Controlled release oxycodone compositions
    61.
    发明申请

    公开(公告)号:US20060057210A1

    公开(公告)日:2006-03-16

    申请号:US11207144

    申请日:2005-08-17

    IPC分类号: A61K31/485 A61K9/14

    摘要: A method for substantially reducing the range in daily dosages required to control pain in approximately 90% of patients is disclosed whereby an oral solid controlled release dosage formulation having from about 10 to about 40 mg of oxycodone or a salt thereof is administered to a patient. The formulation provides a mean maximum plasma concentration of oxycodone from about 6 to about 60 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration from about 3 to about 30 ng/ml from about 10 to about 14 hours after repeated “q12h” (i.e., every 12 hour) administration through steady-state conditions. Another embodiment is directed to a method for substantially reducing the range in daily dosages required to control pain in substantially all patients by administering an oral solid controlled release dosage formulation comprising up to about 160 mg of oxycodone or a salt thereof, such that a mean maximum plasma concentration of oxycodone up to about 240 ng/ml from a mean of up to about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration up to about 120 ng/ml from about 10 to about 14 hours after repeated “q12h” (i.e., every 12 hour) administration through steady-state conditions are achieved. Controlled release oxycodone formulations for achieving the above are also disclosed.

    Immediate release tablet cores of acetaminophen having sustained-release coating
    66.
    发明授权
    Immediate release tablet cores of acetaminophen having sustained-release coating 有权
    具有持续释放包衣的对乙酰氨基酚立即释放片芯

    公开(公告)号:US06210714B1

    公开(公告)日:2001-04-03

    申请号:US09505935

    申请日:2000-02-14

    IPC分类号: A61K922

    CPC分类号: A61K9/2866

    摘要: A controlled release tablet for oral administration is disclosed which has a tablet core including an insoluble therapeutically active agent having an aqueous solubility of less than or equal to about 5 mg/ml in a sufficient amount to render a therapeutic effect. The core provides rapid release of said therapeutically active agent upon exposure to aqueous solutions. The tablet core is coated with a controlled release coating permitting sustained release of said therapeutically active agent when said coated tablet is exposed to aqueous solutions.

    摘要翻译: 公开了一种用于口服给药的控释片剂,其具有含有足够量的水溶解度小于或等于约5mg / ml的不溶性治疗活性剂的片芯,以产生治疗效果。 核心在暴露于水溶液时提供所述治疗活性剂的快速释放。 当所述包衣片剂暴露于水溶液时,片剂核芯涂覆有控释包衣,允许所述治疗活性剂的持续释放。

    Controlled release oxycodone compositions
    68.
    发明授权
    Controlled release oxycodone compositions 失效
    对照释放羟考酮组合物

    公开(公告)号:US5656295A

    公开(公告)日:1997-08-12

    申请号:US618344

    申请日:1996-03-19

    摘要: A method for substantially reducing the range in daily dosages required to control pain in approximately 90% of patients is disclosed whereby an oral solid controlled release dosage formulation having from about 10 to about 40 mg of oxycodone or a salt thereof is administered to a patient. The formulation provides a mean maximum plasma concentration of oxycodone from about 6 to about 60 ng/ml from a mean of about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration from about 3 to about 30 ng/ml from about 10 to about 14 hours after repeated "q12h" (i.e., every 12 hour) administration through steady-state conditions. Another embodiment is directed to a method for substantially reducing the range in daily dosages required to control pain in substantially all patients by administering an oral solid controlled release dosage formulation comprising up to about 160 mg of oxycodone or a salt thereof, such that a mean maximum plasma concentration of oxycodone up to about 240 ng/ml from a mean of up to about 2 to about 4.5 hours after administration, and a mean minimum plasma concentration up to about 120 ng/ml from about 10 to about 14 hours after repeated "q12h" (i.e., every 12 hour) administration through steady-state conditions are achieved. Controlled release oxycodone formulations for achieving the above are also disclosed.

    摘要翻译: 公开了一种用于大大减少约90%患者中控制疼痛所需的日剂量范围的方法,其中向患者施用具有约10至约40mg羟可待酮或其盐的口服固体控释剂量制剂。 所述制剂提供给药后平均约2至约4.5小时约6至约60ng / ml的羟考酮的平均最大血浆浓度,并且平均最小血浆浓度为约3至约30ng / ml,约10 通过稳态条件重复“q12h”(即每12小时)至约14小时。 另一个实施方案涉及通过施用包含高达约160mg羟考酮或其盐的口服固体控制释放剂量制剂来显着降低在基本上所有患者中控制疼痛所需的日剂量范围的方法,使得平均最大值 在给药后平均高达约2至约4.5小时,羟考酮的血浆浓度高达约240ng / ml,重复“q12h”后约10至约14小时的平均最小血浆浓度高达约120ng / ml “(即每12小时一次)通过稳态条件实现。 还公开了用于实现上述目标的控释羟考酮制剂。

    Controlled release oxycodone compositions
    69.
    发明授权
    Controlled release oxycodone compositions 失效
    对照释放羟考酮组合物

    公开(公告)号:US5266331A

    公开(公告)日:1993-11-30

    申请号:US800549

    申请日:1991-11-27

    摘要: A solid controlled release, oral dosage form, the dosage form comprising a therapeutically effective amount of oxycodone or a salt thereof in a matrix wherein the dissolution rate in vitro of the dosage form, when measured by the USP Paddle Method of 100 rpm in 900 ml aqueous buffer (pH between 1.6 and 7.2) at 37.degree. C. is between 12.5% and 42.5% (by weight) oxycodone released after 1 hour, between 25% and 55% (by weight) oxycodone released after 2 hours, between 45% and 75% (by weight) oxycodone released after 4 hours and between 55% and 85% (by weight) oxycodone released after 6 hours, the in vitro release rate being independent of pH between pH 1.6 and 7.2 and chosen such that the peak plasma level of oxycodone obtained in vivo occurs between 2 and 4 hours after administration of the dosage form.

    摘要翻译: 固体控制释放的口服剂型,所述剂型包含基质中治疗有效量的羟考酮或其盐,其中当通过USP桨法以100rpm在900ml中测量时,剂型的体外溶出速率 在37℃下的水性缓冲液(pH在1.6和7.2之间)在1小时后释放的羟考酮的12.5%至42.5%(重量),2小时后释放的羟考酮的25%至55%(重量),45% 和4小时后释放的75%(重量)羟考酮和6小时后释放55%至85%(重量)羟考酮的体外释放速率与pH在1.6至7.2之间的pH无关,并选择使峰值等离子体 体内获得的羟考酮水平在施用剂型后2至4小时发生。