Pirarubicin freeze-dry preparations and preparation method thereof

A technology for pirarubicin and freeze-dried preparations, which is applied in the field of pirarubicin liposome freeze-dried preparations and their preparation, can solve the problems of poor preparation stability, poor anti-tumor activity, large toxic and side effects of the reticuloendothelial system, etc. problems, to achieve the effect of improving stability, improving anti-tumor activity, and reducing toxic and side effects

Inactive Publication Date: 2010-07-14
深圳万乐药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Chinese patent application CN1931178A discloses "pirarubicin liposome and preparation method thereof", which provides a common liposome preparation that solves the targeted administration of pirarubicin. The affinity of pirarubicin and the reduction of the toxic and side effects of pirarubicin have played a certain role, but there are still disadvantages such as poor stability of the preparation, large toxic and side effects of the reticuloendothelial system caused by passive targeting, and poor anti-tumor activity

Method used

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  • Pirarubicin freeze-dry preparations and preparation method thereof

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Effect test

Embodiment 1

[0030] Pirarubicin 10g

[0031] Hydrogenated Soy Lecithin 63g

[0032] Cholesterol 35g

[0033] PEG2000-Dipalmitoylphosphatidylethanolamine 4g

[0034] Poloxamer 188 1.5g

[0035] a-Tocopherol 40mg

[0036] Sucrose 625g

[0037] Preparation method: Dissolve the prescribed amount of pirarubicin, hydrogenated soybean lecithin, cholesterol, PEG2000-dipalmitoylphosphatidylethanolamine and a-tocopherol in absolute ethanol, remove the absolute ethanol by rotary evaporation to make a uniform lipid film. The lipid film was hydrated with PH7.4 phosphate buffer containing the prescribed amount of poloxamer 188 and sucrose in a constant temperature water bath at 60°C with nitrogen gas for 30 minutes, then transferred to an ice bath to cool, and then was homogenized with a high-pressure milk homogenizer (high-pressure homogenizer). 408kg / cm 2 2 times, low pressure 102kg / cm 2 1 time) Dispersion treatment, filtration with 200nm microporous membrane, and lyophilization in a lyophiliz...

Embodiment 2

[0066] Pirarubicin Hydrochloride 12g

[0067] Hydrogenated Soy Lecithin 75g

[0068] Cholesterol 42g

[0069] PEG2000-Dipalmitoylphosphatidylethanolamine 5g

[0070] Poloxamer 188 2g

[0071] a-Tocopherol 50mg

[0072] Sucrose 900g

[0073] Preparation method: Dissolve the prescribed amount of pirarubicin hydrochloride, hydrogenated soybean lecithin, cholesterol, PEG2000-dipalmitoylphosphatidylethanolamine and a-tocopherol in absolute ethanol, and remove the absolute ethanol by rotary evaporation to make a uniform lipid The lipid film was hydrated with PH6.5 phosphate buffer solution containing the prescribed amount of poloxamer 188 and sucrose, filled with nitrogen in a constant temperature water bath at 50°C for 60 minutes, then transferred to an ice bath to cool, and then homogenized with a high-pressure milk homogenizer. (high pressure 510kg / cm 2 2 times, low pressure 102kg / cm 2 1 time) Dispersion treatment, filtration with 100nm microporous membrane, and lyophiliza...

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Abstract

The invention discloses a pirarubicin freeze-dried preparation. The preparation is composed of the following components with the contents: 8 to 12g of pirarubicin or pirarubicin hydrochloride, 50 to 75g of hydrogenated soybean lecithin, 28 to 42g of cholesterol, 3 to 5g of PEG2000-1, 2-dipalmitoyl-glycero-3-phosphoethanolamine, 1.2 to 2g of poloxamer 188, 32 to 50mg of Alpha-tocopherol and 450 to900g of sucrose. The preparation has good anti-cancer function, small toxicity and high stability, and the target of the drug is improved simultaneously. The invention further discloses a preparationmethod of the pirarubicin freeze-dried preparation.

Description

technical field [0001] The invention relates to a lyophilized preparation of pirarubicin, in particular to a lyophilized pirarubicin liposome preparation and a preparation method thereof. Background technique [0002] As an antineoplastic drug, pirarubicin has a good curative effect on malignant lymphoma and acute leukemia, and is effective on breast cancer, head and neck cancer, gastric cancer, malignant tumors of the urinary system, ovarian cancer, endometrial cancer, and cervical cancer. . [0003] At present, liposome preparation is a better choice in solving the targeted drug delivery of tumor drugs. Chinese patent application CN1931178A discloses "pirarubicin liposome and preparation method thereof", which provides a common liposome preparation that solves the targeted administration of pirarubicin. The affinity of pirarubicin and the reduction of the toxic and side effects of pirarubicin have played a certain role, but there are still disadvantages such as poor prep...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/704A61K9/19A61K47/32A61P35/00
Inventor 吴静左鸿宇曾嘉铨王长平张汉利宝玉荣郭才旺
Owner 深圳万乐药业有限公司
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