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Crystalline solid dispersion-a strategy to slowdown salt disproportionation in solid state formulations during
Haichen Nie1, Wei Xu2, Lynne S Taylor3
1Department of Industrial and Physical Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN, 47907, United States; Formulation Sciences, Teva Pharmaceuticals, 145 Brandywine Parkway, West Chester, PA, 19380, United States.
International Journal of Pharmaceutics
|December 17, 2016
Summary
Embedding active pharmaceutical ingredient (API) salts into polymeric matrices effectively reduces salt disproportionation. This formulation strategy enhances drug stability during storage and manufacturing processes like wet granulation.
Area of Science:
- Pharmaceutical Science
- Materials Science
- Drug Delivery
Background:
- Salt disproportionation in active pharmaceutical ingredient (API) salts can negatively impact product performance.
- Mitigating API salt disproportionation in solid formulations presents formulation challenges.
- Understanding factors influencing salt disproportionation is crucial for drug stability.
Purpose of the Study:
- To explore novel formulation strategies for reducing API salt disproportionation.
- To investigate the use of polymeric matrices to prevent salt disproportionation.
- To assess the influence of polymer properties on salt disproportionation.
Main Methods:
- Dispersing pioglitazone hydrochloride salt crystals into various polymeric matrices.
- Evaluating the effect of polymer physicochemical properties (hygroscopicity, acidity) on salt disproportionation.
- Investigating the impact of acidifiers in granulation fluid on salt disproportionation during wet granulation.
Main Results:
- Embedding crystalline API salts into polymeric carriers successfully reduced salt disproportionation.
- Polymer properties, including hygroscopicity and substituent acidity, significantly affected pioglitazone hydrochloride salt disproportionation.
- Incorporating acidifiers into granulation fluid further retarded salt disproportionation during wet granulation.
Conclusions:
- Polymeric carriers are effective in mitigating API salt disproportionation in solid formulations.
- Physicochemical properties of polymers play a critical role in controlling salt stability.
- Acidifiers can provide additional benefits in preventing salt disproportionation during pharmaceutical processing.
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