Determination of pharmacokinetic properties in the intact animal remains a major bottleneck in drug discovery. Cassette dosing involves administration of a cocktail of drugs to individual animals. Here we describe the cassette dosing properties of a 107-membered library of 2,6,9-trisubstituted purine cyclin-dependent kinase 2 (CDK2) inhibitors. A three-step parallel synthesis approach produced ...

retention behavior of molecules mostly depends on their chemical structure. retention data of biologically active molecules could be an indirect relationship between their structure and biological or pharmacological activity, since the molecular structure affects their behavior in all pharmacokinetic stages. in the present paper, retention parameters (rm0) of biologically active 1,2-o-isopropyl...

There are numerous computational tools which support the design of new potential ligands. They assist in evaluation compound activity as well optimization physicochemical and pharmacokinetic properties. Nowadays, they an indispensable element drug process; both time money can be saved with their application.

Canakinumab is a high-affinity human monoclonal anti-interleukin-1β (IL-1β) antibody of the IgG1/κ isotype designed to bind and neutralize the activity of human IL-1β, a pro-inflammatory cytokine. Canakinumab is currently being investigated on the premise that it would exert anti-inflammatory effects on a broad spectrum of diseases, driven by IL-1β. This paper focuses on the analysis of the pha...

Concomitant use of several drugs by ICU( Intensive Care Unit) patients is often unavoidable. In these patients, pharmacokinetic drug interactions are very likely. The current study was designed to evaluate these interactions in patients hospitalized in an ICU of a teaching hospital in Tehran, Iran. A questionnaire was designed and used to collect study data. The study was done in the ICU of a t...

Concomitant use of several drugs by ICU( Intensive Care Unit) patients is often unavoidable. In these patients, pharmacokinetic drug interactions are very likely. The current study was designed to evaluate these interactions in patients hospitalized in an ICU of a teaching hospital in Tehran, Iran. A questionnaire was designed and used to collect study data. The study was done in the ICU of a t...

the bioavailability of two dipyridamol tablet formulations of (dipyridamole from tolidaru and persantin from boehringer) was compared in 14 healthy male volunteers who received a single dose of 25 mg of the test (t) and the reference (r) products in a randomized balanced 2-way crossover design. plasma samples were obtained over a 16 h interval and dipyridamole concentrations determined by hplc ...

concomitant use of several drugs by icu( intensive care unit) patients is often unavoidable. in these patients, pharmacokinetic drug interactions are very likely. the current study was designed to evaluate these interactions in patients hospitalized in an icu of a teaching hospital in tehran, iran. a questionnaire was designed and used to collect study data. the study was done in the icu of a t...

a rapid, sensitive and reproducible hplc method using amperometric detector was developed and validated for the analysis of clarithromycin in human plasma. the separation was achieved on a monolithic silica column (mz- c8 125×4.0 mm) using acetonitrile- methanol-potassium dihydrogen phosphate buffer (40:6:54,v/v), with ph of 7.5, as the mobile phase at a flow rate of 1.5 ml/min. the assay enabl...