Total bufadienolide solid lipid nanometer particle freeze-dried injection and preparation method thereof

A technology of solid lipid nanometer and total bufolide, applied in the preparation of total bufolide solid lipid nanoparticle freeze-dried injection, solid lipid nanoparticle freeze-dried injection and its preparation, total bufolide In the field of solid lipid nanoparticle freeze-dried injections, it can solve the problems of blood vessel tingling, frequent medication, and fishy smell, and achieve the effects of prolonging biological half-life, improving tumor cell targeting, and reducing toxic and side effects

Active Publication Date: 2015-06-17
HEFEI HUAFANG PHARMA SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current existing dosage forms are ordinary tablets, oral liquids, capsules and injections, etc., which have many disadvantages such as frequent taking, large dosage, fishy smell when taken orally, blood vessel tingling caused by injection, and phlebitis.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The preparation of embodiment 1 total bufolide solid lipid nanoparticles

[0036]Put 2mg of total bufolide, 30mg of glyceryl monostearate, 2mg of stearic acid, and 80mg of lecithin into 1mL of a mixed solution of absolute ethanol and acetone (volume ratio 1:1), and heat to 70°C to form oil Mutually. Add 80mg of Tween 80 into 4mL of water for injection, and heat to 70°C to form the aqueous phase. The oil phase was slowly added dropwise to the water phase, and the whole process was carried out under stirring at 700 rpm. The stirring process continued for 3 hours until the organic solvent evaporated to form colostrum. Pour the colostrum into 10mL of ice water (made from water for injection, a mixture of ice and water at a temperature of 0°C) and stir for 2 hours at a stirring speed of 700rpm to obtain total bufolide solid lipid nanoparticles grain.

[0037] Detection: the average particle size of total bufolide solid lipid nanoparticles is 208.4nm, the polydispersity i...

Embodiment 2

[0038] The preparation of embodiment 2 total bufolide solid lipid nanoparticles

[0039] Put 2 mg total bufolide, 32 mg trimyristin, and 80 mg lecithin into 1 mL of a mixed solution of absolute ethanol and acetone (volume ratio 1:1), and heat to 70°C to form an oil phase. Add 80mg of Tween 80 into 4mL of water for injection, and heat to 70°C to form the aqueous phase. The oil phase was slowly added dropwise to the water phase, and the whole process was carried out under stirring at 700 rpm. The stirring process continued for 3 hours until the organic solvent evaporated to form colostrum. Pour the colostrum into 10mL of ice water (made from water for injection, a mixture of ice and water at a temperature of 0°C) and stir for 2 hours at a stirring speed of 700rpm to obtain total bufolide solid lipid nanoparticles grain.

[0040] Detection: the average particle diameter of total bufolide solid lipid nanoparticles is 211.5nm, the PDI is 0.25, and the encapsulation efficiency is...

Embodiment 3

[0041] The preparation of embodiment 3 total bufolide solid lipid nanoparticles

[0042] Put 2mg of total bufolide, 32mg of beeswax, and 80mg of lecithin into 1mL of a mixed solution of absolute ethanol and acetone (volume ratio 1:1), and heat to 70°C to form an oil phase. Add 80mg of Tween 80 into 4mL of water for injection, and heat to 70°C to form the aqueous phase. The oil phase was slowly added dropwise to the water phase, and the whole process was carried out under stirring at 700 rpm. The stirring process continued for 3 hours until the organic solvent evaporated to form colostrum. Pour the colostrum into 10mL of ice water (made from water for injection, a mixture of ice and water at a temperature of 0°C) and stir for 2 hours at a stirring speed of 700rpm to obtain total bufolide solid lipid nanoparticles grain.

[0043] Detection: the average particle size of total bufolide solid lipid nanoparticles is 215.1nm, the PDI is 0.28, and the encapsulation efficiency is 65...

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Abstract

The invention discloses total bufadienolide solid lipid nanometer particle freeze-dried injection and a preparation method thereof and belongs to field of the solid lipid nanometer particle freeze-dried injection and the preparation method thereof. The invention firstly discloses a total bufadienolide solid lipid nanometer particle which comprises the following components: total bufadienolide, solid lipid, a lipid-soluble emulsifying agent, a water-soluble emulsifying agent and water for injection. The total bufadienolide solid lipid nanometer particle is added with a freeze-drying protective agent and then freeze-dried to obtain the total bufadienolide solid lipid nanometer particle freeze-dried injection. After the total bufadienolide solid lipid nanometer particle freeze-dried injection disclosed by the invention is redissolved, the measured particle size of the total bufadienolide solid lipid nanometer particle is 190nm to 250nm, the polydispersity index is 0.18 to 0.3, the encapsulation efficiency is 30% to 80%, the tumor cell targeting property of the total bufadienolide can be effectively improved, and toxic and side effects are alleviated.

Description

technical field [0001] The invention relates to freeze-dried injections, in particular to total bufolide solid lipid nanoparticles freeze-dried injections, and the invention also relates to a preparation method of said total bufolide solid lipid nanoparticles freeze-dried injections, belonging to solid lipids Nanoparticle freeze-dried injection and its preparation field. Background technique [0002] Total bufolide is a fat-soluble compound extracted from the traditional medicinal material Bufodidae animal Bufo bufo or black-framed toad skin as the main raw material. Bufalin, Bufalin-3-hemisuberin, Bufalin 3-succinyl arginine, Cinobufalin 3-succinyl arginine, etc. The antitumor effect of bufolide compounds has been widely studied and reported at home and abroad since the 1990s. Studies have shown that it has obvious antitumor activity and can transform tumor cells into normal cells (inducing tumor cell differentiation), induce tumor cell apoptosis, inhibit tumor cell angio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/51A61K9/19A61K35/65A61K47/26A61K47/04A61K47/10A61K47/32A61K47/18A61P35/00
Inventor 张亮亮何勇杨贤龙吴宗好
Owner HEFEI HUAFANG PHARMA SCI & TECH
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