Heilmann K
Curr Med Res Opin. 1983;8 Suppl 2:3-9. doi: 10.1185/03007998309109818.
The history of pharmaceuticals has reflected a concern with the development of new chemical entities. Only recently has the importance of dosage form design been recognized as a vital component of effective therapy. Not only has the time and expense involved in the research of the new molecules escalated dramatically, but it has been discovered that many of these products might be improved through incorporation in rate-controlled dosage forms. Conventional formulations have provided vehicles with which to introduce agents into the body. New therapeutic systems offer great versatility since they permit localized treatment of specific tissues, sophisticated methods of animal experimentation, and controlled-release methods for systemic delivery. These new dosage forms are diverse, precise, and adaptable in many therapeutic situations. A membrane-controlled gastro-intestinal therapeutic (GIT) system resembling a conventional tablet in external appearance has recently been developed. This system is designed for the constant, controlled release over a period of 10 to 12 hours of drug in solution and uses osmotic activity as the source of energy. The GIT system, as used for 'Osmosin' (sodium indomethacin trihydrate), differs from conventional sustained-release and other controlled-release dosage forms in that the rate of release is not dependent upon pH to release the medication and is designed, therefore, to overcome the problems associated with unpredictable release patterns.
药物学的历史反映了对新化学实体研发的关注。直到最近，剂型设计的重要性才被视为有效治疗的关键组成部分。不仅新分子研究涉及的时间和费用大幅增加，而且还发现许多此类产品通过制成控释剂型可能会得到改进。传统制剂提供了将药物引入体内的载体。新的治疗系统具有很大的通用性，因为它们允许对特定组织进行局部治疗、采用复杂的动物实验方法以及用于全身给药的控释方法。这些新剂型多样、精确且适用于多种治疗情况。最近开发出一种外观类似传统片剂的膜控胃肠道治疗（GIT）系统。该系统设计用于在10至12小时内持续、控释溶液中的药物，并利用渗透活性作为能量来源。用于“奥索辛”（三水合吲哚美辛钠）的GIT系统与传统缓释和其他控释剂型的不同之处在于，其释放速率不依赖于pH来释放药物，因此旨在克服与不可预测的释放模式相关的问题。
