[The pharmacokinetics of medamine and its solid polymeric form (medapek) in experimental larval alveolar echinococcosis in cotton rats]. / Farmakinetika medamina i ego tverdoi polimernoi formy (medapek) pri éksperimental'nom larval'nom al'veoliarnom ékhinokokkoze khlopkovykh krys.

Our study has shown that after single administration of its substance or its polymer formulation, medamine rapidly absorbs into blood, by penetrating into the host's viscera and tissues and parasitic larvocysts and excretes from the experimental animals' body at hour 24. Examining the distribution of medamine in the viscera and tissues has revealed that it penetrates into the rat viscera and tissue with blood and accumulated in the tissues. At the same time medamine given as a substance accumulates more in the excretory organs and medapec retains in the muscle tissue and brain longer. Medapec shows higher maximum concentrations at lower values of the pharmacokinetic curve area. Noticeable accumulation of medamine in the larvocysts of experimental animals confirms its chemotherapeutical activity.

[The technology for manufacturing antiparasitic preparations. 9. The new preparation tizanox and an evaluation of its anti-Hymenolepis activity]. / Tekhnologiia proizvodstva protivoparazitarnykh preparatov. 9. Novyi preparat tizanoks i otsenka ego protivogimenolepidoznoi aktivnosti.

The paper describes a procedure for manufacturing the new anthelminthic Tizanox. It shows it necessary to administer a larger dose of the drug than that of azinox (praziquantel) to treat experimental hymenolepiasis. However, the lower toxicity of Tizanox enhances its chemotherapeutical index.

Choosing the calibration model in assay validation.

Data transformations and weighting schemes are normally used to obtain the best-fit of standard curves in bioanalysis and the calibration model is usually selected during prevalidation. In the present study, a comparison has been made between unweighted and weighted (1/x, 1/x2, and 1/square root of x) regression models with or without an intercept in achieving the best-fit for the standard curve of CDRI compound 81/470, a new anthelmintic agent, in cow milk. Validation samples in milk at the LLOQ, medium, and high concentrations were also analysed by each of the calibration models. An unweighted regression equation with an intercept overestimated the concentrations at the LLOQ. An unweighted equation without intercept and weighted equations with or without an intercept significantly minimized the bias at the LLOQ without distorting the results at higher concentrations. Hence, an unweighted equation for a straight line passing through the origin was found to be the best model for a standard curve of 81/470 in milk. Similar results were obtained for 81/470 and UMF-078 in serum and plasma, respectively. Bioanalysts should routinely test these models to obtain the best fit model for their calibration curves as part of their assay validation not during prevalidation.

Estimation of anthelmintic compound 81/470 in cow's milk by high-performance liquid chromatography: method development and validation.

CDRI compound 81/470 is a new broad spectrum anthelmintic agent and is being developed for veterinary use. HPLC assay method for 81/470 in cow milk was developed and validated. The sample preparation consisted of protein precipitation, followed by extraction with ether. Separation was achieved on a C18 column using acetonitrile-buffer (pH 6, 50 mM) mobile phase and the compound was quantitated using fluorescence detector. The recovery of 81/470 was above 90% and was consistent over the calibration range of 10-1000 ng ml-1. Accuracy and precision were determined by analyzing replicate samples and were found to be within acceptable limits. Five freeze-thaw cycles of spiked milk and storage of processed dry residues at -30 degrees C for 7 days did not have any detrimental effect on the stability of 81/470.

[The technology for manufacturing antiparasitic preparations. 5. The development of a technology for producing the anthelmintic triclonate and the evaluation of its therapeutic efficacy in monieziasis]. / Tekhnologiia proizvodstva protivoparazitarnykh preparatov. 5. Razrabotka tekhnologii polucheniia antigel'mintika triklonata i otsenka ego lechebnoi éffektivnosti pri moniezioze.

A procedure has been developed to manufacture the anthelminthic Triclonate. The agent was tested for the treatment of sheep's natural monieziasis infection and it was found to have a high activity.