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Camptothecin medical lipidosome composition and preparation method thereof

A technology of liposome composition and camptothecin, applied in drug combination, liposome delivery, pharmaceutical formulation, etc., can solve problems such as difficult to reach tumor sites, achieve good clinical value, stabilize physiological pH, and reduce toxic and side effects Effect

Active Publication Date: 2013-03-13
SHENZHEN NEPTUNUS PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, another problem worth noting is that we must ensure that the drug in the liposome can be stably encapsulated in the liposome and will not leak the drug before reaching the tumor site
Studies have shown that the hydroxycarboxylates of camptothecin drugs after ring opening have a very strong binding ability to plasma proteins, leading to burst release of camptothecin drug liposomes [《Influence of serum and albumins from different species on stability of camptothecin-loaded micelles" ("Journal of Controlled Release, Volume 104, Issue 2, 18May2005, Pages 313321") and "Research on Preparation and Quality Evaluation of Hydroxycamptothecin Liposomes" ("Pharmaceutical and Clinical Research" 2008 No. 4 4 Pages 274-277)], the drug is quickly cleared, and it is often difficult to reach the tumor site to exert its drug effect

Method used

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  • Camptothecin medical lipidosome composition and preparation method thereof
  • Camptothecin medical lipidosome composition and preparation method thereof
  • Camptothecin medical lipidosome composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Embodiment 1, adopt double emulsification method to prepare camptothecin class drug liposome composition

[0038] Prepare camptothecin class drug liposome composition, adopt double emulsification method, comprise the following steps:

[0039] (1) 56g of soybean lecithin, 8g of cholesterol and 2.8g of vitamin E are co-dissolved in an appropriate amount of dichloromethane solvent as the organic phase;

[0040] (2) Add 5 g of 10-hydroxycamptothecin to 25 mL of saturated meglumine solution, stir at 50°C until clear, and cool to room temperature as the water phase;

[0041] (3) Mix the solutions of step (1) and step (2) according to the volume ratio of the organic phase and the aqueous phase at 2:1, and stir at 8000 rpm for 1 minute at high speed to prepare W / O colostrum;

[0042] (4) Quickly pour W / O colostrum into 450ml water for injection for secondary emulsification, and stir at 5000 rpm for 10 minutes;

[0043] (5) On a rotary evaporator, remove the organic solvent by...

Embodiment 2

[0047] Embodiment 2, adopt double emulsification method to prepare camptothecin class drug liposome composition

[0048] Prepare camptothecin class drug liposome composition, adopt double emulsification method, comprise the following steps:

[0049] (1) 72g of hydrogenated soybean lecithin, 33g of cholesterol and 1.0g of vitamin E are co-dissolved in an appropriate amount of dichloromethane solvent as the organic phase;

[0050] (2) Add 9.0 g of 10-hydroxycamptothecin to 50 mL of saturated meglumine aqueous solution, stir at 50°C until clear, and cool to room temperature as the water phase;

[0051] (3) Mix the solutions of step (1) and step (2) according to the volume ratio of the organic phase and the aqueous phase at 10:1, and stir at a high speed of 14000 rpm for 1 minute to prepare W / O colostrum;

[0052] (4) Quickly pour W / O colostrum into 4L water for injection for secondary emulsification, and stir at 5000 rpm for 30 minutes;

[0053] (5) On a rotary evaporator, remo...

Embodiment 3

[0057] Embodiment 3, adopt double emulsification method to prepare camptothecin drug liposome composition

[0058] Prepare camptothecin class drug liposome composition, adopt double emulsification method, comprise the following steps:

[0059] (1) 48g egg yolk lecithin, 15g cholesterol and 2.5g vitamin E are co-dissolved in an appropriate amount of dichloromethane solvent as the organic phase;

[0060] (2) Add 5 g of irinotecan to 20 mL of saturated meglumine aqueous solution, stir at 50°C until clear, and cool to room temperature as the water phase;

[0061] (3) Mix the solutions of step (1) and step (2) according to the volume ratio of the organic phase and the aqueous phase at 5:1, and stir at 8000 rpm for 1 minute at high speed to prepare W / O colostrum;

[0062] (4) Quickly pour W / O colostrum into 450mL water for injection for secondary emulsification, and stir at 5000 rpm for 10 minutes;

[0063] (5) On a rotary evaporator, remove the organic solvent by evaporating unde...

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Abstract

The invention provides a camptothecin medical lipidosome composition. The camptothecin medical lipidosome composition is prepared from the following raw materials and supplementary materials in parts by weight: 5 to 25 parts of camptothecin medicine, 40 to 100 parts of phospholipid, 6 to 50 parts of cholesterol, 1 to 8 parts of vitamin E, and 10 to 100 parts of amino compound. According to a preparation method of the camptothecin medical lipidosome composition, the camptothecin medical lipidosome composition is prepared in a multi-emulsion way and an inverted evaporation way. The aqueous solution of the amino compound has a solubilizing effect respect to the camptothecin medicine, and can generate a water-soluble compound under the effect of intermolecular interaction or ionic bond effect. The compound is stable in physiological pH (Potential of Hydrogen) and higher in solution concentration, and can be wrapped in the inner cavity of lipidosome, therefore, the amount of the medicine in transfer can be increased, and the problem that the lactonic-ring type camptothecin medicine is subjected to high ring opening to result in leakage due to the influence of the pH and the plasma proteins can be avoided. The compound is stably wrapped in the lipidosome, and can reach the tumor part under the targeting effect of the lipidosome and then act in form of lactonic ring under the acidic condition of the tumor cells; and the compound has the advantages of increasing effect and reducing toxicity.

Description

technical field [0001] The invention relates to the field of camptothecin drugs, in particular to a camptothecin drug liposome composition and a manufacturing method thereof. Background technique [0002] Camptothecin is an alkaloid extracted from Camptotheca involucrata, a plant unique to my country. Camptothecin and its derivatives can selectively inhibit topoisomerase I from interfering with DNA replication and transcription, thereby achieving the effect of killing cells. The advantages of camptothecin drugs are broad anti-cancer spectrum, no cross-resistance, and are effective against various malignant tumors such as primary liver cancer, gastric cancer, head and neck skin cancer, chronic myelogenous leukemia, rectal cancer and bladder cancer. Based on the above characteristics, camptothecin drugs are regarded as plant anticancer drugs with significant influence worldwide after paclitaxel. [0003] From the perspective of molecular structure, the parent structure of cam...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/4745A61K47/48A61P35/00
Inventor 杨经安王志国崔婧李宁王丽丽
Owner SHENZHEN NEPTUNUS PHARMA RES INST CO LTD
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