Pyrrole Gastric Acid Injection via Cyclodextrin Stabilization

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Solution Overview

Problem

Current proton pump inhibitors are not available in injectable form, which limits their use for patients requiring rapid therapeutic action, especially those with gastrointestinal bleeding or acute peptic ulcers who cannot tolerate oral administration. Additionally, existing lyophilized powder forms require numerous excipients, are costly, and have stability issues that prevent terminal sterilization.

Innovation Solution

An injectable composition containing a pharmaceutically acceptable salt of a pyrrole compound, specifically the hydrochloride salt represented by formula II, combined with a stabilizer such as edetate, which improves solubility and stability, reducing the need for additional excipients and allowing for terminal sterilization.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Productivity

If proton pump inhibitors are formulated as oral solid preparations, then manufacturing is simple and cost-effective, but compliance is poor for patients requiring rapid therapeutic action

Engineering Contradiction:

Improvemanufacturing efficiencyVSAvoidpatient compliance

Core Design Contradiction:

ProductivityVSEase of operation

Solution Approach 1:

The patent changes the physical state parameter from solid (tablet) to liquid (injection solution), enabling rapid therapeutic action through parenteral administration while maintaining manufacturing feasibility through the use of cyclodextrin inclusion complexes that stabilize the active ingredient in solution form

Inventive Principle:

Principle #35Parameter changes

2Speed

If proton pump inhibitors are formulated as lyophilized powder for injection, then rapid onset of therapeutic action is achieved, but the number of excipients and packaging costs increase

Engineering Contradiction:

Improveonset of therapeutic actionVSAvoidnumber of excipients

Core Design Contradiction:

SpeedVSDevice complexity

Solution Approach 1:

The patent extracts and removes unnecessary excipients from the formulation by using cyclodextrin inclusion complexes that provide stabilization functionality internally, eliminating the need for multiple separate excipients required in traditional lyophilized powder formulations

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent creates a composite inclusion complex where the active ingredient is encapsulated within cyclodextrin molecules, forming a stable complex that can be directly formulated as an injection solution without requiring additional stabilizing excipients or lyophilization processing

Inventive Principle:

Principle #40Composite materials

3Reliability

If terminal sterilization is applied to lyophilized powder for injection, then sterility assurance is maximized, but production costs increase due to stability constraints

Engineering Contradiction:

Improvesterility assuranceVSAvoidproduction cost

Core Design Contradiction:

ReliabilityVSEase of manufacture

Solution Approach 1:

The patent provides beforehand cushioning by using cyclodextrin inclusion complexes to pre-stabilize the active ingredient against degradation, creating a formulation that is inherently stable enough to withstand terminal sterilization conditions without requiring expensive cold chain storage or specialized packaging

Inventive Principle:

Principle #11Beforehand cushioning (Prior cushioning)

4Speed

If lyophilized powder for injection is used, then rapid therapeutic action is achieved, but storage requirements become more stringent

Engineering Contradiction:

Improveonset of therapeutic actionVSAvoidstorage stability

Core Design Contradiction:

SpeedVSStability of the object's composition

Solution Approach 1:

The patent changes the physical state from solid (lyophilized powder) to liquid (injection solution) while maintaining stability through cyclodextrin inclusion complexes, enabling the formulation to be stored at conventional temperatures without requiring cold chain storage while still providing rapid therapeutic action through parenteral administration

Inventive Principle:

Principle #35Parameter changes

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 injectable composition provides a rapid and effective therapeutic action for gastric acid-related diseases, with improved stability and safety, meeting the clinical requirements for quick onset of action and reducing adverse reactions from excipients.

Implementation Method 1

a stabilizer, where the stabilizer is an edetate

Methodology Applied

Scientific EffectChelation:

Data Source

PatentEP4566602A1Pharmaceutical composition containing pyrrole gastric acid secretion inhibitor and preparation method therefor

Publication Date: 2025.06.11 JIANGSU CAREFREE PHARM CO LTD

AI summary

A pharmaceutical composition containing a pyrrole gastric acid secretion inhibitor and a preparation method therefor are provided. The pharmaceutical composition includes a pharmaceutically acceptable salt of a compound represented by formula I, and a stabilizer. Also provided is a method for preparing the pharmaceutical composition. The method is simple, cost-effective, and suitable for industrial mass production. At present, no injectable composition of the pharmaceutical compound is available clinically.