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A microemulsion medicinal composition containing Docetaxel for treating knub and its preparation method

A technology of docetaxel and composition, applied in the field of microemulsion pharmaceutical composition and preparation thereof, can solve the problems of large particle size of submicroemulsion, complicated process, poor stability and the like

Inactive Publication Date: 2008-04-09
郑飞雄
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, many improvements have been proposed for the targeting and low toxicity of this type of drug, such as making this type of drug into fat emulsion (submicroemulsion), liposome, nanoparticle, etc., but there are still deficiencies in the prior art , such as poor stability, low drug loading, unclear targeting, complex production process, etc.
In addition, such preparations, such as submicron emulsions, have large particle sizes, and most of them adopt a two-step emulsification preparation method, which is cumbersome and requires heating during the preparation process, which is not easy for industrialized large-scale production.

Method used

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  • A microemulsion medicinal composition containing Docetaxel for treating knub and its preparation method
  • A microemulsion medicinal composition containing Docetaxel for treating knub and its preparation method
  • A microemulsion medicinal composition containing Docetaxel for treating knub and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Docetaxel, soybean oil for injection, and lecithin weighed according to the above-mentioned amount are dissolved in the ethanol of the amount, and the phosphate buffer (pH7.4) of the amount is added and gently stirred to spontaneously form a milk.

[0083] The particle size distribution of the docetaxel microemulsion was measured by a LS230 laser particle size analyzer (Beckman, USA), and the result was 54.43 ± 4.53nm. Zeta potential was determined to be -24.3 mV.

[0084] The in vitro release of docetaxel from a microemulsion pharmaceutical composition was studied by dialysis. Get 2ml of the microemulsion pharmaceutical composition and place it in a dialysis bag, which is attached to the stirring paddle of the dissolution apparatus at a temperature of 37° C. and a rotating speed of 50 rpm. The release medium is water with a volume of 250mL. Samples were taken at the set time to measure the concentration of docetaxel, and the corresponding release rate was cal...

Embodiment 2

[0088] The docetaxel, MCT, soybean lecithin, and vitamin E weighed according to the above-mentioned amounts were ultrasonically dissolved in the amount of anhydrous propylene glycol, and the amount of water for injection was added under magnetic stirring to form a microemulsion spontaneously.

[0089] The particle size distribution of the docetaxel microemulsion was measured by a LS230 laser particle size analyzer (Beckman, USA), and the result was 46.57 ± 6.78nm. Zeta potential was determined to be -28.3 mV.

[0090] The in vitro release of docetaxel from a microemulsion pharmaceutical composition was studied by dialysis. Get 2ml of the microemulsion pharmaceutical composition and place it in a dialysis bag, which is attached to the stirring paddle of the dissolution apparatus at a temperature of 37° C. and a rotating speed of 50 rpm. The release medium is water with a volume of 250 mL. Samples were taken at the set time to measure the concentration of docetaxel, and...

Embodiment 3

[0094] Mix the docetaxel, IPM, lecithin, and glycerin weighed according to the above-mentioned amounts evenly, add the amount of water for injection, and magnetically stir to form a microemulsion spontaneously.

[0095] The particle size distribution of the docetaxel microemulsion was measured by LS230 laser particle size analyzer (Beckman, USA), and the result was 29.65 ± 5.13nm. Zeta potential was determined to be -30.02mV.

[0096] The in vitro release of docetaxel from a microemulsion pharmaceutical composition was studied by dialysis. Get 2ml of the microemulsion pharmaceutical composition and place it in a dialysis bag, which is attached to the stirring paddle of the dissolution apparatus at a temperature of 37° C. and a rotating speed of 50 rpm. The release medium is water with a volume of 250mL. Samples were taken at the set time to measure the concentration of docetaxel, and the corresponding release rate was calculated, and the result was 28.34±5.16% release...

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Abstract

The invention relates to a microemulsion medicament composition for remedying tumour and the preparation method thereof, in particular to a microemulsion medicament composition containing Docetaxel and the preparation method threreof. The microemulsion medicament composition is prepared by emulsifying the Docetaxel, an oil phase substance, phospholipid, stabilizing agent and dispersion medium according to the required component proportion. The preparation method can adopt an emulsion process, the grain of the obtained microemulsion is 10-100 nm and distributed evenly, the Zeta electric potential is from minus10 to minus 40 mV, and can be used for vein administration. The microemulsion medicament composition for remedying the tumour can be prepared into various medicament forms, which comprise liquid preparation, solid preparation, external use reparation, aerosol and lyophilizing preparation. The preparation method of the invention can adopt the conventional process equipment, the production efficiency is high, the quality of a product is reliable, the needle through is good, the term of validity is above two years, and the invention is convenient for the industrialized large production.

Description

technical field [0001] The invention relates to a microemulsion pharmaceutical composition for treating tumors and a preparation method thereof, in particular to a microemulsion pharmaceutical composition containing docetaxel and a preparation method thereof. Background technique [0002] Docetaxel (Docetaxel) is a semi-synthetic paclitaxel derivative developed by the American Rhone-Poulene Rorer Chemical Company, also known as docetaxel, chemical name: [2aR-(2aα, 4β, 4αβ, 6β, 9α, ( αR * , βS * ), 11α, 12α, 12aα, 12bα)]-β-[[(1,1 dimethylethoxy)carbonyl]amino]-α-hydroxyphenylpropanoic acid [12b-acetoxy-12-benzoyloxy -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-1H-cyclodecapenta[3,4]benzo[1,2-b]oxetan-9-yl]ester trihydrate; its molecular formula For: C 43 h 53 NO 14 ·3H 2 O; molecular weight: 807.89. [0003] Docetaxel and paclitaxel belong to microtubule depolymerization inhibitors, which...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61K9/06A61K9/107A61K9/12A61K9/19A61K9/20A61K9/48A61K47/34A61K47/44A61P35/00A61K47/10A61K47/24
Inventor 赵秀丽陈大为郑飞雄
Owner 郑飞雄
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