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Preparation, characterization and in vitro dissolution study of Nitrazepam: Cyclodextrin inclusion complex
1Department of Pharmaceutics and Pharmaceutics Technology, S. K. Patel College of Pharmaceutical Education and Research, Ganpat University, Kherva, Gujarat, India.
Journal of Pharmacy & Bioallied Sciences
|October 16, 2012
Summary
This study prepared Nitrazepam inclusion complexes with cyclodextrins, significantly enhancing drug dissolution rates. Lyophilization with Sulfobutyl ether β-cyclodextrin yielded the best results for improved drug delivery.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Chemistry
Background:
- Nitrazepam is a water-insoluble drug with poor dissolution rates, limiting its therapeutic efficacy.
- Cyclodextrins, such as Hydroxypropyl-β-cyclodextrin (HPβCD) and Sulfobutyl ether β-cyclodextrin (SBEβCD), are known to improve the solubility and bioavailability of poorly soluble drugs.
Purpose of the Study:
- To prepare and characterize inclusion complexes of Nitrazepam with HPβCD and SBEβCD.
- To evaluate the impact of complexation on the dissolution rate and release profile of Nitrazepam.
- To identify the optimal cyclodextrin and preparation method for enhancing Nitrazepam's dissolution.
Main Methods:
- Phase solubility studies were conducted to determine the stoichiometry and spontaneity of complex formation.
- Inclusion complexes were prepared using physical mixing, kneading, spray-drying, and lyophilization.
- Complex characterization involved Differential Scanning Calorimetry (DSC), Fourier-Transform Infrared Spectroscopy (FTIR), Scanning Electron Microscopy (SEM), and Powder X-ray Diffraction (PXRD).
- In vitro dissolution studies were performed to assess the impact of complexation on Nitrazepam release.
Main Results:
- Phase solubility profiles indicated an AP-type interaction, suggesting 2:1 stoichiometric inclusion complexes.
- Negative Gibbs free energy values confirmed the spontaneous nature of Nitrazepam solubilization.
- Lyophilization proved to be the most effective method for successful inclusion complex formation.
- Complexation significantly improved Nitrazepam's solubility, wettability, and in vitro dissolution rate.
- The complex prepared with SBEβCD via lyophilization exhibited the most substantial enhancement in dissolution rate.
- Similarity factor analysis revealed significant differences in release profiles between complexed and uncomplexed Nitrazepam.
Conclusions:
- Inclusion complexation with HPβCD and SBEβCD effectively enhances the dissolution rate of Nitrazepam.
- Lyophilization is a suitable method for preparing stable and effective Nitrazepam-cyclodextrin inclusion complexes.
- SBEβCD, when complexed with Nitrazepam via lyophilization, offers the greatest potential for improving Nitrazepam's in vitro drug release.
- Tablets formulated with these cyclodextrin complexes demonstrate superior Nitrazepam release profiles compared to conventional formulations.
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