Enteric Absorption Promoters Enhance Oral Bioavailability of Plant Actives
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Current treatments for benign prostatic hyperplasia (BPH) using β-sitosterol, oligomeric proanthocyanidins, and curcumin face challenges due to low oral bioavailability, requiring high dosages and often causing side effects, which are not practically manageable for patients, especially those with renal, hepatic, or hypertensive issues.
Innovation Solution
Combining β-sitosterol, oligomeric proanthocyanidins, and curcumin with enteric absorption promoters like bromelain, piperine, L-arginine, and sucroester in an oral formulation to enhance bioavailability and reduce dosages, administered in gastro-resistant forms such as tablets or capsules to improve absorption and reduce adverse effects.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If high dosages of β-sitosterol, oligomeric proanthocyanidins, and curcumin are administered to achieve therapeutic effect, then the treatment effectiveness against BPH is improved, but the side effects and hepatorenal burden increase
Solution Approach 1:
The patent introduces enteric absorption promoters (bromelain, piperine, L-arginine, sucroester) as intermediary substances that facilitate the absorption of the active ingredients. These promoters act as mediators between the gastrointestinal tract and the active principles, enhancing bioavailability without requiring increased dosages of the therapeutic agents themselves.
Solution Approach 2:
The patent changes the physicochemical parameters of the formulation by incorporating substances that modify absorption characteristics. The enteric promoters alter the dissolution and absorption parameters of β-sitosterol, oligomeric proanthocyanidins, and curcumin, enabling effective delivery at lower doses while maintaining therapeutic efficacy.
2Reliability
If high dosages of active ingredients are used to overcome low oral bioavailability, then the therapeutic effect is achieved, but the practical manageability and patient compliance deteriorate
Solution Approach 1:
Enteric absorption promoters serve as intermediaries that bridge the gap between oral administration and systemic absorption. By facilitating better bioavailability, these promoters enable effective treatment at dosages that are practical for patient compliance and manageable in clinical settings.
3Ease of operation
If conventional anti-inflammatory drugs or 5-α-reductase inhibitors are administered, then the symptoms are managed, but the risk of adverse effects in patients with renal, hepatic, or hypertensive issues increases
Solution Approach 1:
The patent employs plant-based active ingredients (β-sitosterol, oligomeric proanthocyanidins, curcumin) that act as temporary, naturally degradable therapeutic agents. These substances provide symptom management through their anti-inflammatory and 5-α-reductase inhibitory effects while being metabolized and eliminated without accumulating toxic effects, making them safer for patients with compromised organ function.
Solution Approach 2:
The formulation combines multiple plant-derived active ingredients with complementary mechanisms of action. This composite approach provides synergistic therapeutic effects for symptom management while distributing the metabolic burden across multiple substances with different elimination pathways, reducing the risk of adverse effects compared to single-agent conventional therapies.
Data Source
AI summary
The present invention concerns a combination of β-sitosterol, oligomeric proanthocyanidins, curcumin having anti -inflammatory and antiproliferative activity for use in the treatment of urological disorders and formulations thereof in combination with suitable excipients and/or diluents. Formulations for oral use associated with at least a promoter of enteric absorption selected among bromelain, L-arginine base, at least one ester of sucrose with fatty acids and pipeline, in particular in the form of a food supplement or medicament, are particularly effective as they exert a significant anti -inflammatory activity and reduce the prostatic volume at dosages of single active ingredients that are much lower than those described in the literature. This effectiveness is due to a mechanism for the promotion of enteric absorption not previously described, original and not explainable as the sum of the actions of the single promoters.