Controlled release preparation

Abstract

The invention discloses a controlled release preparation with improved performance. The controlled release preparation comprises a core containing medicament and a controlled release film covering the outside of the core and being almost insoluble in water as well as stomach and intestines digestive juice. The controlled release film comprises particulate matters of a water soluble medicinal additive, the water-soluble medicinal additive is covered by a polymer film which can be soluble in the stomach and / or intestines digestive juice but almost insoluble in water, the polymer and the medicinal additive can not produce chemical reaction or can produce chemical reaction but do not produce water-insoluble non-gaseous products and the pharmaceutically unacceptable products, and the amount ofthe polymer is no more 700% of that of the medicinal additive. The invention also discloses a preparation method of the controlled release preparation. The controlled release preparation has the advantages of improved medicament release reproducibility, reduced medicament release lag time, accelerated medicament release and improved bioavailability, can realize located controlled release, delayedcontrolled release and interval type or pulse type controlled release of the medicament in the gastrointestinal tract, and the like.

Description

technical field [0001] The present invention relates to a controlled release preparation. More specifically, the present invention relates to a controlled-release preparation with improved properties, especially a zero-order release controlled-release preparation. The invention also relates to a preparation method of the controlled-release preparation. Background technique [0002] Some water-insoluble polymers control drug release by coating in controlled-release formulations, especially zero-order release controlled-release formulations. Due to the water insolubility of the polymer, it is often necessary to form micropores in the coating film to improve the permeability (permeability) of the controlled release coating film to facilitate the penetration of water and the release of the drug, especially the low solubility of the drug and the overall When the surface area is small. [0003] So far, there are three typical representatives of related film-coated controlled-re...

AI Technical Summary

Problems solved by technology

But there are also many defects: the water-soluble porogen exists in the coating film in a monomolecular state, and the aperture size of the micropores is limited by the molecular size of the water-soluble porogen, and the aperture is much smaller than that prepared in a suspension state (such as US4629619). It is not conducive to the penetration of drugs with a large molecular radius; therefore, when the permeability of the coating film can meet the requirements of practical applications, especially when the solubility of the drug is low and the total surface area of ​​​​the preparation is small, its mechanical strength is very weak; The actual available channels are not easy to control, and the production reproducibility is poor

It is precisely because of this interdiffusion and penetration between polymers that the interface between the macromolecular porogen and the controlled-release coating film becomes more and more blurred with time, and the micropores that can be formed also become blurred with time. The pore size becomes more and more blurred, and the pore size becomes unstable, so that the drug release behavior becomes unstable, and the drug release stability or reproducibility becomes poor due to in vitro factors.

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