Paclitaxel liposome and preparation method thereof

A paclitaxel and liposome technology, applied in the field of medicine, can solve problems such as side effects, water insolubility of paclitaxel, and achieve the effects of reducing toxic and side effects, enhancing anti-tumor effect, and long duration of action

Inactive Publication Date: 2012-02-22
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The purpose of the present invention is to solve the water insolubility and side effects of paclitaxel and prepare thermosensitive liposomes, long-circulation liposomes and thermosensitive long-circulation liposomes

Method used

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  • Paclitaxel liposome and preparation method thereof
  • Paclitaxel liposome and preparation method thereof
  • Paclitaxel liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] prescription:

[0029] Paclitaxel 0.4g

[0030] Soybean Lecithin for Injection 20.0g

[0031] Cholesterol 2.4g

[0032] Excipient D 5.0g

[0033] Octylamine 0.1g

[0034] Vitamin E 0.2g

[0035] Buffered saline to 200mL

[0036] Preparation Process:

[0037]Dissolve the prescribed amount of paclitaxel, soy lecithin for injection, cholesterol, excipient D, and vitamin E in an organic solvent and pour it into a pear-shaped bottle, then add a small amount of buffered salt solution containing stearylamine, ultrasonically make it into a uniform milk, and use a rotary evaporator. The organic solvent was removed under reduced pressure to form a gel, and the mixture was vortexed and distilled under reduced pressure at intervals to obtain a white homogeneous liposome solution, which was then adjusted to 200 mL with a buffer solution. Then, the pyrogen is removed by granulation through a pressurized membrane (0.22 μm), and then it is divided into vials for freeze-drying to...

Embodiment 2

[0039] prescription:

[0040] Paclitaxel 0.4g

[0041] Soybean Lecithin for Injection 20.0g

[0042] Cholesterol 2.4g

[0043] Excipient D 5.0g

[0044] Octylamine 0.1g

[0045] Vitamin E 0.2g

[0046] Buffered saline to 200mL

[0047] Preparation Process:

[0048] Dissolve the prescribed amount of paclitaxel, soy lecithin for injection, cholesterol, excipient D, and vitamin E in an organic solvent and pour it into a pear-shaped bottle, then add a small amount of buffered salt solution containing stearylamine, ultrasonically make it into a uniform milk, and use a rotary evaporator. The organic solvent was removed under reduced pressure to form a gel, and the mixture was vortexed and distilled under reduced pressure at intervals to obtain a white homogeneous liposome solution, which was then adjusted to 200 mL with a buffer solution. Then, the pyrogen is removed by granulation through a pressurized membrane (0.22 μm), and the pellets are divided into ampoules for freezin...

Embodiment 3

[0050] prescription:

[0051] Paclitaxel 0.4g

[0052] Soybean Lecithin for Injection 20.0g

[0053] Cholesterol 2.4g

[0054] Excipient D 5.0g

[0055] Sucrose 5.0g

[0056] Mannitol 0.1g

[0057] Octylamine 0.1g

[0058] Vitamin E 0.2g

[0059] Buffered saline to 200mL

[0060] Preparation Process:

[0061] Dissolve the prescribed amount of paclitaxel, bean lecithin for injection, cholesterol, excipient D, and vitamin E in an organic solvent and pour it into a pear-shaped bottle, spin and evaporate the organic solvent to dryness in a water bath at 30 rpm and 60 °C, and make it in a glass bottle. A dry film was formed on the wall, and the prescribed amount of sucrose and mannitol were dissolved in 200 mL of buffered saline solution, poured into a pear-shaped bottle, and rotated at 40 rpm at room temperature (25 °C) for hydration until the surface of the bottle was dry. The membrane was completely eluted and the resulting crude suspension was hydrated at room temperat...

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Abstract

The invention belongs to the technical field of medicine and discloses paclitaxel liposomes and a preparation method thereof, mainly including long-circulation liposomes, paclitaxel thermosensitive liposomes and paclitaxel thermosensitive long-circulation liposomes. Its composition is 1%-30% paclitaxel, 1%-95% phospholipid, 0%-30% cholesterol, 0%-50% heat-sensitive excipient D, 0%-50% excipient G, 0-80% lyoprotectant, 0-10% octadecylamine, 0.001-50% antioxidant, appropriate amount of buffer salt. These are three new paclitaxel liposome preparations, which solve the problem of paclitaxel’s water insolubility. The long circulation of long-circulation liposomes and the thermosensitivity of thermosensitive liposomes can prolong the circulation time of paclitaxel in the body, improve the targeting of tumors, and thus enhance its anti-tumor effect.

Description

technical field [0001] The invention belongs to the technical field of medicine, relates to thermosensitive liposomes, long-circulating liposomes and thermosensitive long-circulating liposome preparations of antitumor drug paclitaxel, and also relates to a preparation method of these liposomes. Background technique [0002] Paclitaxel is a monomeric compound with definite and strong anti-cancer effect discovered by humans in the late 20th century. It is known as a milestone in the human race to conquer cancer, especially in the treatment of breast cancer, ovarian cancer, non-small cell lung cancer and other malignant tumors. Oncology has become the drug of choice. [0003] At present, the paclitaxel injection in clinical application includes domestic paclitaxel , Taxol , imported Taxol (American BMS company), Anzatax (Australia Fauliding Company) and other products, these products all use the surfactant solubilization method to solve the shortcoming of paclitaxel bei...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/337A61P35/00
Inventor 邓英杰王浩
Owner SHENYANG PHARMA UNIVERSITY
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