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Stable everolimus tablet

The technology of everolimus tablet and velimus tablet, which is applied in the field of medicine, can solve the problems of many related substances, influence drug stability, poor stability, etc., and achieves simple preparation process, simple and feasible workshop safety control, The effect of safe production operation

Active Publication Date: 2015-06-24
CHIA TAI TIANQING PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, from the perspective of everolimus structure, it belongs to macrolide drugs, is easy to hydrolyze, and has poor stability under acid-base conditions, and the granulation of this patent embodiment with water inevitably affects the stability of the drug. From the implementation From the perspective of the effect of the example, although the dissolution rate is better, there are more related substances

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Preparation Process:

[0034] Take the prescribed amount of everolimus, and process it through jet milling so that the median particle size D50 does not exceed 100 μm. Mix everolimus with BHT, lactose, HPMC, PVPP, and magnesium stearate evenly, and press into tablets to obtain the product.

Embodiment 2

[0037] Preparation Process:

[0038] Take the prescribed amount of everolimus, process it through jet milling, so that the median particle size D50 does not exceed 80 μm, mix everolimus with BHT, lactose, PVPP, and magnesium stearate evenly, and press into tablets to obtain the product.

Embodiment 3

0.5%

[0042] Preparation Process:

[0043] Take the prescribed amount of everolimus, process it through jet milling, so that the median particle size D50 does not exceed 50 μm, mix everolimus with BHT, lactose, and magnesium stearate evenly, and press into tablets to obtain the product.

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PUM

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Abstract

The invention provides a stable everolimus tablet containing one or several selected from everolimus, 2,6-tert-butyl-4-methylphenol, a filling agent, an adhesive, a disintegrating agent and a lubricating agent, wherein everolimus is micronized before being tabletted, and the micronized median particle diameter D50 does not exceed 100mu m. The everolimus tablet prepared by the invention has the advantages of relatively high dissolution rate, favorable stability, low production cost, stable and controllable process parameters and the like.

Description

technical field [0001] The invention belongs to the technical field of medicine, in particular to a stable everolimus tablet. Background technique [0002] Rapamycin, an immunosuppressive lactam macrolide produced by Streptomyces hygroscopicus, is an extremely potent immunosuppressant and has been shown to have antineoplastic and antifungal activity. Everolimus is a derivative of rapamycin, the structure is shown below, also known as 40-O-(2-hydroxy) ethyl rapamycin, English name everolimus, is an mTOR inhibitor. mTOR is a downstream effector of the mammalian PI3k / Akt pathway, a highly conserved serine / threonine protein kinase, which regulates other kinases, such as 40S ribosomal 6 kinase (S6K), cell cycle-dependent protein kinase (CDKP ) and phosphorylation of eukaryotic translation initiation factor (4EB), which play an important regulatory role in protein translation. [0003] Everolimus [0004] Everolimus (everolimus) was developed by Novartis, Switzerland, and was...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/436A61K47/10A61P37/06A61P35/00A61P31/10
Inventor 张勇王少平高敏姣陈智林方晓志
Owner CHIA TAI TIANQING PHARMA GRP CO LTD