rss_2.0European Pharmaceutical Journal FeedSciendo RSS Feed for European Pharmaceutical Journal Pharmaceutical Journal 's Cover of medicines in a psychiatric hospital in Cyprus<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Background</title><p>The incidence of drug shortages has surged in recent years and it poses a major threat to public health worldwide. It can also downgrade the quality of care provided to patients. Data concerning shortages pertinent to mental health care are scarce, while treatment continuity is vital to avert disease recurrence and deterioration of patients’ mental health.</p></sec> <sec><title style='display:none'>Objective</title><p>The scope of this study is to elucidate the attitudes and perceptions of mental health professionals regarding drug shortages in Cyprus in a tertiary health institute, through a specially designed questionnaire.</p></sec> <sec><title style='display:none'>Results</title><p>The most frequently reported effects of psychiatric drug shortages were the impaired efficacy of the alternative therapeutic regimen, re-admission of patients, delays in care provision and increased frequency of adverse events. Concerning the loss of working hours in managing drug shortages, the majority responded that they dedicate 1 to 5 working hours to this per week. Informing the patient about alternative medication and the ongoing shortages were the first strategies to minimise the effects of shortages, as attested by 74% and 72% of responders, respectively. The proposed solutions for drug shortages included thorough investigation of the root causes, the elaboration of an e-based database, drawing up a national annual report and assuming legal responsibility of pharmaceutical companies. Drug shortages constitute an important burden in the field of mental health care in Cyprus. Given the serious impact of the problem and the externalities of mental health disorders, appropriate measures must be swiftly taken to ensure timely and effective administration of the appropriate therapeutic regimen.</p></sec> </abstract>ARTICLE2022-05-13T00:00:00.000+00:00The Evaluation of Cardiovascular Risk in Diabetic Patients<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>AIM</title> <p>The aim of the study was to evaluate cardiovascular risk in patients with diabetes mellitus type 2 according to gender.</p> </sec> <sec><title style='display:none'>METHODS</title> <p>The monitoring was designed as a retrospective analysis of data obtained from the documentation of the diabetic outpatients treated with the dipeptidyl peptidase-4 inhibitors (DPP4is) or sodium–glucose co-transporter-2 (SGLT2). Cardiovascular risk was assessed according to UKPDS risk engine.</p> </sec> <sec><title style='display:none'>RESULTS</title> <p>The levels of HbA1c decreased throughout the whole study. Sixty per cent of patients achieved an HbA1c level &lt;8% after 18 months. Both men and women had similar glycaemic compensation. Men had a significantly higher risk of fatal coronary heart disease (CHD) (<italic>p</italic> &lt; 0.001), stroke (<italic>p</italic> &lt; 0.01) and fatal stroke (<italic>p</italic> &lt; 0.01) compared to women. We found the risk of fatal CHD to be 38-fold higher in men compared to women (<italic>p</italic> &lt; 0.01).</p> </sec> <sec><title style='display:none'>CONCLUSION</title> <p>Potential cardiovascular effects of antidiabetic treatment should be clearly defined with possible different effects according to gender. We found a much higher risk in men than women, even when their glycaemic compensation was comparable.</p> </sec> </abstract>ARTICLE2022-04-04T00:00:00.000+00:00Cultural Adaptation and Validation of the EORTC QLQ-BR45 to Assess Health-Related Quality of Life of Breast Cancer Patients<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Background</title> <p>The European Organization for Research and Treatment of Cancer (EORTC) QLQ-BR23 is considered a premier module for breast cancer patients that is utilised synchronously with the core questionnaire. However, new and scalable treatments on breast cancer patients’ quality of life (QoL) need a more accurate and comprehensive tool to be assessed. Therefore, the EORTC introduced the newly updated module EORTC QLQ-BR45. Hence, the current study aims to perform cultural adaptation, pilot testing and assessment of the psychometric properties of the Egyptian Arabic translation of the EORTC QLQ-BR45 module on Egyptian breast cancer patients.