Reddy L Hari Vardhan, Murthy R S R
Pharmacy Department, Faculty of Technology and Engineering, Kalabhavan, M.S. University of Baroda, Vadodara-390001, Gujarat, India.
Crit Rev Ther Drug Carrier Syst. 2002;19(6):553-85. doi: 10.1615/critrevtherdrugcarriersyst.v19.i6.20.
The identification of new diseases and the resistance shown toward existing drugs calls for the introduction of new therapeutic molecules. In response, a large number of chemical entities have been introduced, of which some have absorption over the entire gastrointestinal tract (GIT), some have absorption windows (i.e., absorption sites, especially the upper part of the small intestine), and some have poor solubility in intestinal media altogether. The drugs belonging to the second and third categories, and the drugs required for local action in the stomach, require a specialized delivery system. All the above requirements can be met and effective delivery of the drugs to the absorption window, for local action and for treatment of gastric disorders such as gastro-esophageal reflux, can be achieved by floating dosage systems (FDS). To date, a number of FDS involving various technologies, carrying their own advantages and limitations, were developed, such as single- and multiple-unit hydrodynamically balanced systems (HBS), single- and multiple-unit gas-generating systems, hollow microspheres, and raft-forming systems. Various factors such as gastrointestinal physiology, dosage form characteristics, and patient-related factors control the behavior of FDS. This review discusses the anatomy and physiology of the stomach, the gastric emptying process, factors affecting the gastric retention of dosage forms, and various techniques adopted in the development of FDS.
新疾病的识别以及对现有药物产生的耐药性促使人们引入新的治疗分子。作为回应,大量化学实体已被引入,其中一些在整个胃肠道(GIT)均有吸收,一些具有吸收窗(即吸收部位,尤其是小肠上部),还有一些在肠道介质中的溶解度总体较差。属于第二类和第三类的药物以及需要在胃部局部起作用的药物需要专门的给药系统。通过漂浮剂型系统(FDS)可以满足上述所有要求,并实现将药物有效递送至吸收窗,以实现局部作用以及治疗诸如胃食管反流等胃部疾病。迄今为止,已开发出许多涉及各种技术的FDS,它们各有优缺点,例如单单元和多单元流体动力学平衡系统(HBS)、单单元和多单元产气系统、中空微球和筏状形成系统。胃肠道生理学、剂型特性和患者相关因素等各种因素控制着FDS的行为。本综述讨论了胃的解剖结构和生理学、胃排空过程、影响剂型胃滞留的因素以及FDS开发中采用的各种技术。