Weighted Floating Dosage Form for Gastric Retention

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Solution Overview

Problem

Current gastric-retentive dosage forms face challenges in maintaining prolonged gastric residence time while being compact enough for easy swallowing and avoiding passage through the pyloric sphincter, with concerns of expansion-related malfunctions and potential blockages.

Innovation Solution

An elongate dosage form with a cylindrical shape, weighted at one end to float perpendicular to the gastric fluid surface, ensuring it remains in the stomach by resisting passage through the pyloric sphincter without relying on expansion or size increase, utilizing a weighting agent like barium sulphate to achieve this orientation.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Duration of action of moving object

If a dosage form is made large in size to resist passage through the pyloric sphincter, then gastric retention is improved, but the dosage form becomes difficult to swallow

Engineering Contradiction:
Improvegastric residence timeVSAvoidease of swallowing
Core Design Contradiction:
Duration of action of moving objectVSEase of operation

Solution Approach 1:

The dosage form is divided into two distinct parts: a buoyant body for gastric retention and a separate weighting agent that can be positioned at one end. This segmentation allows the dosage form to achieve the necessary size for pyloric resistance while maintaining a compact configuration for easy swallowing.

Inventive Principle:
Principle #1Segmentation

Solution Approach 2:

The invention introduces weight distribution as a new dimension of control. By positioning a weighting agent at one end of the buoyant body, the dosage form achieves directional orientation (perpendicular floating) that enhances gastric retention without increasing overall size, thus maintaining swallowability.

Inventive Principle:
Principle #17Another dimension (Dimensionality change)

2Duration of action of moving object

If a dosage form uses expansion mechanisms to increase size in the stomach, then gastric retention is improved, but the risk of malfunction and blockage increases

Engineering Contradiction:
Improvegastric residence timeVSAvoidrisk of malfunction and blockage
Core Design Contradiction:
Duration of action of moving objectVSReliability

Solution Approach 1:

The invention extracts the expansion mechanism entirely from the dosage form design. Instead of using swellable polymers or gas-generating agents that can malfunction, the dosage form maintains a constant size throughout gastric residence, eliminating the reliability issues associated with expansion mechanisms.

Inventive Principle:
Principle #2Taking out (Extraction)

Solution Approach 2:

The dosage form uses simple, inert materials (buoyant material and weighting agent) that maintain their physical properties throughout gastric residence without undergoing chemical changes or expansion, providing reliable and predictable performance.

Inventive Principle:
Principle #27Cheap short-living objects (Disposable)

3Duration of action of moving object

If a dosage form is made buoyant to float on gastric contents, then gastric retention is improved, but the dosage form may pass too rapidly through the pyloric sphincter

Engineering Contradiction:
Improvegastric residence timeVSAvoidpassage speed through pyloric sphincter
Core Design Contradiction:
Duration of action of moving objectVSSpeed

Solution Approach 1:

The dosage form uses asymmetric weight distribution with a weighting agent positioned at one end of the buoyant body. This creates an asymmetric floating orientation where the weighted end dips into the gastric contents while the other end remains at the surface, enhancing retention by reducing passage velocity through the pyloric sphincter.

Inventive Principle:
Principle #4Asymmetry

Solution Approach 2:

The invention controls passage speed by manipulating the orientation dimension rather than the size dimension. The perpendicular floating orientation caused by weight bias creates a larger effective profile as the dosage form attempts to pass through the pyloric sphincter, slowing its transit without increasing overall dimensions.

Inventive Principle:
Principle #17Another dimension (Dimensionality change)

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 dosage form effectively prolongs gastric residence time, allowing for sustained drug absorption and reducing the need for frequent dosing, while being designed for comfortable swallowing and minimizing the risk of blockages.

Implementation Method 1

the dosage form is weight biased such that it is heavier at one end than the other end

Methodology Applied
Scientific EffectBuoyancy: Archimedes' Principle (Buoyancy)

Implementation Method 2

weighted at one end with an appropriate weighting agent such that it floats in an aqueous fluid

Methodology Applied
Scientific EffectDensity gradient: Density Gradient

Implementation Method 3

weighted at one end with an appropriate weighting agent such that it floats in an aqueous fluid not with its long axis parallel to the surface of the fluid, but rather substantially perpendicular to it

Methodology Applied
Scientific EffectGravity: Gravitation

Data Source

PatentUS10076500B2Floating gastric retentive dosage form
Publication Date: 2018.09.18 JAGOTEC AG
  • US10076500B2 patent drawing
  • US10076500B2 patent drawing
  • US10076500B2 patent drawing

AI summary

An elongate dosage form of generally cylindrical shape having two opposing ends, the dosage form being buoyant in gastric fluid, wherein the dosage form is weight biased such that one end is heavier than the other end. The dosage form is adapted to float on gastric fluid with its long axis substantially perpendicular to the surface of the fluid with its heavier end pointing generally downwards and into the fluid.