</p> </sec> <sec><title style='display:none'>Patients and Methods</title> <p>First, a review of the existing Arabic translation and the modified preliminary translation was sent to a professional proofreader. Then, comprehensibility of the Egyptian Arabic translation was pilot tested on a sample of 13 breast cancer patients. Afterwards, 74 patients with proven locally advanced breast cancer receiving neoadjuvant chemotherapy at Beni-Suef University Hospital, Beni-Suef, Egypt were interviewed. A second interview was conducted post-surgery for patients receiving target therapy, endocrine therapy or radiotherapy. The psychometric properties of the EORTC QLQ-BR45 were assessed in terms of reliability, convergent and divergent validity.</p> </sec> <sec><title style='display:none'>Results</title> <p>Adequate internal consistency reliability (Cronbach’s α coefficients &gt;0.7) was demonstrated for the questionnaire, except for body image scale (α = 0.51) and systemic therapy side effects scale (α = 0.63). Multi-trait scaling analysis exhibited acceptable convergent and divergent validity, and scaling success was observed for all questionnaire items.</p> </sec> <sec><title style='display:none'>Conclusion</title> <p>The Egyptian Arabic version of the EORTC QLQ-BR45 module is valid and adequately reliable. These results support using the EORTC QLQ-BR45 in future breast cancer clinical trials.</p> </sec> </abstract>ARTICLE2022-04-04T00:00:00.000+00:00Development and Validation of Bioanalytical Method for Determination of Nebivolol and Valsartan in Human Plasma by Using RP-HPLC<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Aim</title> <p>Nebivolol and valsartan are used in the treatment of hypertension. So, this study was conducted for the purpose of determining bioavailability/bioequivalence of nebivolol and valsartan in human plasma.</p> </sec> <sec><title style='display:none'>Materials and Methods</title> <p>The chromatographic separation was performed on Symmetry C18 (150 × 4.6 mm, 5 μm) column using 0.01 N potassium dihydrogen phosphate (pH 3.0):acetonitrile (60:40) as the mobile phase at a flow rate of 1.0 mL/min and a detector wavelength of 280 nm. The retention times of nebivolol and valsartan in plasma were found to be 3.1 and 4.3 min, respectively.</p> </sec> <sec><title style='display:none'>Results</title> <p>The method was validated statistically and by recovery studies. The linearity concentration was acceptable in the range of 0.5–10 ng/mL for nebivolol and 400–8000 ng/mL for valsartan. The lower limits of quantification were 0.5 ng/mL for nebivolol and 400 ng/mL for valsartan, which reached the levels of both drugs possibly found in human plasma. Per cent recoveries were obtained as 97.78% and 98.11% for nebivolol and valsartan, respectively.</p> </sec> <sec><title style='display:none'>Conclusion</title> <p>The proposed method is simple, rapid, accurate, precise and gives us knowledge about the pharmacokinetics and therapeutic drug monitoring in clinical laboratories.</p> </sec> </abstract>ARTICLE2022-03-12T00:00:00.000+00:00Effects of Demographic Characteristics and Consumer Behavior in the selection of Retail Pharmacies and Over-the-Counter Medicine<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Aim</title> <p>The study aimed to provide new insights into consumer behaviour by identifying the key demographic factors that influence the choice of pharmacy and over-the-counter (OTC) medicine.</p> </sec> <sec><title style='display:none'>Materials and Methods</title> <p>A cross-sectional study was conducted in an urban area (Thessaloniki, Greece), surveying a convenience sample of 314 consumers with a structured questionnaire. Data analysis was conducted using the chi-square test, one-way analyses of variance (ANOVAs) and Spearman's rho correlation coefficient.</p> </sec> <sec><title style='display:none'>Results</title> <p>Respondents with a lower educational level and retired consumers tended to make their purchases in a single pharmacy (<italic>p</italic> &lt; 0.001). Older participants were more likely to consider the pharmacy staff and additional services to be important factors (<italic>p</italic> &lt; 0.01). Students were the only group to prefer a formal relationship with the pharmacy staff (<italic>p</italic> &lt; 0.001). Participants with a lower educational level tended to know exactly what they would buy (<italic>p</italic> &lt; 0.05), whereas women made more unscheduled purchases of OTCs (<italic>p</italic> &lt; 0.05). Respondents with a higher income assigned more importance to the product's country of origin (<italic>p</italic> &lt; 0.05) and manufacturing company (<italic>p</italic> &lt; 0.01) and less importance to the pharmacist's opinion than those of a lower income (<italic>p</italic> &lt; 0.05).</p> </sec> <sec><title style='display:none'>Conclusions</title> <p>The educational level, occupation and age of consumers have a marked effect in their selection of pharmacy, and along with gender and personal income, in their choice of OTC medicine. Our findings yield implications for the management of community pharmacies.