PEG Chewable Solid Formulation for Constipation Management

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Solution Overview

Problem

Current PEG-based solid dosage forms for gastrointestinal health and constipation management face challenges in achieving the right balance of structural integrity, palatability, and manufacturing ease, particularly for healthy subjects who require a low-dose, chronic regimen without causing discomfort or inconvenience, and existing formulations often include unpleasant taste and mouthfeel issues.

Innovation Solution

A solid formulation comprising 50-90% w/w polyethylene glycol (PEG) with an average molecular weight of 2,000 to 10,000 Da, combined with 10-40% w/w of sorbitol, lactose, dextrates, cellulose, xylitol, or mannitol, and optional flavorings and lubricants, which is designed to be chewable or suckable, minimizing electrolytes and osmotic agents to enhance palatability and manufacturing properties.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Strength

If PEG is formulated as a solid dosage form with high structural integrity, then manufacturing and handling become easier, but chewability and palatability deteriorate

Engineering Contradiction:
Improvestructural integrityVSAvoidchewability
Core Design Contradiction:
StrengthVSEase of operation

Solution Approach 1:

The patent combines PEG with multiple excipients including mannitol, sorbitol, lactose, and starch to create a composite tablet formulation. This composite structure maintains structural integrity for easy manufacturing and handling while the excipient components improve chewability and palatability, resolving the contradiction between strength and ease of operation.

Inventive Principle:
Principle #40Composite materials

Solution Approach 2:

The patent optimizes the molecular weight of PEG (selecting specific ranges) and adjusts the proportions of various excipients to achieve the right balance. By changing physical and chemical parameters of the formulation components, the tablet achieves both sufficient structural integrity and acceptable chewability for patient compliance.

Inventive Principle:
Principle #35Parameter changes

2Quantity of substance

If PEG is administered in high doses as aqueous solution, then laxative effect is achieved, but convenience and portability deteriorate

Engineering Contradiction:
ImprovePEG doseVSAvoidconvenience
Core Design Contradiction:
Quantity of substanceVSEase of operation

Solution Approach 1:

The patent transforms PEG from an aqueous liquid solution form into a solid tablet dosage form. This phase transition allows the same therapeutic dose of PEG to be delivered in a portable, convenient solid format that does not require carrying large volumes of liquid or using preparation vessels, thereby improving convenience while maintaining the required quantity of substance.

Inventive Principle:
Principle #36Phase transitions

3Reliability

If electrolytes and osmotic agents are added to enhance laxative capability, then therapeutic effect improves, but taste and mouthfeel deteriorate

Engineering Contradiction:
Improvelaxative capabilityVSAvoidpalatability
Core Design Contradiction:
ReliabilityVSEase of operation

Solution Approach 1:

The patent removes or minimizes electrolytes and additional osmotic agents from the formulation. Instead, it relies on PEG as the primary active ingredient with excipients like mannitol and sorbitol that provide both structural benefits and improved taste/mouthfeel properties, thereby maintaining laxative capability while eliminating unpleasant taste and mouthfeel.

Inventive Principle:
Principle #2Taking out (Extraction)

4Quantity of substance

If multiple units of solid dosage form are consumed to achieve therapeutic dose, then adequate PEG intake is ensured, but patient compliance deteriorates

Engineering Contradiction:
ImprovePEG intakeVSAvoidpatient compliance
Core Design Contradiction:
Quantity of substanceVSEase of operation

Solution Approach 1:

The patent consolidates the required therapeutic dose of PEG into a single tablet formulation by optimizing the concentration of PEG and combining it with excipients that improve palatability and chewability. This merging of dose and improved properties into one unit reduces the number of tablets patients need to take, thereby improving patient compliance while ensuring adequate PEG intake.

Inventive Principle:
Principle #5Merging (Combining)

Data Source

PatentEP2635264B8Formulations comprising polyethylene glycol
Publication Date: 2018.07.18 NORGINE BV

AI summary

The present invention concerns a solid formulation for oral administration as a solid comprising polyethylene glycol and a further solid such as mannitol. The formulation may be used to prevent gastrointestinal disorders such as constipation in healthy subjects. In some embodiments, the solid formulation is chewable or suckable.