A New Crystalline Ketoprofen Sodium Salt: Solid-State Characterization, Solubility, and Stability

Area of Science:

• Pharmaceutical Sciences
• Solid-State Chemistry

Background:

• Ketoprofen (KTP) is an Active Pharmaceutical Ingredient (API) with poor aqueous solubility.
• Ketoprofen salts are explored to enhance solubility, absorption, and therapeutic onset.
• Developing novel salt forms can improve drug delivery and efficacy.

Purpose of the Study:

• To synthesize and characterize a novel crystalline ketoprofen sodium salt (KTP-Na).
• To compare the physicochemical properties, particularly solubility and stability, of KTP-Na with commercial ketoprofen (KTP-R1).
• To evaluate the potential of KTP-Na as an alternative for solid dosage forms.

Main Methods:

• Synthesis and crystallization of ketoprofen sodium salt (KTP-Na).
• Characterization using X-ray powder diffraction (XRD), FTIR, DSC, and TGA.
• Solubility studies in aqueous solvents.
• Accelerated stability testing under controlled humidity and temperature.

Main Results:

• A novel crystalline KTP-Na was successfully synthesized and characterized.
• KTP-Na exhibited approximately 80-fold higher aqueous solubility compared to KTP-R1.
• KTP-Na demonstrated lower physical stability due to high hygroscopicity, leading to potential amorphization.
• XRD, FTIR, DSC, and TGA confirmed KTP-Na as a distinct form from KTP-R1.

Conclusions:

• KTP-Na presents a viable alternative to KTP-R1 for solid dosage forms due to significantly enhanced solubility.
• The high hygroscopicity of KTP-Na necessitates strict moisture control during storage and formulation.
• Further development should focus on mitigating moisture uptake to ensure the physical stability of KTP-Na.