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

Tablet containing everolimus and preparation method thereof

A technology for everolimus and tablets, which is applied in the field of everolimus-containing tablets and its preparation, can solve problems affecting product properties and potential safety hazards, and achieve convenient operation, improved safety, and improved hydrophilicity sexual effect

Active Publication Date: 2013-05-15
SHANDONG NEWTIME PHARMA
View PDF4 Cites 12 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The antioxidant di-tert-butyl-p-cresol is added to Novartis's marketed preparations, which affects the properties of the product and brings safety risks to patients

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
  • Tablet containing everolimus and preparation method thereof
  • Tablet containing everolimus and preparation method thereof
  • Tablet containing everolimus and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] 1.1 Preparation of everolimus and crospovidone mixture

[0033] Everolimus 1 part

[0034] 4 parts absolute ethanol

[0035] Crospovidone 0.5 parts

[0036] Preparation process: after dissolving everolimus in absolute ethanol, add to crospovidone, and dry under reduced pressure to obtain mixture A;

[0037] 1.2 Preparation of Everolimus Tablets

[0038] Mixture A 1 part

[0039] Lactose 80 parts

[0040] 1 part magnesium stearate

[0041] Mix the mixture A with lactose and magnesium stearate, and press into tablets.

Embodiment 2

[0043] 2.1 Preparation of everolimus and crospovidone mixture

[0044] Everolimus 1 part

[0045] 400 parts of absolute ethanol

[0046] Crospovidone 100 parts

[0047] Preparation process: after dissolving everolimus in absolute ethanol, add to crospovidone, and dry under reduced pressure to obtain mixture A;

[0048] 2.2 Preparation of Everolimus Tablets

[0049] Mixture A 1 part

[0050] 1 part lactose

[0051] Magnesium stearate 0.01 parts

[0052] Mix the mixture A with lactose and magnesium stearate, and press into tablets.

Embodiment 3

[0054] 3.1 Preparation of everolimus and crospovidone mixture

[0055] Everolimus 1 part

[0056] Chloroform 80 parts

[0057] 30 parts of crospovidone

[0058] Preparation process: after dissolving everolimus in chloroform, adding to crospovidone, drying under reduced pressure to obtain mixture A;

[0059] 3.2 Preparation of Everolimus Tablets

[0060] Mixture A 1 part

[0061] Mannitol 0.8 parts

[0062] Talcum powder 0.05 parts

[0063] Mix the mixture A with lactose and magnesium stearate, and press into tablets.

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 a tablet containing everolimus and a preparation method thereof. The preparation method comprises the following steps of dissolving everolimus in an organic solvent, jetting the solution to crospovidone, carrying out reduced pressure drying, uniformly mixing the mixture obtained by the previous step, a filler and a lubricant, and carrying out tabletting, wherein a weight ratio of everolimus to crospovidone is 1: (0.5 to 100). The tablet is conducive to fast dissolution of everolimus in a gastrointestinal tract body fluid. The preparation method has simple processes, is convenient for operation and is suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of western medicine preparations, and in particular relates to a tablet containing everolimus and a preparation method thereof. Background technique [0002] Everolimus is a derivative of sirolimus, an inhibitor of mTOR, a serine threonine kinase downstream of the PI3K / AKT pathway, which was first developed by Novartis in Switzerland. First launched in Sweden in 2003, everolimus can slow down the growth of renal cancer cells and reduce the mortality rate by 67%. By inhibiting the growth and proliferation of tumor cells, it directly acts on tumor cells; by inhibiting angiogenesis, it leads to tumor blood vessel distribution reduce and play an indirect role. [0003] Everolimus is a white to slightly yellow powder, lipophilic, and its solubility in water is less than 0.01% (g / ml) at 25°C, so it is particularly important to improve its dissolution rate. [0004] Patent CN102138903A discloses an oral pharmaceu...

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): A61K9/20A61K31/436A61K47/32A61P35/00
Inventor 赵志全郝贵周陈小伟方克忠
Owner SHANDONG NEWTIME PHARMA
Features
  • Generate Ideas
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

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

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com