Cinacalcet Oral Solution Solubility and Taste Masking
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Solution Overview
Problem
Cinacalcet and its pharmaceutically acceptable salts have poor water solubility and a bitter taste, making it difficult to develop effective oral liquid dosage forms that are convenient for patients, especially children and the elderly, and existing suspension forms suffer from instability and poor flow behavior.
Innovation Solution
An oral pharmaceutical solution comprising a pharmaceutically acceptable cinacalcet salt combined with a mixture of propylene glycol and polyethylene glycol, a polyol, polyvinylpyrrolidone, and a buffer, which provides improved solubility, taste masking, and stability, preventing precipitation and ensuring reproducible bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Ease of manufacture
If oral solid dosage forms (tablets) are used for cinacalcet, then ease of management is improved, but patient compliance deteriorates due to difficulty in swallowing
Solution Approach 1:
The patent changes the physical state parameter of the dosage form from solid (tablet) to liquid (oral solution), making it suitable for patients who have difficulty swallowing tablets while maintaining ease of administration through simple oral ingestion
2Ease of operation
If oral liquid dosage forms are developed for cinacalcet, then patient compliance is improved, but formulation complexity increases due to poor water solubility
Solution Approach 1:
The patent introduces polyethylene glycol as an intermediary substance that mediates between the poorly water-soluble cinacalcet and the aqueous environment, enabling the formation of a clear oral solution without requiring complex suspension or emulsion systems
Solution Approach 2:
The patent changes the solubility parameter of cinacalcet by using polyethylene glycol as a solvent system, transforming it from a poorly water-soluble substance into a form that can be delivered as a clear oral liquid solution
3Quantity of substance
If cinacalcet oral solution is formulated, then solubility is improved, but taste bitterness worsens
Solution Approach 1:
The patent uses polyethylene glycol as a taste-masking intermediary that not only improves solubility but also masks the bitter taste of cinacalcet, making the oral solution palatable for patients
Solution Approach 2:
The patent changes the chemical environment parameters by using polyethylene glycol as the solvent system, which simultaneously improves solubility and masks the bitter taste through its interaction with the active substance
4Quantity of substance
If suspension dosage form is used, then solubility issues are addressed, but stability deteriorates due to precipitation and poor flow behavior
Solution Approach 1:
The patent changes the physical state parameter from suspension (heterogeneous) to clear solution (homogeneous), eliminating precipitation issues and ensuring long-term stability during storage
Solution Approach 2:
The patent creates a homogeneous clear solution system where cinacalcet is uniformly dissolved in the polyethylene glycol-based solvent system, eliminating the heterogeneity and instability inherent in suspension formulations
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 solution offers a stable, palatable, and flexible dosing regimen with enhanced patient compliance, avoiding the issues of bitterness and instability seen in previous formulations, and provides improved bioavailability and organoleptic characteristics.
Implementation Method 1
An oral pharmaceutical solution comprising a pharmaceutically acceptable cinacalcet salt combined with a mixture of propylene glycol and polyethylene glycol
Implementation Method 2
a buffer, wherein the pH of the solution is from 4.0 to 7.5
Data Source
AI summary
Oral pharmaceutical solution comprising a pharmaceutically acceptable cinacalcet salt and a pharmaceutically acceptable carrier comprising a mixture of propylene glycol and a polyethylene glycol, or a mixture of two polyethylene glycols, a polyol, a polymer selected from polyvinylpyrrolidone and/or copovidone, water, and a buffer, wherein the pH of the solution is from 4.0 to 7.5.