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Published on: August 9, 2022
Solid dispersion of prednisolone: solid state characterization and improvement of dissolution profile
Mohanraj Palanisamy1, Jasmina Khanam
1Department of Pharmaceutical Technology, Jadavpur University, Kolkata, West Bengal, India. krpmohanraj@gmail.com
Drug Development and Industrial Pharmacy
|September 16, 2010
Summary
Solid dispersions significantly improved the dissolution of prednisolone (PRD), a poorly soluble drug. This formulation strategy enhances drug solubility and bioavailability for better therapeutic outcomes.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Pharmacy
Background:
- Dissolution testing is crucial for evaluating pharmaceutical dosage form efficacy.
- Poor drug solubility at physiological pH can lead to adverse effects.
- Prednisolone (PRD) is a Class II biopharmaceutics system drug with limited solubility.
Purpose of the Study:
- To enhance the dissolution properties of prednisolone (PRD).
- To investigate solid dispersions as a strategy for improving PRD dissolution.
Main Methods:
- Prepared solid dispersions using various water-soluble carriers and drug:carrier ratios.
- Employed different preparation methods to optimize formulations.
- Characterized solid dispersions using Fourier transform infrared (FTIR) spectroscopy, powder X-ray diffraction, and thermal analysis.
- Compared in vitro dissolution behaviors of optimized formulations.
Main Results:
- Prednisolone (PRD) formed stable complexes with carriers (K(a) = 9.5-597.2 M(-1)).
- In vitro dissolution rate of PRD was significantly improved in solid dispersions compared to physical mixtures or PRD alone.
- Improved wettability, dispersibility, reduced crystallinity, and increased amorphous fraction contributed to enhanced dissolution.
- Fourier transform infrared (FTIR) spectroscopy and powder X-ray diffraction confirmed drug-carrier interactions with hydroxypropyl-β-cyclodextrin (HP-βCD) and polyethylene glycol (PEG).
- Differential scanning calorimetry (DSC) revealed reduced drug crystallinity in solid dispersions with HP-βCD, polyvinylpyrrolidone-co-vinyl acetate 64, and PEG.
Conclusions:
- Solid dispersions with selected excipients effectively accelerate the dissolution of poorly water-soluble drugs.
- This approach offers a powerful tool for improving the bioavailability of challenging pharmaceutical compounds.
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