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Lipid microsphere injection of taxane derivative tm-2 and preparation method thereof

A technology of lipid microspheres and derivatives, applied in the field of medicine, can solve the problems of increasing drug encapsulation rate, prolonging drug half-life, poor water solubility of TM-2, physical and chemical stability, etc., to achieve increased physical and chemical stability, protection Drug activity, effect of reducing local and vascular irritation

Inactive Publication Date: 2017-07-14
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0008] The invention provides a lipid microsphere injection of a taxane derivative TM-2 and a preparation method thereof, the purpose of which is to solve the poor water solubility of TM-2 and the physical and chemical stability issues, increase the encapsulation rate of the drug, prolong the half-life of the drug, and prepare a long-term stable TM-2 lipid microsphere injection that can withstand autoclaving

Method used

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  • Lipid microsphere injection of taxane derivative tm-2 and preparation method thereof
  • Lipid microsphere injection of taxane derivative tm-2 and preparation method thereof
  • Lipid microsphere injection of taxane derivative tm-2 and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Preparation of TM-2 lipid microsphere injection; specification: 0.01mg / ml

[0033]

[0034] Preparation:

[0035] (1) Weigh the prescription amount of glycerin, poloxamer 188 and polyethylene glycol-polyaspartic acid copolymer, add appropriate amount of water for injection, heat and stir in a magnetic stirrer at 30-80°C to disperse evenly to obtain a water phase .

[0036] (2) Weigh the prescription amount of medium-chain triglyceride (MCT), egg yolk lecithin, oleic acid, cholesterol and TM-2, stir and disperse evenly at 30-80° C. to obtain a clear drug-containing oil phase.

[0037] (3) Add the drug-loaded oil phase into the water phase under stirring by a high-speed tissue grinder, and stir at 8000 rpm for 3-5 minutes.

[0038] (4) Cool the colostrum to room temperature, dilute to full volume with water for injection, adjust the pH value to 4.0-9.0 with sodium hydroxide or hydrochloric acid solution, transfer to a high-pressure homogenizer, and control the homoge...

Embodiment 2

[0041] Preparation of TM-2 lipid microsphere injection, specification: 10mg / ml

[0042]

[0043] Preparation:

[0044] (1) Weigh the prescription amount of glycerin, poloxamer 188 and polyethylene glycol-polyaspartic acid copolymer, add appropriate amount of water for injection, heat and stir in a magnetic stirrer at 30-80°C to disperse evenly to obtain a water phase .

[0045] (2) Weigh soybean oil, medium-chain triglyceride (MCT), egg yolk lecithin, oleic acid, cholesterol and TM-2 at 30-80° C. and stir to disperse evenly to obtain a clear medicated oil phase.

[0046] (3) Add the drug-loaded oil phase into the water phase under stirring by a high-speed tissue grinder, and stir at 10,000 rpm for 3-5 minutes.

[0047] (4) Cool the colostrum to room temperature, dilute to full volume with water for injection, adjust the pH value to 4.0-9.0 with sodium hydroxide or hydrochloric acid solution, transfer to a high-pressure homogenizer, and control the homogenization temperatu...

Embodiment 3

[0050] Preparation of TM-2 Lipid Microsphere Injection Specification: 2mg / ml

[0051]

[0052] Preparation:

[0053] (1) Weigh the prescription amount of glycerin, poloxamer 188 and polyethylene glycol-polyaspartic acid copolymer, add appropriate amount of water for injection, heat and stir in a magnetic stirrer at 30-80°C to disperse evenly to obtain a water phase .

[0054] (2) Weigh soybean oil, medium-chain triglyceride (MCT), egg yolk lecithin, oleic acid, cholesterol and TM-2 at 30-80° C. and stir to disperse evenly to obtain a clear medicated oil phase.

[0055] (3) Add the drug-loaded oil phase into the water phase under stirring by a high-speed tissue grinder, and stir at 10,000 rpm for 3-5 minutes.

[0056] (4) Cool the colostrum to room temperature, dilute to full volume with water for injection, adjust the pH value to 4.0-9.0 with sodium hydroxide or hydrochloric acid solution, transfer to a high-pressure homogenizer, and control the homogenization temperature...

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Abstract

A lipid microsphere injection of taxane derivative TM-2 and preparation method thereof belong to the technical field of medicines. The lipid microsphere injection includes following components: the TM-2, oil for injection, an emulsifier, cholesterol, a polyethylene glycol-polyaspartic acid co-polymer, an auxiliary emulsifier, a stabilizing agent, an isoosmotic adjusting agent and water for injection. The preparation method comprises following steps: (1) uniformly mixing the TM-2 with an oil-soluble medium and dispersing the mixture in a water phase; (2) performing high-speed stirring to prepare a primary emulsion; and (3) performing high-pressure homogenization to obtain a preparation and then sterilizing the preparation through a high-pressure rotational sterilizing method. Compared with a reference preparation taxane lipid microsphere injection, The TM-2 lipid microsphere injection shows a better antitumor activity. The TM-2 lipid microsphere injection not only is better than the reference preparation taxane lipid microsphere injection in effectives, but also is good in stability. The TM-2 lipid microsphere injection reduces toxicity of the TM-2 and is enhanced in curative effects. Meanwhile, the TM-2 lipid microsphere injection is tolerant of high-temperature pressurized sterilization and is suitable for industrialized production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a taxane derivative TM-2 lipid microsphere injection and a preparation method thereof. Background technique [0002] Cancer is a chronic disease that seriously endangers human health, and countless people die from cancer all over the world every year. Overcoming the difficulty of cancer has become an urgent task for medical workers and chemical workers. Therefore, finding effective anticancer drugs has become a research hotspot. The research and development of anti-cancer drugs is a worldwide topic, especially the screening of new anti-cancer drugs from natural products has become a hot spot in the research and development of anti-cancer drugs. [0003] Taxol (Paclitaxe, Taxol TAX) was first extracted and isolated from the bark of Pacific short-leaved yew (Taxus drvifolia) by American scientists Wall and Wani in 1971, and later reported by Schiff and Horwitz, profe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/337A61K47/34A61K47/24A61K47/28A61P35/00
Inventor 唐星王艳娇张岩何海冰
Owner SHENYANG PHARMA UNIVERSITY
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