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Silymarin-phospholipid complex and preparation method thereof

A technology of silymarin phospholipid and silymarin, which is applied in the directions of drug delivery, drug combination, pharmaceutical formulation, etc., can solve the problems of low oral bioavailability and poor water solubility, and achieves increased bioavailability, fat solubility, and drug efficacy. quick effect

Inactive Publication Date: 2014-04-30
江苏健佳药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Silymarin currently on the market has good fat solubility, poor water solubility, and low oral bioavailability. Therefore, it is necessary to adopt a certain process to obtain silymarin with both water solubility and fat solubility.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 Preparation of milk thistle extract

[0034] After screening the full-grained milk thistle seeds, first remove the oil in them by mechanical pressing to obtain milk thistle seed cakes. Take 500 grams of cakes and add 2000ml of acetone. After soaking for 2 hours, heat to 60 degrees Celsius and extract for 16 hours. Concentrate at 60 degrees Celsius for 6 hours, then dry at 85 degrees Celsius for 1 hour to obtain 48.7 grams of milk thistle extract.

Embodiment 2

[0035] Example 2 Preparation of silymarin

[0036] 48.7 grams of the milk thistle extract prepared in Example 1 were added to 200 grams of normal hexane and stirred at 600 RPM for 0.5 hour, and then left to stand for 30 minutes to remove the normal hexane solution by suction filtration (lipophilic properties such as oil in the solution) Substance); Repeat three times to obtain deoiled milk thistle extract; then add the deoiled milk thistle extract to 200 grams of 50% mass concentration of ethanol solution and stir for 0.5 hours after suction filtration to obtain a clear filtrate, The clarified filtrate was concentrated in vacuum at 75 degrees Celsius for 2.5 hours, and then the concentrated paste was spread on a stainless steel baking tray, dried in vacuum at 80 degrees Celsius for 3 hours, and pulverized to obtain 29.2 grams of dry powder of silymarin.

Embodiment 3

[0037] Example 3 Preparation of silymarin-phospholipid complex

[0038] 10 grams of silymarin prepared in Example 2 were dissolved in 300 grams of ethanol to form a solution and ultrasonicated at 400 W at 50° C. for 15 minutes. 50 g of soybean lecithin was dissolved in 500 g of ethanol to form a solution and sonicated at 400 W at 50°C for 15 minutes.

[0039] Immediately mix the above two solutions and sonicate again at 400 W at 50°C for 0.5 h, then heat the sonicated mixed solution at 70°C for 1 h, and immediately cool in an ice bath overnight after heating. The above mixed solution was irradiated with an infrared lamp for 20 minutes, and then evaporated under reduced pressure to remove ethanol. After the solvent was completely evaporated to dryness, it was then air-dried at 45° C. to obtain 53.1 grams of dry product of silymarin phospholipid complex.

[0040]

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PUM

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Abstract

The invention relates to the technical field of pharmaceutical preparations, in particular to a silymarin-phospholipid complex and a preparation method thereof and a silybin-phospholipid complex soft capsule prepared from the complex. According to the silymarin-phospholipid complex and the preparation process, a phospholipid complex is prepared from silymarin, so that the water solubility of the silymarin is greatly improved, the lipid solubility and water solubility of the obtained complex are balanced, and the bioavailability is greatly improved; moreover, the silymarin-phospholipid complex soft capsules prepared from the complex also have high bioavailability, and are convenient to take; the utilization of the silymarin is greatly promoted.

Description

Technical field [0001] The present invention involves the field of drug preparation technology, especially involving water pistol phospholipid complexes and their preparation processes, as well as soft capsules obtained from the piloted pheasine phospholipids obtained with this complex. [0002] Background technique [0003] Water Flying Thistle is from the chrysanthemum plant water flying thistle (purple flower) (purple flower) ( Silybum Marianum (L.) GAERTN) The seeds of the seeds extracted.It is a kind of yellow or brown powder. Its main ingredients are water flying Jimin, Flying Flying Jimin, Water Flying Timing, and Water Flying Ting Ting.Water Flying Thistle is an excellent liver protective plant. It was recorded in classics in Greece and Rome as early as the 1st century AD.The main effective ingredients of the liver protection in the water flying thistle are water pistula.Water pheasine can protect and stabilize hepatocytes, fight hepatocyte necrosis, reduce fat degenerati...

Claims

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Application Information

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IPC IPC(8): A61K47/24A61K31/357A61K9/48A61J3/07A61P1/16
Inventor 周勇周晓娟梁呈元吴素琴伍晓月
Owner 江苏健佳药业有限公司
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