Influence of the Anionic Part of 1-Alkyl-3-Methylimidazolium-Based Ionic Liquids on the Chromatographic Behavior of Perazine in RP-HPTLC

1-Alkyl-3-methylimidazolium-based ionic liquids (tetrafluoroborate, L-(ţ)-lactate and ethyl sulfate) were used as mobile phase additives to assess the effect of its anionic part on the retention mechanism of perazine in pharmaceutical formulation in reversed-phase highperformance thin-layer chromatography (RP-HPTLC) method. In all cases, significant changes and improvements in the retention factor were observed when ionic liquids were added to the mobile phase. We found that the chromatographic behavior of the basic analyte depends on the utilized ionic liquid as well as its various anions. Enhancement of separation confirms silanol suppressing potency of employed ionic liquids and their positive impact on chromatographic separation of basic drugs. Among selected ionic liquids, the optimum distribution parameters such as shape and quality of spots, high precision, and accuracy in qualitative and quantitative determination characterize the system with [EMIm][BF4] as mobile phase modifier. Our proposed HPTLC method for determination of perazine in oral tablets was also subjected to subsequent validation procedure in accordance with ICH guidelines and proved to be suitable, inexpensive, and convenient method in a pharmaceutical analysi

Ionic Liquids as Mobile Phase Additives for Feasible Assay of Naphazoline in Pharmaceutical Formulation by HPTLC–UV–Densitometric Method

A specific and reliable High-Performance Thin Layer Chromatography (HPTLC) with densitometry detection method has been developed for determination of naphazoline nitrate in nasal drops. The best separation of basic analyte, without spot tailing, was achieved using the mobile phase composed of acetonitrile:water (60:40,v/v) with 1.5 % (v/v) imidazolium-class ionic liquid added and the plates covered with stationary phase based on the RP-18 with F254S (10cm x 20cm). The presented results confirm that imidazolium tetrafluoroborate ionic liquids are efficient suppressors of free silanols, which are considered to be responsible for troublesome and irreproducible chromatographic determinations of basic compounds. The developed chromatographic system was found to be convenient in use and at the same time providing a repeatable assay of naphazoline nitrate in nasal drops, which could not be obtained with the use of standard silanol suppressing mobile phase additives, like triethylamine (TEA) or dimethyloctylamine (DMOA)

Alpha-methylacyl-CoA racemase and hepsin as urinary prostate cancer markers

Background: Because of the numerous limitations of prostate-specific antigen (PSA), α-methylacyl-CoA racemase (AMACR) and hepsin have recently been suggested as potential biomarkers in prostate cancer (PC). This report presents a comparison study of the presence of AMACR and hepsin in urine collected before and after digital rectal examination (DRE) as a previously suggested diagnostic marker for PC. Methods: Seventy-six urine samples (38 before and 38 after prostate massage) from patients with benign prostatę hyperplasia (BPH) and 66 urine samples (33 before and 33 after prostate massage) from patients with PC were analyzed. PC was confirmed by prostate biopsy. Urinary levels of AMACR and hepsin were determined by ELISA and related to the tumor stage, Gleason score and PSA level. Results: AMACR and hepsin levels in urine collected after prostate massage were higher only in the PC group. There were no correlations between AMACR levels, hepsin levels, tumor stage and Gleason score. AMACR and hepsin did not differentiate between BPH and PC with better true positive and false negative rates than serum PSA. Conclusions: AMACR and hepsin were unable to diagnose PC with better true positive and false negative rates than PSA. An additional procedure combined with other markers should be applied for the reliable diagnosis of PC

Impact of mild therapeutic hypothermia on bioavailability of ticagrelor in patients with acute myocardial infarction after out-of-hospital cardiac arrest

Background: Out-of-hospital cardiac arrest (OHCA) frequently occurs in the early phase of acute myocardial infarction (MI). Survivors require percutaneous coronary intervention (PCI) with concomitantdual antiplatelet therapy. Target temperature management, including mild therapeutic hypothermia (MTH), should be applied in comatose patients after resuscitation. However, an increased risk of stent thrombosis in patients undergoing hypothermia is observed. The aim of this study was to assess the impact of MTH on pharmacokinetics of ticagrelor in cardiac arrest survivors with MI treated with MTH and PCI.Methods: In a prospective, observational, single-center study pharmacokinetics of ticagrelor were evaluated in 41 MI patients, including 11 patients after OHCA undergoing MTH (MTH group) and 30 MI patients without OHCA and MTH (no-MTH group). Blood samples were drawn before administration of a 180 mg ticagrelor loading dose, and 30 min, 1, 2, 4, 6, 12, and 24 h after the loading dose.Results: In patients treated with MTH total exposure to ticagrelor during the first 12 h after the loading dose and maximal plasma concentration of ticagrelor were significantly lower than in the no-MTH group (AUC(0–12): 3403 ± 2879 vs. 8746 ± 5596 ng·h/mL, difference: 61%, p = 0.01; Cmax: 475 ± 353 vs. 1568 ± 784 ng/mL, p = 0.0002). Time to achieve maximal ticagrelor plasma concentration was also delayed in the MTH group (tmax for ticagrelor: 12 [6–24] vs. 4 [2–12] h, p = 0.01).Conclusions: Bioavailability of ticagrelor was substantially decreased and delayed in MI patients treated with MTH after OHCA. Trial registration: ClinicalTrials.gov Identifier: NCT0261193

Does morphine administration affect ticagrelor conversion to its active metabolite in patients with acute myocardial infarction? A sub-analysis of the randomized, double-blind, placebo- -controlled IMPRESSION trial

