Vinorelbine Bitartrate lipsome freeze-drying powder injection and its preparation method

A vinorelbine bitartrate and liposome technology, which is applied in liposome delivery, freeze-drying delivery, powder delivery, etc., can solve the problems of high toxicity and side effects, clinical application limitations, etc., and achieve good stability and stable drug loading Quantity, improve the effect of curative effect

Inactive Publication Date: 2008-12-03
ZHEJIANG UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after intravenous injection of the drug, the side effects are relatively large, and the common ones are bone marrow suppression, gastrointestinal toxicity, and hair loss. In addition, long-term use will cause weakness of the lower limbs
These toxic side effects make the clinical application of vinorelbine very limited

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052]Weigh 600mg of soybean phospholipids (purity>76% phosphatidylcholine) and 100mg of cholesterol, dissolve them in ether, mix well, place the solution in a ground round bottom flask, and use a rotary evaporator on a constant temperature water bath at 30-32℃ The organic solvent was evaporated under reduced pressure at 100 rpm, so that the membrane-forming materials such as phospholipids formed a uniform lipid film at the bottom of the flask; 30ml ether was added to the above lipid film to dissolve, and 10mg vinorelbine was added to 5ml (2- 10ml) PH7.4 phosphate buffer, then add it to the above lipid membrane solution, and use a rotary evaporator at 32°C to remove the organic solvent until the lipid membrane is hydrated and becomes a milky white liposome suspension. Ice-bath lattice ultrasound (ultrasonic cell crusher) reduces the particle size. Vitamin E 0.3 mg and 300 mg mannitol were dissolved in liposomes, and after aseptic filtration (membrane filter pore size 0.2 μm), the ...

Embodiment 2

[0055] Weigh 600mg lecithin (purity>93% phosphatidylcholine) and 100mg cholesterol and dissolve in 30ml ether; then dissolve vinorelbine in 10ml pH7.4 buffer, mix the above two liquids for emulsification, and then Use a rotary evaporator to remove the organic solvent at ℃ until the mixture becomes a milky white liposome suspension. Ice bath lattice ultrasound (ultrasonic cell pulverizer) reduces the particle size. Vitamin E 0.3 mg and 300 mg mannitol were dissolved in liposomes, and after aseptic filtration (membrane filter pore size 0.2 μm), the final dispersion was divided into vials, and then freeze-dried.

[0056] The vinorelbine liposome preparation of the present invention is a freeze-dried product for injection, and the product quality is stable. The stability test is carried out at 25±2°C. The results show that the product is stable at 25±2°C, and all indicators are in quality Within the range specified by the standard; the low-temperature retention sample is investigated ...

Embodiment 3

[0058] Weigh 5 mg of vinorelbine bitartrate, 300 mg of soy phospholipids (purity> 76% phosphatidylcholine) and 30 mg of cholesterol, dissolved in ether, and mix well. Place the solution in a ground round-bottom flask at 30-32°C. On a constant temperature water bath, use a rotary evaporator at 100 rpm and under reduced pressure to evaporate the organic solvent, so that the phospholipid and other film-forming materials form a uniform lipid film at the bottom of the flask; add 30 ml of ether to the above lipid film to dissolve, and add 5 ml ( 2-10ml) PH7.4 phosphate buffer solution, ultrasonic emulsion in a water bath, remove the organic solvent with a rotary evaporator at 30°C, until it becomes a milky white liposome suspension, and then the high pressure emulsion uniformly reduces the particle size. Vitamin E 0.3 mg and 500 mg mannitol were dissolved in liposomes, and after aseptic filtration (membrane filter pore size 0.2 μm), the final dispersion was divided into vials, and then ...

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Abstract

The invention relates to an antineoplastic vinorelbine bitartrate liposome, its freeze-dried powder injection and preparing process, wherein the preparation comprises liposome of vinorelbine bitartrate and pharmaceutically acceptable carrying agent, the liposome of vinorelbine bitartrate contains the following constituents: vinorelbine bitartrate, phosphatide, cholesterin and vitamin E, their weight ratio being 1 : 1-100 : 1-15 : 0.01-0.05.

Description

Technical field: [0001] The invention relates to a liposome preparation of an antitumor drug vinorelbine bitartrate. Background technique: [0002] Vinorelbine Bitartrate (common name Vinorelbine Bitartrate), is a semi-synthetic vinca alkaloid, its mechanism of action is basically the same as that of vinblastine (VLB) and vincristine (VCR), mainly through blocking The formation of microtubules in the process of cell mitosis, which stops cell division in the middle of mitosis, is a cell cycle specific drug. Like other vinblastines, vinorelbine can also inhibit the circulation of amino acids and the metabolism of glutathione; it depends on the Ca of calmodulin 甘 -ATPase activity; cell biological oxidation and nucleic acid and oil biosynthesis. It is mainly used clinically for non-small cell lung cancer, metastatic breast cancer, advanced ovarian cancer, malignant lymphoma, etc. However, after intravenous injection of the drug, the toxic and side effects are relatively large, such a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K9/127A61K31/475A61P35/00
Inventor 金一沈圆圆杨雯姝陈长潭王安行
Owner ZHEJIANG UNIV
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