</p> </sec> </abstract>ARTICLE2022-03-01T00:00:00.000+00:00Amelioration of the Abnormalities Associated with Metabolic Syndrome by L-Norvaline in Hyperlipidemic Diabetic Rats<abstract> <title style='display:none'>Abstract</title> <p>The present study was designed to assess the treatment effect of arginase inhibitor, L-Norvaline in abnormalities associated with high fat diet (HFD) and fructose-induced metabolic syndrome. The HFD and fructose was fed to the rats for a period of 45 days. Animals having body weight of 350 g and fasting blood sugar level of more than 250 mg/dl were considered as hyperlipidemic diabetic rats (HDR) and selected for the study. The HDR were divided into three groups having six animals each. The HDR received L–Norvaline (10 mg/kg/day, i.p.) and standard drug, gemfibrozil (60 mg/kg/day, p.o.), for a period of 30 days. Various hormonal, biochemical and tissue parameters were evaluated at the end of the study. Both treatments significantly decreased body weight, BMI, fasting blood sugar and insulin level and improved insulin resistance in HDR as compared to the toxicant control group. A significant improvement was observed in the lipid profile, levels of nitrate, leptin, C-reactive protein and adiponectin in HDR. L-Norvaline also caused slight decrease in the malondialdehyde level, though, no prominent effect was observed on the level of superoxide dismutase and reduced glutathione in the pancreas of HDR, as compared to the toxicant control group. L-Norvaline treatment also improved the histo-architecture of pancreatic cells. Results of the present study concludes that L-Norvaline caused significant alleviation of the abnormalities of MetS indicating that it can be used as potential treatment strategy for managing the symptoms of metabolic syndrome.</p> </abstract>ARTICLE2022-02-09T00:00:00.000+00:00Non-Absorbable Oral Gentamicin Sulphate: Biopharmaceutical and Dosage Form Evaluation<abstract> <title style='display:none'>Abstract</title> <p>Gentamicin sulphate is an antibiotic belonging to the aminoglycosides and to class III of the Biopharmaceutical Classification System (BCS). Gentamicin sulphate is highly water soluble, but has very low intestinal permeability. The wide use is because of its broad spectrum of activity. In the current study, the suitability of administering gentamicin sulphate orally for local action against susceptible gastrointestinal tract (GIT) bacteria was investigated. The possibility of the drug escaping into the systemic circulation even in the presence of some permeation enhancers was ascertained. Representatives of potential GIT bacteria pathogens were evaluated for their susceptibility to the drug at concentrations obtainable in the GIT using standard microbiological methods. Dose levels that will inhibit these potential bacteria pathogens were also established, as well as the frequency of their administration. Different batches of oral capsules of 250 mg gentamicin sulphate were formulated and their release profiles ascertained using standard methods. The results showed that the selected representatives of the GIT potential pathogenic bacteria were all susceptible to gentamicin sulphate. The drug at its plausible dosage levels of 14.28 mg/kg (1,000 mg/70 kg), 10.71 mg/kg (750 mg/70 kg) and 7.14 mg/kg (500 mg/70 kg) did not cross the mucosal barrier into the systemic circulation even in the presence of some permeation enhancers. The drug's frequency of administration were found to be on 8-hourly bases. Gentamicin sulphate (250 mg) granules formulated with polyethylene glycol (PEG 4000) as granulating aid were quick drying because the granules were not hygroscopic. The formulated gentamicin sulphate capsule batch released enough concentration of the drug that inhibits the test organism within 2 min of dissolution. The above stated doses are acceptable in the dosage form design; it is possible to formulate non-absorbable oral gentamicin sulphate dosage form for local activity in the GIT using existing conventional solid dosage formulating equipment.</p> </abstract>ARTICLE2021-04-02T00:00:00.000+00:00The Effect of Different Extracts of Beetroots as Antioxidant and Anti-Anaemia On Phenylhydrazine-Induced Rats<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Aim</title><p>evaluate antioxidant and anti-anaemia activity of dichloromethane, hydroethanolic, and alkaloids-free hydroethanolic extracts of beetroot (<italic>Beta vulgaris</italic> (L.) subsp. <italic>vulgaris</italic>) on phenylhydrazine-induced rats.