Current Issue : April - June Volume : 2014 Issue Number : 2 Articles : 2 Articles
Steroidal esters of 17-oximino-5 androsten-3�Ÿ-ol were synthesized from dehydroandrosterone acetate. These compounds were tested for their antiproliferating activity and 5a-Reductase inhibitory activity in comparison to finasteride. Decreased androgen levels have been found in serum of animals treated with newly synthesized compounds. These compounds have shown better cytotoxicity as comparison to the clinically used drug finasteride. Therefore these compounds can be useful in the treatment of androgen dependent disorders of prostate alone or by synergistic effect they can decrease the size of prostate due to their antiproliferating activity. The compound TRB-263 was synthesized from the diosgenin involving marker degradation, oximation, Beckmann rearrangement, acid hydrolysis, oximation and esterification.All the phaemacokinetics parameters were determined using male wistar rats by the RP-HPLC.Male wistar rats were selected for the determination of all the pharmacokinetic parameters of TRB-263 by the oral administration of both finasteride and TRB-263, 0.4 ml of blood samples were collected from retro orbital plexus at 0, 0.5, 0.75, 1, 2, 3, 4, 6, 8, 10, 12, 16 in heparinised tubes and after i.v. injection of finasteride and TRB-263, 0.4 ml of blood samples were collected from retro orbital plexus of at 0, 0.5, 0.75, 1, 2, 4, 6, 8, 10, 12, 16....
One of the most quick and comprehensive way of determining the in-vivo pharmacokinetic profile is gamma scintigraphic study of labelled bio-medicals, materials and pharmaceuticals with radiation emitting isotopes. The formation of chemical bond between isotope and drug using a chelating agent gives a formulation called as radiopharmaceutical. Binding of two components is radiolabeling. The tagging of radionuclide helps in tracing the bioavailability and bio-distribution study of radiolabelled compound to the target organ. The method adopted in radiolabeling evaluates radiochemical purity by quality control parameter like ITLC which determines the labelling efficiency. Therefore, in nuclear medicine it can be said that higher the labelling efficiency, better the in-vivo evaluation of pharmacokinetic profile of drug. The administration of dosage form tagged with radionuclide can provide vital information about the in-vivo behaviour, extent, rate and site, mode of drug release and morphology of the target organ in animal or human being within the limits of ethical norms....
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