Irinotecan nano lipid binding preparation and preparation method thereof

A nano-lipid bundle preparation, the technology of irinotecan, is applied in the directions of pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc. Enhance tumor-targeted enrichment, long-term circulation, and uniform particle size distribution

Active Publication Date: 2014-04-23
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

There are many reasons: high-density lipoprotein in blood is the main component that destroys liposomes; because it can activate the complement system, liposomes are easy to be penetrated and cracked; phospholipase can degrade phospholipids; serum albumin can combine with phospholipids to form complexes, thereby Decreased stability of nanoassemblies composed of phospholipids

Method used

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  • Irinotecan nano lipid binding preparation and preparation method thereof
  • Irinotecan nano lipid binding preparation and preparation method thereof
  • Irinotecan nano lipid binding preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] 1. Preparation of precursor of irinotecan lipid bundle preparation

[0061] 1. Weigh 1.2g of phospholipid (Germany Lipoid Company) and 0.3g of ethanol, dissolve to obtain solution A.

[0062] 2. Weigh 0.5g irinotecan, 2.5g ethanol, 3.0g Solutol HS15 (German BASF company), 1.8g glycerol, dissolve at room temperature to obtain solution B.

[0063] 3. Mix solution A and solution B, stir and mix at room temperature to obtain a clear and transparent irinotecan lipid bundle preparation precursor, which is protected under nitrogen and sealed for storage. figure 2 Display: The precursor of irinotecan lipid bundle preparation is a clear and transparent liquid.

[0064] Two, the preparation of irinotecan lipid bundle preparation

[0065] Dilute the irinotecan lipid bundle preparation precursor prepared in step 1 with 20 times the volume of physiological saline to obtain irinotecan nano-preparation. image 3 The middle left test tube shows the irinotecan lipid beam formulation...

Embodiment 2

[0070]1. Preparation of precursor of irinotecan lipid bundle preparation

[0071] 1. Weigh 1.2g of phospholipid (Germany Lipoid Company) and 0.3g of ethanol, dissolve to obtain solution A.

[0072] 2. Weigh 0.2g irinotecan, 2.5g ethanol, 3.0g Solutol HS15 (German BASF company), 1.8g glycerol, dissolve at room temperature to obtain solution B.

[0073] 3. Mix solution A and solution B, stir and mix at room temperature to obtain a clear and transparent irinotecan lipid bundle preparation precursor, which is protected under nitrogen and sealed for storage. Similar results figure 2 , The precursor of irinotecan lipid bundle preparation is a clear and transparent liquid.

[0074] Two, the preparation of irinotecan lipid bundle preparation

[0075] Dilute the irinotecan lipid bundle preparation precursor prepared in step 1 with 20 times the volume of normal saline to obtain the irinotecan lipid bundle preparation. Similar results image 3 In the middle left test tube, the irin...

Embodiment 3

[0079] 1. Preparation of precursor of irinotecan lipid bundle preparation

[0080] 1. Weigh 1.2g of phospholipid (Germany Lipoid Company) and 0.3g of ethanol, dissolve to obtain solution A.

[0081] 2. Weigh 0.8g irinotecan, 2.5g ethanol, 3.0g Solutol HS15 (German BASF company), 1.8g glycerol, dissolve at room temperature to obtain solution B.

[0082] 3. Mix solution A and solution B, stir and mix at room temperature to obtain a clear and transparent irinotecan lipid bundle preparation precursor, which is protected under nitrogen and sealed for storage. Similar results figure 2 , The precursor of irinotecan lipid bundle preparation is a clear and transparent liquid.

[0083] Two, the preparation of irinotecan lipid bundle preparation

[0084] Dilute the irinotecan lipid bundle preparation precursor prepared in step 1 with 20 times the volume of normal saline to obtain the irinotecan lipid bundle preparation. Similar results image 3 In the middle left test tube, the iri...

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Abstract

The invention relates to an irinotecan nano lipid binding preparation and a preparation method thereof. The irinotecan nano lipid binding preparation contains phospholipid, polyethylene glycol-dodecahydroxycy stearate, glycerol, ethanol and irinotecan, as well as an aqueous solvent for injection. The irinotecan nano lipid binding preparation is even in grain size, and as the lipid binding preparation, capable of reducing the toxicity of the irinotecan with long circulation effect and enhancing the tumor targeted enrichment effect and improving the compliance of a patient, and the preparation method is simple in process, high in repeatability and applicable to industrial production.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical nano-lipid bundle preparations, in particular to an irinotecan nano-lipid bundle preparation and a preparation method thereof. Background technique [0002] Irinotecan (CPT-11), which was approved by the FDA in 1998 for the standard chemotherapy regimen to treat the recurrence and exacerbation of metastatic colorectal cancer, is the re-approval of the US FDA after pentafluorouracil (5-FU) for more than 40 years Chemotherapy drugs for the first-line treatment of metastatic colorectal cancer. It is a derivative of camptothecin, which selectively binds and inhibits topoisomerase I, and covalently binds with the Topo-DNA complex to form a stable Topo-drug-DNA complex, thereby inhibiting the DNA reconnection step, so that the DNA strand cleavage, leading to apoptosis. It has a higher curative effect on small cell lung cancer, small cell lung cancer, cervical cancer, ovarian cancer and colorect...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/34A61K47/24A61K31/4745A61P35/00
CPCA61K9/1075A61K31/4745A61K47/24A61P35/00
Inventor 梁兴杰赵元元柳娟李盛亮薛向东陈飞金叔宾张吉梅李鸿基甘雅玲姜永刚
Owner THE NAT CENT FOR NANOSCI & TECH NCNST OF CHINA
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