Piperazine-cyclodextrin complexes
    3.
    发明授权
    Piperazine-cyclodextrin complexes 失效
    哌嗪 - 环糊精复合物

    公开(公告)号:US06596706B1

    公开(公告)日:2003-07-22

    申请号:US09530592

    申请日:2000-05-08

    IPC分类号: A61K31724

    摘要: The present invention relates to a compound represented by formula (1): wherein Q, which may have a substituent, represents an aryl group, a heterocyclic group, a diarylmethyl group, or an aralkyl group; R, which may have a substituent, represents a bicyclic nitrogen-containing heterocyclic group or a phenyl group; and Z represents a C1-C3 alkylene group, a C2-C4 alkenylene group, a C1-C3 alkylene group having one hydroxyl group, a carbonyl moiety, a C1-C2 alkylene group containing one carbonyl moiety at one end or an intermediate position of the carbon chain, or an oxalyl group; or salts thereof and a piperazine-cyclodextrin complex combined with a water-soluble cyclodextrin derivative. The complex exhibits enhanced water solubility, excellent stability, and low topical stimulation and is useful as a therapeutic agent for circulatory diseases and diseases of the brain region.

    摘要翻译: 本发明涉及由式(1)表示的化合物:其中可具有取代基的Q表​​示芳基,杂环基,二芳基甲基或芳烷基; R可以具有取代基,表示双环含氮杂环基或苯基; Z表示C1-C3亚烷基,C2-C4亚链烯基,具有一个羟基的C1-C3亚烷基,羰基部分,在一端或中间位置含有一个羰基部分的C1-C2亚烷基 碳链或草酰基; 或其盐和与水溶性环糊精衍生物组合的哌嗪 - 环糊精复合物。 复合物表现出增强的水溶性,优异的稳定性和低的局部刺激,并且可用作循环系统疾病和脑区疾病的治疗剂。

    Aromatic composition and method for controlling aroma
    4.
    发明授权
    Aromatic composition and method for controlling aroma 失效
    用于控制香气的芳香组合物和方法

    公开(公告)号:US5238915A

    公开(公告)日:1993-08-24

    申请号:US833452

    申请日:1992-02-06

    IPC分类号: A61K8/73 A61Q13/00

    摘要: Aromatic compositions which comprise perfumes included in cyclodextrins whose inclusion ability depends on a pH of a solution containing the perfumes and cyclodextrins and pH-adjusting substances whereby a release rate of the perfume can be controlled, are described. Aromatic compositions are also disclosed, which comprise perfumes coated or covered with materials whose solubility depends on the pH of a solution containing the coated perfumes, and a pH-adjusting substance to change the pH as desired. Methods for controlling the release rate of the perfumes are also described.

    摘要翻译: 包含环糊精中的香料的芳香族组合物,其包合能力取决于含有香料和环糊精的溶液的pH值以及pH调节物质,从而可以控制香料的释放速率。 还公开了芳香族组合物,其包含涂覆或被其溶解度取决于含有涂覆香料的溶液的pH的材料覆盖的香料,以及根据需要改变pH的pH调节物质。 还描述了用于控制香料释放速率的方法。

    Sustained release drug preparation
    6.
    发明授权
    Sustained release drug preparation 失效
    持续释放药物制剂

    公开(公告)号:US4869904A

    公开(公告)日:1989-09-26

    申请号:US127699

    申请日:1987-12-02

    摘要: Now is provided a new sustained release drug preparation comprising such an inclusion complex of a medical compound with a hydrophobic cyclodextrin derivative, e.g. ethylated cyclodextrins, which sustains or retards the dissolution and release of the medical compound at a controlled rate from the inclusion complex and hence from the drug preparation containing the inclusion complex, so as to maintain the concentration of the medical compound in blood at an effective level for prolonged time. This drug preparation may further contain a second type of an inclusion complex of the medical compound with a hydrophilic cyclodextrin or hydrophilic cyclodextrin derivative, in mixture with the first type of the inclusion complex of the medical compound with a hydrophobic cyclodextrin derivative, to maintain the controlled release of the medical compound from the drug.

    Preparation for percutaneous absorption
    8.
    发明授权
    Preparation for percutaneous absorption 失效
    经皮吸收制剂

    公开(公告)号:US5854281A

    公开(公告)日:1998-12-29

    申请号:US676250

    申请日:1996-12-10

    摘要: The present invention provides a preparation for percutaneous absorption comprising as an effective component a prostaglandin I.sub.2 derivative and a fatty acid or a derivative thereof, or a mixture of two or more of these, which has high percutaneous permeability of the PGI.sub.2 derivative. Particularly, the present invention provides a preparation for percutaneous absorption comprising 5,6,7-trinor-4,8-inter-m-phenylene PGI.sub.2 derivative and a C.sub.6 -C.sub.24 fatty acid, a salt thereof or an ester thereof, or a mixture of two or more of these, which has high percutaneous permeability of the PGI.sub.2 derivative. This preparation for percutaneous absorption suggests a possibility to last pharmacological effects and to reduce side effects. Thus, the preparation is expected to be used for therapy of various diseases, aiming at topical and systemic actions.

    摘要翻译: PCT No.PCT / JP95 / 02350 Sec。 371日期1996年12月10日第 102(e)日期1996年12月10日PCT 1995年11月16日PCT PCT。 WO96 / 15793 PCT出版物 日期:1996年5月30日本发明提供一种经皮吸收制剂,其含有作为有效成分的前列腺素I2衍生物和脂肪酸或其衍生物,或其两种以上的混合物,其具有PGI2衍生物的高经皮渗透性 。 特别地,本发明提供了一种经皮吸收制剂,包括5,6,7-三硝基-4,​​8-​​间间苯二胺PGI 2衍生物和C 6 -C 24脂肪酸,其盐或其酯或其混合物 的两种或更多种,其具有PGI2衍生物的高经皮渗透性。 用于经皮吸收的这种制剂表明可能会持续药理作用并减少副作用。 因此,该制剂预期用于各种疾病的治疗,旨在局部和全身性的作用。