High-Load Dexamethasone Tablet Formulation
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
There is a need for pharmaceutical compositions containing high loads of dexamethasone that improve compliance with recommended dosing regimens, particularly for conditions like multiple myeloma, where existing formulations do not effectively provide the required high loading of the active pharmaceutical ingredient.
Innovation Solution
A pharmaceutical composition comprising 15 to 25 weight percent dexamethasone or its pharmaceutically acceptable salt or solvate, combined with a filler, binder, disintegrant, and lubricant, formulated into a high-load unit dosage form, preferably as an uncoated tablet, which is prepared through a process involving wet granulation and drying, followed by admixture with a lubricant, to ensure effective oral administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If existing pharmaceutical formulations are used, then the composition can be manufactured with standard dosing, but the load of dexamethasone (active pharmaceutical ingredient) is insufficient for high-dose treatment requirements
Solution Approach 1:
The patent changes the concentration parameter of dexamethasone in the pharmaceutical composition, formulating it at high loads (15-25 weight percent) to meet the requirements for high-dose treatment while maintaining manufacturability through standardized tablet compression processes
Solution Approach 2:
The patent creates a composite pharmaceutical composition combining dexamethasone with appropriate excipients and formulation components, achieving both high active ingredient load and manufacturability through optimized composite material design
2Reliability
If dexamethasone is administered at high doses, then treatment efficacy is improved, but patient compliance with dosing regimens deteriorates due to complex dosing schedules
Solution Approach 1:
The patent segments the dosing regimen into convenient single-dose tablet formulations, where each tablet contains a predetermined high load of dexamethasone (15-25 weight percent), allowing patients to receive effective doses through simple single-dose administration rather than complex multi-dose schedules
Solution Approach 2:
The patent performs preliminary formulation of high-load dexamethasone tablets during manufacturing, so that the high-dose requirement is already built into the product structure, eliminating the need for complex dosing calculations or multiple tablets during actual use
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 provides a high-load unit dosage form of dexamethasone, enhancing compliance with recommended dosing regimens by offering improved bioavailability and immediate release of the active ingredient, suitable for treating multiple myeloma, either alone or in combination with anti-cancer drugs like thalidomide.
Implementation Method 1
wet granulating dexamethasone or a pharmaceutically acceptable salt or solvate thereof, a binder, a filler, and a disintegrant to obtain a wet granulate
Implementation Method 2
drying the wet granulate of step (i) to obtain a dry granulate having a Loss on Drying (LOD) % of about 1.5% to about 5%
Data Source
AI summary
A pharmaceutical composition useful for the treatment of multiple myeloma in combination with an anti-cancer drug is provided. The pharmaceutical composition includes high-dose dexamethasone or a pharmaceutically acceptable salt or solvate thereof.