Rosuvastatin Orally Disintegrating Tablet for Fast Dissolution

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Solution Overview

Problem

Existing rosuvastatin formulations face challenges such as poor solubility leading to low bioavailability, unpleasant taste, difficulty in swallowing, and lengthy onset of action, particularly affecting patient compliance and therapeutic efficacy, especially in aged and physically disabled individuals.

Innovation Solution

A rapidly disintegrating tablet formulation of rosuvastatin using direct compression method, comprising rosuvastatin calcium, microcrystalline cellulose, mannitol, croscarmellose sodium, and sucralose, designed to disintegrate quickly in the mouth, enhance dissolution, and improve taste masking.

Engineering Contradictions & Design Principles

VSEngineering Contradiction Analysis

1Ease of operation

If conventional tablets and capsules are used for rosuvastatin administration, then the drug can be delivered orally, but the tablets are difficult to swallow and have unpleasant taste

Engineering Contradiction:

Improveease of swallowingVSAvoidunpleasant taste

Core Design Contradiction:

Ease of operationVSObject-affected harmful factors

Solution Approach 1:

The tablet is designed to segment into small particles rapidly upon contact with saliva, transforming from a single large dose form into multiple small particles that are easier to swallow and distribute throughout the mouth, reducing the unpleasant taste concentration

Inventive Principle:

Principle #1Segmentation

Solution Approach 2:

Saliva acts as an intermediary medium that triggers the disintegration mechanism. The tablet incorporates disintegrants that interact with saliva to initiate rapid breakdown, allowing the drug to be delivered in a form that is easier to manage and less unpleasant to taste

Inventive Principle:

Principle #24Intermediary (Mediator)

2Productivity

If conventional tablets are used, then the drug can be administered orally, but the onset of action is lengthy

Engineering Contradiction:

Improverate of drug absorptionVSAvoidonset of action time

Core Design Contradiction:

ProductivityVSLoss of time

Solution Approach 1:

The tablet is pre-formulated with disintegrants and solubility enhancers that are activated upon contact with saliva. This preliminary preparation ensures that the drug structure is already optimized for rapid breakdown and absorption, eliminating the need for extended dissolution time required by conventional tablets

Inventive Principle:

Principle #10Preliminary action

Solution Approach 2:

The tablet incorporates excipients and formulations that change the physical parameters of the drug upon contact with moisture. This transforms the drug from a stable, slow-dissolving form into a rapidly disintegrating structure, significantly increasing the rate of absorption and reducing onset time

Inventive Principle:

Principle #35Parameter changes

3Reliability

If rosuvastatin is formulated as conventional tablets, then the drug can be delivered, but poor solubility leads to low bioavailability

Engineering Contradiction:

ImprovebioavailabilityVSAvoidpoor solubility

Core Design Contradiction:

ReliabilityVSObject-affected harmful factors

Solution Approach 1:

The tablet incorporates solubility enhancement excipients that act as intermediaries between the poorly soluble rosuvastatin and the dissolution environment. These excipients facilitate the dissolution process by interacting with the drug molecules and the solvent, significantly improving bioavailability

Inventive Principle:

Principle #24Intermediary (Mediator)

Solution Approach 2:

The tablet uses composite formulation combining rosuvastatin with specific excipients known to enhance solubility. This composite structure leverages the beneficial properties of each component, where the excipients compensate for the poor solubility of the active ingredient, ensuring reliable and consistent bioavailability

Inventive Principle:

Principle #40Composite materials

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 formulation ensures rapid drug disintegration and dissolution, improves patient compliance by masking the unpleasant taste, and maintains stability, thereby enhancing bioavailability and therapeutic effectiveness.

Implementation Method 1

The tablet disintegrates rapidly upon contact with saliva

Methodology Applied

Scientific EffectCapillary action: Capillary Action

Implementation Method 2

croscarmellose sodium, a superdisintegrant

Methodology Applied

Scientific EffectSwelling:

Implementation Method 3

microcrystalline cellulose

Methodology Applied

Scientific EffectBulk formation:

Implementation Method 4

mannitol

Methodology Applied

Scientific EffectSolubility: Solvation

Implementation Method 5

sucralose

Methodology Applied

Scientific EffectTaste masking:

Data Source

PatentUS20260108515A1A rapidly disintegrating tablet of rosuvastatin and its process of preparation

Publication Date: 2026.04.23 NOVUMGEN LTD

AI summary

The present invention relates to a rapidly disintegrating tablet that can disintegrate in the buccal cavity upon contact with saliva in less than 1 minute, preferably in less than 40 seconds. The tablet comprises rosuvastatin or pharmaceutically acceptable salts thereof, as well as a combination of excipients that include at least one disintegrating agent and at least one diluent agent. The present invention is based on enhancing the disintegration and dissolution of the drug for oral administration.