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Sustained release paracetamol formulations

机译:扑热息痛缓释制剂

摘要

The present disclosure is directed to twice daily sustained release pharmaceutical composition of paracetamol having an immediate release phase of paracetamol and a sustained release phase of paracetamol, said composition having unique and advantageous pharmacokinetic properties and a pharmaceutical composition comprising only a sustained release phase of paracetamol having unique and advantageous pharmacokinetic properties. The formulations are useful for the treatment of analgesia or pain. The formulation preferably contains 2000mg paracetamol administered in two tablets, each tablet having 1000mg of paracetamol present in a sustained release phase and an immediate release phase, in which the ratio of the paracetamol in the sustained release phase to the immediate release phase is about 80-90% to 10-20%, and wherein the sustained release phase comprises from 0.5% to 3% w/w of a pre-gelatinized starch and a matrix forming polymer of hydroxypropylmethyl cellulose, wherein the hydroxypropylmethyl cellulose contains a high viscosity hydroxypropylmethyl cellulose having a viscosity between 3500 and 6000 centipoise, and a low viscosity hydroxypropylmethyl cellulose having a viscosity between 10 and 30 centipoise, wherein, said high viscosity hydroxypropylmethyl cellulose and said low viscosity hydroxypropylmethyl cellulose are respectively present in an amount from 4% to 6% by weight, and from 1% to 2% by weight of the sustained release phase.
机译:本公开涉及具有对乙酰氨基酚的立即释放阶段和对乙酰氨基酚的持续释放阶段的对乙酰氨基酚的每日两次持续释放药物组合物,所述组合物具有独特和有利的药代动力学性质,以及仅包含对乙酰氨基酚的持续释放阶段的对乙酰氨基酚具有以下特征的药物组合物:独特而有利的药代动力学特性。该制剂可用于治疗镇痛或疼痛。所述制剂优选包含分两片给药的2000mg对乙酰氨基酚,每片含有1000mg对乙酰氨基酚的持续释放阶段和即释阶段,其中对乙酰氨基酚在持续释放阶段与即释阶段的比率约为80- 90%至10-20%,并且其中所述持续释放相包含0.5%至3%w / w的预糊化淀粉和羟丙基甲基纤维素的形成基质的聚合物,其中所述羟丙基甲基纤维素包含具有以下特征的高粘度羟丙基甲基纤维素:粘度在3500至6000厘泊之间,以及粘度在10至30厘泊之间的低粘度羟丙基甲基纤维素,其中,所述高粘度羟丙基甲基纤维素和所述低粘度羟丙基甲基纤维素的存在量分别为4重量%至6重量%。占缓释相的1%至2%(重量)。

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