Dynamic pH Control Apparatus for In Vitro Dissolution Testing

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Solution Overview

Problem

Current in vitro dissolution testing methods for pH-dependent drug coatings fail to accurately simulate the gastrointestinal environment, leading to inconsistent drug-release characteristics in vivo due to differences in buffer characteristics and rapid pH changes that do not reflect physiological conditions.

Innovation Solution

An apparatus and method that utilize a bicarbonate-based medium with automated pH control, temperature regulation, and gas bubbling to mimic the gastrointestinal pH changes, allowing for stable and realistic simulation of in vivo conditions, including the use of carbon dioxide for pH reduction and helium for pH increase, to test the solubility and dissolution of dosage forms.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If conventional stirred tanks with buffering systems are used for in vitro dissolution testing, then the testing process is simple to operate, but the pH changes do not reflect physiological conditions in the human gut

Engineering Contradiction:
Improveease of operationVSAvoidreliability
Core Design Contradiction:
Ease of operationVSReliability

Solution Approach 1:

The patent implements dynamic pH control by replacing static buffering systems with a automated pH control system that dynamically adjusts pH levels to simulate physiological conditions in the human gastrointestinal tract, resolving the contradiction between operational simplicity and physiological accuracy

Inventive Principle:
Principle #15Dynamics

Solution Approach 2:

The patent changes the pH parameter over time to match in vivo conditions, using automated control to transition between different pH stages (stomach, small intestine, large intestine) rather than maintaining constant pH levels, thereby improving reliability while maintaining ease of operation through automation

Inventive Principle:
Principle #35Parameter changes

2Productivity

If rapid single switch from acid environment to appropriate pH is used, then the testing procedure is quick and efficient, but it does not reflect the gradual pH changes in the human gut

Engineering Contradiction:
ImproveproductivityVSAvoidmeasurement precision
Core Design Contradiction:
ProductivityVSMeasurement precision

Solution Approach 1:

The patent applies periodic action by implementing staged pH transitions that progressively move through different pH levels to simulate the gradual environment changes in the gastrointestinal tract, replacing rapid single switches with controlled sequential changes that maintain both efficiency and measurement precision

Inventive Principle:
Principle #19Periodic action

Solution Approach 2:

The system performs preliminary action by pre-programming the pH transition profile to match physiological conditions before testing begins, allowing the automated system to execute precise pH changes without manual intervention, thus maintaining productivity while improving measurement precision

Inventive Principle:
Principle #10Preliminary action

3Ease of manufacture

If buffers with significantly different characteristics from physiological buffering are used, then the testing system is easy to manufacture and operate, but the test results fail to predict in vivo behavior accurately

Engineering Contradiction:
Improveease of manufactureVSAvoidreliability
Core Design Contradiction:
Ease of manufactureVSReliability

Solution Approach 1:

The patent changes the buffer characteristics to match physiological conditions by using bicarbonate-based buffers with pH levels and compositions that replicate the human gastrointestinal environment, improving reliability while maintaining ease of manufacture through standardized buffer formulations

Inventive Principle:
Principle #35Parameter changes

Solution Approach 2:

The patent implements feedback control by continuously monitoring pH levels and automatically adjusting buffer composition and pH control to maintain physiological accuracy, ensuring test results reliably predict in vivo behavior while keeping the system easy to operate through automated compensation

Inventive Principle:
Principle #23Feedback

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 apparatus effectively maintains a stable bicarbonate-based medium, enabling accurate prediction of in vivo drug-release profiles and improving the consistency of drug delivery by simulating the dynamic pH changes in the gastrointestinal tract, thus enhancing the efficacy of pH-dependent drug formulations.

Implementation Method 1

supplying a pH reducing fluid into the solvent medium to reduce the pH of the solvent medium... supplying carbon dioxide to the solvent medium to stabilise the pH of the solvent medium

Methodology Applied
Scientific EffectCarbon dioxide dissolution and acidification: Solvation

Implementation Method 2

supplying a pH increasing fluid into the solvent medium to increase the pH of the solvent medium... supplying helium to the solvent medium

Methodology Applied
Scientific EffectGas sparging and pH adjustment: Sparging

Implementation Method 3

temperature regulation... The bath 10 and test chambers 12 are held within test device 16 which provides for appropriate heating and cooling of the stabilisation liquid 14

Methodology Applied
Scientific EffectTemperature regulation: Heating

Implementation Method 4

utilisation of a bicarbonate based medium as a solvent medium... supplying carbon dioxide to the solvent medium to stabilise the pH of the solvent medium

Methodology Applied
Scientific EffectBuffering:

Data Source

PatentEP2844999B1Apparatus and method for testing medicaments
Publication Date: 2020.02.26 UCL BUSINESS LTD
  • EP2844999B1 patent drawingFigure 1
  • EP2844999B1 patent drawingFigure 2
  • EP2844999B1 patent drawingFigure 3

AI summary

Apparatus for testing the solubility of a medical dosage form includes a chamber (12) for holding a solvent medium (18), in the preferred embodiment a bicarbonate based buffer system. The apparatus also includes a pH probe (66) which is connectable to a supply of carbon dioxide (32, 34),as well as to a supply of helium (40), the supplies being controlled by a control unit (50). The control unit (50) monitors changes in pH of the solvent medium (18) and, as appropriate, feeds pH increasing and/or p H reducing gas from the supplies(32, 34, 40) into the chamber (12). The control unit (50) is able to maintain a uniform pH during testing or to provide a dynamically adjustable pH during testing, for example to three or more different pH levels in order to test the performance of a drug carrier at different levels of acidity or alkalinity for example, mimicking the conditions of the gastrointestinal tract. The apparatus(20) and associated method are particularly suitable for testing and developing dosage forms for oral delivery of drugs.