Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Bifendate nano crystal preparation and preparation method thereof

A biphenyl diester and nano-crystal technology, which is applied in the direction of making medicines into special physical or taking forms of devices, powder delivery, digestive system, etc. Effect

Inactive Publication Date: 2012-05-23
SHANDONG UNIV
View PDF6 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the absence of relevant reports in the prior art, a bifendate with good curative effect, good biocompatibility, high bioavailability, stable system, suitable for large-scale industrial production, and low cost has been developed. Nanocrystalline preparations and preparation methods are difficult, requiring creative work, a large number of tests and condition screening

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
  • Bifendate nano crystal preparation and preparation method thereof
  • Bifendate nano crystal preparation and preparation method thereof
  • Bifendate nano crystal preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Embodiment 1: Preparation of bifendate nanocrystalline preparation

[0040] Weigh 0.2g of biphenyl diester and dissolve it in 5ml of dimethyl sulfoxide, pour it into 100ml of aqueous solution containing 0.05g of povidone (k30) and 0.2g of lecithin under stirring at low temperature, and after ultrasonication at low temperature for 40min, then undergo high-pressure The micro-fluidic nanodisperser was used to homogenize twice under the pressure of 6990 psig and 11650 psig respectively, and then homogenized 10 times under the pressure of 23300 psig to obtain the bifendate nano-crystal suspension.

[0041] Take the above suspension and add mannitol according to the ratio of 5% (w / v, g / ml), stir and dissolve, divide into vials according to 2mL / bottle, put it into the ultra-low temperature refrigerator quickly, and freeze it at -80°C for 24 hours , and then take it out and quickly put it on the shelf of the freeze dryer whose temperature has dropped to -50°C, cover with a vacu...

Embodiment 2

[0043] Embodiment 2: Preparation of bifendate nanocrystalline preparation

[0044] Weigh 2.5g bifendate and dissolve it in 5ml dimethyl sulfoxide, pour it into 100ml aqueous solution containing 5g povidone (K30) and 1g lecithin under stirring at low temperature, after ultrasonication at low temperature for 40min, then pass through high-pressure microjet nanometer The disperser was homogenized twice under the pressure of 6990 psig and 11650 psig respectively, and then homogenized 10 times under the pressure of 23300 psig to obtain the bifendate nano-crystal suspension.

[0045] Take the above suspension and add mannitol according to the ratio of 5% (w / v, g / ml), stir and dissolve, divide into vials according to 2mL / bottle, put it into the ultra-low temperature refrigerator quickly, and freeze it at -80°C for 24 hours , and then take it out and quickly put it on the shelf of the freeze dryer whose temperature has dropped to -50°C, cover with a vacuum cover, turn on the vacuum pum...

Embodiment 3

[0046] Embodiment 3: Preparation of bifendate nanocrystalline preparation

[0047] Weigh 5g of bifendate and dissolve it in 5ml of dimethyl sulfoxide, pour it into 100ml of an aqueous solution containing 2.5g of hydroxypropyl cellulose and 2g of lecithin under low-temperature stirring, and after ultrasonication at low temperature for 40min, pressurize at 6990psig and 11650psig Homogenize 2 times respectively, and then homogenize 10 times under 23300 psig pressure to obtain bifendate nano-crystal suspension.

[0048] Take the above suspension and add mannitol at a ratio of 5% (w / v), stir and dissolve, then pack into vials at 2mL / bottle, quickly put into an ultra-low temperature refrigerator, and freeze at -80°C for 24 hours, then take it out quickly Put it on the shelf of a lyophilizer whose temperature has dropped to -50°C, cover with a vacuum cover, turn on the vacuum pump switch, and freeze-dry for 48 hours. After the freeze-drying is completed, take it out and pack it with...

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
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention discloses a bifendate nano crystal preparation, which comprises 200 weight parts of raw material of bifendate and 20 to 400 weight parts of auxiliary material of stabilizing agent. A preparation method comprises the following steps of: (1) dispersing the stabilizing agent serving as a dispersion medium in double distilled water to obtain a suspension A; (2) dispersing the bifendate in an organic solvent to obtain a coarse suspension B; (3) dispersing the coarse suspension B in the suspension A under the ultrasonic condition to obtain a suspension C; (4) homogenizing the suspension C by using a high pressure microfluidization nano dispersion instrument to obtain bifendate nano crystal suspension; and (5) performing freeze drying on the prepared bifendate nano crystal suspension, or adding a freeze drying protective agent and performing freeze drying to obtain the bifendate nano crystal preparation. The bifendate nano crystal preparation can be prepared into injection or oral preparations such as tablets, capsules and the like when applied.

Description

technical field [0001] The invention relates to a bifendate nano crystal preparation and a preparation method thereof Background technique [0002] Bifendate: It is the intermediate of the artificial synthesis of schisandra, and it is the first high-efficiency and low-toxic liver-protecting drug with a new structure in my country. Its chemical name is 4,4'-dimethoxy-5,6,5',6'-dimethyldioxy-2,2'-dicarboxylate biphenyl, and its molecular formula is: C 20 h 18 o 10 , Molecular weight: 419.36. This product is a white crystalline powder, odorless and tasteless, almost insoluble in water, slightly soluble in methanol and ethanol, easily soluble in chloroform and dimethylformamide quaternary pyridine, showing certain fat solubility. [0003] Clinical studies have shown that the main pharmacological effects of bifendate are: (1) Significant hepatoprotective and enzyme-lowering effects: it can significantly reduce serum glutamic pyrumic transaminase (GPT) and aspartate transamina...

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): A61K9/19A61K31/36A61P1/16A61J3/02
Inventor 张典瑞刘悦王言才段存贤贾乐姣冯飞飞王飞虎郑丹丹刘光璞郝蕾蕾
Owner SHANDONG UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products