Compound sustained-release preparation containing apixaban and preparation method thereof

Abstract

The invention discloses a compound sustained-release preparation containing apixaban and a preparation method thereof. The preparation is composed of apixaban particles, edoxaban sustained-release pellets and other pharmaceutically acceptable auxiliary materials, wherein the edoxaban sustained-release pellets are composed of blank pellet cores, isolation coating layers and drug-containing layers from inside to outside in order; the drug-containing layers are composed of edoxaban, hydroxypropyl cellulose and a filler; a drug-containing dispersion solution is sprayed onto the coated pellet coresby a bottom spraying coating method to obtain drug-loaded quick-release pellets, and then the drug-loaded quick-release pellets are coated with sustained-release coating layers to obtain the drug-containing layers; and the apixaban particles are obtained by granulation of apixaban, microcrystalline cellulose, hydroxypropyl cellulose and cross-linked sodium carboxymethyl cellulose. The compound sustained-release preparation provided by the invention can take effect quickly, can release drugs stably for a long time, reduces the number of drug taking times of patients, improves the compliance, and improves the safety of drug use of patients, thereby meeting the needs of treatment and meeting the requirements of clinical medication.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a preparation method of edoxaban and apixaban compound sustained-release tablets. Background technique [0002] Apixaban is a novel oral direct factor Xa inhibitor with the chemical formula 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl) )phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide. Molecular formula is C 25 h 25 N 5 o 4 , the molecular weight is 459.50. The structural formula is as follows: [0003] [0004] Activation of coagulation factor Xa, whose main practical role is generation of thrombin by restricted proteolysis of prothrombin, plays an important role in linking intrinsic and extrinsic activation mechanisms in the final common pathway of coagulation. Generation of thrombin, the final serine protease in the pathway to generate a fibrin clot from its precursor, is amplified by the formation of the prothrombinase...

AI Technical Summary

Problems solved by technology

[0012] In order to overcome the problems of unstable blood drug solubility and slow drug release rate in the early stage after taking edoxaban ordinary tablets, the object of the present invention is to provide a compound slow-release preparation containing apixaban and a preparation method thereof. Doxaban Apixaban Compound Sustained-release Tablets, apixaban releases drugs quickly in the early stage, and edoxaban releases steadily in the later stage. The two work together to obtain better therapeutic effects and improve patient compliance

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