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Ginsenoside docetaxel liposome as well as preparation method and application thereof

A technology of ginsenoside and docetaxel, which is applied in the directions of liposome delivery, pharmaceutical formulations, and medical preparations of inactive ingredients, etc., can solve the problems of not giving the relationship between pharmacokinetics and toxicology, and achieve good medicines. Synergistic effect, reduced side effects, improved Glut1 targeting

Pending Publication Date: 2022-07-08
SHANGHAI GINSOME PHARMATECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the prior art does not provide any derivation relationship between the above-mentioned components and ratio and process and pharmacological activity, pharmacokinetics and toxicology for this optimum ratio

Method used

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  • Ginsenoside docetaxel liposome as well as preparation method and application thereof
  • Ginsenoside docetaxel liposome as well as preparation method and application thereof
  • Ginsenoside docetaxel liposome as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0150] Example 1 Preparation of compound ginsenoside Rg3 docetaxel liposome for injection

[0151] 1. Prescription: egg yolk lecithin 10g, ginsenoside Rg3 1g, docetaxel 1g, glucose 25g, absolute ethanol 40ml, chloroform 40ml, water for injection 200ml.

[0152] 2. Film formation: prepare a mixed solvent of absolute ethanol and chloroform (1:1) in the prescribed amount for use.

[0153] Add the prescription amount of docetaxel to the mixed solvent to dissolve for later use, then add the prescription amount of ginsenoside Rg3 and egg yolk lecithin into the mixed solvent, heat to dissolve, transfer into a 1L rotary steamer, concentrate under reduced pressure, and the water bath temperature is 55 ° C , rotating speed 50 rev / min, vacuum degree -0.089~-0.1MPa, rotary steam until all the solvent is completely volatilized.

[0154] 3. Hydration: Preparation of glucose solution: Add 25g of anhydrous glucose to 100ml of water for injection, stir and dissolve, and then prepare a 0.25mg / ...

Embodiment 2

[0164] Example 2 Preparation of Compound Ginsenoside Rg3 Docetaxel Liposomes for Injection

[0165] The prescription amount of the ginsenoside Rg3 in Example 1 was increased to 1.5 g, and the others were the same as in Example 1, and the compound ginsenoside Rg3 docetaxel liposome for injection was prepared.

Embodiment 3

[0166] Example 3 Preparation of Compound Ginsenoside Rg3 Docetaxel Liposomes for Injection

[0167] 1. Prescription: egg yolk lecithin 10g, ginsenoside Rg3 1.5g, docetaxel 1g, glucose 25g, absolute ethanol 40ml, chloroform 40ml, water for injection 200ml.

[0168] 2. Film formation: the same as the film formation method of Example 1.

[0169] 3. Hydration: the same as the hydration method of Example 1.

[0170] 4. High-speed shearing and extrusion: the above-mentioned liposome solution was rapidly sheared at 2000 rp / min for 5 min at room temperature.

[0171] The temperature of the liposome solution was controlled at 35-45 °C, an extrusion device was connected, an extrusion plate with a 150 nm aperture was installed, and the extrusion was performed under a pressure of 800 psi.

[0172] 5. Subsequent steps are the same as those in Example 1.

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Abstract

The invention discloses a compound ginsenoside docetaxel liposome as well as a preparation method and application thereof. The invention provides a compound ginsenoside docetaxel liposome. The compound ginsenoside docetaxel liposome is prepared from the following components in parts by mass: 8-18 parts of phospholipid, 1-1.5 parts of ginsenoside, 1 part of docetaxel and 20-35 parts of a freeze-drying protective agent, the ginsenoside docetaxel plastid does not contain one or more of cholesterol, soybean oil and sodium oleate. The ginsenoside docetaxel liposome disclosed by the invention has better active targeting property of Glut1 (Glut1); the drug effect of the ginsenoside docetaxel liposome is improved by more than two times compared with that of the conventional ginsenoside docetaxel liposome; the toxicity of the liposome is reduced by more than 1.5 times compared with that of the conventional ginsenoside docetaxel liposome and is reduced by more than 4-6 times compared with that of the conventional cholesterol docetaxel liposome; the in-vivo toxicity accumulation risk is low.

Description

technical field [0001] The invention relates to a compound ginsenoside docetaxel liposome, a preparation method and application thereof; further discloses a compound ginsenoside docetaxel liposome with high efficiency and low toxicity for injection, its preparation method and application. Background technique [0002] Liposome is a kind of directional drug delivery system, which belongs to a special dosage form of targeted drug delivery system. It can encapsulate drugs in nanometer-sized particles, which are similar to bilayers in biological membrane structures. Microvesicles enter the human body and are mainly phagocytosed by the reticuloendothelial system, and change the distribution of the encapsulated drug in the body, so that the drug is mainly accumulated in the target tissue, thereby improving the therapeutic index of the drug, reducing the therapeutic dose of the drug and reducing the drug toxicity. [0003] The present invention is a technical innovation based on C...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K47/24A61K47/26A61K31/704A61K31/7048A61K31/337A61P35/00
CPCA61K9/1277A61K47/24A61K47/26A61K31/704A61K31/7048A61K31/337A61P35/00A61K2300/00
Inventor 王建新王丹陈颖江詹华杏
Owner SHANGHAI GINSOME PHARMATECH CO LTD
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