Preparation of peptide containing biodegradable microspheres by melt
process
    1.
    发明授权
    Preparation of peptide containing biodegradable microspheres by melt process 失效
    通过熔融法制备含可生物降解微球的肽

    公开(公告)号:US5665428A

    公开(公告)日:1997-09-09

    申请号:US547962

    申请日:1995-10-25

    摘要: Peptide/protein biodegradable drug delivery devices are prepared as microspheres without the use of solvents by a polymer melt process. A melt of thermostable polypeptides and an appropriate low melting block copolymer mixture is prepared and dispersed in an appropriate fluid medium such as air, water or an immiscible organic fluid without using any organic solvent to form microdroplets. The fluid medium is cooled to solidify the microdroplets into microspheres and then collected and purified or further processed as drug delivery devices. These biodegradable microspheres are suitable as implantable or injectable pharmaceutical formulations. Following administration as solid microspheres into the body of a warm blooded animal, the formulations absorb water from the body to form a hydrogel from which the polypeptide is released continuously over an extended period of time.

    摘要翻译: 肽/蛋白质可生物降解的药物递送装置通过聚合物熔融方法制备为不使用溶剂的微球。 制备热稳定多肽和合适的低熔点嵌段共聚物混合物的熔体并将其分散在合适的流体介质如空气,水或不混溶的有机流体中,而不使用任何有机溶剂形成微滴。 将流体培养基冷却以将微滴固化成微球,然后收集并纯化或进一步加工为药物递送装置。 这些可生物降解的微球体适合作为可植入或可注射的药物制剂。 在作为固体微球体施用于温血动物的体内后,制剂吸收来自身体的水以形成水凝胶,多肽在延长的时间段内连续释放。

    Thermosensitive biodegradable polymers based on poly(ether-ester)block
copolymers
    2.
    发明授权
    Thermosensitive biodegradable polymers based on poly(ether-ester)block copolymers 失效
    基于聚(醚 - 酯)嵌段共聚物的热敏生物降解聚合物

    公开(公告)号:US5702717A

    公开(公告)日:1997-12-30

    申请号:US548185

    申请日:1995-10-25

    摘要: A system and method for the parenteral delivery of a drug in a biodegradable polymeric matrix to a warm blooded animal as a liquid with the resultant formation of a gel depot for the controlled release of the drug. The system comprises an injectable biodegradable block copolymeric drug delivery liquid having reverse thermal gelation properties. The delivery liquid is an aqueous solution having dissolved or dispersed therein an effective amount of a drug intimately contained in a biodegradable block copolymer matrix. The copolymer has a reverse gelation temperature below the body temperature of the animal to which it is administered and is made up of (i) a hydrophobic A polymer block comprising a member selected from the group consisting of poly(.alpha.-hydroxy acids) and poly(ethylene carbonates) and (ii) a hydrophilic B polymer block comprising a polyethylene glycol. Prior to use the liquid is maintained at a temperature below the reverse gelation temperature of the block copolymer. The liquid is parenterally administered into the animal by intramuscular, intraperitoneal, subcutaneous or similar injection with the liquid forming a gel depot of the drug and biodegradable block polymer as the temperature of the liquid is raised by the body temperature of the animal the reverse gelation temperature of the block copolymer. The drug is released at a controlled rate from the copolymer which biodegrades into non-toxic products. The degradation rate can be adjusted by proper selection of the poly(.alpha.-hydroxy acid) utilized in forming the biodegradable hydrophilic A block.

    摘要翻译: 一种用于将可生物降解的聚合物基质中的药物肠胃外递送至温血动物作为液体的系统和方法,其中形成用于控释药物的凝胶储库。 该系统包括具有反向热凝胶化特性的可注射的可生物降解的嵌段共聚物药物递送液体。 输送液体是其中溶解或分散有效量的药物,其密封地包含在可生物降解的嵌段共聚物基质中。 该共聚物具有低于其施用的动物的体温的反向凝胶化温度,并且由以下组成:(i)疏水性A聚合物嵌段,其包含选自聚(α-羟基酸)和聚 (碳酸亚乙酯)和(ii)包含聚乙二醇的亲水性B聚合物嵌段。 在使用之前,液体保持在低于嵌段共聚物的反胶凝温度的温度。 液体通过肌内,腹膜内,皮下或类似的注射而肠胃外施用于动物中,液体形成药物的凝胶储存库和可生物降解的嵌段聚合物,因为液体的温度由动物的体温升高,反向凝胶化温度 的嵌段共聚物。 该药物以可控制的速率从生物降解成无毒产物的共聚物释放。 可以通过适当选择用于形成可生物降解的亲水性A嵌段的聚(α-羟基酸)来调节降解速率。

    Biodegradable mixed polymeric micelles for gene delivery
    3.
    发明授权
    Biodegradable mixed polymeric micelles for gene delivery 有权
    用于基因递送的可生物降解的混合聚合胶束

    公开(公告)号:US06210717B1

    公开(公告)日:2001-04-03

    申请号:US09209631

    申请日:1998-12-11

    IPC分类号: A61K950

    摘要: A biodegradable, mixed polymeric micelle used to deliver a selected nucleic acid into a targeted host cell contains an amphiphilic polyester-polycation copolymer and an amphiphilic polyester-sugar copolymer. The polyester-polycation copolymer forms an electrostatic interaction with polyanionic nucleic acids, and the polyester-sugar copolymer directs the micelle-nucleic acid complex to cells in vivo. Additional copolymers with similar properties may also be included. The composition improves delivery efficiency by providing a particulate gene carrier for which particle size and charge density are easily controlled by multivariate means. Various kinds of ligands and other functional compounds may be also be introduced using the composition. The composition may be used in a method for transforming a targeted host cell with a selected nucleic acid.

