Modified-Release Oral Contraceptive Composition for Cycle Control
Find Innovative SolutionsGenerate Solutions
Solution Overview
Problem
Existing combined oral contraceptives (COCs) with low doses of ethinyl estradiol (EE) face issues of adverse events, irregular bleeding patterns, and reduced contraceptive efficacy, leading to non-compliance and increased pregnancy risk.
Innovation Solution
A prolonged-release oral contraceptive composition comprising 2 mg of dienogest and equal to or less than 0.02 mg of EE, with at least 80% of EE intended for slow release, providing a reliable contraceptive efficacy and acceptable bleeding pattern.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Object-affected harmful factors
If the dose of ethinyl estradiol (EE) is reduced to decrease incidence of VTEs and adverse events, then safety is improved, but cycle control deteriorates and unscheduled bleeding increases
Solution Approach 1:
The patent applies dynamic dosing by implementing a biphasic regimen where EE dose varies across the cycle (30 mcg in first phase, 20 mcg in second phase) while DNG remains constant at 2 mg. This dynamic adjustment allows maintaining adequate cycle control during the first phase while reducing VTE risk during the second phase, resolving the contradiction between safety and reliability
Solution Approach 2:
The patent changes the dosage parameters of EE from fixed low dose to variable dose across phases. By adjusting EE concentration parameter (30→20 mcg) while maintaining DNG parameter constant, the formulation achieves both reduced adverse events and maintained cycle control through parameter optimization
2Object-affected harmful factors
If the dose of ethinyl estradiol (EE) is reduced to reduce symptoms of breast tenderness, nausea and dizziness, then tolerability is improved, but unscheduled bleeding increases
Solution Approach 1:
The biphasic formulation dynamically adjusts EE dosage (30 mcg then 20 mcg) combined with constant DNG (2 mg), allowing the system to provide sufficient estrogen coverage initially to prevent unscheduled bleeding, then reduce dosage to minimize adverse symptoms like breast tenderness and nausea, thus resolving the contradiction between tolerability and bleeding pattern reliability
Solution Approach 2:
The patent creates a composite hormonal formulation combining EE and DNG in specific ratios that change across phases. The composite effect of reduced EE (20-30 mcg) with optimized DNG (2 mg) produces a synergistic effect that reduces adverse symptoms while maintaining adequate endometrial support to prevent unscheduled bleeding
3Object-affected harmful factors
If a low dose combination of EE and DNG is used to improve safety profile, then adverse events are reduced, but contraceptive efficacy may be compromised
Solution Approach 1:
The patent implements dynamic dosing where EE varies (30 mcg first phase, 20 mcg second phase) while DNG remains constant at 2 mg throughout the cycle. This dynamic approach ensures adequate ovulation inhibition and contraceptive efficacy during the first phase while reducing adverse events in the second phase, resolving the contradiction between safety and efficacy
Solution Approach 2:
The formulation optimizes hormonal parameters by adjusting EE concentration (30→20 mcg) while maintaining DNG at 2 mg. This parameter optimization ensures the DNG/EE ratio remains sufficient for contraceptive efficacy while the absolute EE dose stays low enough to minimize adverse events, resolving the safety-efficacy contradiction
Data Source
AI summary
The invention relates to a new modified release oral pharmaceutical form comprising 17α-cyanomethyl-17-β-hydrox-yestra-4,9-dien-3-one (dienogest) and 17aα-ethinylestradiol (ethynyl estradiol), its method of production and its medical and non-medical uses, in particular its use in contraception.