Unlock instant, AI-driven research and patent intelligence for your innovation.

Silibinin double-layer slow-release tablets and preparation method thereof

A technology for silibinin and sustained-release tablets, which is applied in the directions of pill delivery, digestive system, drug combination, etc., can solve problems such as low drug content, achieve good reproducibility, reduce the number of drug administrations, and uniform effective blood drug concentration Effect

Inactive Publication Date: 2014-09-03
SICHUAN ACAD OF CHINESE MEDICINE SCI
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The cumulative drug release of the prepared solid dispersion was 69.3% at 2 hours, and the solubility of silibinin was improved. and in the in vitro release test of sustained-release preparations, it only shows that the cumulative release amount of 12h is more than 80%, and its technical scheme is not supported by the examples of sustained-release preparations, and it is not in accordance with the Chinese Pharmacopoeia on the application of sustained-release preparations. Select 3 points to characterize the drug release requirements of in vitro sustained-release preparations; the stability test has no examples and relevant data to support the conclusion

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Silibinin double-layer slow-release tablets and preparation method thereof
  • Silibinin double-layer slow-release tablets and preparation method thereof
  • Silibinin double-layer slow-release tablets and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] formula Dosage SLB API 10g PEG6000 25g Poloxamer 25g SDS 5g

[0047] Preparation process: Prepared by solvent-melt method. Weigh 10g of silibinin, add a small amount of 80% ethanol (1:10, w / v), and dissolve it by ultrasonic oscillation; weigh 25g each of PEG6000 and poloxamer in an evaporating dish, heat in a water bath at 70°C, and wait until After complete melting, pour into the silibinin solution, add 5g of SDS, stir evenly, evaporate the solvent, place the resulting mixture in a -38°C freezer, stir rapidly to solidify, place for 24h, take it out and place in a vacuum drying oven for 24h , crushed, and passed through a 80-mesh sieve to obtain a solid dispersion.

Embodiment 2

[0049]

[0050] Preparation process: Mix silibinin solid dispersion, MCC, PVPP, and L-HPC through an 80-mesh sieve, add 6g of micropowder silica gel and mix evenly to obtain immediate-release layer granules; Part of the raw material of Binbin is replaced by the same amount of lactose, and 20ml of 5% PVPk30 ethanol solution is added to make a soft material, passed through a 26-mesh sieve to granulate, dried at 45°C, granulated with a 24-mesh sieve, and added with 1% magnesium stearate Mix evenly to obtain blank slow-release layer granules. The sustained-release granules and immediate-release granules are punched into a double-layer sustained-release tablet with an 8 mm shallow concave.

Embodiment 3

[0052]

[0053] Preparation process: Mix the quick-release part of the excipients evenly by sieving, replace the SLB solid dispersion with an equivalent amount of MCC, and obtain the quick-release layer granules; mix the silybin raw material drug, HPMCk4M, and lactose evenly by grinding, add 20ml of 5% PVPk30 ethanol solution is used to make soft materials, passed through a 26-mesh sieve to granulate, dried at 45°C, sized with a 24-mesh sieve, added 1% magnesium stearate and mixed evenly to obtain sustained-release layer granules. The sustained-release granules and immediate-release granules are punched into a double-layer sustained-release tablet with an 8 mm shallow concave.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
hardnessaaaaaaaaaa
Login to View More

Abstract

The invention discloses a silibinin double-layer slow-release tablet, which comprises a quick-release layer and a slow-release layer. Wherein, the quick-release layer is mainly composed of silibinin solid dispersion, filler, disintegrant and lubricant, and the slow-release layer is mainly composed of silybin, slow-release material, filler, lubricant and binder. agent composition. Wherein the weight ratio of the silibinin content in the quick-release layer and the slow-release layer is 2:8-3:7. The weight ratio of the quick-release layer to the sustained-release layer is (1.5-2.4):1. The object of the present invention is to provide a silibinin double-layer sustained-release tablet with good patient compliance, less side effects, rapid onset of action and long-lasting stable and effective blood drug concentration. Also disclosed is a preparation method of the silibinin double-layer sustained-release tablet. The preparation process of the method has good reproducibility and high production efficiency, is suitable for industrial mass production, and the prepared double-layer sustained-release tablet has good release uniformity.

Description

technical field [0001] The invention relates to a silibinin double-layer sustained-release tablet and a preparation method thereof, in particular to a silibinin quick-release plus sustained-release double-layer sustained-release tablet and a preparation method thereof, belonging to the field of preparations. Background technique [0002] Silybin (SLB) is an active ingredient extracted from the herb of Compositae, milk thistle. It has obvious protective and stabilizing effects on liver cells, and has different degrees of therapeutic effects on various liver diseases. It is currently recognized as a liver injury repair drug with definite curative effect. Preparations based on it have been widely used in the treatment of acute and chronic hepatitis and liver cirrhosis. Clinically, it is mainly used to treat acute and chronic hepatitis, various liver injuries, liver fibrosis and early liver cirrhosis [Kaur M, Agarwal R. Silymarin and epithelial cancer chemoprevention: How to cl...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/24A61K31/357A61P1/16
Inventor 徐超群阮佳袁志翔詹雁岑菁谭镭
Owner SICHUAN ACAD OF CHINESE MEDICINE SCI