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
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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

[0031] Example 1

[0032] 1.1 Preparation of everolimus and crospovidone mixture

[0033] 1 serving of everolimus

[0034] 4 parts of absolute ethanol

[0035] Cross-linked povidone 0.5 parts

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

[0037] 1.2 Preparation of everolimus tablets

[0038] Mixture A 1 part

[0039] 80 servings of lactose

[0040] Magnesium stearate 1 part

[0041] Mix the mixture A with lactose and magnesium stearate evenly, and compress the tablet to obtain it.

Example Embodiment

[0042] Example 2

[0043] 2.1 Preparation of everolimus and crospovidone mixture

[0044] 1 serving of everolimus

[0045] 400 parts of absolute ethanol

[0046] Cross-linked povidone 100 parts

[0047] Preparation process: Dissolve everolimus in absolute ethanol, add it 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 serving of lactose

[0051] 0.01 parts of magnesium stearate

[0052] Mix the mixture A with lactose and magnesium stearate evenly, and compress the tablet to obtain it.

Example Embodiment

[0053] Example 3

[0054] 3.1 Preparation of everolimus and crospovidone mixture

[0055] 1 serving of everolimus

[0056] 80 parts of chloroform

[0057] Cross-linked povidone 30 parts

[0058] Preparation process: Dissolve everolimus in chloroform, add to crospovidone, and dry 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] Talc 0.05 parts

[0063] Mix the mixture A with lactose and magnesium stearate evenly, and compress the tablet to obtain it.

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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

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Application Information

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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
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