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Nano-micro structure silibinin drug composite powder and preparation method thereof

A technology of compound powder and silibinin, which is applied in the directions of drug combination, pharmaceutical formulation, powder delivery, etc., can solve the problems of large drug particles, expensive equipment, complicated operation process, etc., and achieves simple composition, easy operation and process. simple effect

Active Publication Date: 2010-07-21
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this method can well control the particle size of silibinin particles at about 10 μm, the equipment cost is expensive, the operation process is cumbersome, and the prepared drug particles are relatively large.

Method used

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  • Nano-micro structure silibinin drug composite powder and preparation method thereof
  • Nano-micro structure silibinin drug composite powder and preparation method thereof
  • Nano-micro structure silibinin drug composite powder and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A: Weigh 1g of silibinin bulk drug and dissolve it in 33.3ml of acetone;

[0039] B: Weigh 18.9g of polyethylene glycol and 0.10g of sodium dodecylbenzenesulfonate and dissolve it in 166.5ml of water, put the beaker containing the aqueous solution in an ice-water bath, and control the temperature of the aqueous solution at about 3°C;

[0040] C: under the stirring condition of 2000rpm, pour the crude drug solution prepared in step A into the aqueous solution of step B to obtain a silibinin nanosuspension;

[0041] D: Control spray drier (SD-Basic, Labplant, UK) inlet temperature is 100 ℃, outlet temperature is 60 ℃, feed rate is 5ml / min, compressed air pressure is 0.6MPa, silybin nano-suspension The solution was spray-dried to obtain nano-microstructure silibinin drug composite powder.

[0042]After the composite powder is dispersed in water, the average particle diameter of the particles is 895.1 nm.

Embodiment 2

[0044] A: Weigh 1g of silibinin bulk drug and dissolve it in 100ml of ethanol;

[0045] B: Weigh 0.5g poloxamer and 0.5g sodium stearate and dissolve in 2000ml water, place the aqueous solution in a constant temperature water bath, and control the temperature of the aqueous solution at about 10°C;

[0046] C: under the stirring condition of 1500rpm, pour the crude drug solution prepared in step A into the aqueous solution of step B to obtain a silibinin nanosuspension;

[0047] D: Control spray drier (SD-Basic, Labplant, UK) inlet temperature is 160 ℃, outlet temperature is 90 ℃, feed rate is 40ml / min, compressed air pressure is 0.8MPa, silybin nano-suspension The solution was spray-dried to obtain nano-microstructure silibinin drug composite powder.

[0048] After the composite powder is dispersed in water, the average particle size of the particles is 774.6nm.

Embodiment 3

[0050] A: Weigh 1g of silybin raw material and dissolve it in 50ml of acetone;

[0051] B: Dissolve 5g of polyvinylpyrrolidone and 0.02g of sodium lauryl sulfate in 500ml of water, place the water solution in a constant temperature water bath, and control the temperature of the solution at about 3°C;

[0052] C: under the stirring condition of 1000rpm, pour the crude drug solution prepared in step A into the aqueous solution of step B to obtain a silibinin nanosuspension;

[0053] D: Control spray drier (SD-Basic, Labplant, UK) inlet temperature is 140 ℃, outlet temperature is 71 ℃, feed rate is 20ml / min, compressed air pressure is 0.6MPa, silybin nano-suspension The solution was spray-dried to obtain nano-microstructure silibinin drug composite powder.

[0054] The composite powder can form a colloid after being dispersed in water, the average particle size of the particles is 71.4nm, and the polydispersity index is 0.103.

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Abstract

The invention relates to a nano-micro structure silibinin drug composite powder and a preparation method thereof. The silibinin drug is dissolved into an organic solvent which is mutually soluble with the water, the mixture is added into a water solution containing water-solubility pharmaceutical excipients to obtain nano silibinin drug particle injectable suspension, the injectable suspension is atomized and dried to obtain the nano-micro structure silibinin drug composite powder. The composite powder has good redispersibility and is dispersed in the water to obtain the uniform injectable suspension with the grain diameter of the drug being less than 1000 nm. The method has simple operation, low cost and promising industrialized production prospect. The powder has fast dissolution rate and high biological utilization rate, and can be used for preparing tablet, capsule, granules or suspensions.

Description

Technical field: [0001] The invention relates to a nano-microstructure silybin medicine composite powder and a preparation method thereof, belonging to the field of medicine preparation. Background technique: [0002] Silybin (Silybin), the chemical name is 2,3-dihydro-3-(4-hydroxy-3-methoxyphenyl)-2-hydroxymethyl-6-(3,5,7-tri Hydroxy-4-oxobenzopyran-2-yl)benzodioxane, its structural formula is: [0003] [0004] It is a kind of flavonoid compound extracted from the fruit of milk thistle of Compositae plant. It has obvious protection and stabilizing effect on liver cells, and has different degrees of therapeutic effects on various liver diseases. It is widely used in clinical Chronic hepatitis, liver fibrosis, early cirrhosis, fatty liver, etc. [0005] Silybin is insoluble in water, the dissolution rate is slow, and oral absorption is poor, resulting in low bioavailability. Most of the research on improving the bioavailability of silybin focuses on the development of n...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/357A61P1/16
Inventor 陈建峰张志兵王洁欣乐园沈志刚赵宏
Owner BEIJING UNIV OF CHEM TECH
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