Polymer intensifier in controlled release preparation

Abstract

The invention discloses application of a polymer intensifier in the production or the storage of a controlled release preparation, in particular to the controlled release preparation with zero order release. The invention also discloses the controlled release preparation with improved performance, in particular to the controlled release preparation with the zero order release. The controlled release preparation comprises a core material containing a bioactivator and a polymer controlled release coating which is coated on the core material, is provided with a plurality of medicine release micropores filled with air and contains the polymer intensifier, wherein the contact angle of a polymer and the polymer intensifier is less than 90 degrees, and the medicine release micropores are obtained by sublimating sublimable substances and / or degrading degradable harmless gases. The preparation has higher storage stability, higher production repeatability and better medicine release performance in the medicine release aspect; moreover, a controlled release membrane of the polymer intensifier has better mechanical behavior, therefore, the polymer intensifier has lower dosage pouring release possibility and higher administration safety.

Description

technical field [0001] The invention relates to the use of a polymer enhancer in the production or storage of a controlled-release preparation, especially a zero-order release controlled-release preparation. It also relates to a controlled-release preparation, especially a zero-order release controlled-release preparation and a preparation method thereof. More specifically, it relates to a controlled-release formulation with improved performance, especially a zero-order release controlled-release formulation, which comprises a core material containing biologically active substances and a plurality of air-filled A polymer controlled-release film with drug-releasing micropores and a polymer enhancer, wherein the contact angle between the above-mentioned polymer and the above-mentioned polymer enhancer is lower than 90°, and the above-mentioned drug-release micropores are sublimable and sublimable Substances and / or degradation obtained from substances that degrade to harmless ga...

AI Technical Summary

Problems solved by technology

[0006] For example, there is a big problem with the stability of the preparation: after the controlled-release preparation prepared by this technology is stored for a period of time, its drug release performance or drug release rate often drops significantly, while the drug content in the preparation basically does not change or The magnitude of the change is relatively small

[0008] As another example, the drug release performance or drug release rate of the controlled-release preparation prepared by this technology is often significantly lower than that of the film-controlled release preparation using a water-soluble substance with the same particle size as a pore-forming agent. Membrane controlled-release formulations containing hollow (no pore-forming agent) micropores of the same particle size to control drug release should be faster than, or at least not lower than, membrane-controlled release formulations containing pore-forming agents of the same size, because the The pore agent needs to be dissolved into micropores to control the release of the drug, and the pore-forming agent needs to be dissolved for a certain period of time, so that there will be a certain time lag when the drug is released

[0009] In addition, the mechanical strength of the preparation prepared by the above method is often unsatisfactory, especially when the glass transition temperature (Tg) of the polymer coating is high, because the mechanical strength is not enough, the controlled release coating may be ruptured by external force, Therefore, it may cause dose-dumping of controlled-release preparations, affecting drug safety

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