; and R represents a linear or branched, open-chain or cyclic, saturated or unsaturated hydrocarbon group containing 3 to 25 carbon atomes. This emulsion causes efficient migration of a prodrug of mitomycin C with a carcinostatic action in the form of an injection into the tissues, helps to maintain its blood level, and allows safe administration of an effective dose.
摘要翻译：主要含有通式（I）的丝裂霉素C衍生物0.001〜10％（w / v），单纯脂质0.5〜30％（w / v），磷脂0.05〜2倍（Ⅰ）其中X代表 - （CH 2）nO-或 - （CH 2）n-NHCOO-; n表示0至4的整数; R代表含有3-25个碳原子的直链或支链的开链或环状饱和或不饱和烃基。这种乳剂可以使丝裂霉素C前体药物以制癌作用以注射剂的形式有效地迁移到组织中，有助于维持其血液水平，并允许安全施用有效剂量。

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