Modified-Release Capsaicinoid Beadlets for Enteric Intestinal Delivery

Resolve Bottlenecks,
Find Innovative SolutionsGenerate Solutions

Solution Overview

Problem

Existing capsaicinoid formulations face challenges in handling pungency during preparation and administration, leading to skin irritation and gastric discomfort due to uncontrolled release in the stomach, with prior methods using organic solvents and incomplete intestinal absorption.

Innovation Solution

A modified release formulation using a solvent-free process, comprising capsaicinoids, emulsifiers, gastro-resistant pH-dependent polymers, and release modifying agents, forming non-sticky beadlets that release less than 10% in the stomach and more than 75% in the intestine within an hour, ensuring complete intestinal absorption.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Speed

If capsaicinoids are released in the stomach, then immediate availability is achieved, but gastric discomfort and irritation occur

Engineering Contradiction:

Improverelease speedVSAvoidgastric discomfort

Core Design Contradiction:

SpeedVSObject-affected harmful factors

Solution Approach 1:

The patent uses an enteric coating as an intermediary layer between the capsaicinoid core and the gastric environment. This coating prevents direct contact and release in the stomach, eliminating gastric discomfort while allowing controlled release in the intestine where absorption occurs.

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The formulation applies different release characteristics to different locations in the GI tract. The enteric coating creates a localized release profile that prevents gastric release while enabling intestinal release, optimizing both comfort and absorption at different anatomical sites.

Inventive Principle:

Principle #3Local quality

2Stability of the object's composition

If organic solvents are used in formulation, then capsaicinoid solubility is improved, but safety and environmental concerns arise

Engineering Contradiction:

ImprovesolubilityVSAvoidsafety concerns

Core Design Contradiction:

Stability of the object's compositionVSObject-affected harmful factors

Solution Approach 1:

The patent extracts and eliminates organic solvents from the formulation entirely, replacing them with water-based systems. This removal of harmful substances maintains solubility through alternative mechanisms while improving safety and environmental compatibility.

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The formulation changes the solvent parameter from organic to aqueous-based systems. By modifying the solvent type and using surfactants to enhance solubility in water, the patent achieves the same solubilization effect without the safety and environmental drawbacks of organic solvents.

Inventive Principle:

Principle #35Parameter changes

3Productivity

If capsaicinoids are released quickly in the stomach, then bioavailability increases, but incomplete intestinal absorption occurs

Engineering Contradiction:

ImprovebioavailabilityVSAvoidabsorption completeness

Core Design Contradiction:

ProductivityVSQuantity of substance

Solution Approach 1:

The enteric coating performs a preliminary protective action by preventing premature release in the stomach. This ensures that capsaicinoids are released only when they reach the intestine, the appropriate location for absorption, thereby maximizing both bioavailability and completeness of absorption.

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The formulation maintains continuous protection of the capsaicinoid core from the stomach through the intestine, ensuring that the release and absorption process occurs continuously and completely in the appropriate anatomical region without interruption or premature termination.

Inventive Principle:

Principle #20Continuity of useful action

4Ease of operation

If adhesive materials are used to prevent stickiness, then flowability improves, but additional formulation complexity increases

Engineering Contradiction:

ImproveflowabilityVSAvoidformulation complexity

Core Design Contradiction:

Ease of operationVSDevice complexity

Solution Approach 1:

The enteric coating serves multiple functions simultaneously: it prevents gastric release, provides a barrier against stickiness, and enables controlled intestinal release. By combining these functions in a single component, the patent improves flowability without significantly increasing formulation complexity.

Inventive Principle:

Principle #6Universality (Multi-functionality)

Data Source

PatentUS20260076915A1Modified release formulation comprising capsaicinoids and a process

Publication Date: 2026.03.19 NUTRIVENTIA PTE LTD

AI summary

The present invention relates to a modified release capsaicinoids formulation comprising of active core, at least one emulsifier and at least one gastro-resistant pH dependent polymer. The active core may be coated with at least one release modifying agent and optionally the outermost coating. The invention as described herein also relates to the solvent-free process, wherein emulsion comprising capsaicinoids is entrapped in at least one gastroresistant pH dependent polymer and deposited on non-pareil seeds to get active core, which may be further coated using at least one release modifying agent to get the beadlets. The formulation releases not more than 10% by weight of capsaicinoids in stomach within 2 hours, followed by release of not less than 75% of capsaicinoids in the intestine within 1 hour. The modified release formulation does not exhibit the alcohol dose dumping effect in stomach and it is safe for oral administration to the consumers.