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Topiroxostat microspherical preparation and preparation method thereof

A technology of topicastat and microspheres, applied in the field of topicastat microsphere preparations and their preparation, can solve the problems of limited clinical application, inconvenient taking, etc., and achieves increased route of administration, stable quality, and improved compliance. sexual effect

Active Publication Date: 2017-12-08
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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  • Topiroxostat microspherical preparation and preparation method thereof
  • Topiroxostat microspherical preparation and preparation method thereof
  • Topiroxostat microspherical preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0023] Weigh 10g of topinostat, dissolve in 20mL of dichloromethane as the dispersed phase; weigh 40g of polylactic acid hydroxylactic acid and 3g of Span 80, dissolve in 100mL of ethanol aqueous solution as the continuous phase, slowly drop the dispersed phase into the organic phase Emulsify at 30°C and 2000r / min for 20min, pour the obtained emulsion into 400ml of acetone to solidify, wash the sediment with acetone until there is no oil drop; prepare 5% mannitol solution, take 100mL and add it to the sediment , stir evenly, and vacuum freeze-dry. The vacuum freeze-drying process is to pre-freeze at -40°C for 2 hours, slowly heat up to -5°C for 10 hours in vacuum, slowly heat up to 10°C for 8 hours in vacuum, and continue to heat up to 30°C for 1 hour in vacuum. The encapsulation rate of topicastat in the microspheres was 88.2±4.1%, and the particle size was 0.73±0.02 μm.

Embodiment 2

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

Embodiment 3

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

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Abstract

The invention relates to the technical field of medicines and in particular relates to a topiroxostat microspherical preparation and a preparation method thereof. According to the technical scheme, the topiroxostat microspherical preparation is characterized by comprising the following components in parts by weight: 10-20 parts of topiroxostat, 30-100 parts of a macromolecular carrier, 0-5 parts of an emulsifier and 0-10 parts of a topiroxostat supporting agent. The topiroxostat microspheres are high in encapsulation efficiency, uniform in grain size, stable in quality and simple in preparation process, and the administrating path of topiroxostat is increased, and the patient compliance is enhanced; and moreover, the topiroxostat microspherical preparation also has a long-acting releasing effect of topiroxostat and achieves an unexpected technical effect.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a topicastat microsphere preparation and a preparation method thereof. Background technique [0002] Gout and hyperuricemia are metabolic diseases caused by excessive synthesis of uric acid or insufficient excretion of uric acid in the body, resulting in excessive blood uric acid levels in the body. Urate crystals are deposited in the joints and kidneys, which induce 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 with drugs is an effective way to prevent and treat gout and hyperuricemia. Commonly used drugs include xanthine oxidase (XO) inhibitors allopurinol and febuxostat. and topiroxostat, and the urate excretion enhancers probenecid and benzbromarone. [0003] Topinastat is a selective xanthine oxidoreductase inhibitor without a purine structure. It...

Claims

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Application Information

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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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