    摘要翻译: 用于将选择的核酸递送到靶宿主细胞中的可生物降解的混合聚合物胶束含有两亲性聚酯 - 聚阳离子共聚物和两亲聚酯 - 糖共聚物。 聚酯 - 聚阳离子共聚物与聚阴离子核酸形成静电相互作用,聚酯 - 糖共聚物将胶束 - 核酸复合体引导至细胞体内。 还可以包括具有相似性质的另外的共聚物。 该组合物通过提供通过多变量手段容易地控制粒度和电荷密度的颗粒基因载体来提高递送效率。 也可以使用该组合物引入各种配体和其它官能化合物。 该组合物可以用于用选择的核酸转化靶宿主细胞的方法。

    Patch for tooth whitening
    4.
    发明授权
    Patch for tooth whitening 有权
    修补牙齿美白

    公开(公告)号:US07323161B2

    公开(公告)日:2008-01-29

    申请号:US10729648

    申请日:2003-12-05

    IPC分类号: A61K8/00 A61Q11/00 A61F13/00

    摘要: The patch for tooth whitening of the present invention includes a tooth-adhering layer (1) containing erodible polymer complexes formed by hydrogen bonding of a polymer with a carboxyl group (—COOH) and a polymer with a carbonyl group (—C═O) or ether group (—O—) and a tooth whitening agent; and an erosion rate-controlling layer (2) containing a mixture of a hydrophilic polymer and a film-forming polymer, wherein the patch is in a film form and is characterized by being eroded until extinguished after releasing the tooth whitening agent. When applied to the teeth, the patch releases a peroxide tooth-whitening agent while being hydrated by water in the mouth during a prescribed period, and thereafter, eroded until extinguished, thereby not requiring an additional detaching work from the teeth. Therefore, the patch is convenient in use and greatly reduces an obstruction sensation. Moreover, the patch has an excellent whitening effect.

    摘要翻译: 本发明的牙齿美白用贴剂包括:通过聚合物与羧基(-COOH)的氢键和具有羰基(-CO)或醚的聚合物(-CO)形成的含有可侵蚀聚合物络合物的牙齿粘附层(1) 基团(-O-)和牙齿增白剂; 以及包含亲水性聚合物和成膜聚合物的混合物的侵蚀速率控制层(2),其中所述贴剂是膜形式,其特征在于在释放牙齿增白剂后被侵蚀直到熄灭。 当施用于牙齿时,补片在规定的时间段内释放过氧化物牙齿增白剂,同时在口中水分水合,然后腐蚀直到熄灭,从而不需要从牙齿进一步的分离工作。 因此,贴片使用方便,大大降低了障碍感。 此外,贴剂具有优异的美白效果。

    Dual adhesive transdermal drug delivery system
    5.
    发明授权
    Dual adhesive transdermal drug delivery system 有权
    双胶透皮给药系统

    公开(公告)号:US06791003B1

    公开(公告)日:2004-09-14

    申请号:US10110843

    申请日:2002-08-09

    IPC分类号: A61F1300

    摘要: A dual drug containing adhesive transdermal drug delivery system comprising: a support layer, a first drug containing adhesive layer and a second drug containing adhesive layer each of said layers having a proximal and distal surface wherein each layer is positioned adjacent to the other with each layer having its distal surface laminated to said support layer, and a peelable backing layer positioned over and laminated to the proximal surface of said first and second adhesive layers is disclosed.

    摘要翻译: 一种双重药物的粘合剂透皮药物递送系统,包括:支撑层,含有第一药物的粘合剂层和第二药物含有粘合剂层,每个所述层具有近端表面和远端表面,其中每层与每层相邻地定位 其远侧表面层压到所述支撑层,以及位于所述第一和第二粘合剂层的近侧表面上方并层压到所述第一和第二粘合剂层的近侧表面上的可剥离背衬层。

    TRANSDERMAL ABSORPTION PREPARATION
    7.
    发明申请
    TRANSDERMAL ABSORPTION PREPARATION 审中-公开
    超吸收制剂

    公开(公告)号:US20130165875A1

    公开(公告)日:2013-06-27

    申请号:US13642960

    申请日:2011-04-21

    IPC分类号: A61M35/00

    摘要: The present, invention relates to a transdermal absorption preparation. The transdermal absorption preparation of the present invention comprises a drug-containing adhesive layer, a drug-protective layer and a release layer, wherein the drug-containing adhesive layer contains ropinirole or a salt thereof, rubber, an adhesion-imparting resin, an antioxidant, and a transdermal absorption promoter. Also, the present invention provides a transdermal absorption preparation comprising a drug-containing adhesive layer, a drug-protective layer, and a release layer, wherein the drug-containing adhesive layer contains ropinirole or a salt thereof, acrylic rubber, an anti-crystallisation agent, and a transdermal absorption promoter. When the transdermal absorption preparation of the present invention is used for the treatment of Parkinson's disease or restless leg syndrome, no side effect due to an increase in the initial drug concentration in blood occurs and the skin penetration effect of the drug is excellent.

    摘要翻译: 本发明涉及一种透皮吸收制剂。 本发明的透皮吸收制剂包含含药物的粘合剂层,药物保护层和剥离层,其中含药物的粘合剂层含有罗哌尼罗或其盐,橡胶,赋形树脂,抗氧化剂 ,和透皮吸收促进剂。 另外,本发明提供了含有药物的粘合剂层,药物保护层和剥离层的透皮吸收制剂,其中含药物的粘合剂层含有罗哌尼罗或其盐,丙烯酸橡胶,抗结晶 试剂和透皮吸收促进剂。 当本发明的经皮吸收制剂用于治疗帕金森病或不宁腿综合征时,由于血液中初始药物浓度的增加而引起副作用,药物的皮肤渗透作用优异。