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Octanol–water partition coefficients (log Po/w) of fifteen previously synthesized 17β-carboxamide glucocorticoid derivatives and prednisolone were determined using shake-flask method. The retention behavior of selected compounds was tested in five reversed-phased thin-layer chromatography (RP-TLC) systems, consisting of water and organic solvent (acetonitrile, acetone, ethanol 96%, methanol, or tetrahydrofuran), and chromatography parameters (RM0, S, and C0) were calculated. Simple linear regression (SLR) analysis was performed, and the correlation between log Po/w and chromatography parameters was tested. The most appropriate RP-TLC system for log Po/w prediction was that consisting of water and ethanol 96% as the mobile phase. Statisitical evaluation of the quality of models created using this system proved their reliability for log Po/w prediction of new 17β-carboxamide glucocorticoid derivatives, and the model with the most favorable statistical parameters was underlined.

Background: Nonsteriodal anti-inflammatory drugs (NSAIDs) are numerous and widely used for more than 60 years, but there is still a strong need for developing novel selective NSAIDs. The need is justified by the fact that nonselective NSAIDs can produce serious gastric side effects and that some of the selective NSAID are withdrawn due to their cardiotoxic side effects. Methods: Eight β-hydroxy-β-arylpropanoic acids, which belong to the arylpropanoic acid class of compounds, structurally similar to some nonsteroidal anti-inflammatory drugs (NSAIDs), were docked into 3D catalytic site of both cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2). Seven out of those eight acids were synthesized using already published modification of Reformatsky reaction additionally optimized by increasing temperature. Synthesized compounds were tested in vivo in order to elucidate anti-inflammatory activity, gastric tolerability and impact on liver function of rats. Results: Results of docking studies have indicated that all compounds have potential to selectively inhibit COX-2 isoform, but that the compounds containing polar substituents on phenyl ring are better inhibitors. Results of carrageenan-induced rat paw oedema test have shown that all compounds exhibit dose dependence and good gastric tolerability and none of the tested compounds have shown negative effect on liver function compared to ibuprofen. Conclusion: The compound containing polar nitro group in para position has shown the best docking results, anti-inflammatory activity, low hepatotoxicity and good gastric tolerability.

Summary. The synthesis and characterization of N-[2-[[4-iodo-2,6-bis(1-methylethyl)phenyl]amino]-2-oxoethyl]- N-(carboxymethyl)glycine and N-[2-[(4-iodo-2,6-diethylphenyl)amino]-2-oxoethyl]- N-(carboxymethyl)glycine is presented, as well as a modified and improved synthesis of N-[2-[(2,4-diiodo-6-methylphenyl)amino]-2-oxoethyl]- N-(carboxymethyl)glycine. These compounds are new agents for hepatobiliary imaging.

A simple and reliable HPTLC method has been developed for simultaneous determination of antimycotics (bifonazole and econa-zole nitrate) and preservatives (methyl- and propylparaben) in medicinal creams. Chromatography was performed on silica gel plates with ethyl acetate-n-hexane-methanol-ammonia-diethylamine, 0.5 + 4 + 0.8 + 0.4 + 2 (v/v) as mobile phase. Chroma-tographic zones corresponding to spots of econazole nitrate, bifona-zole, and parabens were scanned in reflectance/absorbance mode at λ= 230, 250, and 300 nm, respectively. The method was successfully applied to simultaneous determination of the compounds in commercially available pharmaceuticals.

HPTLC and HPLC methods have been established for separation and quantitative determination of econazole nitrate. HPTLC was performed on silica gel plates with n-butyl acetate–carbon tetrachloride–methanol–diethylamine, 3 + 6 + 2.5 + 0.5 (v/v), as mobile phase. Chromatographic zones, or spots, of econazole base and nitrate were used to quantify econazole nitrate. HPLC was performed on amino and C8columns with acetonitrile–water, 30 + 70 (v/v), pH 2.5 (adjusted with phosphoric acid), as a mobile phase. The chromatograms were characterized by single peaks of econazole (amino column) or nitrate (C8column). The methods were successfully used for determination of econazole nitrate in spray solution and vaginal pessaries.

A simple and reliable high performance liquid chromatographic (HPLC) method for the quantification of isosorbide 5- mononitrate and inorganic nitrate impurity in raw material and dosage formulations has been developed and validated. The procedure which simultaneously resolves active organic nitrates: isosorbide 5-mononitrate, isosorbide 2-mononitrate and isosorbide 2.5-dinitrate, and main impurities (including related nitrate and acetate esters), may be used as a control of purity of raw material and dosage forms.

This paper describes a simple, rapid, and reliable HPTLC procedure for the determination of cyproterone acetate and ethinylestradiol in tablets. Identification and determination were performed on 10 cm × 20 cm LiChrospher silica gel 60 F254HPTLC plates with cyclohexane—ethyl acetate, 6 + 4 (v/v), as mobile phase. Calibration plots were established showing the dependence of response (peak area) on amount chromatographed. The ranges validated were 250–4000 ng (r= 0.9923) and 100–500 ng (r= 0.9996) for cyproterone acetate and ethinylestradiol, respectively. The suitability of this HPTLC method for quantitative determination of the compounds was proved by validation of precision and accuracy. The method was used for determination of the compounds in commercial pharmaceutical dosage forms (Androcur 10 mg and Diane 35 tablets). The method is simple, reproducible, and accurate and can be used as a more effective option than other chromatographic techniques in routine quality control.