Paclitaxel lipid complexes and micelle composition thereof for injection

A technology of lipid complex and paclitaxel, which is applied in the directions of drug combination, drug delivery, and medical preparations of inactive ingredients, etc., can solve the problems of inconvenient use, non-allergic, pain, etc. of injections, and can prolong the effective time and reduce the inactivation. , the effect of reducing irritation

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

[0006] In order to solve the inconvenience, pain and allergy problems of injections, many people are studying ways such as changing solvents, mak

Method used

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  • Paclitaxel lipid complexes and micelle composition thereof for injection
  • Paclitaxel lipid complexes and micelle composition thereof for injection
  • Paclitaxel lipid complexes and micelle composition thereof for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Take paclitaxel 500mg, egg yolk lecithin 2.0g, cholesterol sodium sulfate 400mg, vitamin E 10mg, dissolve in methanol at 30°C as the organic phase; dissolve PEG400 0.5g in 90ml water for injection, heat to 30°C as the water phase, The organic phase was injected into the water phase under stirring at ℃, and the stirring was continued for 5 minutes, and then the methanol was evaporated under reduced pressure to obtain the paclitaxel lipid complex with blue opalescence, and the average particle size was 70±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.

[0043] 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 physiol...

Embodiment 2

[0045] Take paclitaxel 1.0g, soybean lecithin 3.0g, sodium cholesteryl sulfate 500mg, dissolve in absolute ethanol at 35°C as the organic phase; dissolve PEG200 1.0g in 90ml water for injection, heat to 35°C as the water phase, The organic phase was injected into the water phase under stirring at ℃, and the stirring was continued for 10 minutes, and then the ethanol was evaporated under reduced pressure to obtain the paclitaxel lipid complex with blue opalescence, and the average particle size was measured to be 75±18nm. 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.

[0046] 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 ph...

Embodiment 3

[0048] Take 500 mg of paclitaxel, 10 g of soybean lecithin, and 5 g of sodium cholesterol sulfonate, and dissolve them in tetrahydrofuran at 35°C as the organic phase; dissolve 5 g 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 paclitaxel lipid complex with blue opalescence. , sterilized by filtration with a 0.22 μm microporous membrane, aliquoted into 4ml / bottle, and sterilized at 121°C for 30 minutes to obtain the injection.

[0049] 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 73±12nm.

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Abstract

The invention provides a paclitaxel lipid compound and a micellar compound used in the injection of the paclitaxel lipid compound. The paclitaxel liposome compound is composed of paclitaxel with a therapeutic dose, phospholipid, cholesterol sulfate or/and similar cholesterol derivative, additive and injection water. By means of the lipidization of the paclitaxel, the problem about organic menstruum of an injection and the problem of hypersusceptibility of a surface active agent are solved. A paclitaxel 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 paclitaxel lipid complex and a micelle composition for injection thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Paclitaxel (Paclitaxel), chemical name: 5β, 20-epoxy-1,2α, 4,7β, 10β, 13α-hexahydroxytaxane-11-en-9-one-4,10-diacetic acid The structural formula of ester-2-benzoate-13-[(2'R,3'S)-N-benzoyl-3-phenylisoserine ester is: [0003] [0004] Molecular formula: C47H51NO14 Molecular weight: 853.92. This product is a new type of anti-microtubule drug, which can maintain the stability of tubulin and inhibit cell mitosis by promoting tubulin polymerization and inhibiting depolymerization. In vitro experiments have shown that paclitaxel has a significant radiosensitizing effect, which may cause cells to stop in the G2 and M phases that are sensitive to radiotherapy. Intravenous administration of paclitaxel, the drug plasma concentration showed a biphasic curve. The protein b...

Claims

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Application Information

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