In an effort to find a new oral cephalosporin with well-balanced antibacterial spectrum, good oral absorbability and long plasma half-life, a series of oxyimino aminothiazolyl 3-[(E)- or (Z)-N-substituted carbamoyloxy]propenyl cephems was synthesized and evaluated for antibacterial activity and oral absorbability. The substituents of the carbamoyloxy group affected their in vitro activity and b...

A series of chalcones substituted by a quinoxaline unit at the B-ring were synthesized and tested as inhibitors of breast cancer resistance protein-mediated mitoxantrone efflux. These compounds appeared more efficient than analogs containing other B-ring substituents such as 2-naphthyl or 3,4-methylenedioxyphenyl while an intermediate inhibitory activity was obtained with a 1-naphthyl group. In...

Pravastatin sodium is available for oral administration as 10 mg, 20 mg, 40 mg, and 80 mg tablets. Inactive ingredients include: colloidal silicon dioxide, crospovidone, hydroxypropyl methylcellulose, magnesium stearate, mannitol, meglumine, microcrystalline cellulose and starch. The 10 mg, 20 mg and 80 mg tablets also contain D&C Yellow No 10 Aluminium Lake and the 40 mg tablet also contains D...

DifI'..tial scanning calorimetry (~ and dynamic ~-,!jCaJ thermal analysis (DMTA) were used to characterize the morphology of eolv81t cast hydroXYPl'Opyl ceUuloee (Hpc) films. DSC r-.lta windicative of a aemicryltaUine mat«ial with a melt at 220°C and a ,tran8itioo at 19°C (T1). althoucb an 8dditiCXlal _t wu MIumted by a baseline inftectioo at about ~C (Tt). Cc pcx1din, relaxatiMS wfound by DMTA...

The complete computational study of the methyldopa drug and its derivatives prodrug 1-4(methyldopa-cellulose (Ce), methyldopa-carboxymethyl cellulose(CMC), methyldopa-maleic anhydride cellulose (MAC)and methyldopa-hydroxypropyl cellulose(HPC)) was performed by Density Function theory method with Becker’s three parameter hybrid functional (B3LYP) 6-31G++ (d, p) basis set using Gaussian 09 progra...

The objective of this study was to determine the effect of povidone. hydroxypropyl methylcellulose, hydroxypropyl cellulose, lactose and magnesium stearate on the stability of quinapril hydrochloride. The applied HPLC method was validated by the following parameters: selectivity, precision, linearity and accuracy. Binary 1:4 mixtures of quinapril hydrochloride and selected excipients were stabl...

This study was undertaken to develop tablets of diazepam-hydroxypropyl-β-cyclodextrin inclusion complex that disintegrate within 3 minutes and release 85% of drug within 30 minutes to provide rapid action of the drug through oro-mucosal route. Formation of inclusion complex was verified using X-ray diffraction and differential scanning calorimetric studies. Enhanced of aqueous solubility, as ev...

The present investigation is concerned about the development of floating bioadhesive drug delivery system of venlafaxine hydrochloride which after oral administration exhibits a unique combination of floating and bioadhesion to prolong gastric residence time and increase drug bioavailability within the stomach. The floating bioadhesive tablets were prepared by the wet granulation method using d...