Oral solid pharmaceutical composition containing Fingolimod

A composition and drug technology, which can be used in drug combinations, antipyretic drugs, cardiovascular system diseases, etc., can solve the problems of large excipients, increased adverse reactions, and difficulty in controlling content uniformity.

Inactive Publication Date: 2014-07-09
PHARMA RES INST OF BENCAO TIANYUAN OF BEIJING
View PDF3 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In addition, due to the small size of the solid pharmaceutical composition of fingolimod and its pharmaceutically acceptable salts (the size of the original preparation is 0.5 mg), and the large amount of excipients, it is very difficult to control the uniformity of the content, which may cause each Inconsistent intake affects curative effect and increases adverse reactions

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
  • Oral solid pharmaceutical composition containing Fingolimod
  • Oral solid pharmaceutical composition containing Fingolimod
  • Oral solid pharmaceutical composition containing Fingolimod

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0069] Pharmaceutical compositions using only microcrystalline cellulose as excipients:

[0070]

[0071] Preparation method: Pass the micronized fingolimod hydrochloride through a 200-mesh sieve. The prescribed amount of fingolimod hydrochloride and microcrystalline cellulose are mixed uniformly in equal amounts to obtain the pharmaceutical composition of the present invention. After heating at 60° C. for 40 hours, inspect and check the content changes of impurities and fingolimod hydrochloride. The inspection results show that the impurity content of the composition is 0.14, and the main drug content is 99.9%.

[0072] The composition is compressed into tablets or filled into capsules according to the required dosage.

Embodiment 2

[0074] Pharmaceutical compositions using only microcrystalline cellulose as excipients:

[0075]

[0076]Preparation method: Pass the micronized fingolimod hydrochloride through a 200-mesh sieve. The prescribed amount of fingolimod hydrochloride and microcrystalline cellulose are mixed uniformly in equal amounts to obtain the pharmaceutical composition of the present invention. After heating at 60° C. for 40 hours, inspect and check the content changes of impurities and fingolimod hydrochloride. The inspection results show that the impurity content of the composition is 0.13%, and the main drug content is 101.9%.

[0077] The composition is compressed into tablets or filled into capsules according to the required dosage.

Embodiment 3

[0079] Pharmaceutical compositions using only microcrystalline cellulose as excipients:

[0080]

[0081] Preparation method: Pass the micronized fingolimod hydrochloride through a 300-mesh sieve. The prescribed amount of fingolimod hydrochloride and microcrystalline cellulose are mixed uniformly in equal amounts to obtain the pharmaceutical composition of the present invention. After heating at 60° C. for 40 hours, inspect and check the content changes of impurities and fingolimod hydrochloride. The inspection results show that the impurity content of the composition is 0.15%, and the main ingredient content is 102.2%.

[0082] The composition is compressed into tablets or filled into capsules according to the required dosage.

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 the field of chemical pharmaceutical preparations, especially to an oral solid pharmaceutical composition containing Fingolimod or its pharmaceutically acceptable salt. Specifically, the invention relates to a pharmaceutical composition containing Fingolimod or its pharmaceutically acceptable salt, microcrystalline cellulose and (or) other pharmaceutical excipients or carriers. The pharmaceutical composition provided by the invention has the characteristics of stable preservation performance, high content uniformity, and excellent dissolution performance.

Description

technical field [0001] The invention relates to the field of chemical pharmaceutical preparations, in particular to an oral solid pharmaceutical composition containing fingolimod or a pharmaceutically acceptable salt thereof. Background technique [0002] Fingolimod, chemical name 2-amino-2-(2-[4-octylphenyl]ethyl)-1,3-propanediol, molecular formula C 19 h 33 NO 2 , its structural formula is as follows: [0003] [0004] Fingolimod and its pharmaceutically acceptable salts are newly developed immunosuppressants in recent years, with a unique mechanism of action, strong immunosuppressive effect, and less toxic and side effects. The drug selectively reduces the number of lymphocytes in peripheral blood and tissues, significantly prolongs the survival of transplanted organs of experimental animals, and does not impair the immune response to viruses and immune memory function, with low side effects, and is compatible with CsA, FK506, RAD and other clinical First-line immu...

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): A61K31/137A61K47/38A61P37/06A61P29/00A61P31/12A61P9/00A61P25/00
Inventor 顾群任霞李志刚孙学伟
Owner PHARMA RES INST OF BENCAO TIANYUAN OF BEIJING
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