Tablet containing everolimus, and preparation method thereof

A technology for everolimus and tablets, which is applied to the field of tablets containing everolimus and its preparation, can solve problems such as potential safety hazards, influence on product properties, etc., and achieves improved safety, convenient operation and simple preparation process Effect

Active Publication Date: 2014-02-19
SHANDONG NEWTIME PHARMA
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  • 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 preparation

Method used

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  • 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

Example Embodiment

[0029] Example 1

[0030] 1.1 Preparation of everolimus solid dispersion

[0031] 1 serving of everolimus

[0032] 4 parts of absolute ethanol

[0033] Hydroxypropyl cellulose 0.3 parts

[0034] Preparation process: After dissolving everolimus in absolute ethanol, adding hydroxypropyl cellulose, stirring to dissolve, and then using supercritical fluid technology to prepare, through supercritical fluid rapid expansion method, the solution is decompressed through nozzles and capillary tubes. The supercritical fluid expands rapidly to produce a very fine solid dispersion containing everolimus.

[0035] 1.2 Preparation of everolimus tablets

[0036]

[0037]

[0038] Mix the everolimus solid dispersion with lactose, sodium carboxymethyl starch, and magnesium stearate, and then press the tablet.

Example Embodiment

[0039] Example 2

[0040] 1.1 Preparation of everolimus solid dispersion

[0041] 1 serving of everolimus

[0042] 200 parts of absolute ethanol

[0043] Hydroxypropyl cellulose 80 parts

[0044] Preparation process: After dissolving everolimus in absolute ethanol, adding hydroxypropyl cellulose, stirring to dissolve, and then using supercritical fluid technology to prepare, through supercritical fluid rapid expansion method, the solution is decompressed through nozzles and capillary tubes. The supercritical fluid expands rapidly to produce a very fine solid dispersion containing everolimus.

[0045] 1.2 Preparation of everolimus tablets

[0046]

[0047] Mix the everolimus solid dispersion with lactose, sodium carboxymethyl starch, and magnesium stearate, and then press the tablet.

Example Embodiment

[0048] Example 3

[0049] 1.1 Preparation of everolimus solid dispersion

[0050] 1 serving of everolimus

[0051] 20 parts of absolute ethanol

[0052] Hydroxypropyl cellulose 3 parts

[0053] Preparation process: After dissolving everolimus in absolute ethanol, adding hydroxypropyl cellulose, stirring to dissolve, and then using supercritical fluid technology to prepare, through supercritical fluid rapid expansion method, the solution is decompressed through nozzles and capillary tubes. The supercritical fluid expands rapidly to produce a very fine solid dispersion containing everolimus.

[0054] 1.2 Preparation of everolimus tablets

[0055]

[0056]

[0057] Mix the everolimus solid dispersion with lactose, crospovidone, and magnesium stearate, and then press the tablet.

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PUM

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Abstract

The invention relates to a tablet containing everolimus, and a preparation method thereof. The tablet is prepared by tabletting of everolimus solid dispersion and a pharmaceutically acceptable auxiliary material, wherein the pharmaceutically acceptable auxiliary material comprises a filling material, a disintegrating agent and a lubricant. The everolimus solid dispersion is made of everolimus using a specific carrier material, so that hydrophilicity of everolimus is increased greatly, it is beneficial for rapid dissolving of everolimus in gastrointestinal tract body fluids, and medicine safety is improved.

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, Switzerland. Launched in Sweden for the first time 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; reduce and play an indirect role. [0003] Everolimus is a white to slightly yellow powder, lipophilic, and its solubility in water at 25°C is less than 0.01% (g / ml), so it is particularly important to improve its dissolution rate. [0004] Chinese patent CN102138903A discloses an oral pharmaceutical composition of everolimus, which overcomes the ...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/436A61K47/38A61P35/00
Inventor 赵志全郝贵周丁兵
Owner SHANDONG NEWTIME PHARMA
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