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Study on protolytic equilibria and the effects of pH, cyclodextrins and polysorbate 80 on solubility of raloxifene hydrochloride
No full textThe acid–base equilibria of raloxifene and the mutual influence of pH and solubility enhancers on the solubility of raloxifene
hydrochloride were studied. The apparent ionization constants (pKa*) of raloxifene were determined potentiometrically in
methanol–water mixtures (45%-55% w/w), and the pKa values (pKa1 = 7.21 ± 0.02, pKa2 = 7.86 ± 0.02, pKa3 = 9.97 ± 0.04)
defining ionization in aqueous media were obtained by extrapolating the pKa* values to 0% of methanol. The obtained pKa
values were assigned to the corresponding ionization centers. Based on the ionization constants obtained in this study, the
distribution of the equilibrium forms of raloxifene was calculated. The solubility of raloxifene hydrochloride in 0.01 M
HCl, acetate buffer pH 4.5 and phosphate buffer pH 6.8 was studied with and without the presence of β-CD, HP-β-CD and
polysorbate 80. The most effective solubility enhancer of raloxifene hydrochloride in 0.01 M HCl was polysorbate 80 at a
concentration of 0.5%, while the influence of this enhancer in phosphate buffer pH 6.8 was negligible. The highest solubility
of raloxifene hydrochloride in acetate and phosphate buffer was achieved in the presence of 10–
3 M HP–β-CD which
was 1.3-fold higher in both 0.01 M HCl and acetate buffer and 2.3-fold higher in phosphate buffer than in the presence of
10–
3 M β-CD
Antimicrobial and Cytotoxic Activities of Essential Oil from the Aerial Parts of Pulicaria dysenterica (L.) Bernh. (Asteraceae)
Get PDFThe chemical composition of Pulicaria dysenterica (L.) Bernh. aerial parts essential oil (EO), growing wild in Bosnia and Herzegovina, was presented in the study. In addition to the EO composition, antimicrobial and cytotoxic activities were also tested. The aerial parts of P. dysenterica contained 0.3% of yellow, liquid, fragrant EO. The 51 components identified accounted for 81.09% of the oil. The EO was characterized by the presence of a high concentration of oxygenated sesquiterpenes 51.83% while oxygenated monoterpenes constituted 15.57%, sesquiterpene hydrocarbons 9.32% and non-terpene compounds presented 4.37% of the EO. The dominant compounds were the sesquiterpenes caryophyllene oxide, (E)-nerolidol, β-caryophyllene and monoterpene nerol. The antimicrobial activity of EO was tested against selected ATCC strains of microorganisms, the bacteria Staphylococcus aureus, Pseudomonas aeruginosa and Escherichia coli, and the fungus Candida albicans. The results showed that the investigated EO inhibited the growth of all selected ATCC strains of microorganisms. The best result was obtained against Escherichia coli bacteria with MIC value of 1 mgmL-1. The cytotoxicity of EO was measured against the HeLa cell line using the MTT method with IC50 of 188.52 μgmL-1. This study has provided scientific baseline data on the therapeutic properties of P. dysenterica
Efikasnost superkritične fluidne hromatografije u kreiranju ekološki prihvatljivih rešenja u farmaceutskoj analizi
Get PDFInitially employed primarily at a preparative scale for enantiomer separation of chiral drug
candidates, Supercritical Fluid Chromatography (SFC) is nowadays extensively used in the
analytical mode. Recent advances in SFC separation science have emphasized its potential for
modern and environmentally friendly pharmaceutical analysis.
The aim of this review is to provide a deeper insight into the main fundamental and practical
aspects of the SFC technique in order to familiarize readers with its versatile nature and efficiency
in creating sustainable chromatographic solutions. All considerations are made primarily in the
context of the most widely used mode of operation - achiral SFC. In addition, recent applications
of this promising technique are presented at the end of the article to further promote its use in
pharmaceutical analytical practice.Na početku pretežno korišćena kao preparativna tehnika u enantioseparaciji hiralnih
molekula kandidatâ za lek, superkritična fluidna hromatografija (eng. supercritical fluid
chromatography, SFC) danas se široko koristi u analitičke svrhe. Noviji naučni napori ukazali su
na značaj SFC tehnike u modernoj i ekološki prihvatljivoj farmaceutskoj analizi.
Cilj ovog preglednog rada je pružanje dubljeg uvida u najvažnije fundamentalne i praktične
aspekte SFC tehnike, kako bi se čitaocima približio njen svestrani karakter, te efikasnost u
kreiranju održivih hromatografskih rešenja. Sva razmatranja prevashodno su data u kontekstu
najzastupljenijeg režima rada - ahiralne SFC. Takođe, na kraju rada predstavljene su savremene
primene ove obećavajuće tehnike kako bi se dodatno ohrabrilo njeno usvajanje u farmaceutsku
analitičku praksu
Costs of treating type 2 diabetes mellitus and its complications
Get PDFThe major driver of the costs of treating patients with diabetes mellitus type 2 (DM2) is its complications, which in developing countries are a consequence of poor glycemic control due to the low availability of novel, innovative antidiabetic drugs. We aimed to determine the ratio of direct medical costs arising from DM2 to the direct costs of its complications, as well as their main predictors. This was a retrospective cohort study of health care utilization and direct medical costs for adults with DM2, with (inpatients) or without (outpatients) complications. The utilization data were multiplied by the unit prices of drugs and services reimbursed by the Serbian Republic Health Insurance Fund to obtain direct costs. In total, 205 inpatients and 60 outpatients with DM2 participated in the study. Key drivers of the costs of treating diabetes complications in hospitals are consultations with specialist clinicians (B = 0.025 [0.003–0.047]), use of reserve antibiotics (B = 0.022 [0.007–0.036]), biochemical tests (B = 0.038 [0.022–0.055]) and length of stay in the hospital (B = 0.011 [0.009–0.013]). On the other hand, the number of encounters with general practitioners (B = 0.179 0.115–0.242) and the number of ultrasound examinations are strongly correlated with the total costs of treating outpatients with DM2 (B = 0.234 [0.054–0.414]). None of the outpatients included in the study were prescribed novel antidiabetic drugs. Overall, the costs of treating DM2 in Serbia are considerable and mainly driven by the 2–11-fold higher costs of complications vs. the costs of the disease itself
Oxidative stress in post-covid-19 syndrome
No full textPost-Kovid sindrom javlja se kod približno 10% pacijenata koji preleže akutnu SARS-CoV-2 infekciju, a
karakterišu ga simptomi slični mijalgičnom encefalomijelitisu/sindromu hroničnog umora. Dosadašnje
studije predložile su mitohondrijalnu disfunkciju i
posledično prekomerno formiranje reaktivnih kiseoničnih vrsta kao jednog od ključnih mehanizama
patogeneze post-Kovida. Cilj ovog rada jeste određivanje oksidativno-stresnog statusa kod post-Kovid
pacijenata i ispitivanje njegove moguće veze sa manifestacijom post-Kovid simptoma. U studiji su ispitani uzorci seruma 60 post-Kovid pacijenata. U
svakom uzorku spektrofotometrijski su određeni
sledeći parametri oksidativno-stresnog statusa: totalni oksidativni status (TOS), totalni antioksidativni status (TAS), aktivnost superoksid dismutaze (SOD),
koncentracija uznapredovalih produkata oksidacije
proteina (AOPP), sadržaj ukupnih sulfhidrilnih grupa
(SHG), prooksidativno-antioksidativni balans (PAB),
ishemijom modifikovani albumin (IMA), paraoksonazna aktivnost paraoksonaze 1 (PON1) i koncentracija malondialdehida (MDA). Statistička analiza
podataka pokazala je da su PAB, TOS, MDA, IMA i
AOPP značajno viši (p<0,01), odnosno da su SHG
(p<0,05), TAS, SOD, PON1 (p<0,01) značajno niži
kod post-Kovid pacijenata nego u kontrolnoj grupi.
Naš rad je pokazao povećan oksidativni stres i smanjenu antioksidativnu zaštitu kod pacijenata sa postKovid sindromom.Post-COVID-19 syndrome affects approximately 10%
of patients who have recovered from acute SARS-
CoV-2 infection and is characterised by symptoms
similar to those of myalgic encephalomyelitis/chronic
fatigue syndrome. Recent studies have suggested
mitochondrial dysfunction and consequently exces-
sive generation of reactive oxygen species as one of
the key mechanisms in post-COVID-19 pathogene-
sis. The aim of this study was to measure the main
parameters of oxidative stress in post-COVID-19
patients and to evaluate their possible association
with post-COVID-19 symptoms. Serum samples were
collected from a total of 60 patients with post-
COVID-19 symptoms. Oxidative stress status was
determined in each sample by spectrophotometric
measurements: total oxidative status (TOS), total
antioxidant status (TAS), superoxide dismutase activ-
ity (SOD), advanced oxidation protein product
(AOPP) concentration, total sulfhydryl groups (SHG),
prooxidant-antioxidant balance (PAB), ischemic mod-
ified albumin (IMA), paraoxonase activity of paraox-
onase 1 (PON1), and malondialdehyde concentra-
tion (MDA). Statistical analysis showed that PAB,
TOS, MDA, IMA and AOPP were significantly higher
in post-COVID-19 patients (p<0.01), while SHG
(p<0.05), TAS, SOD and PON1 (p<0.01) were sig-
nificantly lower than in the control group. Our study
shows that patients with post-COVID-19 syndrome
have increased oxidative stress and decreased antiox-
idant defences.Međunarodni XXIII srpski kongres medicinske biohemije i laboratorijske medicine, 16-18. septembar 2024. godine, Posterske sekcij
The construction and interpretation of error grid for quantitative diagnostic assays
No full textSvojstva kvantitativnih dijagnostičkih testova (KDT)
mogu se opisati analitičkom ili kliničkom tačnošću.
Analitička tačnost se procenjuje upore|ivanjem dva
merenja u istim uzorcima, od kojih se jedno izvodi
pomoću KDT, a drugo referentnom metodom.
Tipičan statistički metod za procenu analitičke
tačnosti je linearna regresija, a tipične metričke
veličine analitičke tačnosti su prosečna razlika između
izmerenih vrednosti referentnom metodom i KDT
(MARD engl. – mean absolute relative difference) i
stopa slaganja. Međutim, analitička tačnost ne uka-
zuje na kliničke posledice koje nastaju zbog neslaganje u rezultatima između dve metode. Preporučeni
postupak za procenu kliničke tačnosti je analiza
mrnje grešaka. Ova analiza ukazuje na potencijalne
terapijske greške uzrokovane pogrešnim rezultatima
KDT. Nemaju sve greške merenja isti klinički uticaj.
Male greške će verovatno prouzrokovati manju štetu
po pacijenta u odnosu na velike greške, a šteta uzro-
kovana malim greškama je i manje ozbiljna. Analiza
grešaka pomuću ovog postupka može se koristiti za
svrstavanje grešaka merenja u zone niskog, srednjeg
i visokog kliničkog rizika. Pomoću ove analize procenjuje se procenat grešaka u svakoj zoni rizika. Glavni
korisnici mreže grešaka su proizvođači KDT i regulatorna tela. Zone mreže grešaka su prvenstveno definisane za «point of care« (PoC) za samokontrolu
glukoze u krvi. Za regulatornu upotrebu preporučena
su tri tipa mreže grešaka: Clarke Error Grid, Parkes
Error Grid i Surveillance Error Grid. Sve su zasnovane
na principu konsenzusa, a razlikuju se u odnosu na
definisane zone rizika. ISO 15197 (In vitro diagnostic
test systems — Requirements for blood glucose mon-
itoring for self-testing in managing diabetes mellitus)
navodi da 99% pojedina~nih vrednosti glukoze
izmerenih PoC uređajem kod pacijenata sa dijabetesom tip 1, treba da budu u zonama A i B (zonama
niskog i umerenog rizika za pogrešnu odluku o terapiji). Mreže grešaka su takođe važne za odluke o
nabavci opreme i medicinskih sredstava; nova meto-
da mora imati analitičku i kliničku tačnost sličnu
prethodnoj. Takođe, ova procedura se može koristiti
za procenu učinka KDT tokom postmarketinškog
nadzora. Rezultati mreže grešaka mogu se koristiti za
dobijanje uvida u kliničke performanse KDT, posebno
za praćenje glukoze. Međutim, informacije iz mreže
grešaka ne bi trebalo da zamene analitičku tačnost,
ali mogu pružiti dodatnu vrednost novom KDT.The performance of quantitative diagnostic assays
(QDA) can be described by analytical or clinical accu-
racy. Analytical accuracy is assessed by comparing
two measurements in the same data sets, one per-
formed with the QDA and the other with a reference
method. A typical statistical method for assessing
analytical accuracy is linear regression, and typical
metrics of analytical accuracy are the mean absolute
relative difference (MARD) and the agreement rate.
However, analytical accuracy cannot show the clinical
consequences of different treatment decisions due to
differences in method results. The recommended
tool for assessing clinical accuracy is the error grid
analysis. It shows the potential therapeutic errors
caused by incorrect treatment decisions due to erro-
neous QDA results. Not all measurement errors have
the same clinical impact. Small errors are likely to
cause less harm than large ones, and the harm
caused by small ones is less serious. Error grids can
be used to categorise measurement errors into zones
with low, moderate or high risk for wrong therapeutic
decisions. Error grids also indicate the percentage of
data in each risk zone. The main users of an error
grid are QDA manufacturers and regulatory bodies.
The error grid zones are primarily defined for point-
of-care (PoC) medical devices for blood glucose self-
monitoring. Three error grids, based on a consensus
approach with different zone boundaries, are recom-
mended for regulatory use: Clarke Error Grid, Parkes
Error Grid and Surveillance Error Grid. ISO 15197 (In
vitro diagnostic test systems — Requirements for
blood glucose monitoring for self-testing in manag-
ing diabetes mellitus) specifies that 99% of individual
measured glucose values measured in type 1 diabet-
ics patients should fall into zones A and B (zones of
low and moderate risk for the wrong therapy deci-
sion). Error grids are also important for purchasing
decisions; a new method must have analytical and
clinical accuracy similar to the previous one. They
can also be used to evaluate the performance of
QDA during post-market surveillance. The results of
the error grid can be used to get an overview of the
clinical performance of QDA, especially in glucose
monitoring. However, the information from the error
grid should not replace analytical accuracy but can
provide added value to the new QDA.Međunarodni XXIII srpski kongres medicinske biohemije i laboratorijske medicine,16–18. septembar 2024. godine, Plenarne sekcij
Phenylamides in food: UHPLC/QTOF/MS identification and structural elucidation
No full textUltra-high-performance liquid chromatography coupled with quadrupole time-of-flight mass
spectrometry (UHPLC/Q-ToF/MS) is a powerful technique that has been used for target and
untarget analysis of various bioactive compounds in food and plants. The Q-ToF detector
(quadrupole and ToF mass analysers) have unique characteristics (high resolution, fast acquisition,
wide mass range, and high ion mobility), which enables its application for identification and
structure elucidation of biocompounds. In addition to phenolic compounds, various phenylamides
are being increasingly analyzed recently, due to their health benefits such as neuroprotective (agents
for treatment of Alzheimer's and Parkinson's diseases), anti-aging, anti-cancer, antioxidative, anti-
inflammatory and anti- microbial effects. Phenylamides exist as polyamine (putrescine, spermidine
and spermine) or arylmonoamine (tyramine, tryptamine, dopamine, serotonin, octopamine,
agmatin) conjugates connected with various phenolic acid moieties, and some of them present very
important metabolites of plants and pollen grains. This review is primarily focused on the
application of UHPLC/Q-ToF/MS technique for identification of various phenolic acid-polyamine
derivatives, as well as their recently confirmed glycosylated forms. These phenylamide derivatives
have characteristic MS fragmentation in positive ionisation mode, which can be used for prediction
of their structures. Typical MS fragments can indicate the type of polyamine core, phenolic acid
moieties (coumaroyl, caffeoyl, dihydrocaffeoyl, feruloyl, sinapoyl) and their positions on the
polyamine core, as well as degree/position of glycosylation. Identification of phenylamides is
additionally explained on several representative examples (derivatives) detected in tomato leaves,
pollen samples and red goji berry. The use of this technique in the analysis of food enriched with
phenylamides, as well as their behaviour during in vitro digestion, is also considered. Finally, this
review points out advantages and limitations of UHPLC/Q-ToF/MS technique for identification of
phenylamides with the tendency to facilitate the future characterization of these derivatives
Phenotyping of aging Sprague-Dawley rats: Exploring the relationship between social behavior and locomotor activity
No full textAims: The aging process inevitably influences social behavior and cognition. However, a proportion of the population may resist these changes due to superaging associated with increased movement speed. Therefore, we aimed to phenotype aging animals based on their activity and determine the relationship between locomotor function and social behavior in aging rats
Methods: In 3- and 14-month-old Sprague-Dawley rats, social interaction, memory and locomotion were characterized using resident-intruder test (RIT), social recognition test (SRT) and open-field test, respectively. Animal phenotyping was based on activity level in OF using -3.5 standard deviation of the percentage of time spent in activity for the control as treshold. Behavioral parameters were analyzed using one-way ANOVA with or without repeated measures and Pearson correlation.
Results: Social exploration and total interaction were unaffected in aging animals, while social play was decreased compared to controls in RIT. Aging animals discriminated new vs old conspecific in the first 3min, but not after 10min vs. control in SRT. Controls showed the opposite pattern, with tendency to spend more time with new vs. old conspecific after 10min. Total interaction was reduced in aging animals vs. controls in SRT. Phenotyping revealed two distinct populations of aging animals – both with reduced activity vs. control, but one above and other below the threshold value. No correlation was found between behavioral parameters.
Conclusions: Social interaction and memory assesments were time-dependent in 14-month-old animals possibly due to the attention deficits, and independent of motor decline, suggesting the need for more comprehensive behavioral characterization and interpretation
Changes in some phenolic compounds after thermovinification in cabernet sauvignon wine
No full textTo determine the effects of higher temperature on the extraction of some phenolic
compounds during maceration, two different vinification techniques were used:
thermovinification at 60C and 80C, as well as classic vinification (pigeage).
The study focused on four different phenolic compounds (catechin, epicatechin,
quercetin and trans-resveratrol). Based on these experiments, it can be concluded
that thermovinification improves the phenolic content, at least for the compounds
studied
Fruit products as inhibitors of α-glucosidase
No full textOne of the many products obtained after fruit processing is a wine. Black chokeberry
wines were produced by innovative microvinification procedure. In this procedure,
wines were produced in the absence or presence of sugar and/or enzymatic
preparation glycosidase (EPG). Their chemical and biological activities were
investigated. Selected phenolic compounds were identified and quantified using
UPLC/MS-MS analysis. Inhibitory activity of black chokeberry wine samples
against α-glucosidase was also investigated. It was shown higher content of phenolic
compounds and better inhibitory activity against α-glucosidase for wines made with
addition of sugar and EPG. In summary, phenolic profile and biological activity of
black chokeberry wine depended from microvinification procedure which was used
in the production