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Ginsenoside paclitaxel liposome as well as preparation method and application thereof

A technology of ginsenosides and paclitaxel, which is applied in the directions of liposome delivery, pharmaceutical formulations, medical preparations of inactive ingredients, etc., can solve the problems of not giving the relationship between pharmacokinetics and toxicology, and achieve good drug synergy, The effect of improving drug efficacy and tumor suppressing effect

Pending Publication Date: 2022-05-06
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 paclitaxel liposome as well as preparation method and application thereof
  • Ginsenoside paclitaxel liposome as well as preparation method and application thereof
  • Ginsenoside paclitaxel liposome as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0122] The preparation of embodiment 1 injection compound ginsenoside Rg3 paclitaxel liposome

[0123] 1. Prescription: egg yolk lecithin 10g, ginsenoside Rg3 1g, paclitaxel 1g, glucose 25g, absolute ethanol 40ml, chloroform 40ml, water for injection 200ml.

[0124] 2. Film formation: prepare the prescribed amount of mixed solvent of absolute ethanol and chloroform (1:1) for later use.

[0125] Add the prescribed amount of paclitaxel into the mixed solvent to dissolve for later use, then add the prescribed amount of ginsenoside Rg3 and egg yolk lecithin into the mixed solvent, heat to dissolve, transfer to a 1L rotary evaporator, concentrate under reduced pressure, water bath temperature 55 ° C, speed 50 Rotation / min, vacuum degree -0.089~-0.1MPa, rotary evaporation until the solvent is completely evaporated.

[0126] 3. Hydration: Prepare glucose solution: Add 25g of anhydrous glucose to 100ml of water for injection, stir and dissolve to prepare a 0.25mg / ml glucose aqueous s...

Embodiment 2

[0136] The preparation of embodiment 2 injection compound ginsenoside Rg3 paclitaxel liposome

[0137] The prescription quantity of the ginsenoside Rg3 among the embodiment 1 is increased to 1.5g, other is the same as embodiment 1, prepares compound ginsenoside Rg3 paclitaxel liposome for injection (prescription 2).

Embodiment 3

[0138] The preparation of embodiment 3 injection compound ginsenoside Rg3 paclitaxel liposome

[0139] 1. Prescription: egg yolk lecithin 10g, ginsenoside Rg3 2g, paclitaxel 1g, glucose 25g, absolute ethanol 40ml, chloroform 40ml, water for injection 200ml.

[0140] 2. Film formation: the same as the film formation method in Example 1.

[0141] 3. Hydration: the same as the hydration method in Example 1.

[0142] 4. High-speed shearing and extrusion: the above-mentioned liposome solution was sheared rapidly at 2000rp / min for 5min at room temperature.

[0143] The temperature of the liposome solution is controlled at 35-45° C., an extrusion device is connected, a 150 nm aperture extrusion plate is installed, and extrusion is performed under a pressure of 800 psi.

[0144] 5. Subsequent steps were the same as those in Example 1 to prepare compound ginsenoside Rg3 paclitaxel liposomes for injection (prescription 3).

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Abstract

The invention discloses a compound ginsenoside paclitaxel liposome as well as a preparation method and application thereof. The invention provides a compound ginsenoside paclitaxel liposome. The compound ginsenoside paclitaxel liposome is prepared from the following components in parts by mass: 8-12 parts of phospholipid, 1-1.5 parts of ginsenoside, 1 part of paclitaxel and 25-35 parts of a freeze-drying protective agent. The ginsenoside paclitaxel liposome disclosed by the invention has better active targeting property mediated by Glut1 (Glut1); the efficacy of the ginsenoside paclitaxel liposome is improved by more than two times compared with the conventional ginsenoside paclitaxel liposome; the toxicity is reduced by more than 1.5 times compared with that of the conventional ginsenoside paclitaxel lipidosome and is reduced by more than 4 times compared with that of the conventional cholesterol paclitaxel lipidosome; and the risk of toxicity accumulation in vivo does not exist.

Description

technical field [0001] The invention relates to a compound ginsenoside paclitaxel liposome, its preparation method and application; further discloses a compound ginsenoside paclitaxel liposome for injection with high efficiency and low toxicity, its preparation method and application. Background technique [0002] Liposome is a targeted drug delivery system, which belongs to a special dosage form of the targeted drug delivery system. It can embed drugs in particles with a diameter of nanometers, which are similar to bimolecular layers in the structure of biological membranes. Microvesicles enter the human body and are mainly swallowed 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 lowering the dose of the drug. toxicity. [0003] The present invention is a technol...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/337A61K31/704A61K47/24A61K47/26A61P35/00
CPCA61K31/704A61K31/337A61K9/127A61K9/1277A61K9/0019A61K47/24A61K47/26A61P35/00A61K2300/00
Inventor 王丹王建新缪鹏飞陈颖江詹华杏
Owner SHANGHAI GINSOME PHARMATECH CO LTD
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