Rabdosia rubescens A microglobule medicinal agent and its preparation method

A technology of Rubescensin A and its preparation, which is applied in the field of medicine and can solve the problems of low water solubility of Rubescensin A, low encapsulation efficiency, and low drug loading capacity of emulsions, etc.

Inactive Publication Date: 2005-10-26
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For Rubescensin A emulsion, someone has applied for a patent (Chinese patent, application number: 200310110304.5), and we have also made Rubescensin A into an emulsion, but there is a problem: Rubescensin A is not water-soluble, but It has certain water solubility (we measured that the equilibrium solubility in distilled water at room temperature is close to 1mg/mL), and the drug is highly polar and almost insoluble in fatty acid glycerides such as soybean oil, so the prepared emulsion has a very low drug load. And the encapsulation rate is low, less than 10%
Oridonin A was made into liposomes, and after prescription optimization, the drug loading and encapsulation efficiency were satisfactory, but the

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Preparation of Oridonin A liposome:

[0042] prescription:

[0043]Oridonin 0.5g

[0044] Soy Lecithin 3.0g

[0045] Cholesterol 0.6g

[0046] Vitamin E 0.05g

[0047] 5% sucrose solution to 100mL

[0048] Preparation process: Weigh the prescription amount of Rubescensin A, soybean lecithin, cholesterol and vitamin E, dissolve in 20mL of chloroform-methanol (8:2), transfer to a 1000mL eggplant-shaped bottle, place in a constant temperature water bath at 30°C, and use The organic solvent was removed under reduced pressure by a rotary thin film evaporator, and a uniform lipid film was formed on the bottle wall. Add the prescribed amount of sucrose solution, hydrate for 1 hour, and shake to obtain a liposome suspension. Ultrasound the suspension for 10 minutes (500W) with a probe sonicator to obtain an opalescent liquid, pass the liquid through a 0.2 μm filter membrane and freeze-dry to obtain a powder injection.

Embodiment 2

[0050] Preparation of Oridonin A liposome:

[0051] prescription:

[0052] Oridonin 0.5g

[0053] Soy Lecithin 3.0g

[0054] Cholesterol 0.6g

[0055] Vitamin E 0.05g

[0056] 2% dextran solution to 100mL

[0057] Preparation process: Weigh the prescribed amount of oridonin, soybean lecithin, cholesterol and vitamin E and dissolve them in 50mL of ethanol, inject 100mL of 2% dextran solution at 80°C with a syringe (No. 4.5 needle), and stir while injecting After adding the ethanol solution, continue to stir at 80°C for 0.5h, then continue to stir at room temperature for 2h, dilute the obtained suspension to 100mL with water for injection, and pass through a high-pressure homogenizer (YSNM-1500-0005 Nanomizer at 100MPa) : Japan Yoshida Kikai) 5 times to get the liposome suspension with opalescence, and this suspension is freeze-dried to get powder injection.

Embodiment 3

[0059] Preparation of oridonin A lipid nanoparticles:

[0060] prescription:

[0061] Oridonin 0.5g

[0062] Soy Lecithin 3.0g

[0063] Glyceryl monostearate 5.0g

[0064] Poloxamer 188 2.0g

[0065] 2.5% glycerol solution to 100mL

[0066] Preparation process: Dissolve the prescribed amount of poloxamer 188 in 100mL 2.5% glycerin solution and preheat it at 80°C as the water phase for later use, then add the prescribed amount of oridonin, glyceryl monostearate and soybean lecithin An appropriate amount of absolute ethanol was heated and dissolved as the oil phase and placed in a water bath at 80°C, and the water phase was added while stirring, and then stirred with a high-speed homogenizer for 3 minutes to obtain a rough milk, and passed through a high-pressure milk homogenizer (YSNM-1500-0005 Nanomizer) while it was hot. : Japan Yoshida Kikai company) 100MPa, 6 times, let cool and get the lipid nanoparticle suspension with opalescence. Divid...

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Abstract

A medicine for intravenous injection includes the powder injection of rebescensine A liposome prepared from medicine, coating material, film stabilizer, antioxidizing agent and water-soluble carrier, and the lipid nanoparticles of rebescensine A prepared from medicine, lipid, emulsifier, emulsifying aid and water-soluble carrier. Its preparing process is also disclosed.

Description

Technical field: [0001] The invention relates to the field of medical technology, in particular to a stable and safe oridonin microparticle drug preparation and a preparation method thereof, including oridonin A liposomes and lipid nanoparticles and a preparation method thereof. Background technique: [0002] Oridonin is widely used as an anti-inflammatory and anti-cancer drug in Henan and other places. Oridonin A is the main anti-cancer component. Oridonin A has poor water solubility and cannot be directly formulated into an aqueous solution for use. Injection requirements, Zhengzhou Chemical Pharmaceutical Factory once solubilized oridonin with Tween 80 and propylene glycol for anti-cancer clinical use, but Tween 80 is easy to hemolysis when used for intravenous injection, and its use has been discontinued in developed countries. [0003] Microparticle drug delivery preparations are emerging drug delivery systems in recent years, mainly including liposomes, emulsions, nano...

Claims

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Application Information

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IPC IPC(8): A61K31/352
Inventor 何仲贵徐文孙进孙英华
Owner SHENYANG PHARMA UNIVERSITY
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