Triphasic Oral Drug Regimen for Contraceptive Efficacy and VTE Risk Reduction
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Solution Overview
Problem
Conventional dosing schedules of ethinylestradiol (EE) and cyproterone acetate (CPA) for treating polycystic ovary syndrome (PCOS) and contraception are associated with an increased risk of venous thromboembolism (VTE) due to high estrogen exposure.
Innovation Solution
A triphasic oral drug regimen with EE and CPA, comprising a loading phase, maintenance phase, and resting phase, where EE and CPA are administered in varying dosages and intervals to reduce estrogen exposure, including a loading phase with daily administration, a maintenance phase with alternate dosing of EE and CPA, and a resting phase with no active ingredients, to maintain contraceptive efficacy while minimizing VTE risk.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Reliability
If conventional dosing schedules of ethinylestradiol (EE) and cyproterone acetate (CPA) are used for treating PCOS and contraception, then contraceptive efficacy and anti-androgen effects are maintained, but the risk of venous thromboembolism (VTE) increases due to high estrogen exposure
Solution Approach 1:
The patent divides the conventional single-phase dosing regimen into three distinct phases: loading phase (days 1-14 with daily EE and CPA), maintenance phase (days 15-84 with alternate-day EE and daily CPA), and resting phase (days 85-91 with no active ingredients). This segmentation allows reduced overall estrogen exposure while maintaining contraceptive efficacy through strategic hormone delivery timing
Solution Approach 2:
The patent implements periodic action by administering ethinylestradiol and cyproterone acetate in varying dosages and intervals across different phases. Specifically, the maintenance phase uses alternate-day EE dosing combined with daily CPA, creating a periodic pattern that maintains therapeutic hormone levels and contraceptive efficacy while significantly reducing cumulative estrogen exposure and VTE risk compared to conventional daily dosing
2Reliability
If high dosage of ethinylestradiol is administered to ensure contraceptive efficacy, then contraception is effective, but the risk of venous thromboembolism increases
Solution Approach 1:
The patent applies parameter changes by modifying the dosing parameters of ethinylestradiol and cyproterone acetate across different phases. The loading phase uses higher EE dosages (30-50 μg) to establish effective hormone levels, while the maintenance phase reduces EE dosage (10-30 μg) and frequency (alternate-day dosing) to maintain contraceptive efficacy with reduced estrogen exposure, thereby changing the dosage parameters to balance efficacy and safety
3Reliability
If continuous daily dosing is used to maintain hormone levels, then contraceptive efficacy is maintained, but the risk of venous thromboembolism increases
Solution Approach 1:
The patent segments the continuous dosing regimen into three phases with different dosing patterns. The maintenance phase specifically implements alternate-day ethinylestradiol dosing combined with daily cyproterone acetate, creating interruption periods that reduce cumulative estrogen exposure duration while maintaining contraceptive efficacy through the synergistic effect of both hormones
Solution Approach 2:
The patent implements periodic action through the resting phase (days 85-91) with no active ingredients, creating a hormone-free interval that allows withdrawal bleeding and reduces cumulative estrogen exposure duration. This periodic interruption maintains long-term contraceptive efficacy while reducing VTE risk associated with continuous daily estrogen exposure
Data Source
AI summary
Provided herein are oral drug preparations including cyproterone acetate and ethinylestradiol, dosing regimen for the drug preparations, and methods of treating diseases. The methods provided include the administration of the oral drug preparation to treat one or more symptoms of hyperandrogenic conditions or hyperandrogenic activities, to provide contraception, and to reduce a risk of vascular thromboembolism (VTE) in a subject.