Elemene micro-emulsion

Abstract

The invention discloses an elemene micro-emulsion, which is prepared from raw material components fed in a certain proportion. The raw material components include elemene, surfactant, cosurfactant and water or buffer solution with a pH between 5 and 8, wherein the surfactant is one or any mixture of tween, polyoxyethylene castor oil and polyglycol stearate; the cosurfactant is one or any mixture of ethanol, 1,3-propanediol and glycerin; the pH of the elemene micro-emulsion is in a range between 5 and 8; the concentration of elemene in the elemene micro-emulsion is 1 to 5 g / 100 ml; the feed ratio in part by mass of elemene to surfactant to cosurfactant is 1-5:1-40:1-10; and the unit of mass part / volume part is g / ml. The elemene micro-emulsion has the advantages of improving elemene bioavailability, ensuring steadier blood concentration, reducing toxic side effect compared with the prior preparation, indirectly improving the efficacy of elemene serving as a chemotherapeutic medicament and enhancing the anti-tumor effect of elemene.

Description

(1) Technical field

[0001] The invention belongs to the technical field of medicine, and relates to a microemulsion preparation of an antitumor drug elemene. (2) Background technology

[0002] Elemene is an anticancer drug extracted and separated from traditional Chinese medicine. It has been on the market for more than 10 years. It has exact curative effect and mild side effects. ", "Tenth Five-Year" key projects, national essential drugs, national medical insurance drugs, national pharmacopoeia drugs, the first domestic targeted anti-tumor botanical drugs that have been proven safe and effective with the smallest molecular weight by systematic evaluation of evidence-based medicine (EBM). It is an effective anti-cancer active ingredient extracted from Wenyujin, one of the traditional Chinese medicine "Zhe Bawei". It is a sesquiterpene compound composed of carbon and hydrogen elements, and the main component is β-elemene. Elemene is an effective non-cytotoxic antitumor drug...

Examples

Embodiment 1

[0045] Prescription: Elemene 1g, ethanol 5ml, glycerin 15ml, propylene glycol 15ml, Tween (80) 5g, ethylparaben 50mg, purified water to 100ml.

[0046] Preparation process: Mix the prescription amount of elemene, Tween 80, ethyl paraben, ethanol, glycerin, and propylene glycol, add it into 60ml of water, mix evenly, ultrasonicate at room temperature for 1 hour, let cool to room temperature, and use 0.22μm micropore Membrane filtration, adding purified water to adjust the volume to 100ml, and subpackaging to obtain elemene microemulsion. The prepared microemulsion has a pH of 5.4, a viscosity of 6 mPa·s, and a surface tension of 32.1 mN / m. The average particle diameter of the elemene microemulsion measured by a laser particle size analyzer is 67 nm.

Embodiment 2

[0048] Prescription: Elemene 1g, ethanol 5ml, glycerin 10mL, Tween (80) 5g, polyoxyethylene castor oil (EL) 1.25g, ethylparaben 50mg, purified water to 100ml.

[0049] Preparation process: Dissolve the prescription amount of elemene, Tween (80), polyoxyethylene castor oil (EL), and ethylparaben in ethanol and glycerin, then add 50ml of purified water, stir and mix evenly, and ultrasonicate for 1h at room temperature , set to cool to room temperature, filter with a 0.22 μm microporous membrane, add water to adjust the volume to 100 ml, and then pack into elemene microemulsions. The prepared microemulsion has a pH of 5.26, a viscosity of 4 mPa·s, a surface tension of 34.7 mN / m, and a particle size of 54 nm.

Embodiment 3

[0051] Prescription: Elemene 1g, ethanol 5ml, glycerin 10mL, propylene glycol 5mL, Tween (80) 2.5g, polyoxyethylene castor oil (EL) 3.75g, vitamin C 25mg, ethylparaben 50mg, 0.1M phosphate Buffer (pH7.0) to 100ml.

