ABSTRACT
Radiopharmaceuticals are a special group of drugs since many of them are eventually prepared in the hospital and the nuclear medicine department is therfore responsible for meeting quality criteria such as sterility, radionuclide, radiochemical and chemical purity. In this study radiochemical purity for more than 300 preparations of three different radiopharmaceutical formulations from commercial kits were tested using instant thin layer chromatography. The formulations namely 99mTc-DTPA, 99mTc-MDP and 99mTc-MIBI were obtained from Pars Isotope Co. Several paper chromatographic systems were used in this study. The result showed that the most observed impurities were hydrolyzed reduced 99m technetium. After the preliminary study we decided to change our imaging schedule in the nuclear medicine department and the sequence of imaging was changed. Cosequently, the results showed better radiochemical purities. Our equipments for detetion of radioactivity in paper chromatography were changed, for example the old dose calibrator was replaced by a gamma camera or a more accurate dose calibrator. Also, the thin layer chromatography systems were changed to those recommended by the factory and the new results showed much better radiochemical purities
ABSTRACT
Some N-substituted piperidine structures were synthesized and evaluated for cytotoxic activity against four different cell lines using the standard MTT assay method and Doxorubicin was used as the reference drug. The result of cytotoxic activity as a measurement of IC50 values revealed that three of the synthesized compounds were active against breast cancer cell line. Compound 6a bearing hydroxyl at para position of piperidine ring was the most active compound within this series. The N-subtituted piperidine with propene substructure could be considered as a lead structure for further studies of structure activity relationship to develop more potent compounds in future. The compounds were evaluated against four different cell lines using the standard MTT assay method and doxorubicin was used as the reference drug. The IC50 values were determined by constructing dose-response curves and revealed that three of the synthesized compounds were active against breast cancer cell lines. Compound 6a bearing hydroxyl at para position of piperidine ring was the most active compound within this series
ABSTRACT
The contemporary trends and concepts in pharmacy are widely affected by the emergence of Nano-, Bio- or Info- technologies [NBI] as an attempt to develop different principles of medicine. This commentary is trying to make a think tank room for 50 years ahead of today's pharmacy, where the ambience of pharmacy will be affected by such technologies together with cognition [NBIC] to achieve intelligent, low adverse reaction and holistic action medicals
ABSTRACT
Understanding the geometry and electronic properties of non-steroidal anti-inflammatory drugs [NSAIDs] and the nature of their interactions with human cyclooxygenase-2 [COX-2] is important in the development and design of novel NSAIDs. In this paper, B3LYP/6-311++G [d,p] level of theory was applied to assess the acidity of NSAIDs in the gas phase. Subsequently, the role of intramolecular hydrogen bond on acidity of these compounds was confirmed by means of natural bond orbital [NBO] and quantum theory of atoms in molecules analyses [QTAIM]. Furthermore, by applying the polarized continuum model [PCM] at the B3LYP/6-311++G[d,p] level, the pK[a] value of NSAIDs in aqueous solution was calculated. The maximum error was found to be less than 0.1 pK[a] unit in comparison with the experimental value. This protocol can be used as a tool to predict pK[a] values of NSAIDs in future studies. In the last step, attempts have been made to generate a functional model of the structure of human COX-2 enzyme by means of homology modeling to gain more insight into the nature of interactions between NSAIDs and the active site of this COX-2 enzyme by docking studies. In addition, a mean binding energy for each drug was estimated based on its ionization ratio