两种给药途径的缓控释制剂研究进展

Progress in Study of 2 Administration Routes of Controlled Release Preparations

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。

The in vivo absorption, distribution metabolism and excretion is a continuous process of dynamic change. After the drug being absorbed into the body, blood drug concentration is vulnerable to fluctuating, when the peak blood concentration appears, some side effects may be induced. Therefore, further investigation on drug formulations and process control of its release, is not only nec- essary in clinical treatment, but also has economic benefits in the pharmaceutical industry. In recent years, study of different routes of administration controlled release is more and more widely , this paper reviews the implant and oral route of administration of controlled release formulations. Implant is an important component of controlling agent, because of its high bioavaitability, more and more attention by industry, more and more of the types, more and more wide range of applications has been extended to the treatment of various diseases, such as cancer, cardiovascular, diabetes, eye and other treatments. According to the drug release mechanism and the in vivo process, types of implants can be divided into sustained release implant and controlled release implant. Oral controlled release drug delivery performs best treatment effect primarily through the adjustment of gastrointestinal tract and the absorption rate, which can significantly reduce the potential adverse reactions and increase the medication compliance of patients. While oral r controlled release preparations, for its short development period, high technology, small and rewarding economic risk, belongs to the more active field of preparation development. The following describes the development of several oral controlled release preparations.