Pulsed Release Caffeine Formulations Using pH-Sensitive Polymers

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Solution Overview

Problem

Existing caffeine formulations either result in burst effects or extended release, leading to sudden peaks and drops in caffeine levels, requiring frequent administration and disrupting nighttime rest due to continuous caffeine consumption.

Innovation Solution

Development of pulsed release caffeine formulations using a combination of caffeine, shellac, and release retarding agents such as hydrophilic and lipophilic substances, pH-sensitive polymers, and waxes, which are formulated into particulate systems that release specific percentages of caffeine over 2 to 12 hours at various physiological pH conditions, ensuring sustained caffeine levels without peaks or drops.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If conventional caffeine formulations are used, then immediate release and peak caffeine levels are achieved, but frequent dosing is required and nighttime rest is disrupted

Engineering Contradiction:

Improvecaffeine release speedVSAvoidduration of caffeine effect

Core Design Contradiction:

SpeedVSDuration of action of moving object

Solution Approach 1:

The formulation is divided into multiple particulate systems with different release characteristics (immediate release, sustained release, and delayed release components). Each particulate system contains caffeine combined with specific release retarding agents in varying ratios, creating a segmented structure that releases caffeine at different rates and times throughout the gastrointestinal tract, thereby eliminating the need for frequent dosing while avoiding nighttime disruption.

Inventive Principle:

Principle #1Segmentation

2Duration of action of moving object

If controlled release mechanisms are used, then extended release over 6-10 hours is achieved, but complex multi-layer structures are required

Engineering Contradiction:

Improveduration of caffeine releaseVSAvoidformulation structure complexity

Core Design Contradiction:

Duration of action of moving objectVSDevice complexity

Solution Approach 1:

The patent employs composite particulate systems where caffeine is combined with multiple release retarding agents (hydrophilic substances, lipophilic substances, pH-sensitive polymers, and waxes) in specific ratios. These composite materials provide controlled release functionality through their inherent properties rather than requiring complex multi-layer structural designs, thereby achieving extended release with simpler formulation architecture.

Inventive Principle:

Principle #40Composite materials

3Duration of action of stationary object

If release retarding agents are used to delay release, then enteric coating is required, but additional manufacturing steps are added

Engineering Contradiction:

Improvedelayed release timingVSAvoidmanufacturing process simplicity

Core Design Contradiction:

Duration of action of stationary objectVSEase of manufacture

Solution Approach 1:

The patent utilizes pH-sensitive polymers as release retarding agents that automatically change their release properties in response to pH variations along the gastrointestinal tract. This parameter-based control (pH-triggered release) eliminates the need for additional enteric coating steps and complex manufacturing processes, as the release timing is controlled by the physiological environment rather than additional protective layers.

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 formulations achieve a gradual release of caffeine in pulses over the entire gastrointestinal tract, maintaining effective caffeine levels for a specific time interval without interfering with nighttime rest, providing sustained energy and alertness without the need for frequent dosing.

Implementation Method 1

release retarding agents such as hydrophilic and lipophilic substances, pH-sensitive polymers, and waxes, which are formulated into particulate systems that release specific percentages of caffeine over 2 to 12 hours at various physiological pH conditions

Methodology Applied

Scientific EffectpH sensitivity:

Implementation Method 2

the said particulate system comprises: a) caffeine, b) shellac, c) release retarding agent selected from hydrophilic substances, lipophilic substances, pH sensitive polymers, fatty substances, waxes and the combination thereof

Methodology Applied

Scientific EffectRelease retarding:

Data Source

PatentUS20220151941A1Pulsed release caffeine formulations and a process for preparation thereof

Publication Date: 2022.05.19 OMNIACTIVE HEALTH TECH LTD

AI summary

The present invention describes pulsed release caffeine formulations comprising caffeine particulate systems prepared by using release retarding agents and at least one or more food grade excipients. The present invention also relates to the process for preparation of caffeine formulations, wherein plurality of particulate systems combined to get the pulsed release caffeine formulation comprising release retarding agents, which provide caffeine release in pulses at different physiological conditions. The pulsed release caffeine formulation is prepared as tablets, capsules, soft gel capsules, caplets, oil suspensions or mixed with nutrient supplements for administration to the subjects. Caffeine formulations as described herein release the caffeine over entire GIT in pulses in a period of 2 to 8 hours and can be administered to subjects for boosting energy, improving concentration, cardiovascular health and for weight management.