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    • 1. 发明授权
    • Long-acting oxytetracycline composition
    • 长效土霉素组成
    • US6110905A
    • 2000-08-29
    • US159680
    • 1998-09-24
    • Alan PattersonDrew Holmes
    • Alan PattersonDrew Holmes
    • A61K9/08A61K31/65A61K47/02A61K47/10A61K47/22
    • A61K9/08A61K31/65A61K47/02A61K47/10A61K47/22A61K9/0019
    • An injectable composition of higher residual effect with reduced detrimental effects such as pain at injection site, swelling, tissue irritancy or necrosis and containing as active principle a tetracycline compound, either as the free base or a salt thereof with a physiologically acceptable acid, complexed with a substantially equimolar amount of a magnesium compound, is solubilized in a water miscible solvent system comprising, either (i) a) glycerol formal in an amount of from about 10 to 50% v/v; with b) polyethylene glycol in an amount of from about 1 to 15% v/v; or (ii) from about 25 to about 75% v/v of N-methylpyrrolidone, the composition optionally containing a pH modifier in an amount sufficient to maintain a physiochemically acceptable pH, the balance being made up with water q.s.
    • 具有较高残留效应的可注射组合物,其具有降低的有害作用,例如注射部位疼痛,肿胀,组织刺激或坏死,并且作为活性成分含有四环素类化合物,作为游离碱或其与生理学上可接受的酸的盐,与 基本上等摩尔量的镁化合物溶解在水混溶性体系中,其包含(i)a)约10至50%v / v的量的甘油缩甲醛; 其中b)约1至15%v / v的量的聚乙二醇; 或(ii)约25至约75%v / v的N-甲基吡咯烷酮,所述组合物任选地含有一定量的pH调节剂,其量足以保持生理学上可接受的pH,余量由水补足。
    • 2. 发明授权
    • Long-acting oxytetracycline composition
    • 长效土霉素组成
    • US06310053B1
    • 2001-10-30
    • US09617795
    • 2000-07-17
    • Alan PattersonDrew Holmes
    • Alan PattersonDrew Holmes
    • A61K3165
    • A61K47/02A61K9/0019A61K9/08A61K31/65A61K47/10A61K47/22
    • An injectable composition is described having a higher residual effect with reduced detrimental effects such as pain at injection site, swelling, tissue irritancy or necrosis. The composition contains as active principle a tetracycline compound, either as the free base or a salt thereof with a physiologically acceptable acid, complexed with a substantially equimolar amount of a magnesium compound, and is solubilized in a water miscible solvent system comprising glycerol formal in a an amount of about 40 (v/v); with from about 1% to about 20% (v/v) polyethylene glycol and optionally containing a pH modifier in an amount sufficient to maintain a physiologically acceptable pH. In addition, the composition may further comprise a thickener, such as polyvinyl in an amount of about 10% (w/v). The balance of the composition comprises water.
    • 描述了具有较高残留效应并具有降低的有害作用如注射部位疼痛,肿胀,组织刺激或坏死的可注射组合物。 该组合物作为活性成分含有四环素化合物,其作为游离碱或其与生理上可接受的酸的盐,与基本上等摩尔量的镁化合物络合,并且溶解在包含甘油缩合物的水混溶性溶剂体系中 约为40(v / v); 与约1%至约20%(v / v)的聚乙二醇,并且任选地含有足以维持生理上可接受的pH的量的pH调节剂。 此外,组合物还可以包含约10%(w / v)的增稠剂,例如聚乙烯。 组合物的余量包括水。