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Oral sustained-release pellet of anti-cancer new medicine Tivozanib and preparation method thereof

A technology of slow-release pellets and new drugs, which is applied in the field of medicine, can solve the problems of no sustained-release pellet preparations, etc., and achieve the effects of improving clinical effectiveness and safety, low production cost, and mature technology

Inactive Publication Date: 2017-06-13
WUHAN MAIDESEN MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no oral sustained-release pellet preparation for this new anticancer drug

Method used

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  • Oral sustained-release pellet of anti-cancer new medicine Tivozanib and preparation method thereof
  • Oral sustained-release pellet of anti-cancer new medicine Tivozanib and preparation method thereof
  • Oral sustained-release pellet of anti-cancer new medicine Tivozanib and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] A new anti-cancer drug Tivozanib oral sustained-release pellets:

[0025] Including the pellet core and the coating outside the pellet core, the pellet core ingredients are: Tivozanib 2g, microcrystalline cellulose 10g, lactose 5g, hydroxypropyl methylcellulose 1g; coating ingredients: Eudragit RS100 1g, PEG4000 0.5g , 0.5g triethyl citrate, 0.3g talc, 0.2g titanium dioxide.

[0026] Preparation method: mix Tivozanib with microcrystalline cellulose and lactose, pass through a 100-mesh sieve, mix uniformly, and use hypromellose solution as a binder in a centrifugal coating granulator to make pellets. The coating component coats the pellets. Take the prepared Tivozanib sustained-release pellets and measure the diameter ≤2.5mm. Take the prepared Tivozanib sustained-release pellets and measure the release curves in water, 0.1M hydrochloric acid solution, pH 5.6 carbonate buffer, and pH 7.2 phosphate buffer. The results are shown in figure 1 . The results show that the prepare...

Embodiment 2

[0028] A new anti-cancer drug Tivozanib oral sustained-release pellets:

[0029] Including the pellet core and the coating outside the pellet core, the pellet core ingredients are: Tivozanib 20g, microcrystalline cellulose 30g, mannitol 5g, ethyl cellulose 8g; coating ingredients: polyvinylpyrrolidone 5g, Eudragit RL100 3g, 0.1g PEG4000, 0.5g dimethyl phthalate, 5g talc.

[0030] Preparation method: mix Tivozanib with microcrystalline cellulose and polyvinylpyrrolidone, pass through a 100 mesh sieve, mix well, and use ethyl cellulose solution as a binder in a centrifugal coating granulator to prepare pellets. The pellets are coated with coating ingredients. Take the prepared Tivozanib sustained-release pellets and measure the diameter ≤2.5mm. Take the prepared Tivozanib sustained-release pellets and measure the release curves in water, 0.1M hydrochloric acid solution, pH 5.6 carbonate buffer, and pH 7.2 phosphate buffer. The results are shown in figure 2 . The results show that...

Embodiment 3

[0032] A new anti-cancer drug Tivozanib oral sustained-release pellets:

[0033] Including the pellet core and the coating outside the pellet core. The pellet core ingredients are: Tivozanib 45g, sucrose powder 60g, compressible starch 30g, medicinal calcium carbonate 10g, methylcellulose 6g; coating ingredients: Eudragit NE 30D 25g, PEG4000 3g. Triethyl citrate 3g, talc 10g, sodium lauryl sulfate 20g.

[0034] Preparation method: Mix Tivozanib with hydroxypropyl methylcellulose, microcrystalline cellulose, and compressible starch, then pass through a 100-mesh sieve and mix well. In a centrifugal coating granulator, use methyl cellulose solution as viscous The mixture is made into pellets, and the pellets are coated with coating ingredients. Take the prepared Tivozanib sustained-release pellets and measure the diameter ≤ 2.5mm. Take the prepared Tivozanib sustained-release pellets and measure the release curves in water, 0.1M hydrochloric acid solution, pH 5.6 carbonate buffer, a...

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Abstract

The invention belongs to the field of medicines, and particularly relates to an oral sustained-release pellet of an anti-cancer new medicine Tivozanib and a preparation method thereof. The Tivozanib oral sustained-release pellet is prepared from the following raw materials in parts by weight: 2 to 60 parts of Tivozanib, 10 to 90 parts of thinner, 1 to 25 parts of adhesive, 1 to 45 parts of sustained-release material, 0.5 to 10 parts of pore-foaming agent, 0.5 to 10 parts of plasticizer, and 0.5 to 30 parts of antisticking agent. The preparation method comprises the following steps of firstly, uniformly mixing the anti-cancer new medicine Tivozanib and the sustained-release agent, adding the adhesive, and preparing a pellet core; coating the pellet core by a mixture of the sustained-release material, the pore-foaming agent, the plasticizer and the antisticking agent, so as to obtain the oral sustained-release pellet. The oral sustained-release pellet of the anti-cancer new medicine Tivozanib and the preparation method have the advantages that a patient can orally take the anti-cancer new medicine, and the anti-cancer new medicine is slowly and stably released in an acid solution approximate to gastric acid of a human body; the operation of the preparation method is simple, the technology is matured, the production cost is low, the efficiency is high, and the preparation method is suitable for scaled production.

Description

Technical field [0001] The invention belongs to the field of medicine, and specifically relates to a new anticancer drug Tivozanib oral sustained-release pellets and a preparation method thereof. Background technique [0002] Tivozanib, also known as AV-951, is chemically named N-{2-chloro-4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl}-N'-(5- Methyl-3-isoxazolyl)urea. [0003] Structural formula: [0004] [0005] Tivozanib is an anti-tumor targeted therapy drug. It is a new multi-target anti-angiogenesis inhibitor and anti-cancer drug. It is mainly used to treat kidney cancer. It has shown good efficacy in the first-line treatment of advanced kidney cancer. Its main target The points are vascular endothelial growth factor VEGFR1, 2, and 3. By inhibiting these three vascular endothelial growth factor receptors, they can play a role in treating patients with renal cell tumors. The average survival time of patients after taking Tivozanib is 11.8 months without deterioration. For patient...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/4709A61K47/38A61K47/10A61K47/32A61P35/00
CPCA61K31/4709A61K9/0002A61K9/5026A61K9/5031A61K47/38
Inventor 刘明星童庆
Owner WUHAN MAIDESEN MEDICAL TECH