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药物在体内吸收、分布代谢及排泄是一个连续变化的动态过程,普通制剂药物被体内吸收之后,血药浓度容易发生波动起伏,当血药浓度达高峰时,有可能引发某些不良反应。因此,深入研究药物的剂型并控制其释药过程,不仅是临床医疗所需要,而且在医药工业经济效益上也有重要意义。近年来不同给药途径缓控释制剂的研究越来越广泛,笔者分别对植入和口服2种给药途径缓控释制剂的研究进展进行综述。植入剂是缓控释制剂的一个重要组成部分,因其具有使药物生物活性增强及药物作用时间延长,生物利用度高等特点,愈来愈被行业所重视,研究其种类也越来越多,应用范围也越来越广,已经扩大到各类疾病的治疗,如肿瘤、心血管、糖尿病、眼科等方面的治疗。植入剂的类型根据药物释放的机制和药物在体内的代谢过程,可以分为植入缓释剂和植入控释剂2类。口服缓控释制剂主要通过胃肠道释药及吸收速度的调整,使药物发挥最佳治疗效果。显著减少可能的不良反应,增加病人服药的顺应性;同时口服缓控释制剂开发周期短,技术含量高,经济风险小且回报丰厚,是制剂开发中比较活跃的领域。以下分别介绍几种口服缓控释制剂的发展。
Drug absorption in the body, the distribution of metabolism and excretion is a dynamic process of continuous changes, the general preparation of drugs absorbed by the body, the blood concentration prone to fluctuations, when the plasma concentration reached its peak, it may lead to some adverse reactions. Therefore, in-depth study of drug dosage forms and control of its release process, not only for clinical needs, but also in the pharmaceutical industry is also of great economic significance. In recent years, different routes of administration of sustained-release controlled release of the research is more and more widespread, the author of the implantation and oral administration of two kinds of slow release controlled release formulations are reviewed. Implants are an important part of sustained-controlled release preparation. Because of their characteristics of enhancing the biological activity of drugs and prolonging the action time of drugs, the bioavailability is more and more emphasized by the industry and the types of implants are also increasing , The application is also more and more widely, has been extended to the treatment of various diseases, such as cancer, cardiovascular, diabetes, ophthalmology and other aspects of treatment. The type of implants can be divided into two groups according to the mechanism of drug release and the metabolism of drugs in the body. Oral slow controlled release formulations mainly through the gastrointestinal tract release and absorption rate adjustment, so that drugs play the best therapeutic effect. Significantly reduce the possible adverse reactions and increase patient compliance; at the same time, oral sustained-release controlled-release formulations have a short development cycle, high technical content, small economic risk and good returns, and are active fields in formulation development. The following describes the development of several oral controlled release formulations.