Oryzanol composition and preparation method thereof

A technology of oryzanol and its composition, which is applied in the field of medicine, can solve the problems of patient pain, poor compliance of muscle agglomeration, poor oral effect of oryzanol, and difficulty in controlling the particle size of emulsion, so as to prolong the time of drug effect, improve bioavailability and Therapeutic index, effect of enhancing bioavailability

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

However, this invention still does not fundamentally solve the disadvantages of intramuscular injection caused by oil-soluble preparations, which can easily lead to patient pain, muscle agglomeration, and poor compliance.
Chinese patent application 2004100945568 discloses a technical scheme in which oryzanol raw materials are combined with cholesterol and phospholipids to prepare liposomes. The preparation of the technical scheme of the invention overcomes the problems of poor oral effect and low bioavailability of oryzanol
However, the injection obtained by this scheme is an injection emulsion, which must include an oil phase, and the particle size of the prepared emulsion is relatively difficult to control, and the stability is relatively poor. During the preparation, equipment such as a milk homogenizer is required, and the operation is relatively complicated and the cost is high.
[0004] In the existing technical scheme, the oil-soluble preparation is actually a semi-solid preparation because the vegetable oil cannot be removed, and the stability at room temperature is relatively poor
Virtually all solutions using vegetable oils for solubilization suffer from poor stability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Oryzanol 10mg

[0044] Phosphatidylcholine 50mg

[0045] Ursodeoxycholic acid 50mg

[0046] Mannitol 50mg

[0047] Water for injection to 10ml

[0048] Oryzanol, phosphatidylcholine and ursodeoxycholic acid were dissolved in 2 ml of ethyl acetate, heated to 60°C and stirred until fully dissolved. The organic phase was obtained by distillation under reduced pressure. The water for injection in which mannitol has been dissolved is added to the full amount, and the injection solution of the present invention is obtained by fully stirring and mixing at 60°C. Adjust the pH to 7.0 with sodium hydroxide solution, add 0.05% activated carbon for injection and stir for 30 minutes, after decarburization and filtration, carry out fine filtration with 0.22um microporous membrane, and then pack it into vials.

Embodiment 2

[0050] Oryzanol 2mg

[0051] Soy Lecithin 800mg

[0052] Phosphatidylcholine 200mg

[0053] Taurocholic acid 200mg

[0054] Lactose 80mg

[0055] Water for injection to 10ml

[0056] Oryzanol, taurocholic acid, soybean lecithin, and phosphatidylcholine were dissolved in 5 ml of ethanol, heated to 80° C. and stirred until fully dissolved. The organic phase was obtained by distillation under reduced pressure. Add water for injection to the full amount, and then add lactose at 60° C. and stir and mix well to obtain the injection of the present invention. Adjust the pH to 7.0 with sodium hydroxide solution, add 0.05% activated carbon for injection and stir for 30 minutes, after decarburization and filtration, carry out fine filtration with 0.22um microporous membrane, and then pack it into vials.

Embodiment 3

[0058] Oryzanol 10mg

[0059] Soybean sphingomyelin 60mg

[0060] Sodium Glycodeoxycholate 100mg

[0061] Propylene Glycol 10mg

[0062] Glycine 20mg

[0063] Water for injection to 10ml

[0064] Oryzanol, soybean sphingomyelin, sodium glycodeoxycholate, and propylene glycol were dissolved in 7 ml of dichloromethane, heated to 80° C. and stirred until fully dissolved. The organic phase was obtained by distillation under reduced pressure. The water for injection in which the glycine has been dissolved is added to the full amount, and the injection solution of the present invention is obtained by fully stirring and mixing at 65°C. Adjust the pH to 7.5 with sodium hydroxide solution, add 0.05% activated carbon for injection and stir for 30 minutes, after decarburization and filtration, carry out fine filtration with 0.22um microporous membrane, and then pack into vials.

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PUM

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Abstract

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

Description

technical field [0001] The invention discloses an oryzanol composition, which contains oryzanol, phospholipid, bile acid and / or its salt, and belongs to the technical 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 rice 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 also alleviate various physical disorders and autonomic nervous disorders in women after menopause, and improve the dysfunctio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/575A61K9/127A61K47/24A61P9/00A61P3/00
CPCA61K9/0019A61K31/575A61K9/19A61P3/00A61P3/06A61P5/00A61P9/00A61P25/00
Inventor 郝守祝焦玉焕
Owner BEIJING CENTURY BIOCOM PHARMA TECH
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