Granules containing pranlukast, process for producing the granules, and
method of improving adhesiveness of pranlukast
    4.
    发明授权
    Granules containing pranlukast, process for producing the granules, and method of improving adhesiveness of pranlukast 失效
    含有普鲁司特的颗粒,生产颗粒的方法,以及提高普鲁司特的粘合性的方法

    公开(公告)号:US5876760A

    公开(公告)日:1999-03-02

    申请号:US981083

    申请日:1997-12-12

    IPC分类号: A61K9/16 A61K31/41

    摘要: Spray-dried granules comprising pranlukast (A) and one or more saccharide(s) (B) as essential ingredients and further comprising one or more water-soluble polymer(s) (C) and/or one or more surfactant(s) (D); a process for producing the same; and a method for improving adhesiveness of pranlukast are provided. According to the present invention, the very strong adhesiveness of pranlukast is reduced, and pranlukast-containing granules having little adhesiveness, a narrow particle size distribution, and good flow properties can be produced efficiently. The pranlukast-containing granules of the present invention cause no troubles in continuous production of capsules, tablets, and the like, and the resulting pranlukast-containing granules exhibit excellent disintegrating and dispersing properties.

    摘要翻译: PCT No.PCT / JP96 / 01578 Sec。 371日期1997年12月12日 102(e)日期1997年12月12日PCT提交1996年6月11日PCT公布。 公开号WO96 / 41628 日期1996年12月27日喷雾干燥的颗粒包含普兰昔斯特(A)和一种或多种糖(B)作为必需成分,并且还包含一种或多种水溶性聚合物(C)和/或一种或多种 表面活性剂(D); 其制造方法; 提供了改善普鲁司特的粘合性的方法。 根据本发明,降低了普兰司特的非常强的粘合性,并且可以有效地制备具有很小粘合性,窄粒度分布和良好流动性的含普鲁酮糖的颗粒。 本发明的含有泼草素的颗粒在胶囊,片剂等的连续生产中不会产生麻烦,并且所得的含有普鲁酮糖的颗粒具有优异的崩解和分散性能。

    Long-lasting three-layered pharmaceutical film preparations
    5.
    发明授权
    Long-lasting three-layered pharmaceutical film preparations 失效
    持久的三层药膜制剂

    公开(公告)号:US4483846A

    公开(公告)日:1984-11-20

    申请号:US464174

    申请日:1983-02-07

    CPC分类号: A61K9/7053 A61K9/7092

    摘要: The present invention provides new three-layered pharmaceutical film preparations which comprise one drug-storing middle layer composed of one or more (a) polyvinylpyrrolidone, (b) hydroxypropyl cellulose, (c) plasticizers and (d) organic acids, containing prostaglandin analogues, and two release-controlling layers on both sides of the said middle layer, composed of one or more (a) hydroxypropyl cellulose and (b) plasticizers, containing or not containing prostaglandin analogues, and which may release the drug at the desired concentration lastingly for an extended period of time, with great high biological availability, and can make this release "zero-order release", and further have improved the stability of the drug contained therein, and in which the form of the preparation is not retained at the administered site after administration.

    摘要翻译: 本发明提供新的三层药物膜制剂,其包含一种药物储存中间层,其由一种或多种(a)聚乙烯吡咯烷酮,(b)羟丙基纤维素,(c)增塑剂和(d)含有前列腺素类似物的有机酸组成, 以及由所述中间层两侧的两个释放控制层,由一种或多种(a)羟丙基纤维素和(b)增塑剂组成,所述增塑剂含有或不含有前列腺素类似物,并且可以持续释放所需浓度的药物以用于 延长的时间,具有很高的生物利用度,并且可以使这种释放“零次释放”,并且进一步改善了其中所含药物的稳定性,并且其中制剂形式不保留在给药 管理后的网站。

    Transdermal absorption preparation
    6.
    发明授权
    Transdermal absorption preparation 失效
    透皮吸收制剂

    公开(公告)号:US5723145A

    公开(公告)日:1998-03-03

    申请号:US898646

    申请日:1997-07-22

    IPC分类号: A61K9/70 A61F13/02

    CPC分类号: A61K9/7084

    摘要: The present invention provides a transdermal absorption preparation whereby a drug, which takes effect with a small amount, and is liable to be decomposed, solid at ordinary temperatures, water-soluble and less absorbable into the skin, can be stored stably for a long period of time and, can be transdermally administered at a high releasing ratio and yet releasing slowly, when applied to the skin. The constitution of the present invention is as follows: a transdermal absorption preparation which comprises a drug-storing layer containing a drug and having a drug-releasing face coated with a drug-releasing controlling membrane, wherein said drug-storing layer comprises as a base a heat-sensitive segmented polyurethane represented by the general formula: R--A--(U)--F--(U)--B--R' wherein A and B each represents a polymer of ethylene oxide, propylene oxide, tetramethylene oxide or 1,2-butylene oxide, or a random or block copolymer thereof, R and R' each represents a terminal H, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7 or C.sub.4 H.sub.9, A=B or A.noteq.B, R=R' or R.noteq.R', F represents a constituting structure which is a moiety of a diisocyanate compound excluding two isocyanate groups, and (U) represents a urethane bond, and at least one of A and B is hydrophilic and at the same time at least one of A and B has a characteristic that it melts near the temperature of human skin, and wherein said drug-releasing controlling membrane is a phase-separated membrane comprising a mixture of a crosslinked gelatin phase and the uncrosslinked segmented polyurethane phase.

    摘要翻译: 本发明提供一种经皮吸收制剂,其可以稳定地长时间保存少量效果易于分解的药物,常温下为固体,易溶于水并且难以吸收到皮肤中的药物 的时间,并且可以以高释放比透皮施用,并且当施用于皮肤时缓慢释放。 本发明的构成如下:一种透皮吸收制剂,其包含含有药物的药物储藏层,并且具有涂敷有药物释放控制膜的药物释放面,其中所述药物储存层包含作为碱 由通式为RA-(U)-F-(U)-B-R'表示的热敏分段聚氨酯,A和B各自表示环氧乙烷,环氧丙烷,四氢呋喃或1,2-二氧化碳的聚合物, 环氧丁烷或其无规或嵌段共聚物,R和R'各自表示H,CH 3,C 2 H 5,C 3 H 7或C 4 H 9的末端,A = B或A,等式B,R = R'或R, 构成结构,除二异氰酸酯基以外的二异氰酸酯化合物的部分,(U)表示氨基甲酸酯键,A和B中的至少一个为亲水性,同时A和B中的至少一个具有以下特征: 它在人的皮肤温度附近熔化,并且其中所述药物释放控制 纳米膜是相分离膜,其包含交联明胶相和未交联的分段聚氨酯相的混合物。

    Long-lasting multi-layered film preparation
    7.
    发明授权
    Long-lasting multi-layered film preparation 失效
    持久的多层膜制备

    公开(公告)号:US4552751A

    公开(公告)日:1985-11-12

    申请号:US312458

    申请日:1981-10-19

    CPC分类号: A61K9/7092 A61K31/557

    摘要: The present invention provides multi-layered film preparations which comprise one or more water soluble polymer bases, one or more water insoluble polymer bases, one or more plasticizers and one or more prostaglandins, and optionally contain one or more organic acids, and they are composed of at least two drug release controlling layers and one or more drug storing layers. The multi-layered film preparations of the present invention are characterized by that the prostaglandin(s) containing therein exhibit the desired long-lasting release patterns at the concentration required for therapeutic purpose.

    摘要翻译: 本发明提供了多层膜制剂,其包含一种或多种水溶性聚合物基质,一种或多种水不溶性聚合物基质,一种或多种增塑剂和一种或多种前列腺素,并且任选地含有一种或多种有机酸,并且它们组成 的至少两个药物释放控制层和一个或多个药物储存层。 本发明的多层膜制剂的特征在于,其中含有的前列腺素以治疗目的所需的浓度显示出期望的持久释放模式。

    Adhesive for percutaneous administration
    8.
    发明授权
    Adhesive for percutaneous administration 失效
    用于经皮给药的粘合剂

    公开(公告)号:US4997656A

    公开(公告)日:1991-03-05

    申请号:US356618

    申请日:1989-05-23

    摘要: An adhesive for percutaneous administration having a drug-containing layer composed of a base component mainly comprising a heat-sensitive and water-sensitive amphiphilic polymer and a drug incorporated in the base component. The amphiphilic compound has a characteristic hydrophobicity-hydrophilicity tapered structure, and a variety of liquid or solid or lipophilic (hydrophobic) or hydrophilic drugs of a broad range can stably be dissolved or dispersed therein. The drug in the drug-containing layer remains stable without being released or diffused while the adhesives are stored, and upon application to the skin, the drug is gradually released and diffused into the skin with high availability in a specifically controlled pattern. The present adhesive is especially advantageous for endermic presentation of a slight amount of a substance of high physiological activity which is unstable and is easily decomposed by heat or water.

    摘要翻译: 一种用于经皮给药的粘合剂,其具有由主要包含热敏性和水敏性两亲性聚合物的基础组分和掺入基础组分中的药物组成的药物含有层。 两亲性化合物具有特征性的疏水性 - 亲水性锥形结构,并且可以稳定地溶解或分散各种范围广泛的液体或固体或亲脂性(疏水性)或亲水性药物。 含药层中的药物在粘合剂储存时保持稳定而不被释放或扩散,并且在施用于皮肤时,药物以特定控制的模式以高可用性逐渐释放并扩散到皮肤中。 本发明的粘合剂对于微量的高生理活性物质的外来物质呈现是不利的,并且易于被热或水分解。