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Vinorelbine long circulation liposome preparation and preparation method thereof

A technology of liposome preparations and vinorelbine, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve problems such as affecting curative effect, poor targeting, and increased toxicity, and achieve drug Toxicity and irritation are reduced, the possibility is reduced, and the effect of easy operation

Inactive Publication Date: 2011-01-05
QILU PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Ordinary liposomes are quickly swallowed by the reticuloendothelial system after entering the body, and the main targets are in organs with rich reticuloendothelial systems such as liver, spleen, and bone marrow, and the targeting of other parts is poor
Moreover, it is susceptible to leakage in the body due to the action of proteins, enzymes, etc., which affects the curative effect and increases toxicity.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Embodiment 1. Encapsulation efficiency of vinorelbine liposomes of different drug loading methods

[0060] The liposome membrane materials for encapsulating vinorelbine bitartrate are: hydrogenated soybean phospholipids, cholesterol and mPEG 2000 - DSPE in a mass ratio of 1:0.2:0.1. The method for measuring the encapsulation efficiency adopts micro-column centrifugation: Soak Sephadex G-50 in distilled water overnight, and fully swell. Put it in a 2.5ml syringe, wait for the water to flow down naturally, the height of the gel part is about 1.5 cm, centrifuge at 2000rpm for 4 minutes to remove the water, and the height of the gel column is about 1 cm. Get two parts of prepared vinorelbine bitartrate liposomes, each 0.1ml, one part is in a 10ml volumetric flask, add 0.5ml 10% Triton X-100 and heat at 60 degrees Celsius for 10 seconds, after cooling, the emulsion is broken. Dilute to the mark with water for injection, mix well, and measure the peak area A1 by HPLC. Take...

Embodiment 2

[0073] Example 2. pH Gradient Method Preparation of Vinorelbine Bitartrate Encapsulation Factors Influencing Factors

[0074] Unless otherwise specified, the following factors were investigated under the condition that the drug-to-lipid mass ratio was 1:10 and the drug was loaded at 60°C for 10 minutes. Drug lipid mass ratio is an abbreviation, which means the mass ratio of vinorelbine bitartrate drug to phospholipid, the same below.

[0075] 1. The influence of the pH regulator of the external aqueous phase on the encapsulation efficiency

[0076] The pH of the aqueous phase outside the liposome was adjusted to 7.0 by using different lyes, and the results of measuring the encapsulation efficiency are shown in Table 1.

[0077] Table 1 Effect of external aqueous phase pH regulator on encapsulation efficiency

[0078]

Na 3 PO 4 the solution

Na 2 HPO 4 the solution

NaOH solution

Na 2 CO 3 the solution

NaHCO 3 the solution

Encap...

Embodiment 3

[0095] Embodiment 3.Ethanol influences on encapsulation efficiency of vinorelbine liposome

[0096] After the liposome membrane material was stirred and dissolved in 5%, 10.0%, and 20.0% of the total volume of ethanol in a water bath at 65°C, citrate buffer (300mmol L -1 , pH4.0), hydration, prepare blank liposomes, and homogenizer treatment, reduce the particle size, pass through 0.22 μm microporous membrane to sterilize, and get blank liposomes. The particle size was measured, the drug was loaded according to the pH gradient in "Example 1", and the encapsulation efficiency was measured. The results are shown in Table 6.

[0097] Table 6 Effect of ethanol on encapsulation efficiency of vinorelbine liposome

[0098] Ethanol content (v / v)

[0099] The results showed that there was no significant difference in vinorelbine liposome particle size and encapsulation efficiency when 5.0%-10.0% ethanol remained in the blank liposome. When the residual amount of ethanol rea...

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PUM

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Abstract

The invention relates to a Vinorelbine long circulation liposome preparation and a preparation method thereof, the preparation comprises three sub-packaging units, i.e. an empty liposome, sodium phosphate buffer solution and heavy tartaric acid Vinorelbine; and before being used, the three sub-packaging units are mixed together and heated appropriately. The preparation method has the advantages of simple process and easy operation and is suitable for industrial production, and the Vinorelbine long circulation liposome which is prepared by adopting the method has high encapsulation rate and good stability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and specifically relates to a liposome preparation of vinorelbine, a water-soluble antitumor drug that has a long-term circulation effect in the body and can escape capture by the reticuloendothelial system, and a preparation method thereof. Background technique [0002] Vinorelbine, also known as norvinblastine, is a semi-synthetic tartrate that belongs to the alkaloids of the genus Vinca. It was discovered and synthesized by French scholar Poter in 1924, and was approved by the US FDA in December 1994 for the first-line treatment of non-small cell lung cancer (NSCLC). Vinorelbine is a drug that inhibits microtubule polymerization. It binds microtubules, inhibits microtubule polymerization, induces microtubule depolymerization, and hinders the synthesis of microtubules in tumor cells during mitosis, stopping them in the middle of mitosis. effect. At the same time, it has less inhibit...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/475A61K47/34A61P35/00A61K47/24A61K47/28
Inventor 李伯涛王晶翼杨清敏王栋海杨光丽张明会
Owner QILU PHARMA CO LTD
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