Sustained releasable parenteral pharmaceutical preparations and method
of producing the same
    2.
    发明授权
    Sustained releasable parenteral pharmaceutical preparations and method of producing the same 失效
    持续可释放的肠胃外药物制剂及其制备方法

    公开(公告)号:US5750100A

    公开(公告)日:1998-05-12

    申请号:US734636

    申请日:1996-10-21

    摘要: A parenteral pharmaceutical preparation comprises a matrix containing a physiologically active peptide or protein and a polyglycerol diester of a saturated fatty acid, and the matrix is in a solid form at room temperature. The molecular weight of the physiologically active peptide or protein is 2,000 dalton or more. The saturated fatty acid includes fatty acids having about 16 to 30 carbon atoms such as palmitic acid, stearic acid, etc. The matrix may be in a pillar or granular form. The parenteral pharmaceutical preparation can be used as an injectable solid administered subcutaneously or intramuscularly (for example, a pellet or tablet for implantation), a suppository or the like, and can release the physiologically active peptide or protein sustainedly for a prolonged period of one week or more.

    摘要翻译: 肠胃外药物制剂包含含有生理活性肽或蛋白质的基质和饱和脂肪酸的聚甘油二酯,并且所述基质在室温下为固体形式。 生理活性肽或蛋白质的分子量为2,000道尔顿或更多。 饱和脂肪酸包括具有约16至30个碳原子的脂肪酸,例如棕榈酸,硬脂酸等。基质可以是柱状或颗粒形式。 肠胃外药物制剂可以用作皮下或肌肉内给药的可注射固体(例如,用于植入的丸粒或片剂),栓剂等,并且可以持续释放生理活性肽或蛋白质一周的长时间 或者更多。

    Dissolution liquid for drug in iontophoresis
    4.
    发明授权
    Dissolution liquid for drug in iontophoresis 失效
    药物溶出液在离子电渗疗法中的应用

    公开(公告)号:US5993848A

    公开(公告)日:1999-11-30

    申请号:US659372

    申请日:1996-06-06

    IPC分类号: A61N1/30 A61K31/785 A61F13/00

    CPC分类号: A61N1/30

    摘要: A drug held or supported by an interface comprising a porous matrix is dissolved with a drug dissolution liquid containing a humectant, and the drug is transdermally delivered by iontophoresis. The humectant includes e.g. glycerin and other polyhydric alcohols, sugar alcohols, proline and other amino acids and acidic mucopolysaccharides. The concentration of the humectant may be about 1 to 50% by weight, and the concentration of proline or other amino acid or its salt may be about 1 to 30% by weight. The drug includes (1) a physiologically active peptide or protein with a molecular weight of 100 to 30,000 or (2) a nonpeptide physiologically active compound with a molecular weight of 100 to 1,000.

    摘要翻译: 由包含多孔基质的界面保持或负载的药物与含有保湿剂的药物溶解液溶解,并且通过离子电渗法透皮递送药物。 保湿剂包括例如 甘油等多元醇,糖醇,脯氨酸等氨基酸和酸性粘多糖。 保湿剂的浓度可以为约1至50重量%,脯氨酸或其它氨基酸或其盐的浓度可以为约1至30重量%。 药物包括(1)分子量为100〜30,000的生理活性肽或蛋白质,或(2)分子量为100〜1,000的非肽生理活性化合物。

    Liposome composition whose liposome membrane contains a polyoxyethylene
derivative
    5.
    发明授权
    Liposome composition whose liposome membrane contains a polyoxyethylene derivative 失效
    脂质体组成的脂质体膜含有聚氧乙烯衍生物

    公开(公告)号:US5252336A

    公开(公告)日:1993-10-12

    申请号:US687918

    申请日:1991-06-05

    IPC分类号: A61K9/127 B01J13/02

    摘要: A liposome composition is obtained by using as constituent components of the liposome membrane a polyoxyethylene derivative represented by the general formula:X--O--(CH.sub.2 CH.sub.2 O).sub.n --Y (I)wherein X represents an alkanoyl group or an alkyl group, Y represents a residue of a compound having a negative charge, and n is an integer of 2 to 50, and a phospholipid. The liposome composition has good dispersibility, high drug-encapsulation property and high stability.

    摘要翻译: PCT No.PCT / JP91 / 00481 Sec。 371日期1991年6月5日 102(e)1991年6月5日PCT 1991年4月12日提交PCT公布。 出版物WO91 / 16040 1991年10月31日。脂质体组合物通过以脂质体膜的构成成分作为通式XO-(CH 2 CH 2 O)n Y(I)表示的聚氧乙烯衍生物,其中X表示烷酰基或烷基, Y表示具有负电荷,n为2〜50的整数的化合物的残基和磷脂。 脂质体组成具有良好的分散性,高的药物包封性和高稳定性。

    Stabilized interface for iontophoresis
    7.
    发明授权
    Stabilized interface for iontophoresis 失效
    离子电渗疗法的稳定界面

    公开(公告)号:US5837281A

    公开(公告)日:1998-11-17

    申请号:US614375

    申请日:1996-03-12

    CPC分类号: A61N1/30 Y10T428/249953

    摘要: An interface is formed by incorporating (1) a mixture comprising a water-soluble protein and a drug into a matrix, or preferably (2) a mixture comprising a water-soluble protein and a drug to a porous matrix coated with a cationic surfactant or other ionic surfactant. The coating amount of the ionic surfactant is about 0.1 to 50 .mu.g, and the content of the water-soluble protein is about 0.1 to 1,500 .mu.g, each per 1 cm.sup.2 of the matrix. The water-soluble protein includes an albumin and the drug includes a physiologically active peptide or protein, for example. The use of the stabilized interface inhibits decrease of the drug retaining amount, and insures an effective transdermal drug delivery with a high repeatability and accuracy.

    摘要翻译: 通过将(1)包含水溶性蛋白质和药物的混合物结合到基质中,或优选(2)包含水溶性蛋白质和药物的混合物到包被阳离子表面活性剂的多孔基质上形成界面,或 其他离子表面活性剂。 离子型表面活性剂的涂布量为0.1〜50μg左右,水溶性蛋白质的含量为0.1〜1500μg,每1cm 2的基质。 水溶性蛋白质包括白蛋白,例如,药物包括生理活性肽或蛋白质。 使用稳定化的界面抑制药物保留量的降低,并确保有效的透皮药物递送以高重复性和准确性。

    Iontophoresis method
    10.
    发明授权
    Iontophoresis method 有权
    离子电渗法

    公开(公告)号:US06526316B2

    公开(公告)日:2003-02-25

    申请号:US09207605

    申请日:1998-12-09

    IPC分类号: A61N130

    CPC分类号: A61N1/0432 A61N1/30 A61N1/325

    摘要: A method for transdermal administration of parathyroid hormone by iontophoresis, which comprises applying electric current at least 2 times a day, which method is repeated one to four times each week, or an apparatus for the iontophoresis can be widely applied for not only the prevention or treatment of osteoporosis but also for general bone diseases which require promotion of bone morphogenesis, for example, treatment of ordinary fractures. The method of the present invention produces excellent pharmacological effects such as few side effects and a high bioavailability in long term administration for the prevention and treatment of bone diseases.

    摘要翻译: 通过离子电渗法透皮给药甲状旁腺激素的方法,其包括每天施加电流至少2次,该方法每周重复1-4次,或者用于离子电渗疗法的装置不仅可广泛应用于预防或 治疗骨质疏松症,而且对于需要促进骨形态发生的一般骨病,例如治疗普通骨折。本发明的方法产生优异的药理作用,例如在长期给药中的副作用少,生物利用度高,用于预防 并治疗骨病。