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Cefuroxime axetil solid dispersions prepared using solution enhanced dispersion by supercritical fluids
Seoung Wook Jun1, Min-Soo Kim, Guk Hyun Jo
1National Research Laboratory of Pharmaceutical Technology, College of Pharmacy, Chungnam National University, 220 Gung-dong, Yuseong-gu, Daejeon 305-764, Korea.
The Journal of Pharmacy and Pharmacology
|December 16, 2005
Summary
Cefuroxime axetil (CA) solid dispersions were created using SEDS technology. This method successfully produced amorphous CA, significantly enhancing drug dissolution rates for improved oral formulations.
Area of Science:
- Pharmaceutical Technology
- Materials Science
- Drug Delivery Systems
Background:
- Cefuroxime axetil (CA) is a poorly water-soluble antibiotic.
- Enhancing the dissolution rate of such drugs is crucial for effective oral dosage forms.
- Solid dispersions are a promising approach to improve drug solubility and bioavailability.
Purpose of the Study:
- To prepare Cefuroxime axetil (CA) solid dispersions using Solution Enhanced Dispersion by Supercritical Fluids (SEDS).
- To investigate the solid-state physicochemical properties of the prepared solid dispersions.
- To evaluate the impact of SEDS-prepared solid dispersions on the dissolution rate of CA.
Main Methods:
- Solid dispersions of CA with HPMC 2910/PVP K-30 were prepared via SEDS.
- Physicochemical characterization included Differential Scanning Calorimetry (DSC), Powder X-ray Diffraction (PXRD), Fourier Transform Infrared Spectrometry (FT-IR), and Scanning Electron Microscopy (SEM).
- Dissolution studies were conducted to compare the release rates of CA from solid dispersions, physical mixtures, and the drug alone.
Main Results:
- DSC and PXRD analyses confirmed the absence of crystalline CA in the solid dispersions, indicating an amorphous state.
- FTIR spectroscopy revealed intermolecular hydrogen bonding between CA and the polymers (HPMC 2910/PVP K-30).
- Dissolution studies demonstrated a significant increase in the dissolution rate of CA from the solid dispersions compared to controls.
Conclusions:
- SEDS is an effective technique for preparing amorphous solid dispersions of Cefuroxime axetil.
- The amorphous form of CA in solid dispersions, facilitated by intermolecular hydrogen bonding, leads to enhanced dissolution.
- These findings suggest that SEDS-prepared amorphous CA solid dispersions are highly beneficial for developing effective solid dosage forms.