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A kind of topicastat microsphere preparation and preparation method thereof

A technology of topinostat and preparations, which is applied in the field of topinostat microsphere preparations and its preparation, can solve problems such as inconvenient administration and limitations in clinical application, achieve stable quality, increase drug delivery routes, and improve compliance Effect

Active Publication Date: 2021-02-26
CP PHARMA QINGDAO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the preparations developed above are all oral preparations, and their clinical application has limitations.
Especially for patients with dysphagia, the above-mentioned oral preparations are extremely inconvenient to take

Method used

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  • A kind of topicastat microsphere preparation and preparation method thereof
  • A kind of topicastat microsphere preparation and preparation method thereof
  • A kind of topicastat microsphere preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0023]Weigh 10g of topipristat and dissolve it in 20mL of dichloromethane as the dispersed phase; weigh 40g of polylactic acid hydroxylactic acid and 3g of Span 80 and dissolve them in 100mL of ethanol aqueous solution as the continuous phase, and slowly add the dispersed phase dropwise to the organic phase Emulsify the emulsion at 30°C and 2000r / min for 20 minutes under stirring conditions. Pour the resulting emulsion into 400ml of acetone to solidify, wash the sediment with acetone until there are no oil droplets; prepare a 5% mannitol solution and add 100mL to the sediment In the medium, stir evenly and freeze-dry in vacuum. The vacuum freeze-drying process includes pre-freezing at -40°C for 2 hours, slowly raising the temperature to -5°C and vacuum drying for 10 hours, slowly raising the temperature to 10°C and vacuum drying for 8 hours, and continuing to raise the temperature to 30°C for 1 hour. The encapsulation rate of topipristat in the microspheres is 88.2±4.1%, and the par...

Embodiment 2

[0025]Weigh 20g of Topipristat and dissolve it in 20mL of chloroform as the dispersed phase; Weigh 80g of chitosan and 2g of sodium lauryl sulfate, dissolve into 200mL of ethanol aqueous solution as the continuous phase, slowly add the dispersed phase to the organic In the phase, ultrasonic emulsification for 30 minutes to form an oil-in-water emulsion; the organic solvent is removed by rotary evaporation at 40°C, 100 mL of 3% glucose solution is added, and the product is obtained by vacuum freeze drying. The vacuum freeze-drying process includes pre-freezing at -30°C for 4 hours, slowly raising the temperature to 3°C for 12 hours, slowly raising the temperature to 15°C for 6 hours, and continuing to raise the temperature to 32°C for 2 hours. The encapsulation rate of topistat in the microspheres is 92.5±3.7%, and the particle size is 0.54±0.04μm.

Embodiment 3

[0027]Weigh 15 g of topicastat and dissolve it in 20 mL of dichloromethane; weigh 100 g of polylactic acid and dissolve it in 200 mL of ethanol aqueous solution, mix the two solutions and spray-dry to prepare the topicinostat microsphere preparation. The spray drying conditions are: the atomization pressure is 15MPa, the material liquid temperature is 50°C, the hot air temperature in the spray drying tower is 110°C, and the feed pump speed is 5r / min. The encapsulation rate of topistat in the microspheres is 80.8±2.9%, and the particle size is 0.96±0.07μm.

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Abstract

The invention relates to the technical field of medicine, in particular to a topicastat microsphere preparation and a preparation method thereof. The technical solution adopted by the present invention is a topinostat microsphere preparation, which is characterized in that it contains the following components by weight: 10-20 parts of topinostat, 30-100 parts of polymer carrier, 0-100 parts of emulsifier 5 parts, 0‑10 parts of freeze-dried proppant. The topicastat microspheres prepared by the present invention have high encapsulation efficiency, uniform particle size, stable quality, simple preparation process, increase the route of administration of topicastat, and improve patient compliance; His long-term release effect has unexpected technical effects.

Description

Technical field[0001]The invention relates to the technical field of medicine, in particular to a topipristat microsphere preparation and a preparation method thereof.Background technique[0002]Gout and hyperuricemia are caused by too much uric acid synthesis or too little uric acid excretion in the body, leading to excessive blood uric acid levels in the body. Urate crystals are deposited in the joints and kidneys, which in turn induces metabolic diseases that trigger a series of inflammatory reactions. The disease seriously threatens human health and is the second largest metabolic disease after diabetes. Reducing blood uric acid levels through drugs is an effective way to prevent and treat gout and hyperuricemia. Commonly used clinical drugs include xanthine oxidase (XO) inhibitors allopurinol and febuxostat And topiroxostat (topiroxostat), and uric acid excretion enhancers probenecid and benzbromarone.[0003]Topipristat is a selective xanthine oxidoreductase inhibitor without puri...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/444A61K9/50A61K47/34A61K47/36A61K9/127A61P19/06
CPCA61K9/0002A61K9/127A61K9/5031A61K9/5036A61K31/444
Inventor 陈阳生王明刚刘晓霞孙桂玉臧云龙
Owner CP PHARMA QINGDAO CO LTD
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