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Oxaliplatin liposome and application thereof

An oxaliplatin and liposome technology, which is applied in the directions of liposome delivery, active ingredients of heavy metal compounds, and drug combinations, can solve problems such as difficult industrialized large-scale production, and achieve high encapsulation efficiency, small particle size, raw Inexpensive effect

Active Publication Date: 2013-07-03
HANGZHOU NORMAL UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In Chinese patent 200710025130.0, Chen Xiangfeng et al. adopted filter column separation and purification to improve encapsulation efficiency, but this method is difficult to be used in industrialized large-scale production

Method used

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  • Oxaliplatin liposome and application thereof
  • Oxaliplatin liposome and application thereof

Examples

Experimental program
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Embodiment 1

[0021] Embodiment 1 Oxaliplatin liposome

[0022] Dissolve 4 g of lecithin and 667 mg of cholesterol in 60 mL of dichloromethane, add 20 mL of an aqueous solution containing 80 mg of oxaliplatin, stir for 30 min, sonicate for 20 min, and remove the organic solvent by rotary evaporation at 40°C. After collapse, add 50 mL of aqueous solution containing 400 mg of F68 according to the components, continue to evaporate for 30 min, homogenize under high pressure at 300 bar for 4 min, and dilute to 100 mL with water, then use tangential flow ultrafiltration to separate free oxaliplatin. The tangential flow membrane bag with a molecular cut-off of 10K is used for ultrafiltration, and water is used as the replacement liquid, and the ultrafiltration is repeated 3 times. The encapsulation efficiency is measured by the ultrafiltration centrifuge tube method and the final drug concentration is determined by high performance liquid chromatography. The rate is 96.56%, and the particle size i...

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Abstract

The invention discloses an oxaliplatin liposome and an application thereof. Preparation raw materials of the oxaliplatin liposome comprise oxaliplatin, phospholipid, cholesterol and poloxamer F68; the mass ratio of phospholipid to cholesterol is (3 to 8):1; the mass ratio of oxaliplatin to phospholipid is 1:(30 to 60); and the mass ratio of poloxamer F68 to phospholipid is 1:(5 to 15). The oxaliplatin liposome obtained by the invention has a small particle size and high entrapment efficiency, adopts the cheap raw materials and a simpler process and is suitable for industrial mass production.

Description

(1) Technical field [0001] The invention relates to the field of drug liposomes, in particular to an oxaliplatin liposome and an application thereof. (2) Background technology [0002] Oxaliplatin is a third-generation platinum-based anticancer drug. In 2004, the FDA approved oxaliplatin for injection in combination with 5-fluorouracil and folinic acid for the first-line treatment of advanced colorectal cancer. Oxaliplatin preparations currently on the market include water injection and freeze-dried powder injection. Oxaliplatin has a significant effect on advanced colorectal cancer, and can also treat other gastrointestinal tumors such as gastric cancer. However, with the extensive clinical application of oxaliplatin, its adverse reactions have been continuously discovered and reported. Neurotoxicity, gastrointestinal reactions, and bone marrow suppression are common adverse reactions. [0003] Liposome is a drug delivery system with good biocompatibility. As a delivery...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/282A61P35/00
Inventor 曾昭武肖人钟谢恬王小丽王俊洁周广林刘星言
Owner HANGZHOU NORMAL UNIVERSITY
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