Silibinin slow release micropill with double layers of coatings and preparation method of silibinin slow release micropill

A technology of silybin and sustained-release pellets, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, and pharmaceutical formulations, which can solve the problems of no sustained-release effect, increase in vivo bioavailability, Poor patient compliance and other issues, to achieve the effect of improving relative bioavailability, easy operation, and reducing the number of medications

Active Publication Date: 2014-10-01
JIANGSU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the above-mentioned preparations are common preparations, which simply increase the dissolution of the drug and thus increase the bioavailability in the body, but have no sustained-release effect, and the patient's compliance is poor, and there are no products on the market that have a good sustained-release effect and are highly praised by the industry. Oral sustained-release formulation of silibinin

Method used

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  • Silibinin slow release micropill with double layers of coatings and preparation method of silibinin slow release micropill
  • Silibinin slow release micropill with double layers of coatings and preparation method of silibinin slow release micropill
  • Silibinin slow release micropill with double layers of coatings and preparation method of silibinin slow release micropill

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Weigh 100g of blank ball cores, place them in a Mini-250 extrusion spheronizing fluidized coating machine, and preheat for 30 minutes.

[0043] Weigh 4g silibinin and 8g PVP K respectively 30 , 12g PEG400, 16g Tween 80, added to 200mL 50% ethanol water and magnetically stirred until clarified and uniform, added 1.2g talcum powder, magnetically stirred, and set the coating parameters of the solid dispersion layer: the coating speed was 800rpm, the air inlet speed was 25Hz, The wind speed is 18Hz, and the spray speed of the coating spray gun is 1mL min -1 , the air inlet temperature is 45°C, the material temperature is 40°C, coating is carried out, after the coating is completed, take it out, and dry it in a vacuum oven at 50°C for 2 hours to obtain silibinin solid dispersion pellets. The obtained silibinin solid dispersion pellet is carried out electron microscope observation, and the results are shown in Figure 5 ; Measure the dissolution curve of silybin solid dispe...

Embodiment 2

[0046] Weigh 100g of blank ball cores, place them in a Mini-250 extrusion spheronizing fluidized coating machine, and preheat for 30 minutes.

[0047] Weigh 6g silibinin and 3g PVP K respectively 30 , 6g F68, 6g Tween 80, added to 150mL of 60% ethanol water and magnetically stirred until clarified and homogeneous, added 2g of magnesium stearate, magnetically stirred, and set the coating parameters of the solid dispersion layer: the coating speed is 800rpm, the air inlet speed is 25Hz , the wind speed is 18Hz, and the spray speed of the coating spray gun is 1mL min -1 , the inlet air temperature is 45°C, and the material temperature is 40°C. Carry out coating, take out after coating, and dry in a vacuum oven at 50° C. for 12 hours to obtain silybin solid dispersion pellets. The test results are as in Example 1.

[0048] Take 100g of the silibinin solid dispersion pellets prepared above, weigh 5g EC, 4g dibutyl phthalate, and 3g PEG6000 respectively, add them to 150mL pure et...

Embodiment 3

[0050] Weigh 100g of blank ball cores, place them in a Mini-250 extrusion spheronizing fluidized coating machine, and preheat for 30 minutes.

[0051] Weigh respectively 8g silybin, 40g PVP K 25 , 15g F68, 30g PEG400, 15g Tween 80, 2g soybean lecithin, add to 200mL75% ethanol water and magnetically stir until clarified, add 6.4g talcum powder, magnetically stir, set the coating parameters of the solid dispersion layer: the coating speed is 800rpm , the air inlet speed is 25Hz, the air outlet speed is 18Hz, and the spray speed of the coating spray gun is 1mL min -1 , the inlet air temperature is 45°C, and the material temperature is 40°C. Carry out coating, take out after coating, and dry in a vacuum oven at 50° C. for 12 hours to obtain silybin solid dispersion pellets. The test results are as in Example 1.

[0052] Take 100g of silibinin solid dispersion pellets prepared above, weigh 10g EC, 2g micropowder silica gel, and 3g PEG6000 respectively, add them to 150mL pure eth...

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Abstract

The invention relates to a silibinin slow release micropill with double layers of coatings. The silibinin slow release micropill is formed by a hollow pill core outside which the double layers of coatings are wrapped, wherein the first layer of coating forms a silibinin solid dispersion micropill and comprises silibinin, a solid dispersion carrier, a solubilizer and a sticky-resisting agent which are wrapped outside the hollow pill core so as to form the silibinin slow release micropill; the second layer of coating is formed outside the silibinin slow release micropill and comprises a slow release material, a lubricant and a plasticizer which are wrapped outside the silibinin slow release micropill so as to form silibinin slow release micropill with double layers of coatings. The silibinin slow release micropill provided by the invention is simple and convenient in preparation method, high in industrialized potential, stable in medicine release after being taken orally and high in bioavailability, and has a certain slow release effect.

Description

technical field [0001] The invention relates to an oral solid sustained-release pellet preparation for insoluble drugs and a preparation method thereof, in particular to an oral silybin oral sustained-release pellet preparation and a preparation method thereof. Background technique [0002] Compositae plant milk thistle (silybum marinaum (L) Gaenrt) has been a good drug for liver protection since ancient times, and silymarin is the general name of the effective mixture extracted from milk thistle. Silybin (SLB) is its main active ingredient. Silibinin has various pharmacological activities pharmacologically, including hepatoprotective, antioxidative, anti-inflammatory, anticancer and cardioprotective effects. Significantly maintain liver cells, maintain liver function, and reduce blood lipids. Clinically, it is mainly used to treat liver poisoning, liver cirrhosis, acute and chronic hepatitis, etc. It is currently recognized as a hepatoprotective drug with definite and sign...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/48A61K31/357A61K47/32A61K47/34A61K47/38A61P1/16
Inventor 余江南黄治民朱源徐希明曹霞
Owner JIANGSU UNIV
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