Preparation for percutaneous absorption
    5.
    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。

    Preparation of lipophile:hydroxypropylcyclodextrin complexes by a method
using co-solubilizers
    6.
    发明授权
    Preparation of lipophile:hydroxypropylcyclodextrin complexes by a method using co-solubilizers 失效
    通过使用CO溶剂的方法制备脂质:羟丙基胆碱酯复合物

    公开(公告)号:US5120720A

    公开(公告)日:1992-06-09

    申请号:US585792

    申请日:1990-09-20

    IPC分类号: A61K9/18 A61K47/48

    CPC分类号: B82Y5/00 A61K47/48969

    摘要: The dissolution of lipophilic compounds in aqueous solutions of hydroxypropylcyclodextrins can be accelerated by the addition of co-solubilizers, such as ethanol or ammonia, which again can be removed, together with water, by evaporation or by freeze-drying leaving lipophile: hydroxypropylcyclodextrin complexes as a residue. The co-solubilizer method was used successfully with steroid drugs (5-androstene-3.beta.,17.beta.-diol, 4-androstene-3,17-dione, dehydroepiandrosterone, dexamethasone, 5-.alpha.-dihydro-testosterone, 6-methylprednisolone, and testosterone), peptides (gramicidin S) and a macrocyclic antibiotic (amphotericin B). The complexes prepared in this manner were amorphous and possessed satisfactory stability.

    摘要翻译: 亲水性化合物在羟丙基环糊精的水溶液中的溶解可以通过加入共增溶剂如乙醇或氨来加速,这可以通过蒸发或通​​过冷冻干燥再次与水一起除去,使亲脂性:羟丙基环糊精复合物作为 一个残留物 使用辅助增溶剂方法,使用类固醇药物(5-雄甾烯-3β,17β-二醇,4-雄甾烯-3,17-二酮,脱氢表雄酮,地塞米松,5α-二氢睾酮,6-甲基泼尼松龙, 和睾丸激素),肽(短杆菌肽S)和大环抗生素(两性霉素B)。 以这种方式制备的络合物是无定形的并且具有令人满意的稳定性。