Romidepsin fat microsphere preparation and preparing method thereof

A technology of romidepsin and lipid microspheres, which is applied in the directions of emulsion delivery, freeze-drying delivery, tetrapeptide components, etc., can solve problems such as no reports of romidepsin lipid microsphere preparations, and achieve improved drug safety, Effect of improving compliance and improving targeting

Active Publication Date: 2016-11-23
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] According to the search, there is no relevant repo

Method used

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  • Romidepsin fat microsphere preparation and preparing method thereof
  • Romidepsin fat microsphere preparation and preparing method thereof
  • Romidepsin fat microsphere preparation and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] (1) Weigh 1.0g romidepsin, 5.0g soybean oil, 5.0g medium-chain fatty acid triglycerides, 1.5g soybean lecithin, 0.4g propylene glycol and 0.05g ethanol in a beaker, and use a high-speed shearing machine Shear at high speed for 3 minutes, heat and stir in a magnetic stirring water bath at 60°C at a stirring speed of 500rpm to completely dissolve and obtain an oil phase;

[0051] (2) Weigh 0.9g of sodium chloride and place it in a beaker, add 86.2g of water for injection, heat and stir in a magnetic stirring water bath at 60°C, and stir at a stirring speed of 500rpm to completely dissolve it to obtain an aqueous phase;

[0052] (3) under high-speed stirring, the oil phase and the water phase are mixed, and the pH value is adjusted to 7.0 to obtain colostrum;

[0053] (4) transfer the colostrum to a high-pressure homogenizer, and use 500bar pressure for high-pressure homogenization to obtain a submicron emulsion;

[0054] (5) Nitrogen-filled sub-package, after autoclaving...

Embodiment 2

[0056] (1) Weigh 1.5g romidepsin, 6.5g soybean oil, 10.5g medium-chain fatty acid triglycerides, 2.0g egg yolk lecithin, 0.8g propylene glycol and 0.2g ethanol in a beaker, and use a high-speed shearing machine Shear at high speed for 5 minutes, heat and stir in a magnetic stirring water bath at 65°C at a stirring speed of 500rpm to completely dissolve it to obtain an oil phase;

[0057] (2) Weigh 0.9g of sodium chloride and put it in a beaker, add 77.4g of water for injection, heat and stir in a magnetic stirring water bath at 65°C, and stir at a speed of 400rpm, so that it is completely dissolved to obtain an aqueous phase;

[0058] (3) under high-speed stirring, the oil phase and the water phase are mixed, and the pH value is adjusted to 7.2 to obtain colostrum;

[0059] (4) transfer the colostrum to a high-pressure homogenizer, and use 350bar pressure for high-pressure homogenization to obtain a submicron emulsion;

[0060] (5) Nitrogen-filled sub-package, after autoclavi...

Embodiment 3

[0062] (1) Weigh 2.5g romidepsin, 4.5g safflower oil, 15.5g medium-chain fatty acid triglycerides, 2.0g hydrogenated egg yolk lecithin, and 1.0g propylene glycol in a beaker, and use a high-speed shearing machine to perform high-speed shearing. Cut for 8 minutes, heat and stir at 45°C in a magnetic stirring water bath at a stirring speed of 700rpm to completely dissolve and obtain an oil phase;

[0063] (2) Weigh 4.5g of mannitol and place it in a beaker, add 70g of water for injection, heat and stir at 45°C in a magnetic stirring water bath at a stirring speed of 700rpm, and dissolve it completely to obtain an aqueous phase;

[0064] (3) under high-speed stirring, the oil phase and the water phase are mixed, and the pH value is adjusted to 6.7 to obtain colostrum;

[0065] (4) transfer the colostrum to a high-pressure homogenizer, and use 650bar pressure for high-pressure homogenization to obtain a submicron emulsion;

[0066] (5) Nitrogen-filled sub-package, after autoclavi...

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Abstract

The invention relates to a romidepsin fat microsphere preparation and a preparing method thereof. The romidepsin fat microsphere preparation is prepared from romidepsin, oil for injection, an emulsifying agent, a stabilizing agent, an isoosmotic adjusting agent, a pH modifier and water for injection. The romidepsin fat microsphere preparation has high stability and a good slow-release feature, the targeting ability of romidepsin is improved, and the toxic and side effects of romidepsin are reduced.

Description

technical field [0001] The application relates to the field of pharmaceutical preparations, in particular to a romidepsin lipid microsphere preparation and a preparation method thereof. Background technique [0002] Romidepsin, the English name is Romidepsin, its chemical name is (1S,4S,7Z,10S,16E,21R)-7-ethylidene-4,21-diisopropyl-2-oxa-12, 13-dithio-5,8,20,23-tetraazabicyclo[8,7,6]tricos-16-ene-3,6,9,19,22-pentone, molecular formula C 24 h 36 N 4 o 6 S 2 , is a bicyclic tetrapeptide with a stable hydrophobic structure, and the unique disulfide bond in its structure is the key group for its activity. Romidepsin is a histone deacetylase (HDACs) inhibitor, which was approved by the US FDA as an orphan drug on November 5, 2009. The second HDACs inhibitor approved for marketing in the United States after he (vorinostat) is mainly used for progressive, persistent and recurrent cutaneous T-cell lymphoma who have received at least one other type of systemic therapy at the sa...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/107A61K38/07A61P35/00
Inventor 颜携国陶安进袁建成
Owner HYBIO PHARMA
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