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Dissolution enhancement of cefdinir with hydroxypropyl-β-cyclodextrin
Bohong Guo1, Shufen Zhong, Niying Li
1School of pharmacy, Guangdong Pharmaceutical University , Guangzhou , PR China.
Drug Development and Industrial Pharmacy
|October 4, 2013
Summary
Hydroxypropyl-β-cyclodextrin (HP-β-CD) forms inclusion complexes with cefdinir (CEF), enhancing its aqueous solubility and dissolution rate. This study details the preparation and characterization of these novel CEF-HP-β-CD complexes.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Physical Chemistry
Background:
- Cefdinir (CEF) is an antibiotic with limited aqueous solubility, affecting its bioavailability.
- Cyclodextrins, particularly hydroxypropyl-β-cyclodextrin (HP-β-CD), are known for their ability to form inclusion complexes with poorly soluble drugs.
- Improving CEF solubility and dissolution is crucial for enhancing its therapeutic efficacy.
Purpose of the Study:
- To investigate the formation and solid-state properties of cefdinir-hydroxypropyl-β-cyclodextrin (CEF-HP-β-CD) binary systems.
- To evaluate the impact of complexation on the aqueous solubility and dissolution behavior of cefdinir.
- To characterize the CEF-HP-β-CD inclusion complexes using various analytical techniques.
Main Methods:
- Phase-solubility analysis was employed to study CEF-HP-β-CD interactions in solution.
- Freeze-drying technique was used to prepare CEF-HP-β-CD binary systems in a 1:1 molar ratio.
- Characterization of solid inclusion complexes utilized Fourier Transform Infrared Spectroscopy (FTIR), Differential Scanning Calorimetry (DSC), X-ray Powder Diffractometry (XRD), and Scanning Electron Microscopy (SEM).
Main Results:
- Phase-solubility studies indicated the formation of an A(L) type complex with a stability constant of 65.28 ± 1.3 M⁻¹.
- The aqueous solubility of the CEF-HP-β-CD inclusion complex was found to be 2.36-fold higher than that of pure CEF.
- The dissolution rate of the CEF-HP-β-CD inclusion complex was significantly superior compared to pure CEF and its physical mixture.
Conclusions:
- Cefdinir (CEF) successfully forms inclusion complexes with hydroxypropyl-β-cyclodextrin (HP-β-CD).
- The prepared CEF-HP-β-CD inclusion compounds exhibit altered spectroscopic features and improved physicochemical properties.
- Complexation with HP-β-CD offers a promising strategy to enhance the solubility and dissolution rate of cefdinir for potential therapeutic benefits.
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