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Polyenic taxusol lipid complexes and micelle composition thereof for injection

A technology of lipid complex and docetaxel, applied in the directions of drug combination, liposome delivery, drug delivery, etc., can solve the problems of organic solvent surfactants, allergies, etc., to prolong the effective time, reduce inactivation, irritation, etc. Sex-reducing effect

Inactive Publication Date: 2009-05-27
SHENYANG WOSEN PHARMA INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Solve the problems of organic solvents and surfactant allergies in injections by lipidating docetaxel

Method used

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  • Polyenic taxusol lipid complexes and micelle composition thereof for injection
  • Polyenic taxusol lipid complexes and micelle composition thereof for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Take 500mg of dopeclitaxel, 2.0g of egg yolk lecithin, 400mg of sodium cholesterol sulfate, and 10mg of vitamin E, and dissolve them in methanol at 30°C as the organic phase; dissolve 0.5g of PEG400 in 90ml of water for injection, heat to 30°C as the water phase, The organic phase was injected into the water phase under stirring at 30°C, and the stirring was continued for 5 minutes, and then the methanol was evaporated under reduced pressure to obtain a blue-opalescent dopaclitaxel lipid complex, and the average particle size was 65±15nm. Add water for injection to make up to a total volume of 100ml, filter and sterilize with a 0.22μm microporous membrane, dispense 4ml / tube, and sterilize at 121°C for 30min to obtain an injection.

[0036] Add trehalose 5g to the prepared lipoplex, water for injection to 100ml, filter and sterilize with a 0.22μm microporous membrane, pack 4ml / branch, and freeze-dry under aseptic operation to obtain final product. The freeze-dried prepar...

Embodiment 2

[0038] Take 1.0g of dopaclitaxel, 3.0g of soybean lecithin, and 500mg of sodium cholesterol sulfate, and dissolve them in absolute ethanol at 35°C as the organic phase; dissolve 1.0g of PEG200 in 90ml of water for injection, heat to 35°C as the water phase, and The organic phase was injected into the water phase under stirring at 35°C, and the stirring was continued for 10 minutes, and then the ethanol was evaporated under reduced pressure to obtain the dotaxel lipid complex with blue opalescence, and the average particle size was measured to be 72±120nm. Add water for injection to make up to a total volume of 100ml, filter and sterilize with a 0.22μm microporous membrane, dispense 4ml / tube, and sterilize at 121°C for 30min to obtain an injection.

[0039] Add trehalose 5g to the prepared lipoplex, water for injection to 100ml, filter and sterilize with a 0.22μm microporous membrane, pack 4ml / branch, and freeze-dry under aseptic operation to obtain final product. The freeze-dr...

Embodiment 3

[0041] Take 500mg of dopaclitaxel, 10g of soybean lecithin, and 5g of sodium cholesterol sulfonate, and dissolve them in tetrahydrofuran at 35°C as the organic phase; dissolve 5g of poloxamer 188 in 950ml of water for injection, heat to 35°C as the water phase, and stir at 35°C Inject the organic phase into the water phase, keep stirring for 10 minutes, and then evaporate the tetrahydrofuran under reduced pressure to obtain the dopaclitaxel lipid complex with blue opalescence. For 100ml, use a 0.22μm microporous membrane to filter and sterilize, aliquot 4ml / tube, and sterilize at 121°C for 30min to obtain the injection.

[0042] Add trehalose 5g to the prepared lipoplex, water for injection to 100ml, filter and sterilize with a 0.22μm microporous membrane, pack 4ml / branch, and freeze-dry under aseptic operation to obtain final product. The freeze-dried preparation was diluted with physiological saline, and the average particle size was measured to be 74±18nm.

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Abstract

The invention provides a docetaxel lipid compound and a micellar compound used in the injection of the docetaxel lipid compound, belonging to a pharmaceutical preparation. The docetaxel lipid compound is composed of docetaxel with a therapeutic dose, phospholipid, cholesterol sulfate or / and similar cholesterol derivative, additive and injection water. By means of the lipidization of the docetaxel, the problem about organic menstruum of an injection and the problem of hypersusceptibility of a surface active agent are solved. A docetaxel lipid compound injection provided by the invention has the advantages of small side effect, low blood vessel simulation, high drug-loading rate, narrow particle size distribution, capability of filtering and degerming, good pharmaceutical stability, etc.

Description

technical field [0001] The invention relates to a docetaxel lipid complex and a micelle composition for injection thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Docetaxel, the main ingredient of this product is docetaxel, its chemical name is {2Ar-[2aα, 4β, 4aβ, 6β, 9α(αR*, Bs*), 11α, 12α, 12aα, 12bα ]}-β-{[(1,1-dimethylethoxy)carbonyl]amino}-α-hydroxyphenylpropanoic acid [12b-acetoxybenzoyloxy-2a,3,4,4a,5, 6,9,10,11,12,12a,12b-dodecahydro-4,6,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methylene yl-1H-cyclodecapenta[3,4]benzo[1,2-b]oxetan-9-yl]ester. Its structural formula is: [0003] [0004] Molecular formula: C43H53NO14, molecular weight: 807.88 [0005] Docetaxel is a multi-taxane anti-tumor drug, which plays an anti-tumor effect by interfering with the microtubule network necessary for cell mitosis and interphase cell functions. Docetaxel can bind to free tubulin, promote the assembly of tubulin into stable mi...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61K9/00A61K9/127A61K47/24A61K47/32A61K47/34A61K47/36A61P35/00A61K47/10
Inventor 德瑞克·王李林穗徐飒
Owner SHENYANG WOSEN PHARMA INST
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