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Solid dispersoid of rifamycin-quinazone coupling molecule and application thereof

A solid dispersion, rifamycin technology, applied in the field of medicine, can solve the problems of lack of high dissolution rate and the like

Active Publication Date: 2019-03-12
TENNOR THERAPEUTICS (SUZHOU) LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the prior art, there is also a lack of preparations of rifamycin-quinazinone coupling molecules with high dissolution rate and reliable curative effect

Method used

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  • Solid dispersoid of rifamycin-quinazone coupling molecule and application thereof
  • Solid dispersoid of rifamycin-quinazone coupling molecule and application thereof
  • Solid dispersoid of rifamycin-quinazone coupling molecule and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0123] This example provides a solid dispersion of rifamycin-quinazinone conjugated molecules, the components of which include rifamycin-quinazinone conjugated molecules with the structure shown in formula I, a polymer carrier and a solvent.

[0124]

[0125] The rifamycin-quinazinone conjugate molecule of this example (as shown in Formula I, abbreviated as API or API for convenience) is produced by Danuo Pharmaceutical (Suzhou) Co., Ltd.

[0126] The polymer carrier includes povidone K30 (i.e. polyvinylpyrrolidone K30), povidone VA64 (i.e. polyvinylpyrrolidone VA64), hydroxypropyl cellulose L (HPC-L), polyvinyl caprolactam-polyvinyl acetate - One or more of polyethylene glycol graft copolymer (Soluplus), polymethacrylate (Eutragit EPO, Eudragit EPO) and vitamin E-polyethylene glycol succinate (VE-TPGS) The combination.

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Abstract

The invention provides a solid dispersoid of a rifamycin-quinazone coupling molecule. Components of the solid dispersoid comprise the rifamycin-quinazone coupling molecule in structure as shown in a formula I, a high-molecular carrier, a functional auxiliary material and a solvent. The high-molecular carrier comprises one or combination of povidone K30, povidone VA64, hydroxy propyl cellulose L, apolyvinyl caprolactam-polyvinyl acetate-polyethylene glycol grafted copolymer and polymethacrylate. The functional auxiliary material comprises one or combination of vitamin E polyethylene glycol succinate, lauryl sodium sulfate, meglumine and Tween 80. The formula is as shown in the description. The solid dispersoid of the rifamycin-quinazone coupling molecule can be used as a preparation of a drug for treating bacterial infection.

Description

technical field [0001] The invention relates to a solid dispersion of rifamycin-quinazinone coupling molecules and an application thereof, belonging to the technical field of medicine. Background technique [0002] The rifamycin-quinazinone coupling molecule, with the structure shown in formula I in this manual, is a semi-synthetic broad-spectrum antibacterial drug, composed of rifamycin and quinazinone pharmacophore linked by stable covalent bonds, is A new type of antibacterial drug with a multi-target mechanism of action. The rifamycin-quinazinone conjugate molecule can selectively interact with DNA-dependent RNA polymerase to inhibit the transcription process of bacterial DNA. At the same time, by interacting with DNA topoisomerases (including DNA gyrase and DNA topoisomerase IV), it prevents the mutual conversion between DNA topoisomers and inhibits the process of DNA replication, recombination and transcription. Through the synergistic effect of the coupled pharmacop...

Claims

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Application Information

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IPC IPC(8): A61K31/395A61K31/4375A61K9/14A61K9/70A61K47/32A61K47/38A61K47/22A61K47/34A61P31/04
CPCA61K9/146A61K9/7007A61K31/395A61K31/4375A61K47/22A61K47/32A61K47/34A61K47/38A61P31/04A61K2300/00
Inventor 刘宇徐向毅马振坤
Owner TENNOR THERAPEUTICS (SUZHOU) LTD
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