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Inventi Rapid - Pharmacokinetics & Pharmacodynamics

Articles

  • Inventi:pkd/124/14
    PHARMACOKINETICS STUDIES ON 5?-REDUCTASE INHIBITOR TRB-263 (17-OXIMINO-5 ANDROSTEN-3?-OL)
    Ayushi Chawla, T R Bhardwaj

    Steroidal esters of 17-oximino-5 androsten-3ß-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.

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