Oral nilotinib nano-formulation and preparation method thereof

A technology of nilotinib and nano-preparation, which is applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problems of low solubility and low bioavailability, and achieve product quality. High, improve drug solubility and permeability, the effect of continuous operation

Active Publication Date: 2017-11-07
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The first technical problem to be solved in the present invention is to provide a kind of nilotinib oral nano-preparation; the present invention solves the problem that the drug has low solubility in water and low bioavailability in the human body by preparing nilotinib oral nano-preparation. Advanced issues are beneficial to improve the solubility and permeability of nilotinib, and finally achieve the purpose of improving its bioavailability, so that the dissolution performance of the drug is greatly improved, and the dissolution rate of the drug in 15 minutes reaches 93%-97%

Method used

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  • Oral nilotinib nano-formulation and preparation method thereof
  • Oral nilotinib nano-formulation and preparation method thereof
  • Oral nilotinib nano-formulation and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0043] A kind of preparation of nilotinib oral nano-preparation, the steps are as follows:

[0044] Nilotinib bulk drug (scanning electron microscope picture as figure 1 shown) and N,N-dimethylformamide to make 40mL of nilotinib N,N-dimethylformamide solution with a concentration of 15mg / mL; make 0.2mg of natural water-soluble VE and deionized water 600mL of natural water-soluble VE aqueous solution per mL, add 20mg sodium dodecylbenzenesulfonate to the natural water-soluble VE aqueous solution at the same time to obtain an anti-solvent containing a stabilizer, then add nilotinib solution, and stir for 10min using a mechanical stirrer , the temperature of the reaction system is controlled to be 15°C to obtain a nilotinib drug slurry; the obtained nilotinib drug slurry is freeze-dried to obtain a freeze-dried powder, and the obtained freeze-dried powder is mixed with 400mg lactose, 20mg cross-linked carboxyl Sodium methylcellulose, 15mg talcum powder, and 15mg silicon dioxide ...

Embodiment 2

[0051] Nilotinib raw material drug and N,N-dimethylformamide are made into 20mL of nilotinib N,N-dimethylformamide solution with a concentration of 10mg / mL; into 0.1mg / mL polyvinylpyrrolidone aqueous solution 300mL, add 5mg poloxamer to polyvinylpyrrolidone aqueous solution simultaneously, obtain the anti-solvent containing stabilizer; Adjust the flow rate to be 2mL / min, 30mL / min respectively, collect the product at the outlet of the microchannel reactor, and control the temperature of the reaction system to obtain the nilotinib nano-medicine slurry; the obtained nilotinib nano-medicine slurry The material is freeze-dried to obtain freeze-dried powder; the obtained freeze-dried powder is mixed with 150mg lactose, 10mg crospovidone, 5mg magnesium stearate, 5mg colloidal silicon dioxide, and 5mg talcum powder to prepare nilotinib for oral administration. nano formulations.

[0052] The obtained freeze-dried powder is redispersed with water, and the SEM characterization shows th...

Embodiment 3

[0054] The nilotinib bulk drug and N,N-dimethylformamide are formulated into 40mL of nilotinib N,N-dimethylformamide solution with a concentration of 15mg / mL; polyethylene glycol and deionized water Prepare 800 mL of 0.1 mg / mL polyethylene glycol solution with ethanol, wherein the volume ratio of alcohol to water is 1:5, and simultaneously add 20 mg of sodium dodecylbenzenesulfonate and 50 mg of lactose to the PEG solution to obtain polyethylene glycol containing Anti-solvent of alcohol, sodium dodecylbenzenesulfonate and lactose; Nilotinib solution was added to the anti-solvent, stirred with a magnetic stirrer for 5min, and the temperature of the reaction system was controlled at 20°C to obtain Nilotinib nano Drug slurry; the obtained nilotinib nano drug slurry is spray-dried to obtain a spray-dried powder; the gained spray-dried powder is mixed with 350mg lactose, 60mg crospovidone, 15mg magnesium stearate, and 15mg silicon dioxide to prepare Oral nano-formulations of niloti...

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Abstract

The invention discloses an oral nilotinib nano-formulation which comprises an active ingredient nilotinib, a main auxiliary material, an additional auxiliary material and a stabilizer, wherein the mass content of the nilotinib is 30-55%; the mass content of the main auxiliary material is 20-40%, the mass content of the additional auxiliary material is 2-10%, the mass content of the stabilizer is 2-20%, and the particle size of the oral nilotinib nano-formulation is less than 1 micron. The invention further discloses a preparation method of the oral nilotinib nano-formulation. Due to the prepared oral nilotinib nano-formulation, the problems that the medicine has low dissolubility in water and low bioavailability in a human body and the like are solved, the solubleness and permeability of the nilotinib are improved, and finally the aim of improving the bioavailability is achieved. Therefore, the digestion performance of the medicine is greatly improved, and the drug dissolution reaches 93-97% within 15 minutes.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a nilotinib oral nano-preparation and a preparation method thereof. Background technique [0002] Nilotinib, the chemical name is 4-methyl-3-((4-(3-pyridyl)-2-pyrimidinyl)amino)-N-(5-(4-methyl-1H- Imidazol-1-yl)-3-(trifluoromethyl)phenyl)benzamide is a highly selective oral tyrosine kinase inhibitor developed by Swiss Novartis pharmaceutical company, and its monohydrochloride monohydrate is in In October 2007, it was approved by the U.S. FDA for marketing under the trade name Tasigna, which is clinically used to treat chronic myelogenous leukemia that is ineffective for imatinib mesylate. Its relative molecular mass is 529.5, and its structural formula is as follows: [0003] [0004] Nilotinib has been used clinically. It is a kind of high-affinity multi-targeted drug. Tolerant CML patients had a clear therapeutic effect. Nilotinib has the advantages of high sel...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K47/26A61K47/38A61K47/32A61K31/506A61P35/02
CPCA61K9/0053A61K9/5123A61K9/5138A61K9/5161A61K31/506
Inventor 乐园陈鹏陈丽娜戴田晨林谡轩沈煜栋
Owner BEIJING UNIV OF CHEM TECH
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