Design, Synthesis and Evaluation of Biological activity of certain Novel Triazole schiff bases

ABSTRACT 4-Formyl phenoxy acetic acid (1) obtained from 4-hydroxy benzaldehyde yielded the corresponding Schiff bases (2al-a10) bearing free carboxyl group on treatment with primary amines/acid hydrazides under anhydrous condition. Several 4-amino-3-substituted-5-mercapto-1,2,4-triazoles (3al-a10) were prepared in excellent yields by the condensation of Schiff bases bearing free carboxyl group with thiocarbohydrazide through a single step reaction. Elemental analysis, IR and 1 HNMR data confirmed the structure of the newly synthesized compounds. Synthesized triazole derivatives were investigated for their antibacterial, antifungal, anti-inflammatory and analgesic activities. The tested compounds showed significant anti-inflammatory and antibacterial activities. However these compounds exhibited moderate analgesic and antifungal activities

DESIGN AND IN VITRO EVALUATION OF FAST DISSOLVING FILMS CONTAINING HP ß CD INCLUSION COMPLEXES OF LAMOTRIGINE

Objectives: The objectives of the present study is to design and evaluate fast dissolving films of lamotrigine using HP ß CD inclusion complexes with an aim to achieve rapid drug release thereby controlling the seizures in the shortest possible time. Design: Inclusion complexes of lamotrigine were prepared with hydroxypropyl β cyclodextrin (HP β CD) employing different methods to improve the solubility and mask the bitter taste of the drug. Fast dissolving films were prepared by incorporating the developed inclusion complexes and using hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA) as film forming agents and other suitable excipients by solvent casting method. Results: Inclusion complexes prepared by ultrasonication method resulted in better solubility and dissolution rate compared to other methods studied. The fast dissolving films prepared using inclusion complexes were found to be transparent and smooth in texture. The thickness, drug content, % moisture absorption and moisture loss, folding endurance and weight variation was found to be uniform. In vitro release profiles were inversely proportional to the polymer and directly proportional to superdisintegrant and plasticizer concentration. Optimized formulations (F8 and F12) were subjected for fourier transform infrared spectroscopy (FT-IR) and differential scanning calorimetry (DSC) which revealed the absence of any chemical interactions between the excipients of the formulation. The formulations were found to be stable without any significant changes during the stability studies carried out as per the ICH guidelines. Conclusion: The study revealed the successful development of fast dissolving films of lamotrigine with promising results thereby suggesting the possible use of the developed films in the rapid management of epileptic seizures. Keywords: Fast dissolving films; epilepsy; lamotrigine; inclusion complex; HPMC; PVA; physico-chemical characterization