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Coated tablet with zero-order or near zero-order release kinetics

机译:具有零级或接近零级释放动力学的包衣片剂

摘要

Tablets for the controlled release of an active ingredient in a zero-order or near zero-order fashion are provided. The tablet includes a core and a coating. The core includes at least one active pharmaceutical agent and a polyethylene oxide with a molecular weight of between about 1,000,000 and 10,000,000, preferably between about 4,000,000 and 8,000,000. The core material is optionally, but preferably, coated with a cellulosic material. The active pharmaceutical agent can be hydrophilic, hydrophobic, or amphiphilic. When the active pharmaceutical agent is a hydrophilic agent, it is preferred that the coating is a relatively hydrophobic cellulose, such as ethylcellulose or propylcellulose. However, if the tablet is uncoated, it can provide a near-zero-order release rate rather than a zero-order release rate. When the active pharmaceutical agent is a hydrophobic or amphiphilic agent, the hydrophilic polymeric carrier is the same as in the first embodiment, the coating is a relatively more hydrophilic cellulose. The release rate for the active pharmaceutical agent can be controlled by adjusting the thickness of the coating, and, optionally, by adjusting the concentration of the polymeric excipients, as well as certain non-polymeric excipients which may optionally be present. An advantage of using relatively high molecular weight polyethylene oxide is that the release is pH independent, unlike where ionic polymers such as polyacrylic acids are used. Further, active pharmaceutical agents including functional groups that might react with such polymers can be used without an adverse reaction between the active agent and the polymer.
机译:提供了用于以零级或接近零级方式控制释放活性成分的片剂。片剂包括核和包衣。芯包括至少一种活性药物和分子量为约1,000,000至10,000,000,优选约4,000,000至8,000,000的聚环氧乙烷。芯材料任选地但优选地用纤维素材料涂覆。活性药剂可以是亲水的,疏水的或两亲的。当活性药物试剂是亲水剂时,优选涂层是相对疏水的纤维素,例如乙基纤维素或丙基纤维素。但是,如果平板电脑没有涂层,则可以提供接近零级的释放速率,而不是零级的释放速率。当活性药物试剂是疏水性或两亲性试剂时,亲水性聚合物载体与第一实施方案中的相同,涂层是相对更亲水的纤维素。活性药物的释放速率可通过调节包衣的厚度,以及任选地通过调节聚合物赋形剂以及任选地存在的某些非聚合物赋形剂的浓度来控制。使用相对较高分子量的聚环氧乙烷的一个优点是,释放与pH无关,这与使用离子聚合物(例如聚丙烯酸)不同。此外,可以使用包括可能与这样的聚合物反应的官能团的活性药物,而在活性剂和聚合物之间没有不利的反应。

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