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

Nano-suspension of Hsp90 inhibitor by using benzamide as basic skeleton and preparation method of nano-suspension

A technology of nano-suspension and benzamide, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., which can solve the problems of low bioavailability, strong toxic and side effects, and poor water solubility, etc. problems, to achieve the effect of high bioavailability, high drug content, and stable dissolution rate

Active Publication Date: 2014-12-03
广州少伯控股集团有限公司 +1
View PDF5 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] In order to solve the shortcomings of the above-mentioned BA-Hsp90 inhibitors such as poor water solubility, difficulty in administration, low bioavailability, and strong toxic and side effects, the primary purpose of the present invention is to provide a nano-mixed Hsp90 inhibitor with benzamide as the basic skeleton. Suspension, thereby improving the water solubility and bioavailability of BA-Hsp90 inhibitors

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
  • Nano-suspension of Hsp90 inhibitor by using benzamide as basic skeleton and preparation method of nano-suspension
  • Nano-suspension of Hsp90 inhibitor by using benzamide as basic skeleton and preparation method of nano-suspension
  • Nano-suspension of Hsp90 inhibitor by using benzamide as basic skeleton and preparation method of nano-suspension

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Weigh 0.5 g of poloxamer 188, add 50 ml of three-distilled water, heat at a slight temperature and magnetically stir to fully dissolve; add 0.5 g of SNX-2112 raw material drug, and add wet grinding media (the grinding media are different particle sizes mixed with glass beads or zirconia beads); high-speed wet milling for 24 h to obtain a milky white nanosuspension with a measured particle size of 202 nm and a zeta potential of -11.6mV.

Embodiment 2

[0051] Weigh 800.5 g of Tween, add 50 ml of triple-distilled water, heat at low temperature and magnetically stir to fully dissolve; add 0.5 g of Xbj-B11 raw material drug, circulate through the slit of the high-pressure homogenizer to prepare nano-suspension. Carry out homogenization with high-pressure homogenizer, under the condition of pressure 500 bar, circulate 10 times, 1000bar circulate 5 times, 1500bar circulate 5 times, maintain temperature in homogeneous process below 25 ℃, obtain milky white nano-suspension, The measured particle diameter is 216 nm, and the zeta potential is -21.2mV.

Embodiment 3

[0053] Weigh 0.05 g of SDS, add 50 ml of three-distilled water, heat at low temperature and magnetically stir to fully dissolve; add 0.5 g of Xbj-B16 raw material medicine, and add wet grinding medium (wherein the grinding medium is mixed glass beads of different particle sizes or zirconia beads); high-speed wet milling for 24 h to obtain a milky white nanosuspension with a measured particle size of 190 nm and a zeta potential of -35.4mV.

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
Login to View More

Abstract

The invention discloses a nano-suspension of an Hsp90 inhibitor by using benzamide as a basic skeleton and a preparation method of the nano-suspension. In the nano-suspension, the weight ratio of the Hsp90 inhibitor by using benzamide as the basic skeleton to a surfactant is 1 to 0.1-1 to 10. The nano-suspension has the characteristics of high drug content, small auxiliary dose, high stability, stable dissolution rate and the like, is applicable to multiple administration routes, in particular injection, is capable of overcoming the defects of poor water solubility, difficult administration, low bioavailability, strong toxic and side effects and the like, realizes technical breakthrough in the field, and provides a novel administration preparation with high drug content, high bioavailability and passive targeting to the Hsp90 inhibitors for the first time so as to accelerate the progress of the nano-suspension in clinical application.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a nano-suspension of Hsp90 inhibitor with benzamide as the basic skeleton and a preparation method thereof. Background technique [0002] Benzamide-Hsp90 inhibitor (BA-Hsp90 class) with benzamide as the basic skeleton is a new type of heat shock protein 90 (Hsp90) inhibitor screened in recent years. Hsp90 is an internationally recognized anti-tumor target. Hsp90, also known as stress protein 90, widely exists in prokaryotes and eukaryotes in the biological world, and is one of the most abundant proteins in cells. Since Hsp90 is an essential protein that assists cell DNA replication, and its expression in tumor cells is 210 times higher than that in normal cells, the targeting of Hsp90 inhibitors to cancer cells has been created. In vivo and in vitro experiments have proved that this type of compound has a significant inhibitory effect on the treatment of l...

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 Applications(China)
IPC IPC(8): A61K9/10A61K31/416A61K47/34A61K47/32A61K47/20A61K47/28A61P35/00
Inventor 王一飞董栋夏敏王怀玲
Owner 广州少伯控股集团有限公司
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

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com