Naproxen is one of the most used non-steroidal anti-inflammatory drugs (NSAIDs). It is used to treat pain of various origins, inflammation and fever. Pharmaceutical preparations containing naproxen are available with prescription and over-the-counter (OTC). Naproxen in pharmaceutical preparations is used in the form of acid and sodium salt. From the point of view of pharmaceutical analysis, it is crucial to distinguish between these two forms of drugs. There are many costly and laborious methods to do this. Therefore, new, faster, cheaper and, at the same time, simple-to-perform identification methods are sought. In the conducted studies, thermal methods such as thermogravimetry (TGA) supported by calculated differential thermal analysis (c-DTA) were proposed to identify the type of naproxen in commercially available pharmaceutical preparations. In addition, the thermal methods used were compared with pharmacopoeial methods for the identification of compounds, such as high-performance liquid chromatography (HPLC), Fourier-transform infrared spectroscopy (FTIR), UV-Vis spectrophotometry, and a simple colorimetric analyses. In addition, using nabumetone, a close structural analog of naproxen, the specificity of the TGA and c-DTA methods was assessed. Studies have shown that the thermal analyses used are effective and selective in distinguishing the form of naproxen in pharmaceutical preparations. This indicates the potential possibility of using TGA supported by c-DTA as an alternative method.

• Publikační typ
• časopisecké články MeSH

Pacienta s obtížně léčitelným astmatem (OLA) můžeme charakterizovat jako pacienta s nedostatečnou kontrolou astmatu i přes dodržování nastaveného komplexního léčebného režimu včetně antiastmatické terapie. Příčinou může být i perzistující eozinofilie jako podklad OLA. Biologická léčba protilátkou proti interleukinu 5 (mepolizumabem) přinesla našemu pacientovi značný benefit v podobě přerušení dlouhodobé léčby systémovými kortikoidy. Nadšení z léčebného úspěchu vystřídal po roce a půl nejasný septický stav s kožními příznaky a trombózou levé dolní končetiny, neúspěšně léčený antibiotickou terapií zaměřenou na chronickou kolonizaci Staphylococcus aureus. Ačkoliv je sedimentace erytrocytů (FW) dnes již často opomíjeným vyšetřením s omezeným klinickým významem a je nahrazována pouze vyšetřením C-reaktivního proteinu (CRP), v řadě případů je její provedení důležitým diagnostickým ukazatelem. Platí to zejména pro autoimunitní onemocnění, jako je tomu v prezentovaném případě, kdy následné nasazení imunosupresivní terapie v podobě systémových kortikosteroidů vrátilo pacienta zpět do běžného života.

Patients with the “difficult to treat asthma” (DTA) can be characterized as the patients with uncontrolled asthma despite adherence to a set of complex treatment regimen of asthma. In some cases persistent eosinophilia might be reason for DTA. Biological therapy using antibodies to interleukin 5 (IL-5) (mepolizumab) has brought considerable benefit to our patient enabling the long-term interruption of treatment with systemic cortico - steroids. Enthusiasm for DTA control without systemic corticosteroid was after 18 months replaced by unclear sepsis with cutaneous symptoms and deep venous thrombosis of left leg, unsuccessfully treated with antibiotics obviously given to treat chronic colonization with Staphylococcus aureus. Although the erythrocyte sedimentation rate (ESR) seems to be have limited meaning for clinical evaluation, and is usually replaced by the C-reactive protein test (CRP), in many cases the ESR could be the really important diagnostic indicator. This is especially true for some autoimmune disorders, as demonstrated in this case study, when the subsequent medical treatment with systemic corticosteroids returned the patient to normal life.

• MeSH
• antibakteriální látky terapeutické užití   MeSH
• autoimunitní nemoci MeSH
• bronchiální astma * diagnóza   farmakoterapie   MeSH
• diagnostické zobrazování využití   MeSH
• duplexní dopplerovská ultrasonografie využití   MeSH
• horečka MeSH
• hormony kůry nadledvin terapeutické užití   MeSH
• klinické laboratorní techniky využití   MeSH
• krevní sedimentace MeSH
• lidé středního věku MeSH
• lidé MeSH
• PET/CT využití   MeSH
• polymyalgia rheumatica diagnóza   farmakoterapie   MeSH
• revmatoidní faktor MeSH
• svalová únava MeSH
• syndrom systémové zánětlivé reakce * MeSH
• trombóza diagnóza   farmakoterapie   MeSH
• výsledek terapie MeSH
• Check Tag
• lidé středního věku MeSH
• lidé MeSH
• mužské pohlaví MeSH
• Publikační typ
• kazuistiky MeSH

