Drug discovery and development is a complex and time consuming process which requires multidisciplinary expertise (Pracha-yasittikul et al., 2015a). It is true that bioac-tive compounds will become useless if their pharmacokinetic properties are not adequate. Pharmacokinetic properties include absorption (A), distribution (D), metabolism (M), excretion (E) and toxicity (T), or ADMET. ADMET prop...

the aim of this study was to characterize the effect of typhoid fever on pharmacokinetic parameters of levofloxacin (lf) and compare the pharmacokinetic parameters of the said antibiotic in healthy human volunteers and patients with typhoid fever. total of 12 subjects were divided into two groups “a” (healthy volunteers) and “b” (typhoid patients). single oral dose of lf 500 mg was given and 5 ...

Coxibs such as celecoxib, rofecoxib and valdecoxib are introduced as selective COX-2 inhibitors to the market. It has been reported that inhibition of COX-2 beside traditional effects of NSAIDs, reduces the risk of colorectal, breast and lung cancers and slow the progress of Alzheimer’s disease. Zarghi et al. reported 8-benzoyl-2-(4-(methylsulfonyl)phenyl)quinoline-4-carboxylic acid (AZGH 102) ...

Severe sepsis and septic shock are major problems as the result of high rates morbidity andmortality in intensive care units (ICUs). In the presence of septic shock, each hour of delay inthe administration of effective antibiotics is associated with a measurable increase in mortality.Aminoglycosides are effective broad-spectrum antibiotics that are commonly used in ICUs forthe treatment of life...

The efficacy of methotrexate (MTX) as an antimetabolite chemotherapeutic agent highly depends on its blood circulation half-life. In our previous study, different conjugates of MTX (MTX-PEG) were synthesized, their physicochemical properties were investigated and MTX-PEG5000 was finally selected as optimum drug-conjugate for further investigations. In the current work, first the stability of MT...

Antibody-drug conjugates (ADC) are an emerging drug class that uses antibodies to improve cytotoxic drug targeting for cancer treatment. ADCs in current clinical trials achieve a compromise between potency and physicochemical/pharmacokinetic properties by conjugating potent cytotoxins directly to an antibody at a 4:1 or less stoichiometric ratio. Herein, we report a novel, polyacetal polymer-ba...

The aim of the present study was to investigate the local pharmacokinetic properties and the systemic safety of vancomycin-impregnated cancellous bone grafts in the treatment of spondylodiscitis. Between 2010 and 2012, 8 patients (5 females, 3 males, mean age 68.75 y.) were treated with this method. Local vancomycin concentrations reached median values of 179 µg/mL (maximum 365 µg/mL) on day 1,...

Statins are the treatment of choice for the management of hypercholesterolaemia because of their proven efficacy and safety profile. They also have an increasing role in managing cardiovascular risk in patients with relatively normal levels of plasma cholesterol. Although all statins share a common mechanism of action, they differ in terms of their chemical structures, pharmacokinetic profiles,...

The pharmacokinetic characteristics of testosterone propionate were studied in normal men after a single im dose of 25 mg testosterone propionate-19,19,19-d3. Plasma levels of testosterone propionate-19,19,19-d3, its active metabolite testosterone-19,19,19-d3, and endogenous testosterone were measured by gas chromatography-mass spectrometry. Testosterone propionate-19,19,19-d3 was gradually tra...

BACKGROUND AND OBJECTIVE Insulin degludec is a basal insulin with a slow and distinct absorption mechanism resulting in an ultra-long, flat, and stable pharmacokinetic profile in patients with diabetes mellitus. The aim of this study was to examine the effect of hepatic impairment on the single-dose pharmacokinetics of insulin degludec. METHODS Twenty-four subjects, allocated to one of four g...