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Ursolic acid pills and preparation method thereof

A technology of ursolic acid and dripping pills, which is applied in the direction of pill delivery, can solve the problems of ursolic acid dissolution barriers, etc., and achieve the effect of rapid dissolution, good shape and high dissolution rate

Inactive Publication Date: 2012-10-24
SHANDONG ACAD OF CHINESE MEDICINE +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although the preparation process and formula of the above-mentioned drop pills have improved the dissolution rate of the drug to varying degrees, the dissolution rate of ursolic acid is still an obstacle in the application of ursolic acid, and it is necessary to further make the drops by finding a suitable matrix or preparation process. Further increase in pill dissolution rate

Method used

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  • Ursolic acid pills and preparation method thereof
  • Ursolic acid pills and preparation method thereof
  • Ursolic acid pills and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Take 0.5022g of poloxamer 188 and 0.4973g of ursolic acid, mix the two, then add 3 drops of Tween-80, and grind them into fine powder, so that ursolic acid is evenly dispersed in poloxamer 188, Then add 1.3977g PEG4000 and 0.9851g PEG6000, grind them evenly, transfer them to a beaker, melt them in a water bath at 80°C, and use dimethyl silicone oil as the condensate for dripping. The upper 20cm of silicone oil in the condensate is about 50°C. The lower end 25cm of silicone oil is about 20°C. The obtained dropping pills are round in shape, milky white in appearance and well formed.

[0025] Adopt above-mentioned method to prepare three batches of dripping pills continuously, its outward appearance quality is as follows:

[0026] (1) Appearance: milky white pellets, round shape, uniform pellet size, uniform color, moderate hardness.

[0027] (2) Quality difference and dissolution time: According to the provisions of the second appendix of the 2010 edition of the Pharmac...

Embodiment 2

[0030] Take 10g of poloxamer 188 and 10g of ursolic acid, mix the two, then add 1-1.5g of Tween-80 dropwise, and grind them into fine powder, so that ursolic acid can be evenly dispersed in poloxamer 188, Then add 20g of PEG4000 and 20g of PEG6000, grind them evenly, transfer them to a beaker, melt them in a water bath at 80°C, and use dimethyl silicone oil as the condensate for dripping. Silicone oil is about 20°C. The obtained dropping pills are round in shape, milky white in appearance and well formed.

Embodiment 3

[0032] Take 10g of poloxamer 188 and 10g of ursolic acid, mix the two, then drop in 1.5-1.8g of Tween-80, and grind them into fine powder, so that ursolic acid can be evenly dispersed in poloxamer 188, Then add 40g of PEG4000 and 20g of PEG6000, grind them evenly, transfer them to a beaker, melt them in a water bath at 80°C, and use dimethyl silicone oil as the condensate for dripping. Silicone oil is about 20°C. The obtained dropping pills are round in shape, milky white in appearance and well formed.

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Abstract

The invention discloses ursolic acid pills and a preparation method thereof. The ursolic acid pills comprise an ursolic acid active ingredient and a substrate, wherein the substrate is a mixture of polyethylene glycol and poloxamer, and the mass ratio of ursolic acid to substrate is 1:(4-15). Under the cooperative and synergetic effects of different substances, the dissolution property of the ursolic acid pills is greatly improved. The dissolution rate of the prepared ursolic acid pills within 15 minutes can be up to 95% or so; thus, compared with the ursolic acid pills reported at present, the ursolic acid pills disclosed by the invention have the advantages of higher dissolution speed and higher dissolution rate; and the ursolic acid pills disclosed by the invention also have the advantages of simple preparation process, stable quality and favorable forming property, and is suitable for industrial mass production.

Description

technical field [0001] The invention relates to a traditional Chinese medicine drop pill preparation and a preparation method thereof, in particular to a drop pill preparation with ursolic acid as the main active ingredient and a preparation method thereof. Background technique [0002] Ursolic acid, alias ursolic acid, ursolic acid, molecular formula C 30 h 48 o 3 , the molecular weight is 456.68. Ursolic acid is a colorless needle-like crystal, insoluble in water and petroleum ether, soluble in methanol, ethanol, chloroform, ether, ethyl acetate and acetone, etc., with a melting point of 285-287°C. According to reports, ursolic acid has the effects of anti-hepatitis, anti-tumor, anti-oxidation, antibacterial, anti-inflammatory, anti-virus, anti-atherosclerosis, lowering blood fat, and lowering blood sugar. Some preparations with ursolic acid as active ingredients have also been public. Because the solubility of ursolic acid in water is very small, the dissolution rat...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/20
Inventor 闫雪生徐新刚生立嵩李义召于蓓蓓
Owner SHANDONG ACAD OF CHINESE MEDICINE
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