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

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

Active Publication Date: 2008-04-23
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, 4g of PVP-K30, 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, and evaporate at 90rpm When it is nearly dry, evaporate the solvent completely in a water bath at 70°C, put it in a refrigerator at -20°C for 2 hours, then put it in an oven at 60°C for 12 hours, pulverize it, and pass it through an 80-mesh sieve to obtain a solid dispersion, which is set aside.

[0033] 2. Take 7g of solid dispersion, mix with HPMC4000cPa·s 0.5g, L-HPC 1g, 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, and take out , passed through a 16-mesh sieve for sizing, tableting, and the pressure was controlled at 40-60N to obtain 34 nude sustained-release tablets.

[0034] 3. Put 0.058g of IV acrylic resin into a beaker, add 1....

Embodiment 2

[0036] 1. Weigh 2g of SLB, 4g of PVP-K30, 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, and evaporate at 90rpm When it is nearly dry, evaporate the solvent completely in a water bath at 70°C, put it in a refrigerator at -20°C for 2 hours, then put it in an oven at 60°C for 12 hours, pulverize it, and pass it through an 80-mesh sieve to obtain a solid dispersion, which is set aside.

[0037] 2. Take 7g of solid dispersion, mix with 2g of HPMC4000cPa·s and 3g of L-HPC, 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, and then take it out. Sieve through a 16-mesh sieve for granulation, press into tablets, and control the pressure at 40-60N to obtain 48 bare sustained-release tablets.

[0038] 3. Put 0.07g of IV acrylic resin in...

Embodiment 3

[0040] 1. Weigh 2g of SLB, 3g of PVP-K30, 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 of 70°C to accelerate the dissolution), and then rotate in a water bath of 60°C at 90rpm Evaporate to nearly dryness, evaporate the solvent completely 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·s 0.9g, L-HPC 1.35g, 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 Then take it out, pass through a 16-mesh sieve for granulation, and press into tablets with a pressure controlled at 40-60N to obtain 34 bare tablets of sustained-release tablets.

[0042] 3. Put 0.054g of IV acrylic resi...

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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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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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