Rosuvastatin Pellet Composition for Dysphagia and Rapid Release

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Solution Overview

Problem

Solid oral dosage forms of rosuvastatin pose challenges for patients with dysphagia due to size, stickiness, taste, aftertaste, and frequency of administration, necessitating a patient-compliant and chemically stable alternative.

Innovation Solution

A multi-particulate pharmaceutical composition of rosuvastatin pellets with osmotic release modifiers and stabilizers, allowing administration by sprinkling on food or via nasogastric tubing, ensuring chemical stability and rapid drug release.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If solid unit oral dosage forms are used, then the medication can be administered conveniently, but it becomes difficult for patients with dysphagia to swallow due to size, stickiness, and taste

Engineering Contradiction:
Improveease of administrationVSAvoidswallowing difficulty
Core Design Contradiction:
Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The invention divides the single solid unit dosage form into multiple small pellets. Each pellet is tiny and can be easily sprinkled onto soft food, eliminating the swallowing difficulty associated with traditional tablets while maintaining convenient administration through food-based delivery

Inventive Principle:
Principle #1Segmentation

2Quantity of substance

If high percentage loading of rosuvastatin is achieved in each particle, then the dosage form becomes compact with fewer excipients, but maintaining chemical stability becomes challenging

Engineering Contradiction:
Improvedrug loading percentageVSAvoidchemical stability
Core Design Contradiction:
Quantity of substanceVSStability of the object's composition

Solution Approach 1:

The invention uses composite pellet structure containing rosuvastatin combined with specific excipients including osmotic release modifiers and stabilizers. This composite formulation achieves high drug loading (at least 5% by weight of rosuvastatin as sole active ingredient) while maintaining chemical stability throughout shelf life through the synergistic interaction of components

Inventive Principle:
Principle #40Composite materials

3Ease of operation

If the dosage form is designed to be patient-compliant with sprinkling capability, then administration ease improves, but ensuring complete and rapid drug release becomes more difficult

Engineering Contradiction:
Improvepatient complianceVSAvoiddrug release rate
Core Design Contradiction:
Ease of operationVSProductivity

Solution Approach 1:

The invention incorporates osmotic release modifiers that change the physical-chemical parameters of the pellet system. These modifiers enable rapid drug release by creating osmotic pressure gradients that drive quick dissolution and release of rosuvastatin, achieving complete release within minutes even though the pellets are designed for sprinkling administration

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 composition is patient-friendly, chemically stable, and provides complete drug release within minutes, suitable for patients with swallowing difficulties and improving compliance.

Implementation Method 1

the osmotic release modifiers are critical to accelerate release of rosuvastatin from the pellets

Methodology Applied
Scientific EffectOsmotic pressure: Osmotic Pressure

Implementation Method 2

The multiparticulate composition has been found to be not only patient compliant but also chemically stable throughout the shelf life of the product

Methodology Applied
Scientific EffectStabilization:

Data Source

PatentUS12527792B2Stable multiparticulate pharmaceutical composition of rosuvastatin
Publication Date: 2026.01.20 SUN PHARMA ADVANCED RESEARCH CO LTD

AI summary

A stable multi-particulate pharmaceutical composition comprising pellets, the pellets comprising a mixture of rosuvastatin or its pharmaceutically acceptable salts as a sole active ingredient, one or more osmotic release modifiers and one or more stabilizers.