</p></sec> <sec><title style='display:none'>Methods</title><p>Male rats were divided into five groups: normal control group, negative control group, dichloromethane extract group, hydroethanolic extract group, and alkaloids-free hydroethanolic extract group. All groups were induced with phenylhydrazine (30 mg.Kg<sup>−1</sup> BW) for three days, except for the normal control group. After induction, each treatment group received each extract (200 mg.Kg<sup>−1</sup> BW) for 21 days. The haematology parameters (haemoglobin levels, the number of erythrocytes, and haematocrit levels) were measured using Haematology Analyzer, and the antioxidant activity was measured through MDA level parameters in rats. Data were analysed using one-way ANOVA and then continued with the Tukey test.</p></sec> <sec><title style='display:none'>Results</title><p>The results showed that the hydroethanolic extract of beetroot increased the percentage of erythrocytes (33.5%), haemoglobin (25%), and haematocrit (24.4%) to the negative control group, which was comparable to the normal control group (p &gt; 0.05). In addition, the best antioxidant activity was shown in the hydroethanolic extract of beetroot, which is comparable to the normal group (p &gt; 0.05).</p></sec> <sec><title style='display:none'>Conclusion</title><p>The beetroot hydroethanolic crude extract could be potentially produced in a natural pharmaceutical product as a beneficial resource within anti-anaemia and antioxidant activities.</p></sec> </abstract>ARTICLE2021-04-02T00:00:00.000+00:00Retraction Note of qualitative and quantitative content of amino acids in pumpkin seeds for further standardization of the herbal drug<abstract><title style='display:none'>Abstract</title><sec><title style='display:none'>Aim</title><p>Literary sources on qualitative composition, quantitative content of biologically active substances, and standardization methods of pumpkin seeds have been studied. It has been established that, along with Δ7-sterols, whose action is associated with treatment of the prostate gland, pumpkin seeds contain amino acids, cucurbitin in particular, which are responsible for their antihelminthic effect. The aim is to study the qualitative and quantitative content of amino acids in domestic samples of pumpkin seeds in order to clarify the possibility of pumpkin seed standardization for this class of biologically active substances.</p></sec><sec><title style='display:none'>Methods</title><p>The investigation of the possibility of amino acids’ identification in the herbal drug by the thin-layer chromatography (TLC) method was carried out on silica gel 60 F<sub>254</sub> plates, Merck and Silica gel 60, Merck, on aluminum and glass supports in a mixture of the following solvents: butanol–acetone–acetic acid–water (35:35:10:20). The conclusions have been made based on the presence of characteristic zones of amino acids in the chromatograms after the treatment with ninhydrin solution.</p><p>Quantitative determination of amino acids in the herbal drug was carried out by absorption spectrometry using HP spectrophotometer HP-8453 UV-VIS, Hewlett Packard (USA).</p></sec><sec><title style='display:none'>Results</title><p>The chromatographic profile of the amino acid fraction of domestic samples of pumpkin seeds was studied using a TLC technique. In the chromatograms of test solutions from all samples, the zones were detected at the level of histidine, aspartic acid, glutamic acid, glycine, and leucine zones, as well as a zone with color (olive) that differs from the other zones of amino acids and which is possibly a zone of cucurbitin.</p><p>On the basis of the results of qualitative research, the quantitative content of the sum of amino acids according to a UV method developed has been determined, which including purification from the fatty oil, further extraction with an aqueous alcohol solution, selection of aliquots for the reaction with ninhydrin solution, and subsequent determination of the absorbance of the test solution and the solution of glutamic acid at a wavelength of 400 nm.</p><p>It has been established that the content of the sum of amino acids expressed as glutamic acid in domestic samples is about 2%.</p></sec><sec><title style='display:none'>Conclusions</title><p>The research of the possibility of pumpkin seed standardization by the content of amino acids was carried out. The chromatographic profile of the amino acid fraction of domestic samples of pumpkin seeds was studied using a TLC method developed. The quantitative content of the amino acids sum by the absorption spectrophotometry method was investigated. The techniques developed will be recommended for inclusion in the draft of national monograph “Pumpkin seeds.”