Medicament composition and preparation method thereof

A composition and medicine technology, applied in the field of medicine, can solve the problems of poor oral oryzanol effect, complicated operation, low bioavailability and the like

Inactive Publication Date: 2013-04-17
BEIJING CENTURY BIOCOM PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The problem in the application of oryzanol is that oryzanol is insoluble in water and easy to oxidize, which makes it difficult to make oryzanol into a stable preparation
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.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] The preparation of embodiment 1 cycloartenyl ferulic acid ester and 24-methylene cycloartenyl ferulic acid ester compound

[0040] 1. Get commercially available oryzanol raw material (purity is 70%) 1kg, reflux dissolving with the mixed solution of ethyl acetate and absolute ethanol that is 20:1 with 5 times of amount ratio, filter, leave standstill, precipitated crystals are filtered, dry. The dried crystals (purity about 84%) were reconstituted with 8 times the amount of ethyl acetate, filtered, and allowed to stand, and the precipitated crystals were filtered and dried. The above recrystallization steps were repeated 3-5 times.

[0041] 2. Combine and recover the mother liquor filtered out after recrystallization in step 1 until the volume is 2 times that of the contained solute, then let it stand, filter and dry the precipitated crystals.

[0042] 3. The crystals (purity is about 85-87%) in step 2 are dissolved with 8 times the amount of ethyl acetate under reflux,...

Embodiment 2

[0049] Complex 10mg

[0050] Soy Lecithin 50mg

[0051] Hyodeoxycholic Acid 50mg

[0052] Mannitol 80mg

[0053] Water for injection to 10ml

[0054] Dissolve the complex, soybean lecithin, 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 water for injection in which mannitol has been dissolved to the full amount into the above organic phase, and stir well at 60°C to obtain the composition injection of the present invention. Adjust the pH to 7.3 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.

Embodiment 3

[0056] Complex 40mg

[0057] Soy Lecithin 200mg

[0058] Chenodeoxycholic Acid 300mg

[0059] Glycine 100mg

[0060] Water for injection to 10ml

[0061]Dissolve the complex, chenodeoxycholic acid, and soybean lecithin in 5ml of propylene glycol, 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 glycine has been dissolved to the full amount into the above organic phase, and stir thoroughly at 70°C to obtain the composition injection of the present invention. Adjust the pH to 9.0 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 present invention discloses a pharmaceutical composition containing a complex of cycloartenyl ferulate and 24-methylene cycloartanyl ferulate, phospholipids, cholic acids and / or salts thereof. The water-solubility and the stability of the complex of cycloartenyl ferulate and 24-methylene cycloartanyl ferulate have been effectively improved by being made into the pharmaceutical composition of the present invention. And the particle diameter and the stability of the said pharmaceutical composition are superior to that of the existing products. Furthermore, the present invention provides an injectable fluid, an injectable lyophilized powder and a kit containing the pharmaceutical composition as well as the preparation methods thereof.

Description

technical field [0001] The invention relates to a pharmaceutical composition, in particular the invention discloses a pharmaceutical 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 rice bran oil and its oil foot. In rice bran oil oryzanol, the content of cycloartenol ferulate is about 70-80%. After long-term research, researchers have found that oryzanol has a variety of physiological functions. Mainly include: lower blood lipid, lower cholesterol absorption, lower serum cholesterol, prevent lipid oxidation and prevent cardiovascular disease. In addition, oryzanol can also alleviate various physical disorders and autonomic nervous disorders in women after ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/575A61K47/24A61P9/00A61P3/06A61P15/12
CPCA61K9/0019A61K31/575A61K9/19A61P3/00A61P3/06A61P5/00A61P9/00A61P15/12A61P25/00
Inventor 郝守祝焦玉焕
Owner BEIJING CENTURY BIOCOM PHARMA TECH
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