[0052] Preparation process: Dissolve the prescription amount of elemene, Tween (80), polyoxyethylene castor oil (EL), and ethylparaben in ethanol, glycerin, and propylene glycol and mix evenly; dissolve vitamin C in 50ml of PBS buffer, Add the oil phase to the water phase, stir and mix evenly, sonicate at room temperature for 1 hour, cool to room temperature, filter through a 0.22 μm microporous membrane, add buffer to adjust the volume to 100 ml, and divide to obtain elemene microemulsion. The prepared microemulsion has a pH of 6.84, a viscosity of 5 mPa·s, a surface tension of 35.6 mN / m, and a particle size of 60 nm.

(1) Technical field

[0001] The invention belongs to the technical field of medicine, and relates to a microemulsion preparation of an antitumor drug elemene. (2) Background technology

[0002] Elemene is an anticancer drug extracted and separated from traditional Chinese medicine. It has been on the market for more than 10 years. It has exact curative effect and mild side effects. ", "Tenth Five-Year" key projects, national essential drugs, national medical insurance drugs, national pharmacopoeia drugs, the first domestic targeted anti-tumor botanical drugs that have been proven safe and effective with the smallest molecular weight by systematic evaluation of evidence-based medicine (EBM). It is an effective anti-cancer active ingredient extracted from Wenyujin, one of the traditional Chinese medicine "Zhe Bawei". It is a sesquiterpene compound composed of carbon and hydrogen elements, and the main component is β-elemene. Elemene is an effective non-cytotoxic antitumor drug...

Examples

Embodiment 1

[0045] Prescription: Elemene 1g, ethanol 5ml, glycerin 15ml, propylene glycol 15ml, Tween (80) 5g, ethylparaben 50mg, purified water to 100ml.

[0046] Preparation process: Mix the prescription amount of elemene, Tween 80, ethyl paraben, ethanol, glycerin, and propylene glycol, add it into 60ml of water, mix evenly, ultrasonicate at room temperature for 1 hour, let cool to room temperature, and use 0.22μm micropore Membrane filtration, adding purified water to adjust the volume to 100ml, and subpackaging to obtain elemene microemulsion. The prepared microemulsion has a pH of 5.4, a viscosity of 6 mPa·s, and a surface tension of 32.1 mN / m. The average particle diameter of the elemene microemulsion measured by a laser particle size analyzer is 67 nm.

Embodiment 2

[0048] Prescription: Elemene 1g, ethanol 5ml, glycerin 10mL, Tween (80) 5g, polyoxyethylene castor oil (EL) 1.25g, ethylparaben 50mg, purified water to 100ml.

[0049] Preparation process: Dissolve the prescription amount of elemene, Tween (80), polyoxyethylene castor oil (EL), and ethylparaben in ethanol and glycerin, then add 50ml of purified water, stir and mix evenly, and ultrasonicate for 1h at room temperature , set to cool to room temperature, filter with a 0.22 μm microporous membrane, add water to adjust the volume to 100 ml, and then pack into elemene microemulsions. The prepared microemulsion has a pH of 5.26, a viscosity of 4 mPa·s, a surface tension of 34.7 mN / m, and a particle size of 54 nm.

Embodiment 3

[0051] Prescription: Elemene 1g, ethanol 5ml, glycerin 10mL, propylene glycol 5mL, Tween (80) 2.5g, polyoxyethylene castor oil (EL) 3.75g, vitamin C 25mg, ethylparaben 50mg, 0.1M phosphate Buffer (pH7.0) to 100ml.

[0052] Preparation process: Dissolve the prescription amount of elemene, Tween (80), polyoxyethylene castor oil (EL), and ethylparaben in ethanol, glycerin, and propylene glycol and mix evenly; dissolve vitamin C in 50ml of PBS buffer, Add the oil phase to the water phase, stir and mix evenly, sonicate at room temperature for 1 hour, cool to room temperature, filter through a 0.22 μm microporous membrane, add buffer to adjust the volume to 100 ml, and divide to obtain elemene microemulsion. The prepared microemulsion has a pH of 6.84, a viscosity of 5 mPa·s, a surface tension of 35.6 mN / m, and a particle size of 60 nm.

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