A compound slow-release preparation containing apixaban and its preparation method

Abstract

The invention discloses a compound sustained-release preparation containing apixaban and a preparation method thereof. The preparation is composed of apixaban granules, edoxaban sustained-release pellets and other pharmaceutically acceptable auxiliary materials. The edoxaban sustained-release pellets are, from the inside to the outside, successively a blank core, an isolation coat layer, and a drug-containing layer, and the drug-containing layer is composed of edoxaban, hydroxypropyl cellulose, and a filler. It is obtained by spraying the drug-containing dispersion solution onto the coated pellet core by the bottom spray coating method to obtain the drug-loaded immediate-release pellets, and then outsourcing the sustained-release coating layer; It is obtained by granulating with microcrystalline cellulose, hydroxypropyl cellulose and croscarmellose sodium. The compound sustained-release preparation of the invention can take effect quickly, release medicine stably for a long time, reduce the number of times patients take medicine, improve compliance, and improve the safety of patient medicine, thereby meeting the needs of treatment and meeting the requirements of clinical medicine.

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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