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Polyene taxol liposome and its prepn process

A technology of docetaxel and liposomes, which is applied in the directions of liposome delivery, pharmaceutical formulations, and medical preparations containing active ingredients, etc. and other problems, to achieve the effect of prolonging blood circulation time, increasing compliance, and facilitating administration

Inactive Publication Date: 2007-03-21
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

5% of patients will have to stop using taxotere because of allergies, and 6.5% of patients will have allergic edema. There is a serious warning term for allergic shock side effects of this product; Tween-80 is highly viscous, which brings inconvenience to clinical medication; in addition, docetaxel itself has myelosuppression, leukopenia, thrombocytopenia and other toxicities, so , it is urgent to change the dosage form of docetaxel to increase the water solubility of docetaxel and avoid the allergic reaction caused by solvent Tween-80 and the toxic and side effects of docetaxel itself
Although significant progress has been made in the research on the derivatives and preparations of docetaxel, most of them still do not meet the requirements of drug safety and industrial production, and there have been no clinical and market reports so far.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Take 30mg of docetaxel, 200mg of lecithin, 100mg of cholesterol, and 20mg of dipalmitoylphosphatidylethanolamine in a 50ml round bottom flask, add 20ml of chloroform to dissolve, evaporate the organic solvent under reduced pressure on a rotary evaporator, and form a layer on the inner wall of the bottle Lipid film, slowly add 20mmol / L Hepes buffer solution, ultrasonically disperse at room temperature for 30min, make small unicellular liposomes, its average particle size is 57nm, accounting for 80%, all particles are below 100nm, particle size distribution is narrow, It shows that the liposome size is relatively uniform; the liposome can be stable at room temperature for several days and at -20°C for at least 3 months, and no precipitation and degradation of docetaxel can be observed during storage.

Embodiment 2

[0038] Accurately weigh 20 mg of docetaxel, 20 mg of lecithin, and 200 mg of cholesterol, and dissolve them in 10 ml of ether (heating may be appropriate). Then slowly inject this solution into phosphate buffer solution heated to 50-60°C with a syringe, stir with an electronic constant speed stirrer at a speed of 600r / rain until the ether is completely removed, and then dilute to 100mL with phosphate buffer solution, that is Docetaxel liposomes were stored in a 4°C refrigerator for subsequent use.

Embodiment 3

[0040] The liposomes in Example 2 were taken for morphology observation, particle size and distribution determination thereof.

[0041] Take an appropriate amount of liposomes, add an appropriate amount of water for injection to dilute, stain with 1% phosphotungstic acid, and observe particle morphology under a transmission electron microscope.

[0042] Take an appropriate amount of liposome suspension, add an appropriate amount of water to dilute, and measure the particle size and distribution and Zeta potential of liposomes with a Zetamaster photon correlation spectrometer.

[0043] Under the electron microscope, the docetaxel liposomes were uniform and regular spherical particles without aggregation and adhesion.

[0044] The particle size distribution of the docetaxel liposome measured by the experiment is uniform, the average particle size is 120nm, the polydispersity index is 0.158, and the zeta potential is -26.4mv.

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PUM

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Abstract

The present invention provides one kind of polyene taxol liposome capable of being used for injection and oral taking and its solid preparation, and features that polyene taxol is coated with phospholipid matter and additive so as to prepare polyene taxol liposome preparation with small size, high coating rate, high stability and less toxic side effect. The polyene taxol liposome of the present invention has raised targeting effect on cancer cell, enhanced tumor cell killing effect, high curative effect and less toxic side effect. The present invention also provides several preparation processes of polyene taxol liposome, and the preparation processes are simple, low in cost and suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to liposomes containing docetaxel, an antitumor active ingredient, and a preparation method of the liposomes. Background technique [0002] Docetaxel (DOCETAXEL) trade name Taxotere is a semi-synthetic paclitaxel derivative, its anti-tumor mechanism is the same as paclitaxel, and it is a mitosis inhibitor. Arrests cells in the G2 / M phase by promoting tubulin aggregation and delaying microtubule depolymerization, resulting in the formation of stable non-functional microtubule bundles, thereby disrupting mitosis and cell proliferation. Its cytotoxic effect is 1.3 to 12 times that of paclitaxel. In addition, the drug also has the effect of promoting apoptosis. It has been clinically approved for the first-line or second-line treatment of ovarian cancer, breast cancer and non-small cell lung cancer. [0003] Due to the poor water solubility of docetaxel, the cur...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61K9/127A61P35/00
Inventor 李亚平陈伶俐顾王文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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