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Accelerated stability studies on 16-methylene-17 alpha-acetoxy-19-nor-pregn- 4-ene-3,20-dione (Nestorone)
1Population Council, Center for Biomedical Research, New York, New York 10021, USA.
Steroids
|August 1, 1995
Summary
Nestorone contraceptive steroid shows excellent stability in solid form, including Silastic implants. In aqueous solutions, it degrades slowly, influenced by temperature and pH, following a first-order hydrolysis mechanism.
Area of Science:
- Pharmaceutical Chemistry
- Analytical Chemistry
- Drug Stability Studies
Background:
- Nestorone (16-methylene-17 alpha-acetoxy-19-nor-pregn-4-ene-3,20-dione) is a contraceptive steroid.
- Understanding drug stability is crucial for formulation and storage.
- Contraceptive implants require long-term stability assessment.
Purpose of the Study:
- To evaluate the stability of Nestorone in solid and solution states.
- To identify degradation pathways and kinetics.
- To characterize degradation products.
Main Methods:
- Reverse-phase high-performance liquid chromatography (RP-HPLC) was employed.
- Stability studies were conducted under various temperature and pH conditions.
- Mass spectrometry was used for degradation product identification.
Main Results:
- Nestorone demonstrated high stability in solid form (powder and Silastic implants).
- In aqueous solutions, degradation followed a first-order kinetic mechanism.
- Degradation rate increased with temperature and was faster in alkaline media.
- The primary hydrolytic degradation product was identified as 16-methylene-17 alpha-hydroxy-19-nor-pregn-4-ene-3,20-dione.
Conclusions:
- Nestorone exhibits robust stability in solid-state formulations.
- Aqueous solutions of Nestorone are susceptible to hydrolytic degradation, particularly at higher temperatures and alkaline pH.
- The identified degradation product provides insight into the drug's chemical behavior in solution.