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Razvoj i vrednovanje plutajućih tableta norfloksacina s produljenim zadržavanjem u želucu

机译:诺氟沙星胃滞留时间延长片的研制与评价

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摘要

Floating matrix tablets of norfloxacin were developed to prolong gastric residence time, leading to an increase in drug bioavailability. Tablets were prepared by the wet granulation technique, using polymers such as hydroxy propyl methylcellulose (HPMCK4M, HPMCK100M) and xanthan gum. Tablets were evaluated for their physical characteristics viz., hardness, thickness, friability, and mass variation, drug content and floating properties. Further, tablets were studied for in vitro drug release characteristics for 9 hours. The tablets exhibited controlled and prolonged drug release profiles while floating over the dissolution medium. Non-Fickian diffusion was confirmed as the drug release mechanism from these tablets, indicating that water diffusion and the polymer rearrangement played an essential role in drug release. The best formulation (F4) was selected based on in vitro characteristics and was used in vivo radiographic studies by incorporating BaSO4. These studies revealed that the tablets remained in the stomach for 180 ± 30 min in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered desirable for absorption window drugs.
机译:开发出诺氟沙星的漂浮基质片剂以延长胃的停留时间,从而导致药物生物利用度的增加。通过湿法制粒技术,使用诸如羟丙基甲基纤维素(HPMCK4M,HPMCK100M)和黄原胶的聚合物来制备片剂。评价片剂的物理特性,即硬度,厚度,易碎性和质量变化,药物含量和漂浮性。此外,对片剂进行了9小时的体外药物释放特性研究。片剂漂浮在溶出介质上时显示出受控的和延长的药物释放曲线。从这些片剂中,非菲克安扩散被确认为药物释放机理,表明水扩散和聚合物重排在药物释放中起着至关重要的作用。根据体外特征选择最佳制剂(F4),并通过掺入BaSO4将其用于体内放射照相研究。这些研究表明,这些片剂在禁食的人类志愿者中在胃中停留180±30分钟,并表明通过漂浮原理增加了胃保留时间,这被认为是吸收窗药物的理想选择。

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