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1. 发明授权

US08158134B1 Microemulsion preconcentrate, microemulsion and use thereof 有权
标题翻译：微乳液预浓缩液，微乳液及其用途
公开(公告)号：US08158134B1
公开(公告)日：2012-04-17
申请号：US10110212
申请日：2000-10-20
申请人： Andreas Supersaxo , Marc Antoine Weder , Hans Georg Weder
发明人： Andreas Supersaxo , Marc Antoine Weder , Hans Georg Weder
IPC分类号： A61K9/00 , A61K9/46 , C11D17/00
CPC分类号： A61K9/1075 , A61K9/4858 , A61K38/13
摘要： The invention relates to compositions in the form of microemulsion preconcentrates that contain (a) a mixture that consists of a medium-chain triglyceride and an omega-9 fatty acid and/or an omega-6 fatty acid; and (b) a surface-active component that contains a polyoxethylene tenside. When contacted with water or with an aqueous medium these microemulsion preconcentrates form microemulsions. The microemulsions of the O/W type have an average particle size below 150 nm, preferably below 100 nm. The inventive microemulsion preconcentrates and microemulsions are suitable for use as vehicles for substances, namely active agents, that are hardly soluble in water, but soluble in components (a) and/or (b). In the aqueous phase, said microemulsions may contain water-soluble substances.
摘要翻译：本发明涉及微乳液预浓缩物形式的组合物，其含有（a）由中链甘油三酯和ω-9脂肪酸和/或ω-6脂肪酸组成的混合物; 和（b）含有聚氧乙烯表面活性剂的表面活性成分。当与水或水介质接触时，这些微乳液预浓缩物形成微乳液。 O / W型的微乳液的平均粒度小于150nm，优选低于100nm。本发明的微乳液预浓缩物和微乳液适用于难溶于水但可溶于组分（a）和/或（b）的物质即活性剂的载体。在水相中，所述微乳液可含有水溶性物质。

2. 发明申请

US20060292191A1 Use of nanodispersions in pharmaceutical end formulations 有权
标题翻译：在药物末端制剂中使用纳米分散体
公开(公告)号：US20060292191A1
公开(公告)日：2006-12-28
申请号：US11446844
申请日：2006-06-05
申请人： Andreas Supersaxo , Hans Weder , Dietmar Huglin , Joachim Roding
发明人： Andreas Supersaxo , Hans Weder , Dietmar Huglin , Joachim Roding
IPC分类号： A61K9/00
CPC分类号： A61K9/1075 , A61K9/4858 , A61K9/4866 , Y10S514/846 , Y10S514/937 , Y10S514/938 , Y10S514/941 , Y10S514/947
摘要： A nanodispersion comprises (a) a membrane-forming molecule, (b) a coemulsifier and (c) a lipophilic component, in pharmaceutical end formulations, the nanodispersion being obtainable by (α) mixing the components (a), (b) and (c) until a homogeneous clear liquid is obtained, and (β) adding the liquid obtained in step (α) to the water phase of the pharmaceutical end formulations, where steps (α) and (β) may be carried out without high energy mixing or homogenization. The nanodispersions prepared according to this invention are suitable as transport vehicles for pharmaceutical active agents.
摘要翻译：纳米分散体包含（a）在药物末端制剂中的成膜分子，（b）共乳化剂和（c）亲脂性组分，所述纳米分散体可通过（α）混合组分（a），（b）和（ c）直到获得均匀的透明液体，和（β）将步骤（α）中获得的液体加入到药物末端制剂的水相中，其中步骤（α）和（β）可以在没有高能量混合的情况下进行或均质化。根据本发明制备的纳米分散体适合用作药物活性剂的运输工具。

3. 发明授权

US06420394B1 Topically applied pharmaceutical formulation 失效
标题翻译：局部应用药物制剂
公开(公告)号：US06420394B1
公开(公告)日：2002-07-16
申请号：US09057305
申请日：1998-04-08
申请人： Andreas Supersaxo
发明人： Andreas Supersaxo
IPC分类号： A61K4700
CPC分类号： A61K9/0014 , A61K31/192 , A61K31/196 , A61K31/405 , A61K47/02 , A61K47/10 , A61K47/32 , A61K47/38 , Y10S514/944
摘要： The present invention relates to a novel pharmaceutical formulation for the topical application of drugs, particularly non-steroidal anti-inflammatory drugs (NSAID's), comprising a therapeutically effective amount of a drug, sodium phosphate buffer, and, optionally, an alcoholic solvent. It has been found that by the addition of sodium phosphate buffer to such formulations, the permeation of the NSAID can be significantly improved.
摘要翻译：本发明涉及用于局部施用药物，特别是非甾体抗炎药（NSAID's）的新型药物制剂，其包含治疗有效量的药物，磷酸钠缓冲液和任选的醇溶剂。已经发现，通过向这种制剂中加入磷酸钠缓冲液，NSAID的渗透可以显着改善。

