Nitroxoline Lysinate Dual-Layer Tablet for Burst and Sustained Release
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Solution Overview
Problem
The existing pharmaceutical compositions of nitroxoline lack improved water solubility, which hinders its druggability and activity, necessitating a formulation that enhances both dissolution properties and drug release profiles.
Innovation Solution
A pharmaceutical composition of nitroxoline lysinate is developed, comprising a dual-layer structure with specific ratios of active pharmaceutical ingredient, filler, disintegrant, lubricant, glidant, and alkaline substance, optimized for burst release in the early stage and sustained slow release in the later stage, utilizing nitroxoline lysinate monohydrate as the active ingredient.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If nitroxoline is used as an oral antibiotic, then it can treat urinary system infections, but its water solubility is poor which hinders druggability and activity
Solution Approach 1:
The patent changes the chemical form of nitroxoline from free base to lysinate salt, fundamentally altering its solubility parameters. The nitroxoline lysinate salt exhibits significantly improved water solubility compared to parent nitroxoline, directly addressing the solubility issue while maintaining antibiotic activity
Solution Approach 2:
The patent creates a composite pharmaceutical composition with a dual-layer structure containing nitroxoline lysinate salt combined with specific excipients (fillers, disintegrants, lubricants, glidants, and alkaline substances). This composite formulation optimizes both solubility and drug release characteristics, resolving the contradiction between improved solubility and manufacturing performance
2Duration of action of moving object
If a single-layer pharmaceutical composition is used, then the formulation is simple, but it cannot achieve both burst release in early stage and sustained slow release in later stage
Solution Approach 1:
The patent divides the pharmaceutical composition into two distinct layers: a first layer containing nitroxoline lysinate salt with fast-dissolving excipients for burst release (0-2 hours), and a second layer containing the same salt with sustained-release excipients for slow release (2-12 hours). This segmentation enables different release profiles in different temporal stages while maintaining a unified tablet structure
Solution Approach 2:
The patent introduces a vertical dimensional structure by forming a dual-layer tablet where the first layer is compressed at a lower density and the second layer at a higher density. This vertical stratification allows simultaneous achievement of fast and sustained release mechanisms within a single oral dosage form, resolving the contradiction between release profile complexity and formulation simplicity
Data Source
AI summary
Pharmaceutical compositions comprising nitroxoline lysinate, a preparation method therefor and a use thereof. The pharmaceutical compositions comprise a first layer and a second layer. The first layer comprises, based on the total weight of the first layer, 40%-70% of active pharmaceutical ingredient, 10%-30% of filler, 5%-12% of disintegrant, 0.5%-2% of lubricant, 0.1%-1.5% of glidant and 10%-20% of alkaline substance. The second layer comprises, based on the total weight of the second layer, 40%-70% of active pharmaceutical ingredient, 10%-30% of filler, 10%-35% of sustained-release material, 0.1%-2% of lubricant and 0.1%-2% of glidant. The active pharmaceutical ingredient is selected from one or more of nitroxoline lysinate, nitroxoline lysinate crystalline form and nitroxoline lysinate solvate. The pharmaceutical compositions can achieve the purpose of burst release at an early stage and sustained and slow release at a later stage.