Rifamycin-Nitroimidazole Coupling Solid Dispersion for Drug Resistance

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Solution Overview

Problem

Current antibacterial drugs for anaerobic and microaerobic infections, particularly those targeting drug-resistant bacteria, suffer from high resistance rates and inadequate cure rates, necessitating the development of new antibacterial drugs with improved efficacy and safety.

Innovation Solution

A solid dispersion formulation of a rifamycin-nitroimidazole coupling molecule, comprising a rifamycin-nitroimidazole coupling molecule, a polymer carrier, and functional excipients such as hydroxypropyl cellulose-L and sodium lauryl sulfate, is developed to enhance drug solubility and stability, ensuring rapid drug release and reduced resistance development.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Reliability

If conventional antibacterial drugs are used, then treatment is simple and cost-effective, but drug resistance increases and cure rates decrease

Engineering Contradiction:

Improvecurative effectVSAvoiddrug resistance

Core Design Contradiction:

ReliabilityVSObject-generated harmful factors

Solution Approach 1:

The patent combines two different antibacterial pharmacophores (rifamycin and nitroimidazole) into a single coupling molecule through covalent bonding. This merging of two distinct antibacterial mechanisms into one molecule creates a multi-target drug that effectively treats drug-resistant bacteria while maintaining simplicity of administration.

Inventive Principle:

Principle #5Merging (Combining)

Solution Approach 2:

The invention creates a composite antibacterial agent by chemically linking rifamycin and nitroimidazole moieties. This composite structure integrates the antibacterial properties of both parent compounds, producing a molecule with enhanced activity against anaerobes and microaerobes that have developed resistance to conventional single-mechanism drugs.

Inventive Principle:

Principle #40Composite materials

2Speed

If immediate release formulation is used, then drug release is rapid, but solubility and stability are insufficient

Engineering Contradiction:

Improvedrug release speedVSAvoidsolubility and stability

Core Design Contradiction:

SpeedVSReliability

Solution Approach 1:

The patent transforms the physical and chemical parameters of the rifamycin-nitroimidazole coupling molecule by converting it from a crystalline solid to an amorphous solid dispersion. This parameter change in molecular arrangement and physical state dramatically improves solubility and stability while maintaining rapid drug release characteristics.

Inventive Principle:

Principle #35Parameter changes

Solution Approach 2:

The invention utilizes phase transition from crystalline to amorphous state of the coupling molecule. By forming an amorphous solid dispersion, the drug achieves enhanced solubility and stability without sacrificing its rapid release profile, as the amorphous phase provides higher energy state and better dissolution characteristics.

Inventive Principle:

Principle #36Phase transitions

3Reliability

If amorphous solid dispersion is formed, then solubility improves, but manufacturing complexity increases

Engineering Contradiction:

ImprovesolubilityVSAvoidformulation complexity

Core Design Contradiction:

ReliabilityVSDevice complexity

Solution Approach 1:

The patent introduces polymer carriers as intermediary substances to facilitate the formation of amorphous solid dispersion. These carriers act as mediators that stabilize the amorphous state of the coupling molecule and simplify the manufacturing process, making it feasible to produce amorphous formulations using conventional pharmaceutical equipment and techniques.

Inventive Principle:

Principle #24Intermediary (Mediator)

Applied Scientific Principles

This section explains which scientific principles are used to turn an abstract innovation direction into a practical engineering solution.

Function Achieved in This Case

The formulation provides potent antibacterial activity against anaerobes and microaerobes, including drug-resistant strains, with improved sterilization speed and pharmacophore synergy, while maintaining good safety tolerance.

Implementation Method 1

Methodology Applied

Scientific EffectSolvation: Solvation

Implementation Method 2

functional excipients such as hydroxypropyl cellulose-L and sodium lauryl sulfate

Methodology Applied

Scientific EffectMicelle formation: Emulsion

Implementation Method 3

The solid dispersion of the rifamycin-nitroimidazole coupling molecule can be used as a formulation of a drug for treating microbial infection

Methodology Applied

Scientific EffectAmorphous dissolution:

Data Source

PatentEP3868378B1Solid dispersion of rifamycin-nitroimidazole coupling molecules and use thereof

Publication Date: 2025.09.03 TENNOR THERAPEUTICS (SUZHOU) LTD

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AI summary

The present invention provides a solid dispersion of a rifamycin-nitroimidazole coupling molecule, comprising a rifamycin-nitroimidazole coupling molecule of a structure shown in formula I, a polymer carrier, functional excipient and a solvent. The polymer carrier is selected from one or a combination of more of PVP K30, PVP-VA64, HPC-L, HPMC E3, Soluplus and polymethacrylate. The functional excipient comprise one or a combination of more of sodium lauryl sulfate, meglumine, VE-TPGS and Tween 80. The solid dispersion of the rifamycin-nitroimidazole coupling molecule of the present invention can be used as a formulation of a drug for treating microbial infection.