4. 发明授权

US5470582A Controlled delivery of pharmaceuticals from preformed porous polymeric microparticles 失效
标题翻译：药物从预先形成的多孔聚合物微粒的控制递送
公开(公告)号：US5470582A
公开(公告)日：1995-11-28
申请号：US18850
申请日：1993-02-05
申请人： Andreas Supersaxo , Jim H. Kou
发明人： Andreas Supersaxo , Jim H. Kou
IPC分类号： A61K9/00 , A61K9/16 , A61K9/52
CPC分类号： A61K9/1647 , A61K9/0009 , A61K9/1623
摘要： A controlled release pharmaceutical composition comprising a physiologically active agent dispersed in preformed porous polymeric microparticles is provided. The active agent concentration may be up to about 10% by weight to achieve controlled release. Each of the porous microparticles has a plurality of preformed pores into which active agent is loaded and from which the active agent is subsequently released to the environment of use. The compositions are capable of delivering physiologically effective amounts of active agent for at least about thirty days, which delivery may be reversibly controlled by exposure to ultrasound.
摘要翻译：提供了包含分散在预成型多孔聚合物微粒中的生理活性剂的控释药物组合物。活性剂浓度可高达约10重量％以实现控制释放。每个多孔微粒具有多个预成形孔，活性剂被加载到其中，活性剂随后从其中释放到使用环境中。组合物能够递送生理有效量的活性剂至少约30天，该递送可以通过暴露于超声波而被可逆地控制。

5. 发明授权

US5376646A Topical preparations containing the salt of a cholanic acid and a lipid 失效
标题翻译：含有胆酸和脂质盐的局部制剂
公开(公告)号：US5376646A
公开(公告)日：1994-12-27
申请号：US77811
申请日：1993-06-16
申请人： Folker Pittrof , Andreas Supersaxo
发明人： Folker Pittrof , Andreas Supersaxo
IPC分类号： A61K8/14 , A61K8/42 , A61K8/55 , A61K8/63 , A61K8/67 , A61K8/96 , A61K9/107 , A61K47/24 , A61K47/28 , A61Q19/00 , A61K31/685 , A61K31/16 , A61K31/20 , A61K31/535 , A61K31/56
CPC分类号： A61K8/0291 , A61K8/42 , A61K8/553 , A61K8/63 , A61K8/671 , A61K8/678 , A61K9/1075 , A61Q19/00 , Y10S514/947
摘要： Topical preparations containing a salt of a cholanic acid, a lipid, and optionally, one or more other pharmaceutically or cosmetically active substances, are disclosed. These preparations are used in pharmaceutical and/or cosmetic applications.
摘要翻译：公开了含有胆碱酸，脂质和任选的一种或多种其它药学或化妆活性物质的盐的局部制剂。这些制剂用于制药和/或化妆品应用。

6. 发明授权

US6030602A Peptide conjugates for transfecting cells 失效
标题翻译：用于转染细胞的肽缀合物
公开(公告)号：US6030602A
公开(公告)日：2000-02-29
申请号：US782997
申请日：1997-01-14
申请人： Jean-Yves Legendre , Andreas Supersaxo , Arnold Trzeciak
发明人： Jean-Yves Legendre , Andreas Supersaxo , Arnold Trzeciak
IPC分类号： C12N15/09 , A61K9/127 , A61K47/48 , C07F9/10 , C07H21/04 , C07K14/00 , C07K14/195 , C07K14/435 , C07K14/47 , C12N15/64 , A61K51/00 , A61K38/00 , B32B5/16 , C07F9/02
CPC分类号： A61K47/48315 , A61K47/48053 , A61K9/1271 , Y10T428/2984
摘要： The invention relates to conjugates of lipids and basic, membrane disturbing peptides, particularly compounds of the formula(R--CONH).sub.n --R.sup.3 (I)and(R--S--S).sub.n --R.sup.3 (II)wherein R is the hydrocarbyl moiety of a straight-chain or branched-chain, saturated or unsaturated aliphatic carboxylic acid, or a phospholipid moiety having a free valence bond; R.sup.3 is a basic membrane disturbing peptide having a free valence bond at one or two carbon atom(s); and n is 1 or 2. These conjugates can be used as a vector for transfecting a cell with a polynucleotide or any other anionic macromolecule.
摘要翻译：本发明涉及脂质和碱性，膜干扰肽，特别是式（R-CONH）n -R 3（I）和（RSS）n -R 3（II）的化合物的轭合物，其中R是直链 - 链或支链，饱和或不饱和脂族羧酸或具有游离价键的磷脂部分; R3是在一个或两个碳原子上具有游离价键的碱性膜阻断肽; 并且n为1或2.这些缀合物可用作用于用多核苷酸或任何其它阴离子大分子转染细胞的载体。

7. 发明授权

US5759827A Acylated oligopeptides for transfecting cells 失效
标题翻译：用于转染细胞的酰化寡肽
公开(公告)号：US5759827A
公开(公告)日：1998-06-02
申请号：US752129
申请日：1996-11-20
申请人： Jean-Yves Legendre , Andreas Supersaxo , Arnold Trzeciak
发明人： Jean-Yves Legendre , Andreas Supersaxo , Arnold Trzeciak
IPC分类号： C12N15/09 , C07K5/068 , C07K9/00 , C12N15/87 , C12N15/00
CPC分类号： C12N15/87
摘要： Compounds of the formula R.sup.1 --NH--A I wherein R.sup.1 is an acyl moiety of a C.sub.12-40 aliphatic carboxylic acid, A is the residue of a oligopeptide devoid of one amino group, and --NH--A contains at least one positively charged amino acid, or derivatives thereof can be used for transferring anionic macromolecules into cells.
摘要翻译：式R1-NH-A1的化合物，其中R 1是C 12-40脂族羧酸的酰基部分，A是缺少一个氨基的寡肽的残基，并且-NH-A含有至少一个带正电荷的氨基酸，或其衍生物可用于将阴离子大分子转移到细胞中。

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