Estrogen lipoplast preparing method

An estrogen and liposome technology, which is applied in the directions of liposome delivery, medical preparations with inactive ingredients, and medical preparations containing active ingredients, etc. Formatives and plasticizers, the effect of a simple preparation method

Inactive Publication Date: 2009-07-01
NORTHWESTERN POLYTECHNICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In order to overcome the deficiencies of the prior art estrogen medicine sustained-release composition with many additives and complex preparation process, the present invention provides a preparation method of estrogen liposome

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Example 1: 4 mg ethinyl estradiol and 196 mg egg yolk lecithin were dissolved in 10 mL of organic solvent of methanol:chloroform=1:2, placed in a 20 mL test tube, and the test tube was placed on a vortex mixer and oscillated at 1000 r / min for 30 min. Mix ethinyl estradiol and egg yolk lecithin evenly, keep a water bath at 50°C, blow nitrogen into the test tube to let the organic solvent volatilize, and at the same time turn the test tube continuously, and tilt the test tube as far as possible to let the ethinyl estradiol and egg yolk lecithin that evaporate the organic solvent The mixture should try to adhere to the wall of the test tube instead of the bottom of the test tube to ensure complete hydration. Finally, vacuum 90min at a vacuum of 70KPa, the mixture of ethinyl estradiol and egg yolk lecithin adhering to the test tube wall is vacuum sucked into a thin film, turn off the vacuum pump, and add 10mL of phosphate buffer solution pH7.4 into the test tube , immediate...

Embodiment 2

[0015] Example 2: Dissolve 3.54mg of estradiol, 196mg of soybean lecithin, 49.85mg of cholesterol, and 0.19mg of vitamin E in 10mL of organic solvent of methanol:chloroform=1:2, place in a 20mL test tube, and place the test tube in a vortex Shake and mix on the mixer at 2000r / min for 60 minutes to mix estradiol and soybean lecithin evenly. Keep in a water bath at 60°C and blow nitrogen into the test tube to let the organic solvent evaporate. The mixture of estradiol and soybean lecithin without organic solvents should adhere to the wall of the test tube instead of the bottom of the test tube as much as possible to ensure complete hydration during hydration. Finally, vacuum for 120min at a vacuum of 85KPa, the mixture of estradiol and soybean lecithin adhering to the test tube wall is vacuum-sucked into a thin film, turn off the vacuum pump, and add 20mL of phosphate buffer solution pH7.4 into the test tube , immediately placed on a vortex mixer at 3000r / min and vibrated for 18...

Embodiment 3

[0016] Example 3: Dissolve 8.07mg of estriol, 192mg of hydrogenated egg yolk lecithin, and 0.13mg of vitamin E in 10mL of organic solvent of methanol:chloroform=1:2, place in a 20mL test tube, and place the test tube on a vortex mixer Shake at 1500r / min for 40 minutes to mix estriol and hydrogenated egg yolk lecithin evenly; maintain a water bath at 55°C, blow nitrogen into the test tube to let the organic solvent evaporate, and at the same time keep rotating the test tube, and tilt the test tube as far as possible to let the organic solvent evaporate The mixture of estriol and hydrogenated egg yolk lecithin adheres to the wall of the test tube instead of the bottom of the test tube as much as possible to ensure complete hydration; The mixture of egg yolk lecithin was vacuum pumped into a thin film; turn off the vacuum pump, add 15mL of phosphate buffer solution pH7.4 into the test tube, immediately place it on a vortex mixer at 2500r / min and vibrate for 160min, fully hydrate, ...

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PUM

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Abstract

The invention discloses a preparation method of estrogen liposome, which comprises dissolving estrogen, lecithin, cholesterol and vitamin E in an organic solvent with a volume ratio of methanol: chloroform = 1: 2 to form a uniform mixed solution. Rotary evaporation and vacuum suction remove the organic solvent, and then hydrate with a phosphate buffer solution with a pH of 7.0 to 7.4. The phospholipids spontaneously form a lipid bilayer in the water phase, and estrogen inserts into the phospholipid bimolecular membrane to form a stable of emulsion. Then, use an emulsifier to cut for 90 to 150 minutes at a speed of 7000 to 9000 r / min, and then use a polycarbonate filter membrane to squeeze through a liposome extruder to obtain estrogen lipids with a particle size of about 170 ± 30 nm. plastid. Because the phospholipid bilayer membrane is used as the carrier material, the fat-soluble estrogen can be spontaneously wrapped in the phospholipid bilayer, avoiding the addition of excipients and plasticizers, and the preparation method is simple.

Description

technical field [0001] The invention relates to a preparation method of estrogen liposome. Background technique [0002] The document "Chinese Patent Publication No. CN1378840" discloses a sustained-release composition of conjugated estrogen drugs and a preparation method thereof. The composition includes a drug core and a sustained-release layer. The drug core contains conjugated estrogen, and the drug core is sustained-release Layer coating to form a coating film, when the above-mentioned conjugated estrogen drug slow-release composition is in contact with the aqueous liquid in the gastrointestinal tract, the conjugated estrogen and progesterone can be released uniformly. In order to facilitate the production of the drug core, an inert excipient is added therein, and a plasticizer is added to the coating film. Due to the addition of excipients and plasticizers, the proportion of active estrogen ingredients in the forming agent is relatively small, and the preparation meth...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/565A61K47/24
Inventor 陈涛卢婷利陈云商澎胡惠静马玉樊
Owner NORTHWESTERN POLYTECHNICAL UNIV
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