Compound sustained-release preparation containing apixaban and preparation method thereof

A sustained-release preparation, the technology of apixaban, which is applied in the field of preparation of edoxaban-apixaban compound sustained-release tablets, can solve the problems of slow drug release rate, unstable blood drug solubility, etc. Compliance, good therapeutic effect, and safety-improving effect

Active Publication Date: 2021-03-16
浙江诺得药业有限公司 +1
View PDF5 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Compound sustained-release preparation containing apixaban and preparation method thereof
  • Compound sustained-release preparation containing apixaban and preparation method thereof
  • Compound sustained-release preparation containing apixaban and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 4

[0049] Embodiment 4 release evaluation

[0050] Determination of release rate: sample 10 samples of edoxaban and apixaban compound sustained-release tablets prepared in each embodiment, accelerate for 6 months under the conditions of 40°C and 75% RH, and then use the dissolution method according to the release rate determination method. The device of the first method for measuring the degree of concentration uses purified water as the solvent, and the rotating speed is 100 revolutions per minute. It is operated according to the law and measured according to the ultraviolet spectrophotometry method. The absorbance is measured at a wavelength of 237nm; Edoxaban and Apixa are taken separately Take an appropriate amount of reference substance, add the above-mentioned solvent to dissolve and quantitatively dilute to a solution of about 20ug per 1ml, measure the absorbance in the same way, calculate the release rate by the external standard method, and take the average value of all t...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

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...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
IPC IPC(8): A61K31/444A61K31/4545A61K9/22A61K47/38A61K47/14A61P7/02A61P9/14
CPCA61K9/14A61K9/2013A61K9/2054A61K31/444A61K31/4545A61P7/02A61K2300/00
Inventor 胡梦思芦乾潘建斌殷学治
Owner 浙江诺得药业有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap