International Journal of Pharmaceutical Chemistry and Analysis

14-21

Authors: Neelima Dhingra1, T.R.Bhardwaj2

Introduction and positioning of the heteroatom in the parental steroid skeleton has significant effect on the activity profile of these compounds. A substantial amount of biologically relevant azasteroids have been reported as antifungals, antilipemic, neuromuscular blocking agents, local anaesthetics, antimicrobials, and GABA receptor antagonist. Recent work from our laboratory has described the synthesis and evaluation of 17-Oxo-17a-aza-D-homo-5-androsten-3β-yl ester derivatives as potential 5-alpha reductase inhibitors. The current study was undertaken to further investigate the cytotoxicity of the newly synthesized derivative using some more human cancer cell lines. Seven human cancer cell lines have been exposed to 1X 10-5m (single dose) of compounds (1-8), Finasteride, 5-fluorouracil, mitocycin 6 and, adriamycin were used as reference drugs for comparison. The cell growth was measured after 24h, using ELISA reader, after staining with sulforhodamine B dye (SRB), which binds to basic amino acid residues in the trichloroacetic acid (TCA) fixed cells. All the experiments were carried out in quadruplicate. The newly synthesized azasteroids derivatives displayed significant cytotoxicity against liver and neuroblastoma cell lines as compared to standard reference drugs. This together with, earlier reported antiproliferative activity against prostate cancer cell lines (DU-145) and 5-alpha reductase inhibitory activity, indicates that 17a-azasteroids seems to possess potential eliciting in vitro cytotoxicity. Results obtained from these studies shall be used as guidelines for further development of novel compounds to be used chemotherapeutic agents.

28-33

Authors: P. S. Jain*, A. P. Gorle, S. S. Patil, R. S. Chavan, P. R. Bari, S. J. Surana

A new simple, precise, accurate and selective RP-HPLC method has been developed and validated for estimation of salmeterol xinafoate in pharmaceutical formulation. The method was carried out on a Qualisil RP C-18 (250 mm x 4.6 mm, 5 μm) column with a mobile phase consisting of buffer: acetonitrile: methanol (45:25:30 v/v/v), pH adjusted to 6 with diammonium hydrogen orthophosphate and flow rate of 0.5 mL/min. Detection was carried out at 250 nm. The retention time for salmeterol xinafoate was found to be 7.41 min. The salmeterol xinafoate followed linearity in the concentration range of 1- 6 μg/mL (r2= 0.9984). The amount of the drug estimated by proposed method was found to be in good agreement with label claim. The developed method was validated for sensitivity, accuracy, precision, ruggedness and robustness. The LOD and LOQ were found to be 0.10 and 0.29 μg. Salmeterol xinafoate was subjected to acid and alkali hydrolysis, oxidation and thermal degradation. The drug undergoes degradation under acidic, basic, oxidation and thermal conditions. This indicates that the drug is susceptible to acid, base, oxidation and thermal conditions. The degraded product was well resolved from the pure drug with significantly different Retention Time. The proposed method can be used for routine analysis of salmeterol xinafoate in bulk drug and pharmaceutical formulation.

38-41

Authors: Neethu Mathew1,*, M. Sukumar2, T. K Ravi3, Arunkumar R4, Betty Carla5

Various N-[3-Chloro-2-(substituted)-4-oxazetidin-1-yl]-4-(1H-indol-3-yl) butanamide derivatives have been synthesized by the cyclo condensation of Schiff bases with tri ethyl amine and chloro acetyl chloride. The structures of the newly synthesized compounds have been established on the basis of their spectral data. All compounds were evaluated for α-amylase inhibitory activity. All compounds investigated exhibited significant activity, comparable to that of the standard used.

46-50

Authors: Sankalp Yadav1*, Gautam Rawal2

The world is facing the problem of substandard or spurious drugs. These substandard drugs have resulted in life threatening issues, financial loss of consumer and manufacturer and loss in trust on health system. The problem is graver in developing countries where these drugs are easily available to the people. There is an urgent need to address this issue and take measures to control the widespread availability and usage. Although, India has taken some preventive measures to fight against the problem of substandard/spurious drugs for protecting and promoting the public health but, still a lot needs to be done.