Wei Zhen-ping, Huang Lei, Han Jing, Li Yong
Department of nutrition, Peking University College of Public Health, Beijing 100083, China.
Beijing Da Xue Xue Bao Yi Xue Ban. 2004 Aug 18;36(4):439-42.
To develop a pH independent floating sustained release tablet for gastric retention using 5-Fluorouracil (5-Fu) as a model drug.
According to the theory of the Hydro-dynamically Balanced System, the granules for the floating and drug loading layer were prepared separately and pressed together to make two-layer floating tablets for gastric retention. The floating kinetics indexes were measured and the data about drug release studied with media of different pH values.
An excellent floating ability was observed in the media of different acidity for the gastric retentive tablet prepared according to the optimum formulation. The in vitro drug release can be modified by the regulation of the formulation ingredients. At the rotating speed of 100 r/min and in 0.1 mol/L HCl, the drug release was found to conform to first-class dynamics rule.
The two-layer floating tablet made in this experiment,whose floating ability is independent of the gastric acidity variation, is of the possibility to be used for the auxiliary treatment of gastric carcinoma because of its prolonged gastric retention.
以5-氟尿嘧啶(5-Fu)为模型药物,研制一种pH值无关型胃滞留漂浮缓释片。
根据流体动力学平衡系统理论,分别制备漂浮层和载药层颗粒,压制成双层胃滞留漂浮片。测定漂浮动力学指标,并在不同pH值介质中研究药物释放数据。
按照优化处方制备的胃滞留片在不同酸度介质中均表现出优异的漂浮能力。通过调节处方成分可改变体外药物释放。在转速100 r/min及0.1 mol/L盐酸介质中,药物释放符合一级动力学规律。
本实验制备的双层漂浮片漂浮能力不受胃内酸度变化影响,因其胃滞留时间延长,具有用于胃癌辅助治疗的可能性。