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[药物作用延长中的草药医学可能性与问题(作者译)]

[Galenical possibilities and problems in protraction of drug effects (author's transl)].

作者信息

Müller F

出版信息

Arzneimittelforschung. 1976;26(1A):115-21.

PMID:7277
Abstract

In recent years, dosage forms with sustained release have obtained a significant importance. The technological possibilities for manufacturing are described as coating, embedding and matrix procedures. The range of auxiliary substances, which are responsible for the retardation of drug activity, reaches from lipophilic compounds as lipoids, fatty alcohols and compounds which are forming hydrogels as cellulose derivatives and natural polysaccharides to synthetic polymers derived from acrylic acid. The formulation of the dosage forms requires particular care in respect to the amount of initial and maintenance doses. On account of technological processes, for example during manufacturing of tablets, under certain circumstances the liberation rate is altered. In vitro test methods allow comparisons only then when the results can be counter-checked by in vitro experiments. The release of drug follows different mechanisms, which are described, entirely or in part, to be reactions following the time law of zero or first order. In special cases, a linear correlation is observed as a function of square root of time. The calculation of given special equations for events within the dosage form is feasible from blood-level values.

摘要

近年来,缓释剂型已变得极为重要。制造缓释剂型的技术方法包括包衣、包埋和基质法。负责延缓药物活性的辅料范围广泛,从亲脂性化合物如类脂、脂肪醇,到形成水凝胶的化合物如纤维素衍生物和天然多糖,再到源自丙烯酸的合成聚合物。剂型的配方在初始剂量和维持剂量方面需要特别注意。由于技术工艺的原因,例如在片剂制造过程中,在某些情况下释放速率会发生改变。只有当体外试验结果能够通过体内实验进行核对时,体外试验方法才能进行比较。药物释放遵循不同的机制,这些机制全部或部分被描述为遵循零级或一级时间规律的反应。在特殊情况下,会观察到与时间平方根成函数关系的线性相关性。根据血药浓度值可以计算剂型内特定事件的特定方程。

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