Background/Objectives: Increasing drugs' stability and adequately protecting them against degradation will ensure a decrease in their price and broader availability of pharmaceutical substances. This is of great importance, especially for drugs used to treat the most common diseases in the population, such as hypertension. The study examined two newly synthesized substances from the angiotensin I-converting enzyme inhibitor (ACEI) group as potential drugs. ACEIs are among the leading drugs used in the treatment of hypertension in the world. The chemical modifications of the tested substances applied concerned the places most susceptible to degradation. The presented work analyzed the compatibility of new derivatives with selected excipients used in pharmacy. Methods: Thermogravimetric (TGA) and differential thermal analyses (c-DTA) were used as the main methods. In addition, non-thermal methods such as colorimetry analysis, Fourier-transform infrared (FTIR) and UV spectroscopy were used. Results: Based on the conducted studies, it can be concluded that the incompatibility of IND-1 with glucose anhydrous and lactose monohydrate occurs only when the mixture is stored at higher temperatures. For the remaining IND-1 and IND-2 mixtures with excipients, compatibility was demonstrated. Conclusions: The obtained results confirmed the usefulness of the applied thermal analyses (TGA and c-DTA) for assessing the compatibility of the tested potential drugs with excipients. However, in the case of incompatibility reactions of substances occurring under the influence of elevated temperatures, such as the Maillard reaction, it is necessary to use non-thermal methods to obtain the right result.

• Publikační typ
• časopisecké články MeSH

The first [Pd(L(n))(2)(ox)] xH(2)O oxalato(ox) complexes involving 2-chloro-N6-(benzyl)-9-isopropyladenine (L(1); complex 1), 2-chloro-N6-(4-methoxybenzyl)-9-isopropyladenine (L(2); 2), 2-chloro-N6-(2,3-dimethoxybenzyl)-9-isopropyladenine (L(3); 3), 2-chloro-N6-(2,4-dimethoxybenzyl)-9-isopropyladenine (L(4); 4), and 2-chloro-N6-(4-methylbenzyl)-9-isopropyladenine (L(5); 5) have been synthesized by the reactions of potassium bis(oxalato)palladate(II) dihydrate, [K(2)Pd(ox)(2)].2H(2)O, with the mentioned organic compounds (H(2)ox=oxalic acid; x=0 for 1-3 and 5 or 2 for 4). Elemental analyses (C, H, N), FTIR, Raman and NMR ((1)H, (13)C, (15)N) spectroscopies, conductivity measurements and thermal studies (thermogravimetric and differential thermal analyses, TG/DTA) have been used to characterize the prepared complexes. The molecular structures of [Pd(L(2))(2)(ox)] (2) and [Pd(L(5))(2)(ox)].L(5).Me(2)CO (5.L(5).Me(2)CO) have been determined by a single crystal X-ray analysis. The geometry of these complexes is slightly distorted square-planar with two appropriate L(n) (n=2 or 5) molecules mutually arranged in the head-to-head (2) or head-to-tail (5) orientation. The L(n) ligands are coordinated to the central Pd(II) ion via the N7 atoms. The same conclusions regarding the binding properties of L(1)-L(5) ligands can be made based on multinuclear NMR spectra. In vitro cytotoxicity of the complexes 1-5 has been evaluated against human chronic myelogenous leukaemia (K562) and human breast adenocarcinoma (MCF7) cancer cell lines. Significant cytotoxicity has been determined for the complexes 3 (IC(50)=6.2 microM) and 5 (IC(50)=6.8 microM) on the MCF7 cell line, which is even better than that found for the well-known and widely-used platinum-bearing antineoplastic drugs, i.e. oxaliplatin and cisplatin.

• MeSH
• adenin chemie   MeSH
• krystalografie rentgenová MeSH
• lidé MeSH
• ligandy MeSH
• molekulární struktura MeSH
• nádorové buněčné linie MeSH
• organokovové sloučeniny chemická syntéza   chemie   toxicita   MeSH
• oxaláty chemie   toxicita   MeSH
• palladium chemie   toxicita   MeSH
• protinádorové látky chemická syntéza   chemie   toxicita   MeSH
• Check Tag
• lidé MeSH
• Publikační typ
• práce podpořená grantem MeSH