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Cycloartenyl ferulate composition and method for preparing the same

A technology of pineapplenyl ferulic acid ester and composition, which is applied in the field of cycloartenyl ferulic acid ester composition and its preparation, and can solve the problems of slow onset of action, low absorption rate, difficult quality control, etc.

Inactive Publication Date: 2009-07-15
BEIJING CENTURY BIOCOM PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Oryzanol is insoluble in water and easily oxidized, which makes it difficult to make oryzanol into a stable preparation
The isolated cycloartenol ferulic acid ester has poorer solubility and stability under conventional preparation methods
Very low solubility and easy oxidation not only lead to low absorption rate, but also difficult to control the quality in production
Some technical schemes for solving the solubility problem of oryzanol are provided in the prior art, such as CN123428, CN2007100156403, CN2004100945568 etc. disclose technical schemes for improving the solubility of oryzanol, but these schemes have their own defects on the one hand, such as when oil-soluble preparations are used clinically Patients have a strong sense of pain, which can easily lead to muscle agglomeration and slow onset of action; the cost of liposomes is high, and the quality of the production process is not easy to control, etc.
On the other hand these schemes also do not relate to how to solve the solubility problem of cycloartenol ferulic acid ester

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Cycloartenol Ferulate 10mg

[0042] Egg yolk phospholipids 50mg

[0043] Hyodeoxycholic Acid 50mg

[0044] Glucose 100mg

[0045] Water for injection to 10ml

[0046] Dissolve cycloartenol ferulate, egg yolk phospholipid, and hyodeoxycholic acid in 3ml of ethyl acetate, heat to 80°C and stir until fully dissolved. Distilled by evaporation under reduced pressure to obtain an organic phase. Add the water for injection in which the glucose is dissolved to the full amount, stir and mix well at 60°C to obtain the injection solution of the present invention. Adjust the pH to 8.3 with sodium hydroxide solution, add 0.05% activated carbon for injection and stir for 30 minutes, decarburize and filter, perform fine filtration with a 0.22um microporous membrane, and pack into vials.

Embodiment 2

[0048] Cycloartenol Ferulate 10mg

[0049] Soy Lecithin 1000mg

[0050] Chenodeoxycholic Acid 800mg

[0051] Mannitol 200mg

[0052] Water for injection to 10ml

[0053] Dissolve cycloartenol ferulate, chenodeoxycholic acid, and soybean lecithin in 7ml of dichloromethane, heat to 80°C and stir until fully dissolved. Distilled by evaporation under reduced pressure to obtain an organic phase. Add water for injection in which mannitol has been dissolved to the full amount, and fully stir and mix at 70° C. to obtain the injection solution of the present invention. Adjust the pH to 8.0 with sodium hydroxide solution, add 0.05% activated carbon for injection and stir for 30 minutes. After decarbonization and filtration, perform fine filtration with a 0.22um microporous filter membrane, and then pack into vials.

Embodiment 3

[0055] Cycloartenol Ferulate 1mg

[0056] Soy sphingomyelin 500mg

[0057] Glycocholic Acid 400mg

[0058] Ethylene glycol 100mg

[0059] Glycine. 20mg

[0060] Water for injection to 10ml

[0061] Dissolve cycloartenol ferulate, soybean sphingomyelin, glycocholic acid, ethylene glycol, and glycine in 10ml of ethyl acetate, heat to 80°C and stir until fully dissolved. The organic phase was obtained by distillation under reduced pressure. Add water for injection to the organic phase to the full amount, and fully stir and mix at 60°C to obtain the injection solution of the present invention. Adjust the pH to 7.6 with sodium hydroxide solution, add 0.05% activated carbon for injection and stir for 30 minutes, after decarburization and filtration, perform fine filtration with a 0.22um microporous filter membrane, and pack into vials.

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PUM

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Abstract

The invention discloses a pharmaceutical composition of cycloartenyl ferulate oryzanolum, which comprises cycloartenyl ferulate oryzanolum, phospholipid, bile acid and / or salt of bile acid. The pharmaceutical composition effectively improves the water solubility and the stability of the cycloartenyl ferulate oryzanolum and has better grain diameter and stability than the prior product, and further, the invention provides three product forms including injectio, freeze-dried powder and kits of the pharmaceutical composition, and preparation methods thereof.

Description

technical field [0001] The invention relates to a composition. Specifically, the invention discloses a cycloartenol ferulic acid ester composition for injection and a preparation method thereof, belonging to the field of medicine. Background technique [0002] Oryzanol is a natural mixture composed of cycloartenol-based ferulic acid esters and sterol-based ferulic acid esters. The appearance is white to light yellow crystalline powder, odorless, and has a specific fragrance. Oryzanol mainly exists in hair bran oil and its oil feet. In rice bran oil oryzanol, the content of cycloartenol ferulate is about 70-80%. Long-term studies have found that oryzanol has a variety of physiological functions, mainly including: lowering blood lipids, resisting the absorption of cholesterol, lowering serum cholesterol, preventing lipid oxidation and preventing cardiovascular diseases. In addition, oryzanol can alleviate various physical disorders and autonomic nervous disorders in women af...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61K47/24A61P9/00A61P3/06A61P15/12
Inventor 郝守祝焦玉焕
Owner BEIJING CENTURY BIOCOM PHARMA TECH
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