Stabilized Solid Medicinal Forms Using Water-Soluble Drying Agents
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Solution Overview
Problem
Existing solid medicinal forms face challenges in maintaining stability, particularly for moisture-sensitive active ingredients, due to issues with electrostatic charges, poor flowability, and inadequate moisture control, leading to disintegration and instability during storage and handling.
Innovation Solution
Incorporating water-soluble drying agents like trimagnesium dicitrate and calcium chloride into solid medicinal forms to achieve low drying loss and equilibrium moisture content, ensuring effective moisture absorption and retention, thereby stabilizing the active ingredients.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If drying agents like silica gel or molecular sieve are used in sealed packaging, then moisture control is improved, but the active ingredient disintegrates during the prolonged drying period and electrostatic charges cause filling difficulties
Solution Approach 1:
The invention changes the chemical composition parameters of the drying agent by using water-soluble salts (calcium chloride, magnesium chloride, sodium sulfate) instead of conventional insoluble drying agents. This parameter change enables the drying agent to dissolve in the moisture it absorbs, forming a saturated solution that maintains low water activity without requiring prolonged drying time, thus preventing active ingredient disintegration while achieving effective moisture control.
2Quantity of substance
If thermal drying processes are applied to active ingredients and excipients, then moisture content is reduced, but the sensitive active ingredient begins to disintegrate
Solution Approach 1:
The invention replaces the thermal drying process (mechanical/physical system using heat) with a chemical drying mechanism. Water-soluble drying agents chemically bind moisture through dissolution and saturation, achieving moisture reduction without thermal stress that would cause active ingredient disintegration. This substitution of drying mechanism preserves active ingredient stability while effectively reducing moisture content.
3Quantity of substance
If conventional drying agents are used, then moisture absorption capacity is improved, but electrostatic charges are generated causing poor flowability and filling problems
Solution Approach 1:
The invention changes the physical state parameter of the drying agent from insoluble solid particles (conventional drying agents) to water-soluble salts that dissolve upon moisture absorption. This parameter change eliminates electrostatic charge generation while maintaining high moisture absorption capacity through the formation of saturated solutions, thereby preserving excellent flowability and preventing filling problems.
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 use of these agents results in stable solid forms with reduced disintegration and improved chemical stability, maintaining the integrity of moisture-sensitive active ingredients over extended periods.
Implementation Method 1
The stability of solid medicinal forms or solid food supplement forms must be ensured during the entire life thereof. Along with oxygen, in particular water which every active ingredient and every excipient contain in different amounts, is responsible for all kinds of stability
Implementation Method 2
They have virtually no negative influence on the release rate of active ingredients from said solid forms; the highest and firmest possible adsorbability of water in the range of up to 25% relative humidity and a temperature of at most 40° C.; a pH of 5 to 8, preferably 5.5 to 7.5, as the 0.1 molar solution
Data Source
AI summary
The invention relates to solid medicinal forms containing at least one active ingredient and at least one pharmaceutically compatible, water soluble drying agent which is selected from the group consisting of trimagnesium dicitrate and/or calcium chloride, the solid medicinal form having a drying loss of at most 6% and a relative equilibrium moisture content of 25% or less. The invention also relates to solid medicinal forms containing a moisture-sensitive active ingredient and trimagnesium dicitrate.