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Everolimus pharmaceutical composition

A technology of everolimus and composition, which is applied in the direction of drug combination, antineoplastic drugs, and pharmaceutical formulations, and can solve problems affecting drug dissolution and pressure

Active Publication Date: 2018-06-08
HANGZHOU ZHONGMEI HUADONG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the need to add a large amount of solvents, especially organic solvents, in the process of preparing solid dispersions, the solvent removal process will cause huge pressure on production, including time, cost, etc. Most importantly, the conventional volatile solvent removal method may form dense solids Dispersion particles, even if they are ground into fine powder, may affect the dissolution and other properties of the drug. It is also extremely meaningful to provide a new process for preparing this solid dispersion

Method used

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  • Everolimus pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

SD example 1

[0088] SD Example 1: Preparation of Everolimus Solid Dispersion

[0089] composition:

[0090] Everolimus 5mg,

[0091] Antioxidant (BHT) 0.015mg,

[0092] Carrier (PEG1500) 4mg,

[0093] Alkanol 0.075mg,

[0094] Dispersant (colloidal silicon dioxide) 1.5mg,

[0095] (dehydrated alcohol, appropriate amount, the solid content in the suspension that makes above-mentioned each material preparation gained is 10%,)

[0096] Excipient (lactose) 40mg,

[0097] Disintegrant (crospovidone) 10mg.

[0098] Preparation method:

[0099] (i) dissolving / dispersing everolimus, antioxidant, carrier, alkanol, and dispersant in absolute ethanol to obtain a suspension in which the dispersant is dispersed;

[0100] (ii) mixing the excipients and disintegrants which are crushed in advance and can pass through a 150 mesh sieve in a fluidized bed spray granulator to obtain a mixed powder;

[0101] (iii) Spray the fully suspended suspension obtained in step (i) into the mixed powder in a f...

SD example 2

[0110] SD Example 2: Preparation of Everolimus Solid Dispersion

[0111] composition:

[0112] Everolimus 5mg,

[0113] Antioxidant (BHT) 0.01mg,

[0114] Carrier (PEG1000) 5mg,

[0115] Alkanol 0.05mg,

[0116] Dispersant (colloidal silicon dioxide) 1mg,

[0117] (dehydrated alcohol, appropriate amount, the solid matter content in the suspension that makes above-mentioned each material preparation gained is 8%,)

[0118] Excipient (mannitol) 30mg,

[0119] Disintegrant (sodium starch glycolate) 15mg.

[0120] Preparation method:

[0121] (i) dissolving / dispersing everolimus, antioxidant, carrier, alkanol, and dispersant in absolute ethanol to obtain a suspension in which the dispersant is dispersed;

[0122] (ii) mixing the excipients and disintegrants which are crushed in advance and can pass through a 150 mesh sieve in a fluidized bed spray granulator to obtain a mixed powder;

[0123] (iii) Spray the fully suspended suspension obtained in step (i) into the mixed p...

SD example 3

[0131] SD Example 3: Preparation of Everolimus Solid Dispersion

[0132] composition:

[0133] Everolimus 5mg,

[0134] Antioxidant (BHT) 0.02mg,

[0135] Carrier (PEG2000) 3mg,

[0136] Alkanol 0.1mg,

[0137] Dispersant (colloidal silicon dioxide) 2mg,

[0138] (dehydrated alcohol, appropriate amount, the solid matter content in the suspension that makes above-mentioned each material preparation gained is 13%,)

[0139] Excipient (dextrin) 60mg,

[0140] Disintegrant (sodium carboxymethylcellulose) 5mg.

[0141] Preparation method:

[0142] (i) dissolving / dispersing everolimus, antioxidant, carrier, alkanol, and dispersant in absolute ethanol to obtain a suspension in which the dispersant is dispersed;

[0143] (ii) mixing the excipients and disintegrants which are crushed in advance and can pass through a 150 mesh sieve in a fluidized bed spray granulator to obtain a mixed powder;

[0144] (iii) Spray the fully suspended suspension obtained in step (i) into the m...

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Abstract

The invention relates to an everolimus pharmaceutical composition. Specifically, the pharmaceutical composition includes an everolimus solid dispersion in a form of a microparticle; a diluent, a lubricant, an optional disintegrant, an optional binder, wherein the everolimus solid dispersion includes: everolimus, antioxidants, carriers, dispersants. The invention also relates to pharmaceutical useof the everolimus solid dispersion, the everolimus solid pharmaceutical composition and the everolimus solid dispersion. The pharmaceutical composition and the solid dispersion exhibit excellent technical effects such as excellent dissolution properties, physical stability, and chemical stability.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a pharmaceutical composition of everolimus, in particular to a pharmaceutical composition in tablet form, and to a preparation method of the pharmaceutical composition. Background technique [0002] Everolimus (Everolimus) is a sirolimus derivative, a sirolimus target protein (mTOR) inhibitor developed by Novartis, Switzerland, as an anti-tumor drug, also known as 40-O-( 2-hydroxyethyl)-sirolimus or 40-O-(2-hydroxyethyl)-rapamycin. Everolimus CAS registration number 159351-69-6, its chemical name is (1R, 9S, 12S, 15R, 16E, 18R, 19R, 21R, 23S, 24E, 26E, 28E, 30S, 32S, 35R) -1 ,18-Dihydroxy-12-{(1R)-2-[(1S,3R,4R)-4-(2-hydroxyethyl)-3-methoxycyclohexyl]-1-methylethyl} -19,30-dimethoxy-15,17,21,23,29,35-hexamethyl-11,36-dioxa-4-aza-tricyclo[30.3.1.04,9]hexatriaconta-16 ,24,26,28-tetraene-2,3,10,14,20-pentone, molecular formula is C53H83NO14, molecular weight is 958.2, chemical stru...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K9/16A61K47/10A61K31/436A61P35/00
CPCA61K9/1617A61K9/2013A61K31/436
Inventor 韩敏吕祥兰陈丽娜傅立峰周屹峰
Owner HANGZHOU ZHONGMEI HUADONG PHARMA
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