Adrenocorticolytic activity of o,p′-DDD (chloditan) solution in in vitro and in vivo tests

Abstract

A new drug formulation of the adrenal cortex (AC) inhibitor o,p′-DDD (chloditan) was developed as a solution for i.v. injection. Its effects on glucocorticoid hormone production by human AC tissue culture and AC function in dogs were studied. A concentration range of 0.005 – 5.0 mg/mL was established by adding 5% o,p′-DDD solution to the culture medium. Cultivation of specimens of human adrenocortical tissue in the presence of o,p′-DDD solution caused after 24 h a dose-dependent decrease of 11-hydroxycorticosteroid (11-HCS) content by 11.0 – 69.8%. The 11-HCS content in dog blood plasma decreased by an average of 3.5 times; the response to synthetic 1 – 24-corticotropin stimulation, by three times, with daily administration for 3 d of 10 mL of the solution. The 11-HCS blood level was still reduced two weeks after withdrawal of the drug. The proposed o,p′-DDD solution showed adrenocorticolytic activity and could be recommended for clinical trials.

DOI: 10.1007/s11094-012-0835-8

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Cite this paper

@article{Balon2012AdrenocorticolyticAO, title={Adrenocorticolytic activity of o,p′-DDD (chloditan) solution in in vitro and in vivo tests}, author={Ya. G. Bal’on and A. V. Simurov and Ihor P. Paster and L. I. Vakulenko and L. M. Tochilkina and L. A. Kuzminskaya and Nataliia Levchuk}, journal={Pharmaceutical Chemistry Journal}, year={2012}, volume={46}, pages={504-506} }