</p></sec></abstract>ARTICLE2020-11-18T00:00:00.000+00:00Chitosan Hydrogel Improves Bioavailability of Megosin<abstract><title style='display:none'>Abstract</title><sec><title style='display:none'>Background</title><p>The aim of this study was to obtain chitosan hydrogels containing megosin, an antiviral medicinal substance, to prolong its bioavailability. Megosin as an immunomodulating agent possesses at least twice higher virostatic and virucidal activities than gossypol, the megosin precursor, and other imine derivatives of gossypol.</p></sec><sec><title style='display:none'>Materials and Methods</title><p>Chitosan, used in this paper, was obtained by deacetylation of chitin; megosin was obtained on the bases of gossypol. Different concentrations of sodium tripolyphosphate (STPP) were used as the cross-linking agent. The release of megosin from hydrogel samples into blood was conducted on five white rats in four groups.</p></sec><sec><title style='display:none'>Results</title><p>Infrared spectral data demonstrated cross-linkage that the band responsible for NH bending of the uncross-linked chitosan reduced its intensity and moved to a lower wavelength, 1636 cm<sup>−1</sup>. It has been proven that megosin contained in gels does not penetrate into the blood and organs after vaginal administration. Release kinetics of megosin from chitosan hydrogels revealed that within 7 h, up to 52% of megosin is allowed into acidic solution (pH 4.5).</p></sec><sec><title style='display:none'>Conclusion</title><p>This study demonstrates the possibility to prolong bioavailability of megosin for at least 7 h, during which time it is not released into blood. The obtained results show the possibility to use the gel composition to treat vaginal herpes.</p></sec></abstract>ARTICLE2020-11-18T00:00:00.000+00:00Comparative morphological studies of raw parts of the most common species of in Ukraine<abstract><title style='display:none'>Abstract</title><p>This study presents the results of our comparative evaluation of diagnostic morphological characteristics of raw material from 11 species of genus <italic>Thymus</italic> L. of medicinal and raw material importance occurring in Ukraine. The following taxa were evaluated: <italic>T. serpyllum</italic> L., <italic>T. odoratissimus</italic> Mill. (<italic>T. glabrescens</italic> Willd.), <italic>T. borysthenicus</italic> Klokov &amp; Des.-Shost., <italic>T. pallasianus</italic> Heinr. Braun, <italic>T. moldavicus</italic> Klokov &amp; Des.-Shost., <italic>T. calcareus</italic> Klokov &amp; Des.-Shost., <italic>T. alpestris</italic> Tausch ex A. Kern., <italic>T. × dimorphus</italic> Klokov &amp; Des.-Shost., <italic>T. pannonicus</italic> All. s.l. (including <italic>T. marschallianus</italic> Willd.), <italic>T. pulegioides</italic> L. and <italic>T. roegneri</italic> K. Koch (<italic>T. alternans</italic> Klokov). Among wild species of thyme, only raw material of <italic>Thymus serpyllum</italic> is officially allowed for use with the purpose for production of pharmaceuticals and medicines. A comparison of the main characteristics is particularly important in view of the fact that raw material is represented by parts of plants (stems, leaves and flowers), which makes any whole comparison of species hardly possible. This study has revealed that stem pubescence, calyx structure, configuration/arrangement and type of leaf venation can provide valuable information for diagnostics of raw material of <italic>Thymus</italic> species. The results exhibited that according to characters of stem pubescence, calyx structure, shape and size of leaves the most similar are raw material samples of <italic>T. serpyllum</italic> and <italic>T. moldavicus</italic>. However, these species are rather well separated geographically, so the possibility of mixing of their raw material is negligible. Other species have significant morphological differences in certain characteristics by which they can be diagnosed in the raw material.</p></abstract>ARTICLE2020-11-18T00:00:00.000+00:00Therapeutic Drug Monitoring of Venlafaxine and Impact of Age, Gender, BMI, and Diagnosis<abstract><title style='display:none'>Abstract</title><p>Depression is a common mental disorder affecting more than 264 million people in the world and 5.1% of the Slovak population. Although various antidepressant approaches have been used; still, about 40% of patients do not respond to a first-choice drug administration and one third of patients do not achieve total remission. Therapeutic drug monitoring (TDM) is a method used for quantification and interpreting the drug concentrations in plasma in order to optimize the pharmacotherapy. The aim of this study was to measure the plasma concentrations of venlafaxine, the fourth most prescribed antidepressant in Slovakia, as well as its active metabolite and interpret them with the relevant patients’ characteristics.