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Everolimus solid oral medicinal composition

A technology of everolimus and composition, applied in the direction of drug combination, antineoplastic drugs, pharmaceutical formulations, etc., can solve the problems of increasing the complexity of the operation process, increasing the cost, and the existence of potential safety hazards, so as to improve the solubility and stability of the drug non-toxicity, less dust pollution, and simple preparation process

Active Publication Date: 2011-08-03
苏州特瑞药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, whether the intake of organic solvents will affect the drug and excipients, organic solvent residues, equipment problems, personnel safety problems, and residual solvent detection problems not only increase the complexity of the operation process, but also pose safety hazards. At the same time, the cost is greatly increased

Method used

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  • Everolimus solid oral medicinal composition
  • Everolimus solid oral medicinal composition
  • Everolimus solid oral medicinal composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] A prescription for orally disintegrating tablets of everolimus solid oral pharmaceutical composition:

[0037]

[0038]

[0039] The manufacturing process of this embodiment is as follows:

[0040] Weigh the raw and auxiliary materials of the prescribed amount, pass everolimus through a 100-mesh sieve, microcrystalline cellulose, mannitol, lactose, citric acid, crospovidone, and orange essence pass through a 80-mesh sieve, micropowder silica gel, stearin Sodium fumarate is passed through a 100-mesh sieve. Take the prescribed amount of mannitol and put it in the GPCG1.1 fluidized bed coating machine equipped with a bottom spray, adjust the inlet air temperature to 40°C, the outlet air temperature to 25°C, and the material temperature to 25°C to make the mannitol evenly distributed in the fluidized bed. boiling. Adjust the atomization pressure of the spray gun to 2 bar, and the speed of the peristaltic pump to 20 rpm, evenly disperse the prescribed amount of evero...

Embodiment 2

[0042] A prescription for dispersible tablets of everolimus solid oral pharmaceutical composition:

[0043]

[0044]

[0045] The manufacturing process of this embodiment is as follows:

[0046] The raw and auxiliary materials of the prescription amount were weighed, everolimus was passed through a 100-mesh sieve, mannitol, lactose, citric acid, hydroxypropyl cellulose, crospovidone, and banana essence were respectively passed through a 80-mesh sieve, micronized silica gel, hard Magnesium fatty acid passed through a 100-mesh sieve. Take the prescribed amount of mannitol and put it in the GPCG1.1 fluidized bed coating machine equipped with a bottom spray, adjust the inlet air temperature to 40°C, the outlet air temperature to 25°C, and the material temperature to 25°C to make the mannitol evenly distributed in the fluidized bed. boiling. Adjust the atomization pressure of the spray gun to 2 bar, and the speed of the peristaltic pump to 20 rpm, evenly disperse the prescr...

Embodiment 3

[0048] A prescription for a chewable tablet of everolimus solid oral pharmaceutical composition:

[0049]

[0050]

[0051] The manufacturing process of this embodiment is as follows:

[0052] Weigh the raw and auxiliary materials of the prescription amount, everolimus is passed through a 100-mesh sieve, microcrystalline cellulose, mannitol, povidone, lactose, sodium citrate, pregelatinized starch, sodium carboxymethyl starch, apple essence, Peppermint essence is passed through a 80-mesh sieve, and stearic acid and magnesium micropowder silica gel are passed through a 100-mesh sieve. Take the prescribed amount of mannitol and put it in the GPCG1.1 fluidized bed coating machine equipped with a bottom spray, adjust the inlet air temperature to 40°C, the outlet air temperature to 25°C, and the material temperature to 25°C to make the mannitol evenly distributed in the fluidized bed. boiling. Adjust the atomization pressure of the spray gun to 2 bar, and the speed of the p...

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PUM

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Abstract

The invention discloses an everolimus solid oral medicinal composition, which comprises a composition consisting of everolimus or a derivative thereof and excipient, wherein the pH value of aqueous solution of the composition is 5 to 6; and the everolimus or the derivative thereof accounts for 0.05 to 5 percent based on the weight of the composition. The composition can be prepared into a high-bioavailability and non-micronized preparation which overcomes the defects of low dissolubility and stability by the regulation of the pH value of the everolimus or the derivative thereof and the excipient, adoption of the reasonable formula ratio, and uniform dispersion of main ingredients by employing the fluidized bed coating technology.

Description

technical field [0001] The invention relates to a composition in the field of pharmaceutical preparations, in particular to an everolimus solid oral pharmaceutical composition. Background technique [0002] Everolimus (everolimus) is a derivative of sirolimus (sirolimus, also known as rapamycin, ie rapamycin), so everolimus is also called 40-O-(2-hydroxyethyl)-rapa Mycin, or 40-O-(2-hydroxyethyl)-sirolimus. [0003] Everolimus is an inhibitor of mTOR (mammalian target of rapamycin), a serine-threonine kinase downstream of the PI3K / AKT pathway. Everolimus was first developed by Novartis in Switzerland under the trade name Certican. It was launched in Sweden for the first time in 2003 and has fully occupied the European market in 2006. [0004] FDA approved it for patients with advanced kidney cancer who failed sunitinib or sorafenib. According to Novartis research, everolimus can slow down the growth of kidney cancer cells and reduce the death rate by 67%. By inhibiting th...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/16A61K9/20A61K31/436A61P35/00A61P37/06
Inventor 初虹王浩徐家军
Owner 苏州特瑞药业股份有限公司
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