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Ursolate microballoon preparation and its preparing process

A technology of ursolic acid and ursolic acid, applied in anti-inflammatory agents, pharmaceutical formulas, non-central analgesics, etc., can solve the problem of lack of ursolic acid microsphere preparations, difficulty in ensuring safety, and affecting bioavailability and other problems, to achieve medical effects and improve the level of medicine, prolong the action time, and reduce the dose

Inactive Publication Date: 2006-11-08
欧苏 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Ursolic acid is almost insoluble in water, and it is difficult to absorb when taken orally, which affects its bioavailability. The oral dosage form is limited and has not been marketed so far.
There are also applications for soy lecithin, stearic acid [02147711.6], cyanoacrylate [02147712.4], polylactic acid [02147713.2] nano-scale freeze-dried powder injection, but organic solvents such as methanol and acetone are used in the production process, and It is difficult to guarantee the safety of cyanoacrylate, polylactic acid, etc.
There is no report of ursolic acid microsphere preparation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Dissolve 22.5g of glycerin, 12.0g of refined soybean lecithin in water for injection, and 0.6g of ursolic acid in refined soybean oil, respectively heat to about 60°C, mix well, first emulsify fractionally in a tissue masher, and then Emulsified by a high-speed homogenizer to meet the particle size of the preparation. Add water for injection to 1000ml, cool, fill, and sterilize to obtain the ursolic acid microsphere preparation. Can be taken orally or intravenously. This process is a 1000ml prescription, and the production can be expanded, and nitrogen protection is required during the production process.

Embodiment 2

[0036] Dissolve 25.0g of sorbitol in water for injection, 10g of refined lecithin, and 1.0g of ursolic acid. Dissolve in refined corn oil, heat to 70°C respectively, mix well, first emulsify fractionally in a tissue masher, and then The high-speed homogenizer emulsifies to meet the particle size of the preparation. Add water for injection to 1000ml, cool down, and fill to obtain the ursolic acid microsphere preparation.

Embodiment 3

[0038] Dissolve 55.5g of xylitol in water for injection, dissolve 12.0g of refined lecithin, and 10.0g of ursolic acid in refined sesame oil, respectively heat to 80°C, mix well, first fractionally emulsify in a tissue masher, and then The high-speed homogenizer emulsifies to meet the particle size of the preparation. Add water for injection to 1000ml, cool down, and fill to obtain the ursolic acid microsphere preparation.

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PUM

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Abstract

The present invention discloses a kind of ursolic acid lipoid microballoon preparation, and each 1000ml of the ursolic acid lipoid microballoon preparation contains ursolic acid 0.2-50.0g, vegetable oil for injection 50-300g, emulsifier 5-20g, isoosmotic regulator 20-60g and water for injection for the rest. Its preparation process includes dissolving, heating, mixing, emulsifying, cooling, filling and other steps. The present invention overcomes the demerit of water insolubility of ursolic acid, and the ursolic acid lipoid microballoon preparation has less toxic reaction, less stimulation, long medicinal acting period and targeting property. The ursolic acid lipoid microballoon preparation has both disease treating effect and energy providing function.

Description

technical field [0001] The invention relates to an ursolic acid microsphere and a preparation method thereof, in particular to an ursolic acid microsphere preparation for anti-tumor and various inflammations and a preparation method thereof. Background technique [0002] Ursolic acid, also known as ursolic acid and ursolic acid, belongs to the a-amyl alcohol type pentacyclic triterpenoids, which are extracted and isolated from Chinese herbal medicines. Modern pharmacological tests have shown that ursolic acid has various pharmacological effects such as anti-tumor, liver damage protection, anti-bacterial and anti-inflammatory, and anti-virus. Not only is it resistant to a variety of carcinogenic and cancer-promoting substances, but it can also inhibit the growth of a variety of malignant tumor cells. It was listed as one of the most promising tumor prevention drugs in Japan in 1990. [0003] Ursolic acid is almost insoluble in water and is difficult to absorb when taken oral...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61K9/16A61P29/00A61P35/00
Inventor 欧苏尹爱梅
Owner 欧苏
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