Background. Therapy with aspirin and one of the platelet P2Y12 receptor inhibitors, preferably ticagrelor or prasugrel, is the mainstay of acute myocardial infarction (AMI) treatment. Morphine is the most commonly used analgesic in AMI patients. The IMPRESSION study was the first randomized trial to confirm that morphine use in this clinical setting leads to a delayed and attenuated exposure to ticagrelor and its active metabolite (AR-C124910XX). The mechanism underlying this drug-drug interaction remains hypothetical. Material and methods. A post hoc sub-analysis of the IMPRESSION study, a phase IV, single center, randomized, double-blind, placebo-controlled trial, was performed to examine whether morphine administration interferes with the proportion of AR-C124910XX produced from ticagrelor in AMI patients. Pharmacokinetic results of all subjects pretreated with placebo (n = 35) and morphine (n = 35) were analyzed. The ratio of total exposure to AR-C124910XX to total exposure to ticagrelor for 12 h was used to illustrate the rate of ticagrelor metabolism. Total exposure to investigated compounds was measured as the area under the plasma concentration-time curve (AUC). Results. The ratios of AUC(0–12) for AR-C124910XX to AUC(0–12) for ticagrelor were comparable between morphine and placebo pretreated patients (20.9 [13.9–34.6] v. 24.7 [18.1–29.6] %; p = 0.58). Importantly, visual inspection of the relationship between AUC(0–12) for AR-C124910XX and AUC(0–12) for ticagrelor revealed that regression lines for the morphine and placebo groups were located closely to each other, with a tendency for superimposing. Additionally, we observed similar values of slope coefficients for both study arms in the linear regression equations illustrating the relationship between AUC(0–12) for AR-C124910XX and AUC(0–12) for ticagrelor (0.19 [± 0.03] v. 0.21 [± 0.04]; p for the statistical significance of both slope coefficients < 0.0001). Conclusions. In the IMPRESSION study, conversion of ticagrelor to AR-C124910XX in AMI patients was not affected by morphine administration

Engrailed-2 protein as a potential urinary prostate cancer biomarker: a comparison study before and after digital rectal examination

This study was designed to compare and evaluate the presence of engrailed-2 (EN2) protein in urine collected before and after prostate massage as a diagnostic marker for prostate cancer (PCa). We analysed and compared 76 urine samples (38 before and 38 after prostate massage) from the benign group (BPH) and 66 urine samples (33 before and 33 after prostate massage) from patients with PCa confirmed by prostate biopsy. EN2 levels from the PCa and men with BPH (age range 50–82) were related to the tumour stage, Gleason score and prostate-specific antigen. EN2 levels were determined by enzyme-linked immunosorbent assay in urine. The median EN2 levels in urine after prostate massage were significantly different from those determined in urine before prostate massage (1.25 ng/ml in the PCa group and 0.34 ng/ml in the BPH). The mean EN2 levels in PCa patients were 3.76-fold higher than those in non-PCa patients after prostate massage. The distinct influence of prostate massage on EN2 levels was found to be related to the Gleason score and tumour stage. EN2 may be considered a marker of PCa with certain limitations, such as those related to tumour staging. The specificity and sensitivity of the protocol are highly dependent on prostate massag

Enantioselective acetylation of (R,S)-atenolol: The use of Candidarugosa lipases immobilized onto magnetic chitosan nanoparticles inenzyme-catalyzed biotransformation

tThis paper describes the enzyme immobilization protocol as well as the enzymatic method for the directresolution of (R,S)-atenolol. The used magnetic enzyme carriers possess on their surface new-synthetizedchitosan derivatives with free amine groups distanced by ethyl or butyl chain. Additionally the cat-alytic activity of two types of commercially available lipases from Candida rugosa immobilized onto twodifferent magnetic nanoparticles were compared. The highest values of enantioselectivity (E = 66.9), enan-tiomeric excess of product (eep= 94.1%) and conversion (c = 41.84%) were obtained by using lipase fromCandida rugosa OF immobilized onto Fe3O4-CS-EtNH2. The study confirmed that even after 5 reactioncycles the immobilized lipase maintain its high catalytic activity

Current Trends in Software Engineering Bachelor Theses

This article presents short analysis and observations on current trends and directions in conducting engineering theses in the field of computer science. This report is based on collected bachelor theses in AGH Computer Science Department for academic year 2020/2021 as well as the conducted competition for the best engineering theses held during XXII KKIO 2021 Software Engineering Conference. The awarded works are briefly presented as an illustration to the drawn conclusions

Ligand fishing using new chitosan based functionalized AndrogenReceptor magnetic particles

Superparamagnetic nanoparticles with chemically modified chitosan has been proposed as a potentialsupport for the immobilization of the androgen receptor (AR). The study involved comparison of differentAR carriers like commercially available magnetic beads coated with silica (BcMag) and chitosan coatednanoparticles with different amount of amino groups. The immobilization was carried out through cova-lent immobilization of the AR through the terminal amino group or through available carboxylic acids.The initial characterization of the AR coated magnetic beads was carried out with dihydrotestosterone,a known AR ligand. Subsequently, chitosan modified nanporticles with long-distanced primary aminogroups (Fe3O4CS-(NH2)3) (upto 8.34 mM/g) were used for further study to isolate known AR ligands(bicalutamide, flutamide, hydroxyflutamide and levonogestrel) from a mixture of tested compounds inammonium acetate buffer [10 mM, pH 7.4]. The results showed that the selected nanoparticles are apromising semi-quantitative tool for the identification of high affinity compounds to AR and might be ofspecial importance in the identification of novel agonists or antiandrogens