Hydroxycamptothecine lipid nanobundle preparations and preparation methods thereof

A technology of hydroxycamptothecin and lauryl hydroxystearate, which is applied in the field of 10-hydroxycamptothecin nano lipid beam preparation and its preparation, to achieve the effects of simple preparation process, long cycle effect and increasing patient compliance

Active Publication Date: 2014-05-14
THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, how to make the target drug, ie, hydroxycamptothecin, solubilizer, and reagents for surface PEGylation and targeting, into microemulsions has encountered great difficulties in practice.

Method used

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  • Hydroxycamptothecine lipid nanobundle preparations and preparation methods thereof
  • Hydroxycamptothecine lipid nanobundle preparations and preparation methods thereof
  • Hydroxycamptothecine lipid nanobundle preparations and preparation methods thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0050] 1. Preparation of Hydroxycamptothecin Nano Lipid Beam Oil Agent

[0051] 1. Weigh 0.8g of phospholipid (Germany Lipoid Company) and 0.8g of propylene glycol and dissolve to obtain solution A.

[0052] 2. Weigh 0.025g hydroxycamptothecin, 3.0g ethanol, 3.8g Solutol HS15 (Germany BASF company), 0.038g folic acid-PEGDSPE, 2.6g glycerol, dissolve at room temperature to obtain solution B.

[0053] 3. Mix solution A and solution B, stir and mix at room temperature to obtain a clear and transparent hydroxycamptothecin nano-lipid beam oil, which is protected by nitrogen and sealed for storage.

[0054] 2. Preparation of Hydroxycamptothecin Nano Lipid Beam Injection

[0055] Dilute the hydroxycamptothecin nano-lipid beam oil preparation prepared in step 1 with 20 times the volume of physiological saline to obtain a hydroxycamptothecin nano-injection.

[0056] 3. Determination of Microemulsion Particle Size of Hydroxycamptothecin Nano Lipid Beam Injection

[0057] The microemu...

preparation example 2

[0060] 1. Preparation of Hydroxycamptothecin Nano Lipid Beam Oil Agent

[0061] 1. Weigh 0.9g of phospholipid (Germany Lipoid Company) and 3.0g of ethanol, dissolve to obtain solution A.

[0062] 2. Weigh 0.02g of hydroxycamptothecin, 0.9g of propylene glycol, 3.6g of Solutol HS15 (German BASF company), 50mg of cholic acid-PEGDSPE, and 1.6g of glycerin, and dissolve to obtain solution B.

[0063] 3. Mix solution A and solution B, stir and mix at room temperature to obtain a clear and transparent hydroxycamptothecin nano-lipid beam oil, which is protected by nitrogen and sealed for storage.

[0064] 2. Preparation of Hydroxycamptothecin Nano Lipid Beam Injection

[0065] Dilute the hydroxycamptothecin nano-lipid beam oil prepared in step 1 with 20 times the volume of physiological saline to obtain a hydroxycamptothecin nano-lipid beam injection, which is in the form of an emulsion.

[0066] 3. Determination of Microemulsion Particle Size of Hydroxycamptothecin Nanoinjection ...

preparation example 3

[0069] 1. Preparation of Hydroxycamptothecin Nano Lipid Beam Oil Agent

[0070] 1. Weigh 1.0g of phospholipid (Germany Lipoid Company) and 1.0g of propylene glycol and dissolve to obtain solution A.

[0071] 2. Weigh 0.025g hydroxycamptothecin, 3.6g ethanol, 3.8g Solutol HS15 (Germany BASF company), 60mg sialic acid-PEGDSPE, 1.6g glycerol, dissolve at room temperature to obtain solution B.

[0072] 3. Mix solution A and solution B, stir and mix at room temperature to obtain a clear and transparent hydroxycamptothecin nano-lipid beam oil, which is protected by nitrogen and sealed for storage.

[0073] 2. Preparation of Hydroxycamptothecin Nano Lipid Beam Injection

[0074] Dilute the hydroxycamptothecin nano-lipid beam oil prepared in step 1 with 20 times the volume of physiological saline to obtain a hydroxycamptothecin nano-lipid beam injection, which is in the form of an emulsion.

[0075] 3. Determination of Microemulsion Particle Size of Hydroxycamptothecin Nano Lipid Be...

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Abstract

The invention relates to hydroxycamptothecine lipid nanobundle oil and a hydroxycamptothecine lipid nanobundle injection which have an active targeting function, and preparation methods thereof. The hydroxycamptothecine lipid nanobundle oil comprises phospholipid, polyethylene glycol-12-hydroxystearate, glycerol, propylene glycol, ethanol and hydroxycamptothecine and X-PEG-DSPE (polyethylene glycol-distearoyl phosphatidyl ethanolamine), wherein the X-PEG-DSPE is selected from folic acid-PEG-DSPE, cholic acid-PEG-DSPE, CRGDK-PEG-DSPE, sialic acid-PEG-DSPE and oligose-PEG-DSPE. The hydroxycamptothecine lipid nanobundle oil is dissolved in water for injection to obtain the hydroxycamptothecine lipid nanobundle injection which is uniform in particle size, can reduce the toxicity of hydroxycamptothecine, has long-circulation effect and can enhance tumor targeting enrichment and improve patient compliance. The hydroxycamptothecine lipid nanobundle oil and hydroxycamptothecine lipid nanobundle injection are simple in preparation methods and can meet different needs of clinical applications.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical nano-lipid bundle preparations, in particular to a 10-hydroxycamptothecin nano-lipid bundle preparation with active targeting function and a preparation method thereof. Background technique [0002] As a cytotoxic alkaloid, camptothecin (CPT) was isolated from the plant Camptotheca in the 1950s. Combined with topoisomerase 1-DNA complex, it can inhibit the religation step in the process of DNA supercoil structure relaxation, leading to the apoptosis of tumor cells with high topoisomerase expression. Initial studies found that not only the side effects of hemorrhagic cystitis and bone marrow toxicity hindered the further application of camptothecin, but also its low water solubility greatly hindered its clinical application. [0003] Reducing toxicity, increasing solubility and improving efficacy are the directions for the development of camptothecin drugs. Through the structural modificat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/34A61K31/4745A61K9/08A61P35/00
Inventor 梁兴杰赵元元陈飞马晓溦李盛亮薛向东柳娟金叔斌李鸿基张吉梅王义峰甘雅玲姜永刚
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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