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Docetaxel liposome and preparation method thereof

A technology of docetaxel and liposomes, which is applied in the field of medicine, can solve the problems of difficult industrial production, easy oxidation of liquid liposomes, and low drug loading of liposomes, and achieve easy industrial production and short production time , the effect of controllable drug content

Active Publication Date: 2014-03-12
SHENYANG PHARMA UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Chinese patent CN200510029634.0 discloses a conventional preparation method of liquid liposomes of docetaxel, the liquid liposomes prepared by this method are easy to oxidize, the stability is poorer than the liposomes preserved in solid form, and the lipid Low body concentration, limiting the application of formulations
However, the prepared liposomes have low drug loading, and the cost is increased due to the large amount of long-circulation materials used, making it difficult to realize industrial production

Method used

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  • Docetaxel liposome and preparation method thereof
  • Docetaxel liposome and preparation method thereof
  • Docetaxel liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] 1) Dissolve 1g of docetaxel, 25g of soybean lecithin and 3g of cholesterol in 800ml of tert-butanol, add 1% activated carbon to filter out the pyrogen;

[0044] 2) At 40°C, add 50g of sodium chloride carrier powder, and remove the organic solvent under reduced pressure to form a dry powder;

[0045] 3) At 40°C, add 1000ml of hydration medium containing phosphate buffer (PH6.5), reduce the particle size of the hydration solution by external force (probe ultrasound), and filter and sterilize through a 0.22μm filter membrane. Obtain a uniform liposome solution with blue opalescence;

[0046] 4) Add 50g of lactose, remove the water after freeze-drying, and obtain dry docetaxel liposome freeze-dried powder injection, reconstitute into liposome after hydration and shaking before use, and inject it.

[0047] The concentration of docetaxel in the prepared liposome was 1 mg / ml, and the encapsulation efficiency was 93.3%.

Embodiment 2

[0049] 1) Dissolve 5g of docetaxel, 150g of sphingomyelin and 75g of cholesterol in 1000ml of ethanol, add 1% activated carbon to filter out the pyrogen;

[0050] 2) At 45°C, add 200g of sorbitol carrier powder, and remove the organic solvent under reduced pressure to form a dry powder;

[0051] 3) At 45°C, add 1000ml of hydration medium (PH7.4) containing acetate buffer, reduce the particle size of the hydration solution by external force (ultrasonic oscillation), and filter and sterilize through a 0.22μm filter membrane , to obtain a uniform liposome solution with blue opalescence;

[0052] 4) Add 150g of dextran, remove the water after lyophilization, and obtain dry docetaxel liposome lyophilized powder injection, reconstitute into liposome after hydration and shaking before use, and inject it.

[0053] The concentration of docetaxel in the prepared liposome was 5 mg / ml, and the encapsulation efficiency was 89.5%.

Embodiment 3

[0055] 1) Dissolve 2g of docetaxel, 10g of cardiolipin and 2.5g of cholesterol in 600ml of chloroform, add 1% activated carbon and filter to remove pyrogens;

[0056] 2) At 50°C, add 100g of sucrose carrier powder, remove the organic solvent under reduced pressure, and form a dry powder;

[0057] 3) At 50°C, add 1000ml of hydration medium containing carbonate buffer (PH7.4), reduce the particle size of the hydrated solution by external force (high pressure homogenization), and filter through a 0.22μm filter membrane to remove bacteria, to obtain a uniform liposome solution with blue opalescence;

[0058] 4) Add 50g of sorbitol, remove the water after freeze-drying, and obtain dry docetaxel liposome freeze-dried powder injection, reconstitute into liposome after hydration and shaking before use, and inject it.

[0059] The concentration of docetaxel in the prepared liposome was 2 mg / ml, and the encapsulation efficiency was 88%.

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Abstract

The invention belongs to the technical field of medicine and provides a docetaxel liposome suitable for industrial production and a preparation method thereof. The preparation method provided by the invention comprises the following steps: an organic solvent dissolved in a liposome membrane material of main medicine is dispersed into superfine water-soluble proppant micro powder; the organic solvent is recovered under the decompression condition; lipid is adsorbed to a water-soluble carrier to obtain a powder liposome. When the powder liposome is in contact with a hydration medium, the lipid swells and the water-soluble vector is rapidly dissolved so as to form a multilayer liposome in a water phase; a clarified liposome with blue opalescence is obtained by externally applying acting force to reduce the particle size; liposome powder is obtained by adding a freeze-drying protective additive to carry out freezing and drying; liposome solution is obtained by redissolving the liposome powder before use. According to the invention, the liposome is prepared by utilizing a decompression carrier freeze-drying technology; stability of the liposome can be greatly improved; the preparation method is easy for production scale-up and provides a novel thinking for industrialization of the liposome.

Description

technical field [0001] The invention belongs to the technical field of medicine, relates to an anticancer drug docetaxel liposome preparation, and also relates to a preparation method of the preparation. Background technique [0002] Malignant tumors have become intractable and refractory diseases that seriously endanger human health and life, and are known as the "No. 1 killer" in the world. According to the statistical reports of the World Health Organization in recent years, the global cancer incidence rate will increase by 50%, that is, 15 million new cancer patients will be added every year. Not only that, the number of cancer deaths is also rising rapidly around the world. 20% of the world's new cancer patients are in China, and 24% of cancer deaths are in China. It can be seen that the research and development of anti-tumor drugs and new preparations have important social benefits and huge potential markets. Generally speaking, most anticancer drugs have strong toxi...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/127A61K31/337A61P35/00A61J3/02
Inventor 王淑君许文
Owner SHENYANG PHARMA UNIVERSITY
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