Silibinin nano suspension, lyophilized preparation thereof and preparation method of lyophilized preparation

A technology of silibinin and stabilizer, which is applied in the field of silibinin pharmaceutical preparations, can solve the problems of low bioavailability, limited application of silybin, poor water solubility, etc., achieve high drug content, improve chemical and physical Effect of stability and small particle size change

Pending Publication Date: 2022-05-27
CHENGDE MEDICAL UNIV
View PDF0 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Silibinin belongs to BBS Ⅱ drugs, and has poor water solubility a

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 nano suspension, lyophilized preparation thereof and preparation method of lyophilized preparation
  • Silibinin nano suspension, lyophilized preparation thereof and preparation method of lyophilized preparation
  • Silibinin nano suspension, lyophilized preparation thereof and preparation method of lyophilized preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Weigh 10 mg of silibinin bulk drug (Sy), add 1 mL of absolute ethanol for ultrasonic dissolution to obtain a silibinin absolute ethanol solution; weigh 1.00 mg of stabilizer (soluplus: SDS=1:5) and dissolve in 7 mL of pure water In the process, the stabilizer solution was obtained, and the silibinin anhydrous ethanol solution was added dropwise to the stabilizer solution under the action of a cell ultrasonic pulverizer (65w ultrasonic for 31min) to make the dispersion uniform, and the obtained suspension was spun on a rotary evaporator. Steam until there is no alcohol smell to obtain a silibinin nanosuspension. 5% mannitol was added to the silibinin nano suspension, and after lyophilization for 48 hours, the silibinin nano freeze-dried powder was obtained.

Embodiment 2

[0023] Weigh 10 mg of silibinin API (Sy), add 1 mL of absolute ethanol for ultrasonic dissolution to obtain silibinin absolute ethanol solution; weigh 2.00 mg of stabilizer (soluplus: SDS=1:5) and dissolve in 10 mL of pure water In the process, the stabilizer solution was obtained, and the silibinin anhydrous ethanol solution was added dropwise to the stabilizer solution under the action of a cell ultrasonic pulverizer (65w ultrasonic for 31min) to make the dispersion uniform, and the obtained suspension was spun on a rotary evaporator. Steam until there is no alcohol smell to obtain a silibinin nanosuspension. 5% mannitol was added to the silibinin nano suspension, and after lyophilization for 48 hours, the silibinin nano freeze-dried powder was obtained.

[0024] The silibinin nanosuspension and silibinin nano freeze-dried powder prepared in Examples 1-2 were respectively taken to measure particle size and PDI. The results are shown in the table below.

[0025] Table 1 Sil...

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

No PUM Login to view more

Abstract

The invention relates to a silibinin nano suspension, a lyophilized preparation thereof and a preparation method, the silibinin nano suspension comprises silibinin, a stabilizing agent and water, the mass ratio of the silibinin to the stabilizing agent is (1-10): 1, and the lyophilized preparation is a lyophilized preparation of the silibinin nano suspension and a lyophilized preparation of the silibinin nano suspension. The stabilizer is a composition of a polyethylene caprolactam-polyvinyl acetate-polyethylene glycol grafted copolymer and lauryl sodium sulfate, and the mass ratio of the polyethylene caprolactam-polyvinyl acetate-polyethylene glycol grafted copolymer to the lauryl sodium sulfate is (1-5): (1-5). According to the silibinin nano suspension and the preparation method thereof, the particle size of the nano drug is optimized by adjusting the composition of the stabilizer, the preparation method and parameters, and the dissolution rate and the bioavailability of the insoluble bulk drug silibinin are remarkably improved through the finally prepared silibinin nano suspension.

Description

technical field [0001] The invention belongs to the technical field of silibinin pharmaceutical preparations, in particular to a silibinin nanosuspension, a freeze-dried preparation thereof and a preparation method. Background technique [0002] Silybin (Sy) is extracted and isolated from the fruit of the Compositae plant Silybum marianum. It is a flavonoid lignin compound. It has the functions of promoting the recovery of damaged cell membranes and protecting normal liver cells. It has low toxicity and mild adverse reactions. Its liver protection mechanism is to form a protective film for liver cells to block toxic substances, reduce the chance of liver cells being damaged by free radicals, stimulate protein synthesis, promote liver cell repair and promote cell regeneration. [0003] Silibinin belongs to the BBS II class of drugs, with poor water solubility and low bioavailability, which limits the application of silibinin to a large extent. Poorly soluble drugs can increa...

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
IPC IPC(8): A61K9/10A61K9/19A61K31/357A61K47/20A61K47/32A61K47/26A61P1/16
CPCA61K31/357A61K9/10A61K9/19A61K47/32A61K47/20A61K47/26A61P1/16Y02A50/30
Inventor 刘喜纲张领程佳慧常金花刘沛王汝兴
Owner CHENGDE MEDICAL UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap