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A kind of apixaban nano-suspension and preparation method thereof

A nanosuspension, apixaban technology, applied in the field of medicine, can solve problems such as low bioavailability, achieve the effects of less dosage, improved adhesion, and simple process

Active Publication Date: 2021-03-19
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Aiming at the problem of low bioavailability of apixaban, the invention discloses a nanosuspension of apixaban, which can improve the solubility and dissolution rate of the drug, increase the permeability of the drug, and is beneficial to improve the apixaban Oral absorption properties of Ban, enhance drug bioavailability

Method used

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  • A kind of apixaban nano-suspension and preparation method thereof
  • A kind of apixaban nano-suspension and preparation method thereof
  • A kind of apixaban nano-suspension and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0027] Weigh 20 mg of apixaban in 35 ml of water, ultrasonically treat for 10 minutes to fully disperse the drug in water; use a high-speed disperser to cut at 10,000 rpm for 5 minutes to obtain a coarse suspension; perform high-pressure homogenization on the above coarse suspension , first homogenized twice at 800 bar, and then homogenized 12 times at 1800 bar pressure to obtain the apixaban nanosuspension. The measured particle size of the nanosuspension was 754nm, and the polydispersity index (PDI) was 0.378.

Embodiment 2

[0029] Weigh 5 mg of PVPK30 in 50 ml of water, add 20 mg of apixaban under stirring, and ultrasonically treat for 10 min to fully disperse the drug in water; use a high-speed disperser to shear at 10,000 rpm for 5 min to obtain a coarse suspension; The suspension was subjected to high-pressure homogenization, first at 800 bar for 2 times, and then at 1800 bar for 12 times to obtain the apixaban nanosuspension. The measured particle size of the nanosuspension was 386.7nm, and the polydispersity index (PDI) was 0.167.

Embodiment 3

[0031] Weigh 1 mg of sodium taurocholate into 35 ml of water, add 20 mg of apixaban under stirring, and ultrasonically treat for 10 min to fully disperse the drug in water; use a high-speed disperser to shear at 10,000 rpm for 5 min to obtain a coarse suspension; The above coarse suspension was subjected to high-pressure homogenization, first at 800 bar for 2 times, and then at 1800 bar for 12 times to obtain the apixaban nano-suspension. The measured particle size of the nanosuspension was 401.6 nm, and the polydispersity index (PDI) was 0.11.

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Abstract

The invention belongs to the technical field of medicine, and discloses an Aapixaban nanometer mixed suspension and a preparation method thereof. The Aapixaban belongs to novel oral anti-freezing medicine, and is clinically used for preventing and treating thrombus; the Aapixaban has poor water solubility and low seepage performance; the oral bioavailability is limited. The prepared Aapixaban nanometer mixed suspension uses a little amount of glycocholate sodium and polyvinyl lactam-polyvinyl acetate-polyethylene glycol graft copolymerization (Soluplus) as a combined sterilizingstabilizing agent; a high-pressure homogenizing method is used for preparation. The prepared nanometer suspension has the advantages that the medicine dissolution degree and the dissolution-out speed can be improved; the medicine seepage performance is improved; the oral absorption is favorably enhanced; the bioavailability is improved; the recipe process is simple and convenient; the industrialized production is easy.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an apixaban nano-suspension and a preparation method thereof. Background technique [0002] Apixaban (Apixaban) chemical name is (1-(4-methoxyphenyl)-7-oxo-6[4-(2-oxopiperidin-1-yl)phenyl]-4, 5,6,7-tetrahydro-1H-pyrazol[3,4-c]pyridine-3-carboxamide, the molecular formula is C 25 h 25 N 5 o 4 , the molecular weight is 459.50, and its structural formula is as follows: [0003] [0004] Apixaban is a new type of oral anticoagulant, a highly selective and reversible inhibitor of blood coagulation factor Xa, which has been on the market in Europe since 2011 and was jointly developed by Pfizer and Bristol-Myers Squibb; in 2013 Obtained the import drug license issued by the State Food and Drug Administration of China. It is used for adult patients undergoing elective hip or knee replacement to prevent venous thrombosis. It was approved for marketing in China in 2013. The tablet...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/4545A61P7/04B82Y5/00B82Y40/00
CPCA61K9/1075A61K31/4545A61P7/04B82Y5/00B82Y40/00
Inventor 栾立标邵田田
Owner CHINA PHARM UNIV
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