</p><p>The study was of retrospective nature and 28 adult patients in total were included. The concentrations of venlafaxine and its active metabolite O-desmethylvenlafaxine (ODV) in plasma were quantified using the validated UHPLC-MS/MS method. The effects of potential influencing factors were evaluated by a multivariate linear regression model.</p><p>Only 39% of patients reached the venlafaxine active moiety concentrations within the recommended therapeutic range. Plasma concentrations were dependent on age, gender, and duration of the therapy. Venlafaxine metabolism expressed as a metaboliteto-parent concentrations ratio was influenced by a combination of age, gender, and body mass index (BMI). We did not observe any significant difference in plasma concentrations between the patients with a single and recurrent diagnosis of depression. Combining variables made an additive effect on plasma concentrations, for example, active moiety plasma concentrations were higher in older women. In contrast, drug metabolism was higher in older men and men with lower BMI. TDM of venlafaxine is recommended in clinical practice, especially in the elderly when beginning the pharmacotherapy.</p></abstract>ARTICLE2020-11-18T00:00:00.000+00:00Concentration-dependent effect of silymarin on concanavalin A-stimulated mouse spleen cells<abstract><title style='display:none'>Abstract</title><sec><title style='display:none'>Aims</title><p>Silymarin (SIL), a mixture of phenolic compounds, has a pleiotropic mode of action on various cell types, including immune cells. In this study, we investigated the concentration-dependent effect of SIL on proliferation of concanavalin A (CoA)-stimulated mouse spleen T lymphocytes, their viability, and secretion of IFN-g and IL-4 cytokines <italic>ex vivo</italic> in relation to gene expressions of transcription factors nuclear factor kappa B and Foxp3. In addition, metabolic activity of T cells was determined as changes in the mitochondrial membrane potential and apoptosis.</p></sec><sec><title style='display:none'>Material/Methods</title><p>Isolated splenocytes were stimulated with lectin CoA and treated with SIL atthe concentrations of 5, 10, 20, and 40 μg/ml for 70 h and unstimulated cells served as the control. Cultures of splenocytes were evaluated for proliferation index following BrdU incorporation and viability of cells after trypan blue staining. Gene expressions of transcription factors and cytokines were assessed using real-time PCR, whereas ELISA test was applied to measure cytokine secretion. Mitochondrial membrane potential and apoptosis were determined by flow cytometry.</p></sec><sec><title style='display:none'>Results</title><p>We demonstrated that CoA-activated mouse spleen T lymphocytes show different susceptibilities to low (£10 μg/ml) and higher (20 and 40 μg/ml) SIL concentrations. Low concentrations resulted in increased proliferation, cytokine secretion, and mitochondrial membrane potential and reduced transition of cells to apoptosis. High concentration of SIL had the opposite effect without exerting significant cytotoxicity and upregulated genes for cytokines and transcription factors on mRNA level. It is possible that individual subpopulations of T cells induced by CoA were differentially affected by the various SIL concentrations and the dose of 40 μg/ml had the profound suppressive effect. This correlated with the highest expression of Foxp3 factor, indicating that this dose stimulated preferential differentiation to Tregs lymphocytes.</p></sec><sec><title style='display:none'>Conclusions</title><p>Treatment with suitable doses of SIL can provide potential benefits in the modulation of host immune functions in various diseases.</p></sec></abstract>ARTICLE2020-11-18T00:00:00.000+00:00Possibilities of microemulsion application in rectal administration of indomethacin<abstract> <title style='display:none'>Abstract</title> <p>Rectal administration is a suitable route of administration for drugs that are either very irritating to the intestine (e.g., indomethacin) or are more effective when the first-pass effect in the liver is circumvented. Microemulsions are a tool for the improvement of penetration of sparingly soluble drugs. They are mainly used in topical and transdermal drug delivery. However, they find application also in other routes of administration, mainly due to their ability to solubilize sparingly soluble drugs. The selection of a suppository base depends on the physical properties of the drug. The study focused on evaluating the effect of the microemulsion as the solubilizer of sparingly soluble indomethacin in hydrophilic and lipophilic suppository bases compared with Polysorbate 80 as the excipient contained in the microemulsion. The