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Apixaban oral solid preparation and method for preparing same

A solid preparation, apixaban technology, applied in the field of medicine, can solve problems such as being difficult to have versatility and reproducibility

Active Publication Date: 2019-05-24
NANJING CAVENDISH BIO ENG TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although mannitol is an excipient with good water solubility, to solve the dissolution problem of insoluble compounds, due to different production batches of raw materials, there may be some differences in the initial physical state (such as particle size, bulk density, crystal habit, etc.) , the method is difficult to generalize and reproducible

Method used

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  • Apixaban oral solid preparation and method for preparing same
  • Apixaban oral solid preparation and method for preparing same
  • Apixaban oral solid preparation and method for preparing same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0064] Apixaban Tablets

[0065] Components and content:

[0066]

[0067]

[0068] 1. Dissolve hypromellose in water (preparation concentration 2%) and stir to dissolve and clarify;

[0069] 2. Add apixaban under stirring conditions, and continue stirring for 5 minutes after adding to obtain a coarse suspension;

[0070] 3. Put the crude suspension in an ultrasonic instrument and sonicate for 30 minutes to obtain a suspension of apixaban and hypromellose.

[0071] 4. The prepared suspension is sprayed onto the fluidized bed chamber carrier auxiliary materials (microcrystalline cellulose, cross-linked sodium carboxymethyl cellulose) by using fluidized bed technology, and the fan frequency of the fluidized bed is set 5~20Hz, air inlet temperature 40~75℃, material temperature control 30~70℃, atomization pressure 0.1~0.3MPa, the apixaban suspension of hypromellose solution is passed through the peristaltic pump under stirring Spray into the fluidized bed at a spray speed...

Embodiment 2

[0075] Apixaban Capsules

[0076] Components and content:

[0077]

[0078]

[0079] 1. Dissolve hypromellose in water (3% preparation concentration) and stir to dissolve and clarify;

[0080] 2. Add apixaban under stirring conditions, and continue stirring for 5 minutes after adding to obtain a coarse suspension;

[0081] 3. Put the crude suspension in an ultrasonic instrument and sonicate for 30 minutes to obtain a suspension of apixaban and hypromellose.

[0082] 4. The prepared suspension is sprayed onto the fluidized bed chamber carrier auxiliary materials (microcrystalline cellulose, cross-linked sodium carboxymethyl cellulose) by using fluidized bed technology, and the fan frequency of the fluidized bed is set 5~20Hz, air inlet temperature 40~75℃, material temperature control 30~70℃, atomization pressure 0.1~0.3MPa, the apixaban suspension of hypromellose solution is passed through the peristaltic pump under stirring Spray into the fluidized bed at a spray spee...

Embodiment 3

[0086] Apixaban Granules

[0087]

[0088] 1. Dissolve hypromellose in water (preparation concentration 4%) and stir to dissolve and clarify;

[0089] 2. Add apixaban under stirring conditions, continue to stir for 5 minutes after adding to obtain a coarse suspension, and cut the coarse suspension with a high-speed shear at 10,000 rpm for 20 minutes to obtain apixaban and hypromellose solution the suspension;

[0090]3. Using a fluidized bed, spray the prepared suspension onto the fluidized bed chamber carrier auxiliary materials (microcrystalline cellulose, cross-linked sodium carboxymethyl cellulose), and set the operating parameters of the fluidized bed spray As follows: set the fan frequency of the fluidized bed at 5-20Hz, the air inlet temperature at 40-75°C, the material temperature at 30-70°C, the atomization pressure at 0.1-0.3MPa, and mix the hypromellose solution with apixaban The suspension is sprayed into the fluidized bed through a peristaltic pump in the sti...

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Abstract

The invention discloses an apixaban oral solid preparation. The apixaban oral solid preparation comprises apixaban, hydroxypropyl methylcelluloses and vector excipients. The vector excipients are selected from a type or a plurality of types of fillers, disintegrating agents, lubricants and glidants. The apixaban oral solid preparation does not contain surfactants. A method for preparing the apixaban oral solid preparation includes preparing suspension from the apixaban and the hydroxypropyl methylcelluloses; carrying out wet granulation to obtain the apixaban oral solid preparation. The apixaban oral solid preparation and the method have the advantages that under the condition that micronization treatment is not carried out on apixaban crude medicines, the dissolution rates of dissolutionmedia with the pH (potential of hydrogen) of 1.0-6.8 are higher than 85% in 5 min and are higher than 90% in 10 min, and the dissolution media are completely dissolved out in 15 min.

Description

technical field [0001] The invention belongs to the technical field of medicine, and more specifically relates to an oral solid preparation of apixaban and a preparation method thereof. Background technique [0002] Apixaban is a new type of oral antithrombotic drug, which is a reversible inhibitor that directly binds to coagulation factor Xa. This drug has been approved for marketing in the European Union, the United States and other countries. Patients, prevention of venous thromboembolic events (VTE) and other indications. The chemical name of Apixaban 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, English name Apixaban, molecular formula C 25 h 25 N 5 o 4 , the molecular weight is 459.50, and its chemical structure is as follows: [0003] [0004] Apixaban is a white to light yellow crystalline powder, non-hygroscopic, soluble in dimethyl sulfoxide, slightly soluble in methanol and ace...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4545A61K9/10A61K47/38A61P7/02
Inventor 许永翔赵新慧
Owner NANJING CAVENDISH BIO ENG TECH
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