Nano-suspension for silybin-phospholipid complex and preparation method thereof

A technology of nanosuspension and lecithin phospholipid, applied in the field of medicine, can solve the problem of no nano preparation and the like, and achieve the effects of improving clinical curative effect, high dissolution rate and improving bioavailability

Inactive Publication Date: 2011-11-02
INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, silibinin preparations on the market at home and abroad mainly include silibinin capsules, s

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] Co-dissolve equimolar silibinin and refined egg yolk lecithin in hot acetone, keep warm at 55°C for 2 hours, concentrate to a thick paste, quickly add n-hexane, filter, dry the filter cake and pulverize to obtain silybin phospholipid Compound: take 0.25g silibinin phospholipid complex, add appropriate amount of ethanol or acetone to dissolve after heating, slowly inject into water and ultrasonically, concentrate under reduced pressure to remove ethanol, then inject into water containing 0.25g hydroxypropyl cellulose, Mix and stir evenly, add water to 100mL, obtain a milky-white nano-suspension with a bluish opalescence, put it on a high-pressure homogenizer, and cycle 10 times at 20K Psi to obtain a silibinin phospholipid complex nano-suspension. It is also possible to add mannitol with a weight ratio of 20% as a freeze-drying protective agent, pre-freeze in a refrigerator at -80°C for 48h, and freeze-dry in a freeze dryer: temperature -48°C, pressure 0.1mbar, take it ou...

Embodiment 2

[0041]Co-dissolve equimolar silibinin and refined egg yolk lecithin in hot acetone, keep warm at 55°C for 2 hours, concentrate to a thick paste, quickly add n-hexane, filter, dry the filter cake and pulverize to obtain silybin phospholipid Compound: take 0.50g silibinin phospholipid complex, add appropriate amount of ethanol or acetone to dissolve after heating, slowly inject into water and ultrasonically, concentrate under reduced pressure to remove ethanol, and then inject into In the water of hydroxypropyl methylcellulose, mix and stir evenly, add water to 100mL, obtain the nano-suspension of milky white with slightly bluish opalescence, put it on a high-pressure homogenizer, and circulate 15 times under 30K Psi to obtain silibinin Phospholipid complex nanosuspension. It is also possible to add mannitol with a weight ratio of 10% as a freeze-drying protective agent, pre-freeze in a refrigerator at -80°C for 48h, and freeze-dry in a freeze dryer: temperature -48°C, pressure ...

Embodiment 3

[0044] Co-dissolve equimolar silibinin and soybean lecithin in hot acetone, keep warm at 55°C for 2 hours, concentrate to a thick paste, add n-hexane quickly, filter, dry the filter cake and pulverize to obtain silybin phospholipid complex Take 0.50g silibinin phospholipid complex, add appropriate amount of ethanol or acetone to heat and dissolve, slowly inject into water and ultrasonically, concentrate under reduced pressure to remove ethanol, and then inject into 0.50g hydroxypropyl cellulose, 1.0g polysaccharide In the water of Vitone K30, mix and stir evenly, add water to 100mL, get milky white with bluish opalescent nano primary suspension, put it on a high-pressure homogenizer, cycle 12 times at 30K Psi, get silibinin phospholipid complex nano suspension. You can also add mannitol with a weight ratio of 5% as a freeze-drying protective agent, pre-freeze in a refrigerator at -80°C for 48h, and freeze-dry in a freeze dryer: take it out after 48h at a temperature of -48°C a...

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Abstract

The invention discloses a nano-suspension for a silybin-phospholipid complex and a preparation method thereof, wherein the nano-suspension for a silybin-phospholipid complex is prepared by combining a technology of promoting medicine absorption by a phospholipid complex with a solubilizing-targeting technology of nano-suspension; the ingredients of the nano-suspension for silybin-phospholipid complex comprise a silybin-phospholipid complex, a stabilizer and water; the nano-suspension exists in the form of suspension or freeze-dried powder and prepared by combining a microprecipitation method with a high-pressure homogenization method; the method of the invention prepares a nano-suspension hard to dissolve in a medicine, without a need to pre-micronize raw material medicines, which greatly decreases energy consumption; the grain diameter distribution range of the prepared nano-grains is narrow, and the medicine highly disperses in a granular state, which increases the wettability, solubility and solution velocity of the medicine, thereby improving the oral bioavailability thereof; the technique process of the preparation method is simple and easy to realize industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a nano-suspension of silibinin phospholipid complex, and the invention also discloses a preparation method thereof. Background technique [0002] Silybin is a flavonoid lignan compound extracted from the fruit of the Compositae plant Silybum marianum Gaertn. It is widely used as a liver protection drug in the treatment of hepatitis, liver cirrhosis and metabolic toxicity. Liver injury and other diseases, it has anti-oxidation, anti-lipid peroxidation, anti-fibrosis, cell membrane stabilization and the ability to regulate liver regeneration; studies have also found that silibinin also has the effects of lowering blood fat, protecting myocardium and anti-diabetes. effect. Studies in recent years have shown that silibinin can also inhibit the effects of various cancers such as colon cancer, lung cancer, and prostate cancer, making it more and more widely concerned at h...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K9/19A61K31/357A61K47/38A61K47/48A61P35/00
Inventor 王国华张保献聂其霞臧琛赵小妹蒋益轩
Owner INST OF CHINESE MATERIA MEDICA CHINA ACAD OF CHINESE MEDICAL SCI
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