- Sustained release
Sustained-release (SR), extended-release (ER, XR, or XL), time-release or timed-release, controlled-release (CR), or continuous-release (CR or Contin) pills are
tablet s or capsules formulated to dissolve slowly and release adrug over time. The advantages of sustained-release tablets or capsules are that they can often be taken less frequently than instant-release formulations of the same drug, and that they keep steadier levels of the drug in the bloodstream. Sustained-release tablets are formulated so that theactive ingredient is embedded in amatrix of insoluble substance (various: some acrylics, evenchitin , these are oftenpatented ) so that the dissolving drug has to find its way out through the holes in the matrix. In some SR formulations the matrix physically swells up to form a gel, so that the drug has first to dissolve in matrix, then exit through the outer surface.There are certain considerations for the formation of sustained release formulation:
* If the active compound has a long half-life (over six hours), it is sustained on its own.
* If the pharmacological activity of the active compound is not related to its blood levels, time releasing then has no purpose.
* If the absorption of the active compound involves an active transport, the development of a time-release product may be problematic.
* Finally, if the active compound has a short half-life, it would require a large amount to maintain a prolonged effective dose. In this case, a broad therapeutic window is necessary to avoid toxicity; otherwise, the risk is unwarranted and another mode of administration would be recommended.The difference between controlled release and sustained release is that controlled release is a perfectly zero order release; that is, the drug releases over time irrespective of concentration. Sustained release implies slow release of the drug over a time period. It may or may not be controlled release.
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