...
  • 主题
高级搜索  >
历史搜索 清空历史
首页> 外文期刊>Pharmaceutical development and technology >An active film-coating approach to enhance chemical stability of a potent drug molecule.
【24h】

An active film-coating approach to enhance chemical stability of a potent drug molecule.

机译：一种主动涂膜方法，可增强有效药物分子的化学稳定性。

获取原文
获取原文并翻译 | 示例
   

获取外文期刊封面封底 >>

       
页面导航
  • 摘要
  • 著录项
  • 相似文献
  • 相关主题

摘要

Peliglitazar, a PPAR α/γ agonist, was found to undergo acid as well as base catalyzed degradation. The acid catalyzed degradation led to the formation of benzylic alcohol and glycine carbamate and the base catalyzed degradation led to formation of p-hydroxyanisole and an amine degradant. In capsule formulations, the capsules with the lowest drug-loading exhibited maximum instability even at 25 °C/60% RH storage condition. Incorporation of pH-modifiers to maintain 'micro-environmental pH' acidic did not prevent the formation of the base-catalyzed degradants. Traditional dry granulated tablet formulation which is qualitatively similar to the capsule formulations showed the presence of acid-catalyzed degradants even without the presence of an acidifying agent. On the other hand, traditional wet granulated tablet formulation showed mainly base-catalyzed degradants. Stability problems of the tablet formulation were aggravated because the potent molecule required low tablet strengths which resulted in low drug to excipient ratio. To stabilize the molecule, an active film-coating approach was explored. In this approach, the drug was sprayed with the coating material onto non-active containing tablet cores. This approach of trapping the drug particles into the coating material provided tablets with satisfactory chemical stability. The stability enhancement observed in the active coating approach is attributed to the higher drug to excipient ratio in the film coat of non-reactive coating material compared to that in the traditional dry or wet granulated formulations.
机译：发现Pliglitazar，一种PPARα/γ激动剂，会发生酸以及碱催化的降解。酸催化的降解导致形成苄醇和氨基甲酸甘氨酸，而碱催化的降解导致形成对羟基茴香醚和胺降解剂。在胶囊制剂中，即使在25°C / 60％RH的储存条件下，载药量最低的胶囊也表现出最大的不稳定性。掺入pH调节剂以保持酸性的“微环境pH”并不能阻止碱催化降解剂的形成。定性上类似于胶囊剂的传统干粒片剂的配方显示，即使不存在酸化剂，也存在酸催化降解剂。另一方面，传统的湿法制粒片剂制剂主要显示出碱催化降解剂。由于有效分子需要低的片剂强度，导致药物与赋形剂的比率低，使片剂制剂的稳定性问题更加严重。为了稳定该分子，研究了一种活性膜包衣方法。在这种方法中，将药物与包衣材料一起喷涂到不含活性成分的片剂芯上。将药物颗粒捕获到包衣材料中的这种方法为片剂提供了令人满意的化学稳定性。在活性包衣方法中观察到的稳定性增强归因于与传统的干法或湿法制粒配方相比，非反应性涂层材料薄膜衣的药物与赋形剂比率更高。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
获取原文

客服邮箱：kefu@zhangqiaokeyan.com

京公网安备：11010802029741号 ICP备案号：京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有

  • 客服微信

  • 服务号