Oral Pharmaceutical Formulation with Permeability Enhancer
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Solution Overview
Problem
The bioavailability of 1-(2-thien-2'-yl-2-oxo-ethyl)-3-(methanesulfonyl hydrazine carbonyl) pyridinium compounds, particularly when administered orally, is very low, requiring high doses to achieve a therapeutically effective response, which is a limitation in treating diseases associated with advanced glycation end products.
Innovation Solution
An oral pharmaceutical formulation comprising the compound, its pharmaceutically acceptable salts or co-crystals, combined with a permeability enhancing agent and a base or buffer, which creates a suitable microenvironment in the upper GI tract for enhanced absorption, thereby increasing bioavailability.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high doses of the compound are administered orally, then therapeutically effective response is achieved, but bioavailability remains very low
Solution Approach 1:
The patent introduces a permeability enhancer as an intermediary substance that facilitates the absorption of the compound through the gastrointestinal tract. The permeability enhancer creates a microenvironment that improves intestinal permeability, allowing the compound to be absorbed more efficiently without requiring high doses, thus resolving the contradiction between therapeutic effectiveness and oral bioavailability.
2Reliability
If high doses are used to compensate for low bioavailability, then therapeutic response is achieved, but treatment safety and tolerability are compromised
Solution Approach 1:
The patent changes the physical-chemical parameters of the formulation by incorporating a permeability enhancer and adjusting pH conditions. This creates a favorable microenvironment in the upper GI tract that enhances compound absorption, allowing therapeutic doses to be reduced to safe and tolerable levels while maintaining therapeutic response.
3Ease of operation
If the compound is administered in standard oral formulations, then ease of administration is maintained, but absorption in the upper GI tract is insufficient
Solution Approach 1:
The permeability enhancer acts as a mediator that bridges the gap between the compound and the absorption sites in the upper GI tract. It temporarily modifies the intestinal environment to enhance permeability, allowing standard oral formulations to achieve sufficient absorption without compromising ease of administration.
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 significantly boosts the oral bioavailability of the compound, allowing for a therapeutically effective response at lower doses, effectively addressing the low bioavailability issue and improving treatment efficacy for diseases related to advanced glycation end products.
Implementation Method 1
combined with a permeability enhancing agent and a base or buffer, which creates a suitable microenvironment in the upper GI tract for enhanced absorption
Data Source
AI summary
This invention relates to pharmaceutical formulations comprising 1-(2-thien-2'-yl-2-oxo-ethyl)-3-(methanesulfonyl hydrazine carbonyl) pyridinium, its pharmaceutically acceptable salts, salt-cocrystals and co-crystals, particularly 1-(2-thien-2'-yl-2-oxo-ethyl)-3-5(methanesulfonyl hydrazine carbonyl) pyridinium chloride. The formulations are suitable for oral administration and also comprise a permeability enhancer or a suitable base or a mixture thereof. The formulations of this invention are for treating diseases associated with advanced glycation end products