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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
Published on: August 15, 2016
Development of an omeprazole parenteral formulation with hydroxypropyl-beta-cyclodextrin
Chantal Holvoet1, Yvan Vander Heyden, Jacqueline Plaizier-Vercammen
1Department of Analytical Chemistry and Pharmaceutical Technology, Vrije Universiteit Brussel-VUB, Laarbeeklaan, Brussels, Belgium.
Pharmaceutical Development and Technology
|July 7, 2007
Summary
To improve omeprazole solubility and stability for parenteral formulations, cyclodextrins were used. A novel ammonia-based solvent method with hydroxypropyl-beta-cyclodextrin successfully stabilized the drug.
Area of Science:
- Pharmaceutical Science
- Drug Delivery Systems
- Formulation Development
Background:
- Omeprazole exhibits poor solubility and stability in aqueous environments, hindering parenteral formulation.
- Parenteral formulations require high drug loading and stability for effective administration.
Purpose of the Study:
- To develop a stable parenteral formulation of omeprazole with enhanced solubility.
- To investigate the efficacy of cyclodextrins (CDs) as complexation agents and stabilizers for omeprazole.
- To optimize the manufacturing process for a high-concentration omeprazole parenteral preparation.
Main Methods:
- Comparative stability studies of omeprazole in various aqueous media.
- Evaluation of different cyclodextrins, including hydroxypropyl-beta-cyclodextrin (HP-beta-CD), for inclusion complexation.
- Development and testing of an ammonia-based solvent system for omeprazole dissolution.
- Lyophilization of selected formulations to assess final product stability and characteristics.
Main Results:
- Initial attempts using HP-beta-CD at pH 7.4-8.0 resulted in omeprazole degradation before complete dissolution.
- An ammonia-based solvent system facilitated high pH dissolution of omeprazole.
- Selected formulations containing 40 mg omeprazole in 10 mL of 40% HP-beta-CD with initial pH 11-12 met parenteral requirements after lyophilization.
Conclusions:
- A novel manufacturing method utilizing an ammonia-based solvent and HP-beta-CD is effective for creating stable parenteral omeprazole formulations.
- Cyclodextrin complexation significantly enhances the stability and solubility of omeprazole in parenteral preparations.
- The optimized formulation meets critical requirements for parenteral drug products.
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