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Preparation method of oridonin liposome modified with ferritin

A technology of grass A lipid and ferritin, which is applied in the direction of liposome delivery, medical preparations containing non-active ingredients, medical preparations containing active ingredients, etc., can solve the limitation of oridonin A clinical application Membrane adhesion, short biological half-life, etc., to prevent local irritation, improve solubility and dissolution speed, and high absorption rate

Inactive Publication Date: 2016-05-18
张静
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The technical problem mainly solved by the present invention: Aiming at the current problem that Rubescensin A is insoluble in water, has low absorption rate, and short biological half-life in vivo, which limits the clinical application of Rubescensin A, a ferritin-modified Rubescensin A is provided. The preparation method of grass A liposome, the present invention first prepares Oridonin A liposome suspension, then extracts ferritin from pig blood, adds organic solvent after mixing, evaporates under reduced pressure to obtain transparent fat, adds After the phosphate buffer solution is shaken, ultrasonically treated, and freeze-dried, the product prepared by the present invention has a small particle size, improved solubility and dissolution speed in water, high absorption rate, biofilm adhesion, and can be extended The action time of the drug in the body, and the distribution of the drug is even, to prevent local stimulation caused by excessive local concentration. It is mainly used clinically for the treatment of liver cancer, esophageal cancer, leukemia, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 1

[0025] First, weigh 100g of Radix radix stems and 100g of Radix radix leaves, chop them into pieces, add absolute ethanol at a solid-to-liquid ratio of 1:10 for reflux extraction for 2 hours, extract 2 times and combine the extracts under 0.08MPa pressure Distill the extract under reduced pressure to 5% of the original volume to obtain a concentrated solution; add 3 g of lecithin, 0.5 g of cholesterol and 150 mL of absolute ethanol to the prepared concentrated solution, and then add 500 mL of a phosphate buffer solution with a pH of 7.3, and mix After homogenization, concentrate under reduced pressure at 50°C to 1 / 10 of the original volume. After concentration, use a high-speed shearer to pre-disperse at 8000r / min for 15 minutes. After treatment, use a high-pressure homogenizer at 200bar and 400bar respectively Homogenize 3 times under the pressure of 1000bar, homogenize 10 times under 1000bar pressure, obtain Rubescensin A liposome suspension, and add suspension quality 3% glu...

example 2

[0028]First, weigh 150g of Radix radix stems and 150g of Radix radix leaves, chop them into pieces, add absolute ethanol at a solid-to-liquid ratio of 1:10 to carry out reflux extraction for 2.5 hours, extract 2 times, combine the extracts, and extract them under a pressure of 0.085MPa The extract was distilled under reduced pressure to 6% of the original volume to obtain a concentrated solution; 4 g of lecithin, 0.7 g of cholesterol and 175 mL of absolute ethanol were added to the prepared concentrated solution, and then 550 mL of a phosphate buffer solution with a pH of 7.3 was added. After mixing evenly, concentrate under reduced pressure at 55°C to 1 / 10 of the original volume. After concentration, use a high-speed shearing machine to pre-disperse at 9000r / min for 17 minutes, and then use a high-pressure homogenizer at 200bar and 400bar after treatment. Homogenize 4 times under pressure, homogenize 13 times under 1000bar pressure, obtain Oridonin A liposome suspension, and a...

example 3

[0031] First, weigh 200g of Radix radix stems and 200g of Radix radix leaves, chop them into pieces, add absolute ethanol at a solid-to-liquid ratio of 1:10 to carry out reflux extraction for 3 hours, extract 3 times and combine the extracts under a pressure of 0.09MPa Distill the extract under reduced pressure to 8% of the original volume to obtain a concentrated solution; add 5 g of lecithin, 0.9 g of cholesterol and 200 mL of absolute ethanol to the prepared concentrated solution, and then add 600 mL of a phosphate buffer solution with a pH of 7.3, and mix After homogenization, concentrate under reduced pressure at 60°C to 1 / 10 of the original volume. After concentration, use a high-speed shearer to pre-disperse at a speed of 10,000r / min for 20 minutes. Homogenize 5 times under 1000bar pressure, homogenize 15 times under 1000bar pressure, obtain Oridonin A liposome suspension, and add suspension quality 4% glucose as freeze-drying protective agent, after shaking and dissolvi...

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Abstract

The invention discloses a preparation method of oridonin liposome modified with ferritin and belongs to the field of medicament. The preparation method comprises the steps that firstly, oridonin liposome turbid liquid is prepared, then the ferritin is extracted out of pig blood, after mixing is conducted, organic solvent is added, pressure reduction evaporation is conducted, transparent grease is obtained, a phosphate buffer solution is added, shaking table oscillation, ultrasonic treatment and freeze-drying are conducted, and the oridonin liposome modified with the ferritin is obtained. A product prepared through the method is small in particle size, solubility and the dissolving speed in water are raised, the absorption rate is high, biomembrane adhesion is achieved, action time of medicine in the human body can be prolonged, the medicine is distributed uniformly, local irritation caused by overhigh local concentration is prevented, and the oridonin liposome is clinically mainly used for treating liver cancer, esophagus cancer, leukemia and the like.

Description

technical field [0001] The invention discloses a preparation method of ferritin-modified oridonin A liposome, which belongs to the field of pharmaceuticals. Background technique [0002] Dongling grass is a herbaceous plant of the Lamiaceae family, whose stems and leaves can be used as medicine. The plant is widely distributed in the provinces south of the Yellow River Basin, and Jiyuan, Henan Province is the main producing area of ​​the plant. Donglingcao has the effects of clearing heat and detoxifying, reducing inflammation and relieving pain, invigorating the stomach, activating blood circulation and anti-tumor. [0003] Oridonin A, also known as Oridonin, Yanming Cao Ning, is the main active ingredient of Oridonin. Oridonin A is a 7,20-epoxy-type ent-kaurane diterpenoid compound, which is a light yellow needle-like crystal with a very bitter taste, slightly soluble in water, soluble in methanol, ethyl acetate, acetone Modern pharmacology and toxicology studies have s...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/352A61K47/42A61P35/00A61P35/02A61K36/53A61K47/64A61K47/69
CPCA61K9/1271A61K9/1277A61K31/352A61K36/53A61K47/42A61K2236/333A61K2236/39
Inventor 张静王志慧
Owner 张静
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