Dry Mixing Melatonin Tablets for Uniform Content

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Solution Overview

Problem

The challenge lies in developing a rapid-release melatonin formulation in solid dosage form that can be manufactured on a large scale without the need for wet processing steps, as traditional methods face issues with homogeneity and the use of organic solvents, which are hazardous in industrial production.

Innovation Solution

A method involving dry mixing steps, including stepwise addition of micronized melatonin and microcrystalline cellulose, along with fillers, glidants, and disintegrants, to create a solid dosage form that is homogeneously distributed and free from solvent use, facilitating efficient large-scale production.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Manufacturing precision

If wet granulation is used to improve homogeneity of melatonin distribution, then content uniformity is improved, but the process requires organic solvents and reduces large scale production capacity

Engineering Contradiction:

Improvecontent uniformityVSAvoidlarge scale production capacity

Core Design Contradiction:

Manufacturing precisionVSProductivity

Solution Approach 1:

The patent removes the wet granulation step and organic solvent requirements from the manufacturing process, extracting only the essential function of achieving homogeneous distribution through dry mixing techniques with specific excipient combinations

Inventive Principle:

Principle #2Taking out (Extraction)

Solution Approach 2:

The patent changes the physical parameters of melatonin by micronization (reducing particle size to D90 ≤ 30 μm) and modifies the formulation parameters by using specific ratios of excipients (MCC 20-35%, filler 65-75%, glidant 0.2-0.8%, disintegrant 1-3%) to achieve homogeneous distribution without wet processing

Inventive Principle:

Principle #35Parameter changes

2Productivity

If dry mixing is used to maintain large scale production capacity, then productivity is improved, but homogeneity of melatonin distribution deteriorates

Engineering Contradiction:

Improvelarge scale production capacityVSAvoidcontent uniformity

Core Design Contradiction:

ProductivityVSManufacturing precision

Solution Approach 1:

The patent performs preliminary micronization of melatonin before mixing, and pre-establishes optimal excipient ratios and particle size distributions to ensure homogeneous distribution is achieved during the dry mixing process itself, without requiring subsequent wet granulation steps

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The patent uses microcrystalline cellulose (MCC) as an intermediary carrier material that facilitates homogeneous distribution of micronized melatonin particles during dry mixing, with MCC serving as a bridging substance between the active ingredient and other excipients

Inventive Principle:

Principle #24Intermediary (Mediator)

3Manufacturing precision

If organic solvents are used in wet granulation to improve homogeneity, then content uniformity is improved, but safety hazards and manufacturing complexity increase

Engineering Contradiction:

Improvecontent uniformityVSAvoidsafety hazards

Core Design Contradiction:

Manufacturing precisionVSObject-affected harmful factors

Solution Approach 1:

The patent converts the potential harm of requiring wet granulation for homogeneity into a benefit by demonstrating that dry mixing with properly micronized material and optimized excipient ratios can achieve equal or better uniformity without solvent-related safety hazards

Inventive Principle:

Principle #22Blessing in disguise (Convert harm into benefit)

Solution Approach 2:

The patent creates an inert, solvent-free manufacturing environment by using entirely dry processing techniques with food-grade excipients, eliminating the need for organic solvents and their associated safety hazards while maintaining content uniformity

Inventive Principle:

Principle #39Inert atmosphere (Inert environment)

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

This approach enables the production of high-quality, rapidly releasing melatonin tablets with uniform content distribution, overcoming the limitations of traditional methods by eliminating the need for solvents and enhancing manufacturing efficiency.

Implementation Method 1

A method involving dry mixing steps, including stepwise addition of micronized melatonin and microcrystalline cellulose

Methodology Applied

Scientific EffectDry mixing:

Implementation Method 2

rapidly releasing melatonin tablets with uniform content distribution

Methodology Applied

Scientific EffectDissolution:

Data Source

PatentUS20240269079A1Melatonin formulation in solid dosage form

Publication Date: 2024.08.15 AGB PHARMA AB

AI summary

The present invention relates to a melatonin formulation in solid dosage form with a rapid-release profile and methods for preparation thereof. In particular, the present invention relates to a melatonin tablet that can be prepared in a dry mixing process without the need for any solvents, such as organic solvents.