Apixaban nanometer mixed suspension and preparation method thereof

A nano-suspension, apixaban technology, applied in the field of medicine, can solve the problem of low bioavailability, achieve the effect of less dosage, increase bioavailability, and improve drug absorption

Active Publication Date: 2018-12-18
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 dissoluti

Method used

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  • Apixaban nanometer mixed suspension and preparation method thereof
  • Apixaban nanometer mixed suspension and preparation method thereof
  • Apixaban nanometer mixed suspension and preparation method thereof

Examples

Experimental program
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Example Embodiment

[0026] Example 1

[0027] Weigh 20mg apixaban in 35ml water, ultrasonically treat it for 10min to fully disperse the drug in the water; shear it with a high-speed disperser at 10000rpm for 5min to obtain a crude suspension; homogenize the above-mentioned crude suspension under high pressure , First homogenize 2 times at 800bar, and then homogenize 12 times at 1800bar pressure to obtain apixaban nano suspension. The measured particle size of the nanosuspension is 754nm, and the polydispersity index (PDI) is 0.378.

Example Embodiment

[0028] Example 2

[0029] Weigh 5mg PVPK30 in 50ml water, add 20mg apixaban under stirring, and ultrasonically treat for 10min to fully disperse the drug in the water; shear with a high-speed disperser at 10000rpm for 5min to obtain a crude suspension; The suspension was homogenized at high pressure, firstly at 800 bar for 2 times, and then at 1800 bar for 12 times to obtain apixaban nano suspension. The measured particle size of the nanosuspension was 386.7 nm, and the polydispersity index (PDI) was 0.167.

Example Embodiment

[0030] Example 3

[0031] Weigh 1mg sodium taurocholate into 35ml water, add 20mg apixaban under stirring, and ultrasonically treat for 10min to fully disperse the drug in the water; shear with a high-speed disperser at 10000rpm for 5min to obtain a crude suspension; The above crude suspension was homogenized under high pressure, firstly at 800 bar for 2 times, and then at 1800 bar for 12 times to obtain apixaban nano-suspension. The particle size of the nanosuspension was measured to be 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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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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