Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Composition of thrombopoietin receptor stimulant and preparation method thereof

A technology of composition and chelating agent, applied in the field of pharmaceutical preparations, can solve the problems of harsh taking conditions, low flexibility, and reduced compliance of Eltrombopag

Pending Publication Date: 2022-02-18
SUNSHINE LAKE PHARM CO LTD
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The clinical data in the FDA review documents of Eltrombopag show that: when taken with food, the AUC (0-∞) of the drug decreases by 59%, and the Cmax decreases by 65%; when taken together with antacids, the AUC (0-∞) of the drug decreases The Cmax is reduced by about 70%; polyvalent metal ions can chelate with Eltrombopag, which seriously reduces the absorption of the drug
In addition, the in vitro dissolution data of the patent US8052993 shows that the dissolution of tablets containing metal ions is significantly slower than that of tablets without metal ions
In summary, when Eltrombopag reacts with polyvalent metal ions, it not only reduces the dissolution of the drug, but also reduces the absorption of the drug, which is not conducive to the exertion of the drug effect.
[0004] Based on the above reasons, the conditions for taking Eltrombopag are relatively harsh, which greatly increases the difficulty for patients to take the medicine, and the flexibility is low, resulting in a decrease in the compliance of taking the medicine.

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
  • Composition of thrombopoietin receptor stimulant and preparation method thereof
  • Composition of thrombopoietin receptor stimulant and preparation method thereof
  • Composition of thrombopoietin receptor stimulant and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0042] The preparation method of the composition may include one selected from powder direct compression method, wet granulation and direct mixing process.

[0043] In a second aspect, the present invention provides a method for preparing the aforementioned composition.

[0044] A preparation method of a composition, comprising: Eltrombopag or a pharmaceutically acceptable salt thereof, a chelating agent, a filler and optionally selected from a disintegrating agent, a suspending agent, a flavoring agent and an essence At least one of them is sized and mixed to obtain the composition.

[0045] The filler can be added at least twice, and after each addition, mix well before adding the next time.

[0046] The chelating agent can be added in at least two times, and after each addition, mix well before adding the next time.

Embodiment approach

[0047] According to some embodiments of the present invention, a preparation method of a composition includes: granulating Eltrombopag or a pharmaceutically acceptable salt thereof and a chelating agent, mixing, adding the sized filler, and mixing , to obtain the composition.

[0048] According to some embodiments of the present invention, a preparation method of a composition comprises: Eltrombopag or a pharmaceutically acceptable salt thereof, a chelating agent and at least one selected from suspending agents, flavoring agents and essences The granule is sized, mixed, and then the sized filler is added and mixed to obtain the composition.

[0049] According to some embodiments of the present invention, a preparation method of a composition comprises: granulating and mixing Eltrombopag or a pharmaceutically acceptable salt thereof and a chelating agent, and then adding the sized filler and granulated The final disintegrant is mixed, and finally a lubricant is added for mixin...

specific Embodiment approach

[0061] In order to enable those skilled in the art to better understand the technical solutions of the present invention, some non-limiting examples are further disclosed below to further describe the present invention in detail.

[0062] The reagents used in the present invention can be purchased from the market or can be prepared by the methods described in the present invention.

[0063] In the present invention, the food that the Beagle dog adopts under the feeding condition is dog maintenance feed (Beijing Keao Xieli Feed Co., Ltd.), containing magnesium ≥ 1.5g in every kilogram of feed, and containing 7g-10g calcium.

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 relates to an eltrombopag composition and a preparation method thereof, and belongs to the field of pharmaceutical preparations. The composition comprises eltrombopag or a pharmaceutically acceptable salt thereof, a chelating agent and at least one pharmaceutically acceptable auxiliary material. The invention also provides a preparation method of the eltrombopag composition. The eltrombopag composition provided by the invention can eliminate the influence of food and other medicines on absorption, and improve the flexibility and compliance of taking medicines by patients.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a composition of a thrombopoietin receptor agonist and a preparation method thereof. Background technique [0002] Eltrombopag (CAS No.: 496775-61-2) is a thrombopoietin receptor agonist for the treatment of glucocorticoids, immune globulin therapy or poor effect after splenectomy Chronic thrombocytopenic purpura (ITP) in adults or patients over 1 year of age, thrombocytopenia in patients with chronic hepatitis C, and severe aplastic anemia who have had an inadequate response to immunosuppressive therapy. [0003] Eltrombopag must be taken orally on an empty stomach (1h before meals or 2h after meals), and drugs or substances containing polyvalent metal ions (such as: iron ions, calcium ions, zinc ions, magnesium ions) should not be taken 4 hours before or after taking the medicine , such as antacids, calcium-rich products, and mineral supplements. The clinical data i...

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): A61K47/18A61K47/12A61K31/4152A61P7/04A61P7/06
CPCA61K31/4152A61K47/183A61K47/12A61P7/04A61P7/06
Inventor 石添香黄心游劲松黄芳芳陈娴郝鼓鼓
Owner SUNSHINE LAKE PHARM CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com