Edoxaban sustained-release tablet pharmaceutical composition and preparation method thereof

A technology of edoxaban and sustained-release tablets, which is applied in the field of pharmaceutical preparations, can solve problems such as large fluctuations, strong hygroscopicity, poor fluidity, and difficulty in preparation operations, achieving effective release, good stability, and avoiding large fluctuations Effect

Inactive Publication Date: 2018-03-09
TIANJIN HANKANG PHARMA BIOTECH
View PDF1 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Edoxaban is easy to absorb moisture due to its own molecular structure, and the prepared preparation is easily unstable; when it is placed at room temperature for a certain period of time, there will be unsatisfactory dissolution; Bring certain operational difficulty to the preparation
In addition, the edoxaban sustained-release tablets prepared in the prior art still encounter problems that need to be solved, such as unstable sustained release, large fluctuations, difficult selection of excipients, unstable preparations, and easy moisture absorption.

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The preparation of embodiment 1 edoxaban sustained-release tablet

[0021] Prescription ratio:

[0022] Edoxaban 25g

[0023] Hypromellose (60RT10000) 55g

[0024] Hypromellose (SM-1500) 40g

[0025] Lactose 85g

[0026] Povidone K30 12g

[0027] Magnesium Stearate 2g

[0028] Film coating agent 6g

[0029] Process:

[0030] (1) Sift edoxaban, hypromellose (60RT10000), hypromellose (SM-1500) and lactose, and set aside.

[0031] (2) prepare povidone K30 ethanol solution as adhesive, and set aside.

[0032] (3) Weigh the prescribed amount of edoxaban, hypromellose (60RT10000), hypromellose (SM-1500), and lactose, mix them, add binder to granulate, add the prescribed amount of stearic acid after drying Magnesium mix well.

[0033] (4) Tablets.

[0034] (5) Coating: Take the prescribed amount of colored film coating agent to prepare a coating solution (oxygen barrier, light protection). The plain tablets are placed in a coating pan, sprayed with a film coat, and...

Embodiment 2

[0035] The preparation of embodiment 2 edoxaban sustained-release tablets

[0036] prescription:

[0037] Edoxaban 20g

[0038] Hypromellose (75RT4000) 20 g

[0039] Hypromellose (SM-1500) 12 g

[0040] Lactose 40 g

[0041] Povidone K30 3 g

[0042] Magnesium stearate 2 g

[0043] Film coating agent 3 g

[0044] Process:

[0045] (1) Sift edoxaban, hypromellose (75RT4000), hypromellose (SM-1500) and lactose, and set aside.

[0046] (2) prepare povidone K30 ethanol solution as adhesive, and set aside.

[0047] (3) Weigh the prescribed amount of edoxaban, hypromellose (75RT4000), hypromellose (SM-1500), and lactose, mix them, add binder to granulate, add the prescribed amount of stearic acid after drying Magnesium mix well.

[0048] (4) Tablets.

[0049] (5) Coating: Take the prescribed amount of colored film coating agent to prepare a coating solution (oxygen barrier, light protection). plain tablet coating

[0050] In the pot, spray the film coat and dry it.

Embodiment 3

[0051] The preparation of embodiment 3 edoxaban sustained-release tablets

[0052] prescription:

[0053] Edoxaban 50g

[0054] Hypromellose (75RT4000) 25 g

[0055] Hypromellose (SM-1500) 25 g

[0056] Lactose 100 g

[0057] Povidone K30 8g

[0058] Magnesium Stearate 3g

[0059] Film coating agent 6g

[0060] Process:

[0061] (1) Sift edoxaban, hypromellose (75RT4000), hypromellose (SM-1500) and lactose, and set aside.

[0062] (2) prepare povidone K30 ethanol solution as adhesive, and set aside.

[0063] (3) Weigh the prescribed amount of edoxaban, hypromellose (75RT4000), hypromellose (SM-1500), and lactose, mix them, add binder to granulate, add the prescribed amount of stearic acid after drying Magnesium mix well.

[0064] (4) Tablets.

[0065] (5) Coating: Take the prescribed amount of colored film coating agent to prepare a coating solution (oxygen barrier, light protection). plain tablet coating

[0066] In the pot, spray the film coat and dry it.

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

PropertyMeasurementUnit
viscosityaaaaaaaaaa
Login to view more

Abstract

The invention discloses a pharmaceutical composition for edoxaban sustained-release tablets. The sustained-release tablet contains edoxaban, high-viscosity hypromellose, medium-viscosity hypromellose and a water-soluble filler, and also contains Other pharmaceutical excipients. The invention also discloses a preparation method of the edoxaban sustained-release tablet pharmaceutical composition.

Description

technical field [0001] The present invention relates to the field of pharmaceutical preparations, in particular to drug sustained-release solid preparations, in particular to a pharmaceutical composition of Edoxaban sustained-release tablets and a preparation method thereof. Background technique [0002] Edoxaban is a small molecule oral anticoagulant developed by Daiichi Sankyo Co., Ltd., which is a factor X (FXa) blocker. During the blood coagulation process, activated coagulation factor X (FXa) activates prothrombin (FII) into thrombin (FIIa), which promotes the formation of fibrin and thus forms thrombus. Therefore, FXa has become the main target for the development of a new generation of anticoagulant drugs. point. Edoxaban is an oral anticoagulant drug that inhibits thrombus formation through selective, reversible and direct inhibition of FXa, and its selectivity for FXa is 104 times higher than that of FIIa. Clinical trials in Japan and abroad have confirmed that th...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K9/28A61K31/444A61K47/38A61K47/26A61P7/02
CPCA61K9/2054A61K9/0002A61K9/2018A61K9/2806A61K31/444
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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