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Abstract

Aim. The aim of this study is to evaluate the efficiency of proton pump inhibitors in the treatment of gastric and duodenal ulcers as based on literature.

Materials and methods: The materials of this research are the results of 86 original studies on the effectiveness of proton pump inhibitors analysis.

Methods. Descriptive, statistical, retrospective.

Results and Conclusion. According to the clinical random researches, Omeprazole preparations are not included in the list due to proven better effectiveness of Esomeprazole drugs. Moreover, lansoprazole drugs are not included according to proven short-acid inhibitory effect. In addition, the brand of mentioned above preparation does not exist on the pharmaceutical market of Ukraine. Furthermore, rabeprazole preparations are presented in the research by Pariet (brand) and by the effective generic Barol, while pantoprazole preparations are represented in the research by Kontrolok (brand) and by the generic Pultset, as well as by Nolpaza. Herein, the Pantosan effect was not significantly different from the effect of Pultset and Nolpaza, but the preparation is much more expensive. In terms of efficiency (%), 4 week repair of mucosal defects was carried out by way of the following treatment regimens: Barol + Amoxicillin + Clarythromycin (90.9±6.2), Pariet + Amoxicillin + Clarythromycin (83±2.6), Kontrolok + Amoxicillin + Clarythromycin (100±1.3), Pultset + Amoxicillin + Clarythromycin (88±4.1), Nolpaza + Amoxicillin + Clarythromycin (72±4.1), Ezolonh + Amoxicillin + Clarythromycin (87.7±3.8), Neksium + Amoxicillin + Clarythromycin (96.1±3.1).

Abstract

Increased multidrug resistance prompted researchers to search for a new drug that has the ability to overcome antibiotic resistant pathogens. Essential oils have been used in folk medicine for centuries, therefore, they could be employed as an effective alternative to antibiotics without having secondary side effects.

The aim of the present study was to test the antibacterial and antibiofilm activity of the essential oil of Achillea santolina and to ascertain its mode of action.

Minimum Biofilm Inhibitory Concentration (MBIC) susceptibility assays were performed using a biofilm inoculator with a 96-well plate with peg led. Minimum Inhibitory Concentration (MIC) was performed in normal microtitre plates using a twofold dilution series.

Achillea santolina essential oil (ASEO) was able to overcome the resistance of all tested bacteria. The MIC values were in the range of 250-1000 µg/ml, while the MBC values were in the range of 500-2000 µg/ml. ASEO increased leakage of potassium ions from the cell membrane and increased release of cellular materials – suggesting that the cell membrane is the target and site of action of ASEO. Moreover, ASEO was able to inhibit initial adherence of methicillin-resistant Staphylococcus aureus (MRSA) (ATCC 43300) at sub-inhibitory concentrations through alterations to cell membrane.

Abstract

Natural biopolymers are the most likely choice for biomedical applications, and starches can be considered the best materials for such applications. This comes from the fact of their natural origin and their high biodegradable behavior. Native starches have weak hydrogen bonding and a leaching behavior – making it a candidate for drug delivery application. Still, to make starch useful as a drug delivery carrier, this hydrogen bonding must be strengthened. In this work, native sweet potato starch was used, and the hydrogen bonding between starch molecules was enhanced by introducing glycerol as a hydrogen bonding source and sodium alginate (SA) as a thickener. This blend was tested by means of FTIR and DSC, and based on the test results, improved hydrogen bonding had taken place. Furthermore, potato starch microspheres were successfully produced at different flow rates. In the work, a microfluidic capillary device was harnessed to form microsphere generating total flow rates ranging between (0.00031 and 0.00054) cm3/sec. Herein, a starch/sodium alginate/glycerol mixture was used as a dispersed phase and PVA+tween 80 was used as continuous phase. At high flow rates (0.00062-0.00054) cm3/sec, the microspheres took an oval shape. At flow rates (0.00034-0.00048) cm3/sec, the microspheres took a spherical shape. At very low flow rate (0.00031) cm3/sec, the microspheres shell was weak and caused core oozing. In this work, starch microspheres were successfully formed with diameter ranging from (151-263) µm.

Abstract

Aim. The purpose of this study is to reveal the determination of the structure of the main metabolite of morpholinium 2-(4-(2-methoxyphenyl)-5-(pyridin-4-yl)-4H-1,2,4-triazole-3-yl)thio)acetate (an active pharmaceutical ingredient – API) by way of chromatography through mass spectrometry detection, utilizing the liquid chromatography system Agilent 1260 Infinity and mass spectrometry detector (single quadrupole detector Agilent 6120). In the work, the graph of the change in the area of the peak of the metabolite from time after the introduction of the API solution was constructed. Moreover, the charges on the atoms of 2-((4-(2-methoxyphenyl)-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)thio) acetate were calculated and the structure of the methyl derivative was proposed. We saw that the methylation of the active substance during metabolism formed a 5-((carboxymethyl)thio)-4-(2-methoxyphenyl)-1-methyl-3-(pyridin-4-yl)-4H-1,2,4-triazol-1-um cation through N-methyltransferase.

Abstract

Cross-infection involves the transmission of microorganisms through secretions, bodily fluids and excreta, as well as undisinfected surfaces and medical equipment. In the dental office, diseases are transmitted via various routes, e.g. from patient to dentist or other member of dental team, from doctor or dental team member to patient, from patient to another patient, from dental office to community and from community to patient. The study was conducted to evaluate the effectiveness of infection control in dental practices based on the qualitative and quantitative assessment of microbiological contaminants detected on the surface of filling material packaging used in dental offices. The material for research were 9 packages containing dental materials during their use in 3 dental settings. The packages were placed in sterile flasks and rinsed to wash microorganisms from the surfaces. The washes were filtered through membrane filters and cultured under proper aerobic and anaerobic conditions, and at elevated CO2 concentration. Microbial growth on TIO and TSB media was observed. The contamination of most samples remained low as indicated by the growth from one to a maximum of five colonies on TSA. The contamination remained at the level of 10-50 CFU/package, i.e. <100 CFU/single package. The tests evaluating the contamination of dental package surfaces with aerobic bacteria confirmed high hygiene standards observed in dental offices from which the packages were brought.

Abstract

Introduction. Diabetes mellitus is one of the world’s most common diseases, therefore the development and introduction of new effective drugs for diabetes treatment into clinical practice is an important task for the health systems of many countries of the world.

Aim. The aim of our work was to determine and substantiate the quantitative ratio of excipients for the development of the optimal composition of directly compressible ginger dry extract tablets.

Materials and methods. To choose the optimal composition of tablets containing ginger dry extract, the effect of various quantitative ratios of the excipients Kollidon K30 and Neusilin UFL 2 on tablet mass pharmaceutical technical parameters, determined by established methods, was studied. For processing the experimental data, mathematical methods were used: design of experiment, regression analysis and a technique based on the theory of vector optimization.

Results. The interrelation between factors that were studied and technological parameters of tablet mass and compressed tablets were analyzed using regression equations.

Conclusions. The studies conducted allowed to chose the optimal composition of ginger dry extract tablets: ginger dry extract – 60%, Galen IQ 721 – 34.5%, Kollidon K30 – 3.5%, Neusilin UFL 2 – 1%, calcium stearate – 1%. The chosen tablet formulation is characterized by pharmaceutical technical parameters meeting the requirements of the European Pharmacopoeia and the State Pharmacopoeia of Ukraine.

Abstract

Introduction and Aim. The study aims to review the premise according to which a specific set of personal values is characteristic of pharmacy students indicating work in direct contact with the patient and building a therapeutic relationship as a preferred area of professional activity. The theoretical basis for the study draws on the Schwartz model of personal values.

Material and Method. The research was conducted among 211 students at the Faculty of Pharmacy, Medical University in Lublin, aged 21-30 years (M=23.17; SD=1.26). The reference group (n=83) was composed of respondents declaring preference for a professional activity implying direct contact with patients (mainly retail pharmacy). The control group included students declaring preference for a professional path not entailing direct contact with patients. The study employed the Polish version of the Schwartz Value Survey, as well as the authors’ own questionnaire pertaining to career path preference.

Results. Students declaring preference for direct contacts with patients as their chosen career path, compared to respondents declaring preference for the other alternatives were more likely, as compared to the control, to express preference for the personal values of “security” and scored higher in terms of the higher-level value “conservation”. In addition, a higher preference (oscillating around statistical significance) for the personal value “benevolence” of the control group was demonstrated.

Conclusions. The preference for the values revealed by pharmacy students declaring a choice of retail pharmacy gives rise to concern about the possibility of implementing a new model of pharmaceutical care in Poland.

Abstract

Bladder cancer (BC) is a worldwide common disease with a high mortality rate. Recognizing the dynamic changes in plasma that proteases and their inhibitors undergo might be valuable in understanding the carcinogenesis of invasive bladder cancer and in identifying BC patients with poor prognosis. This study aims to determine the activity of the proteolytic enzyme system and their inhibitors in patients with BC. In this paper, the total proteolytic activity, the activity of matrix metalloproteases (MMPs) and serine proteases was analyzed by the method of caseinolytic activity. For detection of activity of some inhibitors of proteolysis, we used the unified method for determining the activity of alpha-1-antitrypsin (α1A) and alpha-2-Macroglobulin (α2M) in human plasma. The level of medium-mass molecules (MMM) was assessed spectrophotometrically by applying the Nikolaichik method.

The activity of MMPs was elevated in all groups of patients. Moreover, the activity of serine proteases was found to be enhanced in patients with Stage I, III and IV BC, while the activity of α1A was up by 1.4 and 1.3 times in patients with Stage I and Stage IV. The most significant increase was observed with regard to the activity of α2M in patients with I and III stages of BC. In addition, the level of MMM correlated with cancer stage. Indeed, the highest increase in the activity of protease inhibitors was observed in Stage I bladder cancer patients, which might signify their protective role at the onset of the bladder carcinogenesis. In contrast, significant growth in activity of α2M in patients with III stage of BC may point at a compensatory mechanism that inhibits tumor growth.

Abstract

In the present work, we provide the results of defining by utilizing Laser diffraction spectroscopy, the kinetic isotopic effect of solvent and constant of dissolution rate κ, s−1 of аn active pharmaceutical ingredient (API) in water with a different content of a stable 21H isotope on the basis of the laws of first-order kinetics. This approach is based on the analysis of the light scattering profile that occurs when the particles of the dispersion phase in the aquatic environment are covered with a collimated laser beam. For the first time, the dependence of the rate of dissolution is demonstrated not only on the properties of the pharmaceutical substance itself (water solubility mg/ml, octanol–water partition coefficient log P oct/water, topological polar surface area, Abraham solvation parameters, the lattice type), but also on the properties of the solvent, depending on the content of stable hydrogen isotope. We show that the rate constant of dissolution of a sparingly hydrophobic substance moxifloxacin hydrochloride (MF · HCl) in the Mili-Q water is: k=1.20±0.14∙10−2 s−1 at 293.15 K, while in deuterium depleted water, it is k=4.24±0.4∙10−2 s−1. Consequently, we have established the development of the normal kinetic isotopic effect (kH/kD >1) of the solvent. This effect can be explained both by the positions of the difference in the vibrational energy of zero levels in the initial and transition states, and from the position of water clusters giving volumetric effects of salvation, depending on the ratio D/H. The study of kinetic isotopic effects is a method that gives an indication of the mechanism of reactions and the nature of the transition state. The effect of increasing the dissolution of the API, as a function of the D/H ratio, we have discovered, can be used in the chemical and pharmaceutical industries in the study of API properties and in the drug production through improvement in soluble and pharmacokinetic characteristics.

Abstract

Epstein-Barr virus-associated gastric carcinoma (EBVaGC) is the most common malignancy caused by EBV infection. Toll-like receptors (TLRs) as major components of innate immune system are crucial in the development of inflammatory processes and carcinogenesis. The aim of our study was to evaluate tissue and serum level of TLR9 in EBV-positive and EBV-negative gastric cancer patients. The study involved 30 EBV(+) and 30 EBV(-) patients. EBV DNA was detected in fresh frozen tumor tissue. In serum samples TLR9 level, transforming growth factor β (TGFβ), interleukin 10 (IL-10) and antibodies against EBV were detected using ELISA tests. TLR9 level was also measured in homogenate of tumour tissue. TLR9 level was statistically lower in EBV(+) patients both in serum and tissue, with statistically higher level in tissue than in serum. Lower level of TLR9 was accompanied by higher level of Epstein-Barr virus capsid antigen (EBVCA), Epstein-Barr virus nuclear antigen (EBNA) and early antigen (EA). A lower level of TLR9 was detected in patients with poorly differentiated cancer (G3) and greater lymph nodes involvement (N3-N4). Lower level of TLR9 in patients with EA may point to TLR9 role in reactivation of EBV infection.