A kind of rosiglitazone nano-preparation and its preparation method and application

A nano-preparation, rosiglitazone technology, applied in the direction of anti-inflammatory agents, pharmaceutical formulations, non-central analgesics, etc., can solve the problems of low absorption and utilization, inability to use, and short duration of biological effects, and achieve improvement Targeting, reducing toxic and side effects

Inactive Publication Date: 2021-04-02
THE FIRST AFFILIATED HOSPITAL OF ARMY MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, studies have found that the traditional oral preparations of rosiglitazone have many disadvantages, such as low absorption and availability, low blood drug concentration in vascular stenosis, and short duration of biological effects.
At the same time, due to the systemic effects of rosiglitazone oral preparations, it has side effects on other target organs, such as liver function damage, edema, anemia, etc. Therefore, patients with abnormal liver function and congestive heart failure cannot use this drug

Method used

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  • A kind of rosiglitazone nano-preparation and its preparation method and application
  • A kind of rosiglitazone nano-preparation and its preparation method and application
  • A kind of rosiglitazone nano-preparation and its preparation method and application

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preparation example Construction

[0025] A preparation method of rosiglitazone nano-preparation, its preparation steps are as follows:

[0026] (1) dissolving rosiglitazone and polylactic acid-polyglycolic acid in an organic solvent;

[0027] (2) ultrasonically disperse lecithin and distearoylphosphatidylethanolamine-polyethylene glycol 2000 with an organic solvent, then add water to continue ultrasonically disperse, and heat at 65 degrees Celsius for 30 minutes, then cool to room temperature;

[0028] (3) Add the solution obtained in (1) dropwise to the solution in (2), stir rapidly for 3 minutes after the dropwise addition, and then continue to stir slowly at room temperature for 1.5 to 2 hours to obtain a nano-preparation suspension of rosiglitazone;

[0029] (4) centrifuging the nano-preparation suspension described in (3), washing with deionized water three times to obtain solidified rosiglitazone nano-preparation.

[0030] Calculated by mass percentage, rosiglitazone is 5.3-6.25%, polylactic acid-polygl...

Embodiment 1

[0039] Weigh 3 mg of rosiglitazone and dissolve 30 mg of polylactic acid-polyglycolic acid in 1 ml of acetonitrile to obtain solution 1. Weigh 6 mg of lecithin and 9 mg of distearoylphosphatidylethanolamine-polyethylene glycol 2000, add them into 0.6 ml of ethanol and ultrasonically dissolve them for 3 minutes with an ultrasonic instrument. Then add 15ml of water and continue ultrasonic dissolution for 3.5 minutes. Then put it in a water bath at 65°C for 30 minutes, take it out and put it at room temperature to obtain solution 2. Add solution 1 dropwise to solution 2. After the dropwise addition, stir rapidly for 3 minutes, and then stir slowly for 1.5 hours with a magnetic stirrer. After the stirring is completed, a nano-preparation suspension of rosiglitazone is obtained. The rosiglitazone nanometer direct suspension was centrifuged at 10000 revolutions with a centrifuge, and the supernatant was discarded. Measure 45ml of deionized water, wash the precipitate three times, ...

Embodiment 2

[0041]Weigh 3 mg of rosiglitazone and dissolve 33 mg of polylactic acid-polyglycolic acid in 1.2 ml of dimethyl sulfoxide to obtain solution 1. Weigh 5 mg of lecithin and 10 mg of distearoylphosphatidylethanolamine-polyethylene glycol 2000, add them into 0.8 ml of ethanol aqueous solution, and perform ultrasonic dissolution for 3.5 minutes by an ultrasonic instrument. Then add 20ml of water and continue ultrasonic dissolution for 3 minutes. Then put it in a water bath at 65°C for 30 minutes, take it out and put it at room temperature to obtain solution 2. Add solution 1 dropwise to solution 2. After the dropwise addition, stir rapidly for 3 minutes, and then stir slowly for 2 hours with a magnetic stirrer. After the stirring is completed, a nano-preparation suspension of rosiglitazone is obtained. The rosiglitazone nanometer direct suspension was centrifuged at 10000 revolutions with a centrifuge, and the supernatant was discarded. Measure 30ml of deionized water, wash the p...

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Abstract

The invention discloses an application of a rosiglitazone nano preparation in treating vascular restenosis. A rosiglitazone composition contains rosiglitazone, a polylactic acid-polyglycolic acid copolymer, lecithin and distearyl phosphatidyl ethanolamine-polyethylene glycol 2000. A rosiglitazone nano preparation is nano particles formed by rosiglitazone, polylactic acid-polyglycolic acid copolymer, lecithin and distearyl phosphatidyl ethanolamine-polyethylene glycol 2000, the structure is of a spherical structure, and the particle size is between 250 nm and 300 nm. The invention also discloses a preparation method of the rosiglitazone nano preparation, and the rosiglitazone nano preparation can effectively treat vascular restenosis after implanting of an intravascular stent, and can reduce the toxicity of rosiglitazone and improve the biological safety.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to a rosiglitazone nano-preparation and its preparation method and application. Background technique [0002] Cardiovascular and cerebrovascular diseases are currently one of the leading causes of death. Among them, vascular stenosis or occlusion is the main cause of stroke. Currently, endovascular therapy and angioplasty are one of the effective means of treating narrowed or occluded blood vessels, which can rapidly improve blood supply to the brain. However, vascular restenosis or thrombus may occur after the implantation of the vascular stent, and the traditional treatment plan is to re-implant the vascular stent at the place of restenosis. The "sandwich cake" treatment of this stent-in-stent will undoubtedly lead to the reduction of the area of ​​the vascular lumen, the occurrence of restenosis, and the formation of late thrombus. Although the use of drug-eluting stents has reduced th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/51A61K47/24A61K47/10A61K31/4439A61P9/10A61P29/00
CPCA61K9/5015A61K9/5031A61K9/5073A61K31/4439A61P9/10A61P29/00
Inventor 胡俊陈康宁吴虹辰张志辉刘涵汤怡然
Owner THE FIRST AFFILIATED HOSPITAL OF ARMY MEDICAL UNIV
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