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Polymer/Amorphous Salt Solid Dispersions of Ciprofloxacin.
Hanah Mesallati1, Lidia Tajber2
1Synthesis and Solid State Pharmaceutical Centre, School of Pharmacy and Pharmaceutical Sciences, Trinity College Dublin, College Green, Dublin 2, Ireland.
Formulating amorphous ciprofloxacin succinate salts into polymer solid dispersions enhanced their stability. However, this approach did not significantly improve drug solubility or permeability compared to amorphous salts.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Drug Delivery
Background:
- Amorphous ciprofloxacin (CIP) succinate salts exhibit suboptimal pharmaceutical properties.
- Solid dispersions offer a strategy to enhance drug characteristics.
Purpose of the Study:
- To improve the pharmaceutical properties of amorphous ciprofloxacin succinate salts.
- To formulate amorphous ciprofloxacin succinate salts into polymer/amorphous salt solid dispersions (ASSDs).
Main Methods:
- ASSDs were prepared using spray drying and ball milling with PVP or Soluplus.
- Characterization included solid-state properties, miscibility, stability, solubility, and permeability assessments.
Main Results:
- ASSDs exhibited enhanced thermal stability and miscibility with polymers.
- Drug solubility in aqueous and biorelevant media was significantly increased.
- Permeability of ASSDs was comparable to amorphous salts but lower than crystalline ciprofloxacin.
Conclusions:
- Formulating amorphous ciprofloxacin succinate salts as ASSDs improved long-term stability.
- The formulation did not significantly alter solubility or permeability compared to amorphous salts.
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