A kind of liposome preparation of topinastat and preparation method thereof

A technology of liposome preparation and topinostat, which is applied in the field of medicine, can solve problems such as inconvenient administration and limitations of clinical application, and achieve the effects of stable quality, increased route of administration, and simple preparation process

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 liposome preparation of topinastat and preparation method thereof
  • A kind of liposome preparation of topinastat and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Take by weighing 90g lecithin, 20g cholesterol and 2g topicastat, add 15mL dichloromethane and make it dissolve completely, evaporate dichloromethane with rotary evaporator, make to form one deck liposome film on the inner wall of round-bottomed flask, residual Put dichloromethane in a desiccator with the lid off to evaporate completely; add 30mL of phosphate buffer solution with pH=7.4 to the flask, and hydrate at 30°C for 2 hours to form an emulsion; use a probe-type ultrasonic instrument to perform ultrasonic treatment for 15 minutes to obtain Liposomes of topinostat. The encapsulation efficiency of topicastat in the liposome was 78.3±3.6%, and the particle size was 549±26nm.

Embodiment 2

[0031] Weigh 50g of distearoylphosphatidylcholine, 45g of cholesterol and 2g of topicastat, dissolve them in 10mL of ether, and slowly inject the resulting solution into the phosphate buffer solution heated to 40°C and stirred by magnetic force through a syringe. The pH of the buffer solution is 6.8, and the obtained suspension is continuously stirred until the ether is removed, and the topirastat liposome is obtained. The encapsulation efficiency of topicastat in the liposome was 84.9±5.1%, and the particle size was 472±34nm.

Embodiment 3

[0033] Weigh 30g of dipalmitoylphosphatidylcholine, 50g of cholesterol and 2g of topicastat, dissolve them in 12mL of ether, and slowly inject the resulting solution into a phosphate buffer heated to 35°C and magnetically stirred through a syringe. The pH of the solution was 7.4, and the resulting suspension was homogenized 3 times by high pressure, and the ether was removed to obtain the topirastat liposome. The encapsulation efficiency of the topicastat in the liposome is 88.0±4.7%, and the particle size is 194±22nm.

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Abstract

The invention relates to the technical field of medicine and particularly relates to a preparation of topiroxostat liposome and a preparation method thereof. The preparation of topiroxostat liposome comprises, by weight, 1 to 3 parts of topiroxostat, 30 to 90 parts of phospholipid and 10 to 50 parts of cholesterol. The preparation of topiroxostat liposome can be processed into a freeze-dried powder injection. The freeze-dried powder injection comprises, by weight, 1 to 3 parts of topiroxostat, 30 to 90 parts of phospholipid, 10 to 50 parts of cholesterol, 5 to 20 parts of a lyoprotectant and 0 to 10 parts of a redissolution aid. The preparation of topiroxostat liposome has high encapsulation efficiency, uniform particle sizes and stable quality. The preparation method has simple processes, increases the administration path of topiroxostat and improves patient compliance. The topiroxostat liposome prolongs the action time of topiroxostat and produces unexpected technical effects.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a liposome preparation of topinastat 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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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/19A61K31/444A61P19/06
CPCA61K9/0019A61K9/127A61K9/19A61K31/444A61K47/10A61K47/26
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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