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Sub-microemulsion used for intravenous injection of polyene yew alcohol phospholipid composite and preparation method thereof

A technology of docetaxel phospholipid and paclitaxel phospholipid, which is applied in the field of medicine to achieve the effects of good stability, good physiological compatibility, and reduced dosage of excipients

Inactive Publication Date: 2009-12-16
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] In summary, there is no clinically available, non-irritating, stable, high-loaded docetaxel preparation

Method used

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  • Sub-microemulsion used for intravenous injection of polyene yew alcohol phospholipid composite and preparation method thereof
  • Sub-microemulsion used for intravenous injection of polyene yew alcohol phospholipid composite and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Docetaxel 100mg

[0044] Soy Lecithin for Injection 1.2g

[0045] Absolute ethanol 5mL

[0046] Soybean oil for injection 5.0g

[0047] Add water for injection to 100mL

[0048] method:

[0049] 1. Dissolve docetaxel and phospholipids in absolute ethanol, stir at room temperature for 2 hours to compound, and prepare the docetaxel-phospholipid complex.

[0050] 2. Preparation of the oil phase: After compounding, add soybean oil for injection, stir and mix evenly, evaporate the organic solvent under reduced pressure to dry up, use it as the oil phase, and heat it to 70°C to keep it warm for later use.

[0051] 3. Preparation of the water phase: Take an appropriate amount of water for injection and heat it to 70°C as the water phase.

[0052] 4. Drop the water phase into the oil phase at a constant temperature of 70°C, stir at a high speed to form colostrum, then adjust the pH value to 4-9, set the volume to 100mL, and then pass the colostrum through a high-pressure h...

Embodiment 2

[0054] Docetaxel 500mg

[0055] Hydrogenated Phospholipids 1.5g

[0056] Diethyl ether 10mL

[0057] V E 0.1g

[0058] MCT 10.0g

[0059] Sodium Cholesterol Sulfate 1g

[0060] Tween 80 0.1g

[0061] Glycerol 2.25g

[0062] Add water for injection to 100mL

[0063] Wherein, the compounding time is 1 h, and other steps are the same as in Example 1, and the docetaxel-phospholipid complex submicroemulsion of the present invention is obtained.

Embodiment 3

[0065] Docetaxel 1.0g

[0066] Soy Lecithin 3.0g

[0067] Dichloromethane 10mL

[0068] Cholesterol 0.3g

[0069] Soybean oil for injection 20.0g

[0070] Poloxamer 188 1g

[0071] Glycerol 2.25g

[0072] Add water for injection to 100mL

[0073] The other steps are the same as in Example 1 to obtain the multiline paclitaxel-phospholipid complex submicroemulsion of the present invention.

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Abstract

The invention belongs to the technical field of medicine and discloses a preparation method of sub-microemulsion used for the intravenous injection of polyene yew alcohol phospholipid composite. The sub-microemulsion of the polyene yew alcohol phospholipid composite is basically prepared from polyene yew alcohol, phospholipid, liquid oil, a surfactant, cholesterol, a cholesterol derivative, or / and a similar cholesterol derivative, an addition agent and water for injection according to the effective therapeutic dose. The sub-microemulsion of the polyene yew alcohol phospholipid composite provided by the invention has high medicine carrying quantity and good preparation stability; and the preparation method is simple, convenient and easy and is easy for realizing industrialization.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a submicron emulsion preparation for injection of a drug phospholipid complex, specifically a docetaxel phospholipid complex submicroemulsion preparation and a preparation method thereof. Background technique [0002] Docetaxel (docetaxel) is a new generation of taxane antineoplastic drugs developed in recent years. This product is a semi-synthetic paclitaxel derivative developed by Aventis, which belongs to the microtubule depolymerization inhibitor. It acts on the microtubule / tubulin system by promoting the assembly of microtubule dimers into microtubules, and by preventing The multimerization process stabilizes microtubules, induces G2 and M phase arrest and apoptosis in cancer cells, and inhibits the growth of tumor tissues. Docetaxel has strong anti-tumor activity against a variety of solid tumors, and has obvious curative effects on breast cancer, non-small cell lung cancer...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/337A61K31/661A61K47/48A61K47/28A61K47/34A61P35/00A61K47/10A61K47/54
Inventor 王东凯和素娜李翔
Owner SHENYANG PHARMA UNIVERSITY
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