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Ursolic acid fat emulsion injection and its prepn

A technology of milk injection and ursolic acid, which is applied in the direction of anti-inflammatory agents, pharmaceutical formulas, emulsion delivery, etc., can solve the problems of ineffective bioavailability and low water solubility, so as to avoid the first-pass effect, complete absorption, The effect of improving bioavailability

Inactive Publication Date: 2006-05-17
广东天之骄药物开发有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ursolic acid is a strongly hydrophobic drug with low water solubility, and the use of general pharmaceutical methods cannot effectively solve the problem of bioavailability. For this reason, someone has declared a related freeze-dried powder injection of ursolic acid: ursolic acid cyanide Acrylic acid ester nano particle freeze-dried powder injection and preparation method (application number is CN02147712.4), ursolic acid soybean lecithin nano particle freeze-dried powder injection and preparation method (application number is CN02147711.6), ursolic acid polylactic acid nano Granular freeze-dried powder injection and preparation method (application number is CN02147713.2)
Although freeze-dried powder injection solves the problem of bioavailability, it has certain limitations in the role of sustained release and targeted drug delivery, especially for patients who are weak after tumor surgery and need to be given a certain amount of energy.

Method used

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  • Ursolic acid fat emulsion injection and its prepn

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Pulverize the ursolic acid so that the particle size of the ursolic acid is less than 80 μm, weigh 100 mg of the pulverized ursolic acid and put it into a container; add 50 g of soybean oil for injection, place the container in a water bath, and heat it to 100° C. Stir until the drug is dispersed, cool down to 80°C, add 25 g of lecithin and 100 mg of vitamin E, and stir until the phospholipid is dissolved to form a uniform mixed phase. Place 800ml of water for injection in another container, add 40g of povidone, 25g of glycerol and 25g of lecithin, stir and dissolve at 80°C to form an aqueous phase; put the mixture containing ursolic acid, soybean oil and lecithin at 80°C, Mix with water containing glycerin, povidone (PVP) and lecithin under mechanical stirring, and adjust the pH value to 6.5-7.0 with 1% sodium hydroxide; add water for injection to 1000ml, and continue mechanically at 80°C Stir for 1 hour to make colostrum, disperse the obtained colostrum by a high-spee...

Embodiment 2

[0027] Pulverize the ursolic acid so that the particle size of the ursolic acid is less than 80 μm, weigh 100 mg of the pulverized ursolic acid and put it into a container; add 50 g of soybean oil for injection, place the container in a water bath, and heat it to 100° C. Stir until the drug is dispersed, cool down to 80°C, add 5 g of lecithin and 100 mg of vitamin E, and stir until the phospholipid is dissolved to form a uniform mixed phase. Place 800ml of water for injection in another container, add 10g of povidone, 20g of glycerol and 5g of lecithin and stir to dissolve at 80°C to form an aqueous phase; the mixture containing ursolic acid, soybean oil and lecithin is heated at 80°C, Mix with water containing glycerin, povidone (PVP) and lecithin under mechanical stirring, and adjust the pH value to 6.5-7.0 with 1% sodium hydroxide; add water for injection to 1000ml, and continue mechanically at 80°C Stir for 1 hour to make colostrum, disperse the obtained colostrum by a hig...

Embodiment 3

[0031]Pulverize ursolic acid so that the particle size of ursolic acid is less than 80 μm, weigh 100 mg of pulverized ursolic acid and put it into a container; add 100 g of soybean oil for injection, place the container in a water bath, and heat it to 100 ° C. Stir until the drug is dispersed, lower the temperature to 80°C, add 6g of lecithin and 100mg of vitamin E and stir until the phospholipid dissolves to form a uniform mixed phase. Put 800ml of water for injection in another container, add 10g of polyethylene glycol, 22g of glycerin and 6g of lecithin and stir to dissolve at 80°C to form a water phase; put the mixed solution containing ursolic acid, soybean oil and lecithin at 80°C , Mix with water containing glycerin, polyethylene glycol and lecithin under mechanical stirring, and adjust the pH value to 6.5-7.0 with 1% sodium hydroxide; add water for injection to 1000ml, and continue mechanical stirring at 80°C for 1 The colostrum is made within an hour, dispersed by a h...

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Abstract

The present invention relates to one kind of ursolic acid fat emulsion injection and its preparation. The fat emulsion consists of ursolic acid as active component and medicinal supplementary material, and consists of ursolic acid 0.01-0.15 wt%, oil for injection 5-30 wt%, emulsifier 1-9 wt%, solubilizer 1-6 wt%, isosmotic agent 2-2.5 wt%, and antioxidant 0.01-0.03 wt%, except water for injection. The present invention has simple preparation process, and the injection may be used clinically in intravenous injection, and has high bioavailability, high stability, raised treating effect, slow releasing and targeting effect, and energy providing effect.

Description

technical field [0001] The invention relates to a medicinal fat emulsion injection, in particular to a ursolic acid fat emulsion injection and a preparation method thereof. Background technique [0002] Ursolic acid is a pentacyclic triterpenoid that exists in natural plants. It exists in many plants in the form of free and glycosides. Ursolic acid is also known as ursolic acid and ursolic acid. , mainly exists in reed, plantain, hawthorn leaves, privet (leaf), rhododendron leaves and other plants, and also exists in traditional Chinese medicine dogwood, prunella, hawthorn, etc., and is one of the active ingredients of these traditional Chinese medicines. At present, the raw materials of ursolic acid in China are mainly extracted from plants such as privet leaves, hawthorn leaves and dogwood. The high-purity ursolic acid component is a light green powder with a special characteristic odor, insoluble in water, soluble in ethanol, and free of foreign matter after dissolving. ...

Claims

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Application Information

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IPC IPC(8): A61K31/56A61K9/107A61P1/02A61P1/04A61P3/10A61P29/00A61P31/04A61P35/00
Inventor 刘永宏韩宇萍吴才梅
Owner 广东天之骄药物开发有限公司
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