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    • 12. 发明申请
    • Transdermal Delivery Form Disposal Systems and Methods
    • 透皮递送形式处置系统和方法
    • US20080226702A1
    • 2008-09-18
    • US12048771
    • 2008-03-14
    • Alan Philip Goldberg
    • Alan Philip Goldberg
    • A61F13/02A61K31/4535A61K31/445
    • A61K9/7023A61K31/445A61K31/4535B09B3/0075B09B2220/14
    • The extraction and use of residual opioids from transdermal dosage forms can be reduced by placement and fixation of used dosage forms onto a surface. The used dosage form can be fixed to the surface such that it cannot be removed without at least partially destroying the matrix containing the opioid, or such that the matrix containing the opioid is rendered at least partially inaccessible to opioid extraction methods. The disposal system for one or more opioid-containing transdermal delivery forms comprises at least one disposal surface for receiving the transdermal delivery form. The at least one disposal surface can comprise one or more structures for fixing a transdermal delivery form to the at least one surface. Alternatively, the transdermal delivery form comprises one or more structures for permanently fixing the transdermal delivery form to the surface. The disposal system can also be used for preventing or reducing diversion of opioids from transdermal delivery forms.
    • 可以通过将使用的剂型放置并固定在表面上来减少透皮剂型的残留阿片样物质的提取和使用。 使用的剂型可以固定在表面上,使得其不能在不至少部分地破坏含有阿片样物质的基质的情况下被除去,或者使含有阿片样物质的基质至少部分地不能用于阿片样物质提取方法。 用于一种或多种含阿片样物质的透皮递送形式的处置系统包括至少一个用于接受透皮递送形式的处置表面。 所述至少一个处置表面可以包括用于将透皮递送形式固定到所述至少一个表面的一个或多个结构。 或者,透皮递送形式包括用于将透皮递送形式永久固定到表面的一种或多种结构。 处置系统也可用于预防或减少阿片类药物从透皮给药形式的转移。
    • 16. 发明授权
    • Sequential benzylic oxidations of the naloxone ring system
    • 纳洛酮环体系的连续苄基氧化
    • US6166211A
    • 2000-12-26
    • US520099
    • 2000-03-07
    • Gary A. CainSpencer Drummond, Jr.
    • Gary A. CainSpencer Drummond, Jr.
    • C07D489/02C07D489/08
    • C07D489/08C07D489/02Y02P20/55
    • The present invention pertains to a process for the preparation of the 10-keto analogs of morphinan compounds. In the case of compounds having a 3-hydroxyl group, the 3-methyl ether protected analog is synthesized by selective phenolic methylation in the presence of the basic amino group. When nalbuphine, morphine, or codeine is used as the starting material, the additional 6-hydroxyl group is protected using acetylation. The protected analog is selectively oxidized by treatment with cerium ammonium nitrate to provide the 10-(S)-hydroxy adduct. The 10-(S)-hydroxy adduct is further oxidized to the 10-keto analog. Any protecting groups that were added prior to oxidation are cleaved subsequent to oxidation to form the desired 10-ketomorphinan.
    • 本发明涉及制备吗啡喃化合物的10-酮类似物的方法。 在具有3-羟基的化合物的情况下,3-甲基醚保护的类似物在碱性氨基存在下通过选择性酚甲基化合成。 当使用纳布啡,吗啡或可待因作为起始原料时,使用乙酰化保护额外的6-羟基。 通过用硝酸铈铵处理选择性地氧化受保护的类似物以提供10-(S) - 羟基加合物。 将10-(S) - 羟基加合物进一步氧化成10-酮类似物。 在氧化之前加入的任何保护基在氧化后被切割以形成所需的10-酮吗啡喃。