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Austocystin D free-drying powder and preparation method thereof

A freeze-drying and powder technology, applied in the field of medicine, can solve problems such as low bioavailability

Inactive Publication Date: 2012-07-11
HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since Austocystin D is a water-insoluble compound, there is no technology that can reduce its toxicity, improve its curative effect and solve the problem of its low bioavailability.

Method used

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  • Austocystin D free-drying powder and preparation method thereof
  • Austocystin D free-drying powder and preparation method thereof
  • Austocystin D free-drying powder and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Austocystin D 50mg,

[0026] Phospholipids 3.0g,

[0027] Cholesterol 250mg,

[0028] Absolute ethanol 90ml

[0029] Water for injection 60ml

[0030] Lactose 3.0g;

[0031] a. Preparation of phospholipid film: Take Austocystin D, phospholipid, and cholesterol, add absolute ethanol to dissolve, 40°C, 0.09MPa reduced pressure rotary steaming for 40min, and form a uniform lipid film on the wall of the flask, set aside;

[0032] b. Hydration: add water for injection, shake, hydrate into light yellow suspension, set aside;

[0033] c. Ultrasound: ultrasonically treat the suspension obtained in step b at 200W and 25KHz for 4 minutes to obtain the Austocystin D suspension, filter it through a 0.22 μm microporous membrane, and pot it under nitrogen protection to obtain the Austocystin D composition suspension, which is ready for use;

[0034] d. Freeze-drying: add lactose to the Austocystin D composition suspension obtained in step c and freeze-dry to obtain the Austo...

Embodiment 2

[0037] Austocystin D 50mg,

[0038] Phospholipids 2.0g,

[0039] Cholesterol 400mg,

[0040] Absolute ethanol 100ml,

[0041] Water for injection 40ml,

[0042] Lactose 2.0g,

[0043] a. Preparation of phospholipid film: Take Austocystin D, phospholipid, and cholesterol, add absolute ethanol to dissolve, 50°C, 0.06MPa reduced pressure rotary steaming for 120min, and form a uniform lipid film on the wall of the flask, set aside;

[0044] b. Hydration: add water for injection, shake, hydrate into light yellow suspension, set aside;

[0045] c. Ultrasound: Ultrasonic treatment of the suspension obtained in step b at 600W and 20KHz for 10 minutes to obtain the suspension of Austocystin D, filtered through a 0.22 μm microporous membrane, potted under nitrogen protection, to obtain the suspension of the Austocystin D composition, and set aside;

[0046] d. Freeze-drying: add lactose to the Austocystin D composition suspension obtained in step c and freeze-dry to obtain the ...

Embodiment 3

[0049]Austocystin D 50mg,

[0050] Phospholipids 4.0g,

[0051] Cholesterol 250mg,

[0052] 120ml absolute ethanol,

[0053] pH6.8 Phosphate Buffer 40ml,

[0054] Lactose 2.0g,

[0055] a. Preparation of phospholipid film: Take Austocystin D, phospholipid, and cholesterol, add absolute ethanol to dissolve, 45°C, 0.05MPa reduced pressure rotary steaming for 80min, and form a uniform lipid film on the wall of the flask, set aside;

[0056] b. Hydration: add pH6.8 phosphate buffer, shake, hydrate into light yellow suspension, set aside;

[0057] c. Ultrasound: Ultrasonically treat the suspension obtained in step b at 400W and 25KHz for 8 minutes to obtain the Austocystin D suspension, filter through a 0.22 μm microporous membrane, and potting under nitrogen protection to obtain the Austocystin D composition suspension, which is ready for use;

[0058] d. Freeze-drying: add lactose to the Austocystin D composition suspension obtained in step c and freeze-dry to obtain the...

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Abstract

An Austocystin D free-drying powder and a preparation method thereof belong to the technical field of medicines. The free-drying powder mainly contains an Austocystin D composition which is composed of Austocystin D, phospholipids and cholesterol according to proportions by weight of 1:20-100:2-10. As the phospholipids and the cholesterol have the characteristics of very good biocompatibility, low toxicity, low irritation and the like, the problem of drug administration of the Austocystin D is solved very well, the active compound Austocystin D has the drug targeting, the bioavailability of the Austocystin D is increased, the toxicity of the Austocystin D can be obviously reduced, and the anti-tumor activity of the Austocystin D is increased.

Description

technical field [0001] The invention relates to a freeze-dried powder and a preparation method thereof, in particular to a freeze-dried powder of a xanone compound Austocystin D from fungi, which belongs to the technical field of medicine. Background technique [0002] Austocystin D is a xanone compound isolated and purified from the solid fermentation product of fungi, and its structure is shown in the figure below. [0003] [0004] In 1974, Steyn PS and others first isolated and purified the compound Austocystin D from the fermentation product of Aspergillus, and there were few reports on its activity after that [Steyn PS, Vleggaar R, J Chem Soc (Perkin I), 1974, 19: 2250-2256] . In vitro experiments have proved that Austocystin D has good anti-tumor activity, especially for multi-drug resistant tumor cell lines, and its activity against MIP101 cells (MDR 1 overexpression) is 1000 times that of SW620 cells (MDR 1 non-expression). times (IC50, 0.001 μg / ml vs 0.9 μg / m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/352A61K47/28A61P35/00
Inventor 高子彬路新华李硕郑智慧张丽男张莉孙勇军谢英花刘磊
Owner HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY