This investigation describes a new precise, sensitive and accurate stereoselective HPLC method for the simultaneous determination of donepezil enantiomers in tablets and plasma with enough sensitivity to follow its pharmacokinetics in rats up to 12h after single oral dosing. Enantiomeric resolution was achieved on a cellulose tris (3,5-dimethylphenyl carbamate) column known as Chiralcel OD, wit...

The present study investigated safety/toxicity profile of fixed dose combination of Ofloxacin-Ornidazole injection in Mus musculus mice at three dose levels, ranging from asymptomatic to high dose. To enhance the antimicrobial spectrum of the quinolones against anaerobic organisms and gram positive bacteria, fixed dose combination of Ofloxacin and Ornidazole injection was introduced. It has bee...

Leprosy, a chronic granulomatous infectocontagious disease transmitted by Mycobacterium leprae, continues to be prevalent today, especially in underdeveloped countries and its paucibacillary form with a single lesion is being treated with rifampicin (600mg), ofloxacin (400mg) and minocycline (100mg) administered as a single dose (ROM scheme). Thus, the objective of the present study was to inve...

We investigated the binding properties of the (R)- and (S)-enantiomers of the muscarinic antagonists trihexyphenidyl, procyclidine, hexahydro-difenidol, p-fluoro-hexahydro-difenidol, hexbutinol, p-fluoro-hexbutinol, and their corresponding methiodides at muscarinic M1, M2, M3 and M4 receptor subtypes. In addition, binding properties of the (R)- and (S)-enantiomers of oxyphencyclimine were studi...

The bioequivalence of oral and intravenous ofloxacin was investigated after the administration of multiple doses of 400 mg every 12 h to 20 healthy male volunteers in a randomized, crossover, open-label study. Ofloxacin concentrations in plasma were evaluated after 4 days of oral or intravenous (1-h infusion) dosing with a 3-day wash-out period between regimens. As expected, delivery to the sys...

After an outbreak of three cases of serogroup B meningococcal disease at a Norwegian college, 84 of 392 (21%) subjects were tonsillopharyngeal carriers of Neisseria meningitidis. To eradicate meningococcal carriage, 80 volunteers received a single dose of 400 mg of ofloxacin. Three days after treatment, all 75 evaluable volunteers were culture negative for N. meningitidis, and after 7 days none...

The two enantiomers of 2',3'-dideoxy-3'-thiacytidine (BCH-189) and their 5-fluoro analogs (FTC) were found to be good substrates for human 2'-deoxycytidine kinase with Km values in the 5.7 to 42.1 microM range. The affinity of the (-)-enantiomers was greater than that of the (+)-compounds. These results may explain the greater in vitro antiviral potency against human immunodeficiency virus and ...

The present manuscript describe simple, sensitive, rapid, accurate, precise and cost effective dual wavelength spectrophotometric method for the simultaneous determination of ofloxacin and cefpodoxime proxetil in combined tablet dosage form. The utility of dual wavelength data processing program is its ability to calculate unknown concentration of components of interest in a mixture containing ...

This work describes the sequential hydrolysis of bambuterol enantiomers and their monocarbamate metabolites (MONO) catalyzed by human butyrylcholinesterase (BChE) as well as the enzyme inhibition resulting from this process. Particular emphasis is given to the contribution given by MONO to the enzyme inhibition because it was not fully characterized in previous works. Bambuterol and MONO enanti...

The stereoselective pharmacokinetics of BOF-4272 enantiomers in rats and dogs was investigated by simultaneously measuring concentrations in arterial, portal, and venous plasma, the liver, and the kidney at 2 h after the oral administration of the racemic drug. The concentrations of BOF-4272 enantiomers were measured using high-performance liquid chromatography. The concentrations of the S(-) e...