Khaldoun A. Al-Sou’od

Chitosan–Sodium Lauryl Sulfate Nanoparticles as a Carrier System for the In Vivo Delivery of Oral Insulin

The present work explores the possibility of formulating an oral insulin delivery system using nanoparticulate complexes made from the interaction between biodegradable, natural polymer called chitosan and anionic surfactant called sodium lauryl sulfate (SLS). The interaction between chitosan and SLS was confirmed by Fourier transform infrared spectroscopy. The nanoparticles were prepared by simple gelation method under aqueous-based conditions. The nanoparticles were stable in simulated gastric fluids and could protect the encapsulated insulin from the GIT enzymes. Additionally, the in vivo results clearly indicated that the insulin-loaded nanoparticles could effectively reduce the blood glucose level in a diabetic rat model. However, additional formulation modifications are required to improve insulin oral bioavailability.

Effect of cyclodextrins on the solubility and stability of candesartan cilexetil in solution and solid state

Guest-host interactions of candesartan cilexetil (CAND) with cyclodextrins (CyDs) have been investigated using phase solubility diagrams (PSD), X-ray powder diffractometry (XRPD), differential scanning calorimetry (DSC) and molecular mechanical modelling (MM). Estimates of the complex formation constant (K(11)) show that the tendency of CAND (pK(a)=6.0) to complex with CyDs follows the order: β-CyD>HP-β-CyD>γ-CyD>α-CyD. Complex formation of CAND with β-CyD (ΔG°=-31.5 kJ/mol) is largely driven by enthalpy change (ΔH°=-32.8 kJ/mol) and slightly retarded by entropy change (ΔS°=-4.6J/mol K). The HPLC results indicate that complex prepared by freeze drying method is chemically not stable due to the formation of amorphous CAND. Also it may suggest formulating CAND with β-CyD by kneading (dispersion) or co-evaporation (real inclusion complex) methods into capsule rather than compressed in tablets, where the compression enhances the instability of CAND. DSC thermograms for CAND/β-CyD complexes proved the formation of inclusion complexes with new solid phase. MM studies indicate the partial penetration of CAND into the β-CyD cavity.

Chapter Seven - Moxifloxacin Hydrochloride

A comprehensive profile of moxifloxacin HCl with 198 references is reported. A full description including nomenclature, formulae, elemental analysis, and appearance is included. Methods of preparation for moxifloxacin HCl, its intermediates, and derivatives are fully described. In addition, the physical properties, analytical methods, stability, uses and applications, and pharmacology of moxifloxacin HCl are also discussed.

Chapter Four – Prasugrel Hydrochloride

A comprehensive profile of prasugrel HCl is reported herein with 158 references. A full description including nomenclature, formulae, elemental analysis, and appearance is included. Methods of preparation for prasugrel HCl, its intermediates, and derivatives are fully discussed. In addition, the physical properties, analytical methods, stability, uses and applications, and pharmacology of prasugrel HCl are also discussed.