DHEA Tablet Granulation for Blister Pack Integration
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Solution Overview
Problem
Incorporating a high concentration of DHEA into small oral tablets, such as those used in hormonal contraceptives, is challenging due to limited space for other essential components, as DHEA becomes the main component, leaving little room for promoters of dissolution and prevention of retrogradation.
Innovation Solution
A tablet comprising a granulate with a high payload of DHEA, prepared by wet granulation of a premix with microcrystalline cellulose, allowing for high DHEA concentrations of 60-90 wt.%, along with other pharmaceutically acceptable ingredients, enabling the manufacture of tablets suitable for oral administration.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If DHEA is incorporated as the main component in small tablets (50-80 mg), then high DHEA dosage can be achieved, but there is insufficient room for other essential tablet constituents needed for dissolution promotion and retrogradation prevention
Solution Approach 1:
The tablet is divided into two distinct granulate components: a first granulate containing high concentrations of DHEA (50-90 wt.%) and a second granulate containing excipients and functional ingredients (disintegrants, lubricants, dissolution promoters). This segmentation allows each granulate to be optimized for its specific function while together forming a complete tablet formulation.
Solution Approach 2:
The essential functional ingredients (excipients, disintegrants, lubricants) are extracted from the DHEA mixture and placed in a separate second granulate. This extraction resolves the space constraint problem by isolating the high-DHEA first granulate from the functional ingredient second granulate, allowing both to coexist in the final tablet without compromising DHEA concentration or tablet manufacturability.
2Quantity of substance
If DHEA concentration in the tablet is increased to 50-90 wt.%, then high androgen restoration effect is achieved, but tabletting becomes difficult due to lack of binding and structural components
Solution Approach 1:
The tablet formulation is segmented into a first granulate for DHEA delivery and a second granulate for structural support. The second granulate contains binding agents, disintegrants, and lubricants that provide tabletting reliability, while the first granulate maintains high DHEA concentration. This segmentation allows both high DHEA content and structural integrity to coexist.
Solution Approach 2:
The tablet is formulated as a composite of two granulates with complementary properties. The first granulate (DHEA-rich) provides the active ingredient, while the second granulate (excipient-rich) provides structural integrity, binding, and dissolution properties. Together they form a composite tablet that achieves both high DHEA concentration and manufacturing reliability.
3Ease of operation
If tablet size is reduced to fit standard contraceptive blister packs, then ease of administration is improved, but the amount of DHEA that can be incorporated is limited
Solution Approach 1:
The tablet is segmented into two granulates where the first granulate is optimized for high DHEA concentration in a compact form factor suitable for blister packs, while the second granulate provides necessary functional ingredients in minimal quantities. This segmentation enables small tablet size without compromising DHEA dosage capability.
Solution Approach 2:
The formulation uses parameter optimization to achieve high DHEA concentration (50-90 wt.%) in the first granulate, allowing sufficient DHEA dosage to be packed into a small tablet volume. The controlled parameters include granulate composition ratios, particle size distribution, and compression forces to maintain both small size and high dosage.
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
Enables the production of tablets with at least 50% DHEA content that dissolves swiftly in water, maintaining physiological androgen levels, improving sexual function, mood, and wellness, while being suitable for incorporation in standard oral contraceptive blister packs.
Implementation Method 1
A tablet comprising a granulate with a high payload of DHEA, prepared by wet granulation of a premix with microcrystalline cellulose
Data Source
AI summary
The present invention relates to a tablet having a weight of 30-200 mg and consisting of:60-100 wt. % of granules consisting of: 50-90% by weight of the granules of dehydroepiandrosterone (DHEA);6-35% by weight of the granules of microcrystalline cellulose;0-20% by weight of the granules of one or more other pharmaceutically acceptable granule ingredients; and0-40 wt. % of one or more other pharmaceutically acceptable tablet components.These tablets can suitably be used to orally administer DHEA in dosages of around 50 mg and are sufficiently small to be incorporated in, for instance, ordinary oral contraceptive blister packs.