High-efficient oral silibinin sustained-release preparation and preparation method thereof

A technology for oral administration of silibinin and silibinin, which is applied in the field of preparation of high-efficiency oral sustained-release preparations of poorly soluble drugs, can solve the problems of reducing the number of drug administrations, not providing in vivo measurement results, etc., and achieves faster release speed and faster release rate. Constant, solubility-enhancing effect

Active Publication Date: 2010-08-25
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese patent application (application number: 200310105255.6) discloses a "silibinin long-acting preparation and preparation method thereof", and the medicine described in this invention is actually limited to water-soluble silybin meglumine salt, not water-soluble Insoluble silibinin; the preparation method is actually only applicable to the preparation of water-soluble drug sustained-release preparations; the invention does not provide relevant in vivo measurement results to prove beneficial effects such as reduced number of medications and significantly improved bioavailability

Method used

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  • High-efficient oral silibinin sustained-release preparation and preparation method thereof
  • High-efficient oral silibinin sustained-release preparation and preparation method thereof
  • High-efficient oral silibinin sustained-release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] 1. Weigh 2g of SLB, 304g of PVP-K, 1g of phospholipid, 0.6g of IV acrylic resin, add 20ml of absolute ethanol to dissolve (if necessary, put it in a 70°C water bath to accelerate the dissolution), put it in a 60°C water bath, 90rpm rotary evaporation to nearly dry , in a 70°C water bath to completely evaporate the solvent, put it in a -20°C refrigerator for 2 hours, put it in a 60°C oven for 12 hours, pulverize it, and pass through a 80-mesh sieve to obtain a solid dispersion, which is set aside.

[0033] 2. Take 7g of solid dispersion, mix it with HPMC4000cPa·s0.5g and L-HPC1g, and then add an appropriate amount of 70% syrup to prepare a soft material. Pass through a 16-mesh sieve to obtain wet granules, bake at 60°C for 30 minutes, and then take them out. Sieve through a 16-mesh sieve for granulation, press into tablets, and control the pressure at 40-60N to obtain 34 bare sustained-release tablets.

[0034] 3. Put 0.058g of IV acrylic resin into a beaker, add 1.0ml o...

Embodiment 2

[0036] 1. Weigh 2g of SLB, 304g of PVP-K, 1g of phospholipid, 0.6g of IV acrylic resin, add 20ml of absolute ethanol to dissolve (if necessary, put it in a 70°C water bath to accelerate the dissolution), put it in a 60°C water bath, 90rpm rotary evaporation to nearly dry , in a 70°C water bath to completely evaporate the solvent, put it in a -20°C refrigerator for 2 hours, put it in a 60°C oven for 12 hours, pulverize it, and pass through a 80-mesh sieve to obtain a solid dispersion, which is set aside.

[0037] 2. Take 7g of solid dispersion, mix with HPMC4000cPa·s2g, L-HPC3g, after mixing, add an appropriate amount of 70% syrup to prepare soft material, pass through a 16-mesh sieve to obtain wet granules, bake at 60°C for 30 minutes, take out, pass through 16 Mesh sieve granulation, tabletting, the pressure is controlled at 40-60N, to obtain 48 bare sustained-release tablets.

[0038] 3. Put 0.07g of IV acrylic resin in a beaker, add 1.5ml of absolute ethanol to dissolve it,...

Embodiment 3

[0040] 1. Weigh 2g of SLB, 303g of PVP-K, 0.8g of phospholipid, 0.4g of IV acrylic resin, add 20ml of absolute ethanol to dissolve (if necessary, put it in a water bath at 70°C to accelerate the dissolution), put it in a water bath at 60°C, and evaporate it at 90rpm to nearly Dry, completely evaporate the solvent in a water bath at 70°C, place in a refrigerator at -20°C for 2 hours, then place in an oven at 60°C for 12 hours, pulverize, pass through an 80-mesh sieve to obtain a solid dispersion, and set aside.

[0041] 2. Take 6.3g of solid dispersion, mix with HPMC4000cPa·s0.9g, L-HPC1.35g, after mixing, add an appropriate amount of 70% syrup to prepare soft material, pass through a 16-mesh sieve to obtain wet granules, and bake at 60°C for 30 minutes Finally, take it out, pass through a 16-mesh sieve for granulation, and press into tablets with a pressure of 40-60N to obtain 34 bare sustained-release tablets.

[0042] 3. Put 0.054g of IV acrylic resin into a beaker, add 1.0m...

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PUM

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Abstract

The present invention relates to a high-effective oral silibinin (SLB) slow-released preparation. Its composition includes (by mass component portion) 1 portion of silibinin, 1.5-2.5 portions of polyvidone-K30, 0.23-0.58 portion of hydroxypropyl methyl cellulose 4000cPa.S, 0.46-1.38 portions of low-substituted hydroxypropyl cellulose. Said invention adopts the combination of solid dispersion technique and slow-released hydrophilic gel skeleton technique to raise the dissolubility of silibinin.

Description

Technical field: [0001] The invention relates to a preparation method of a high-efficiency oral sustained-release preparation of an insoluble drug, in particular a high-efficiency oral silybin sustained-release preparation and a preparation method thereof. Background technique: [0002] Sustained / controlled release preparations (sustained / controlled release preparations) have the advantages of reducing the peak and valley phenomenon of blood concentration, reducing the number of medications and side effects, and improving patient compliance, etc., and are increasingly widely used in clinical practice. The preparation of slow / controlled release preparations usually requires dissolving the drug first, then adding slow / controlled release excipients, and using appropriate technology to make slow / controlled release preparations. Water-soluble drugs are easy to dissolve in water and can be easily made into slow / controlled release preparations. Currently, there are many varieties o...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/357A61K9/22A61K9/28A61K47/38A61P1/16A61P31/14A61P31/20
Inventor 徐希明余江南沈松朱源
Owner JIANGSU UNIV
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