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A nanosuspension of hsp90 inhibitor with benzamide as basic skeleton and preparation method thereof

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

Active Publication Date: 2016-09-07
广州少伯控股集团有限公司 +1
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  • 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

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  • A nanosuspension of hsp90 inhibitor with benzamide as basic skeleton and preparation method thereof
  • A nanosuspension of hsp90 inhibitor with benzamide as basic skeleton and preparation method thereof
  • A nanosuspension of hsp90 inhibitor with benzamide as basic skeleton and preparation method thereof

Examples

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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.

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Abstract

The invention discloses a nanosuspension of an Hsp90 inhibitor with benzamide as a basic skeleton and a preparation method thereof. The weight of the nanosuspension of the Hsp90 inhibitor with benzamide as a basic skeleton and surfactant The ratio is 1:0.1~1:10. The nano-suspension of the present invention has the characteristics of high drug content, small amount of excipients, good stability, stable dissolution rate, etc., and is suitable for various administration routes (especially for injection), which solves the problem of poor water solubility of such compounds , difficulty in drug administration, low bioavailability, strong toxic and side effects, etc., has achieved a technological breakthrough in this field, and for the first time provides a kind of Hsp90 inhibitor that can increase drug content, high bioavailability, and has a passive target New formulations for drug delivery in order to accelerate the process of its 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

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Application Information

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Patent Type & Authority Patents(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
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