reference suppositories were prepared by the traditional moulding technique from <italic>Adeps solidus</italic> or Macrogol suppository base without the previous drug solubilization. The microemulsion-based suppositories were prepared after the initial solubilization of the drug in the microemulsion or Polysorbate 80, followed by the addition of suppository base to maintain the same drug/solubilizer ratio. The suppositories were tested for softening time, hardness, and uniformity of mass. The dissolution test was performed using the dialysis tubing method in the basket apparatus. The amount of indomethacin released into the dissolution medium was determined spectrophotometrically at 320 nm. The results indicate that solubilization of indomethacin in the microemulsion had a positive effect on <italic>in vitro</italic> drug release but not as significant as in the case of Polysorbate 80 used alone. The enhancement ratio for Polysorbate 80 in Adeps suppositories was 2.9, for the microemulsion in Adeps suppositories was 1.1, and for Polysorbate 80 in Macrogol suppositories was 7.4 after 3 hours. The test of uniformity of mass had shown that all suppositories (reference, solubilizer-containing) are within the permitted limits. The softening time was reduced by adding the solubilizer to each type of suppository base.</p> </abstract>ARTICLE2021-09-02T00:00:00.000+00:00Synthesis and Correlation of Aggregation and Antimicrobial Properties of Homochiral Quaternary Ammonium Bromides Derived from Camphoric Acid<abstract> <title style='display:none'>Abstract</title> <p>A group of homochiral quaternary ammonium salts bearing hydrophobic camphoric acid-derived moiety was synthesized and characterized. The aggregation properties of the prepared compounds were evaluated by surface tension measurements, and the critical micelle concentration (CMC) was calculated. The novel quaternary ammonium bromides were tested as antimicrobial and antifungal agents, and their minimal inhibitory concentration (MIC) was evaluated and compared to clinically used benzalkonium bromide (BAB). Correlation of MIC with CMC reveals that monomers of prepared cationic surfactants, instead of micelles, are primarily responsible for antimicrobial activity.</p> </abstract>ARTICLE2021-04-23T00:00:00.000+00:00Rapid and simple CZE-UV method for quality control of B1 and B6 vitamins in drugs and dietary supplements<abstract> <title style='display:none'>Abstract</title> <p>The application of hydrodynamically closed capillary zone electrophoresis combined with convenient ultraviolet (UV) detection allows fast, simple, environmentally friendly and cost-effective analysis of ions or ionisable molecules. This technique has been used to determine two selected B vitamins (thiamine, pyridoxine) in various drug formulations. The developed method was characterised by excellent validation parameters, such as linearity, precision, accuracy, limit of detection and limit of quantification. The total time of analysis was lower than 13.5 min. The results indicate that the method is suitable for implementation in routine quality control of selected B vitamins in pharmaceutical and food samples.</p> </abstract>ARTICLE2021-07-25T00:00:00.000+00:00Nephroprotective Effect of Coenzyme Q10 alone and in Combination with N-acetylcysteine in Diabetic Nephropathy<abstract> <title style='display:none'>Abstract</title> <sec><title style='display:none'>Aim</title> <p>Oxidative stress due to chronic hyperglycaemia is a key factor in the development and progression of various microvascular complications including diabetic nephropathy (DN) and associated renal injury. Treatment with antioxidants is one of the strategies to protect the kidney from oxidative tissue damage to improve renal physiology during DN. The investigation, therefore, was designed to assess the nephroprotective effect of coenzyme Q10 (CoQ10) and N-acetylcysteine (NAC), either alone or in combination in streptozotocin (STZ)-nicotinamide (NAD) induced diabetic nephropathy (DN) in rats.</p> </sec> <sec><title style='display:none'>Methods</title> <p>T2DM induced by STZ (55 mg/kg, i.p.)-NAD (110 mg/kg, i.p.) in Sprague-Dawley rats (220–250 g) was confirmed by the elevated blood glucose level and glycated haemoglobin. DN was assessed by renal function tests. The diabetic rats were treated with CoQ10 (10 mg/kg, p.o.) and/or NAC (300 mg/kg, p.o.) for 8 weeks after confirmation of DN. Oxidative tissue damage due to STZ-NAD was estimated by malondialdehyde (MDA), superoxide dismutase (SOD) and catalase (CAT), reduced glutathione (GSH), myeloperoxidase (MPO) and nitric oxide (NO) in the renal homogenate.</p> </sec> <sec><title style='display:none'>Results</title> <p>Data showed significant alteration in serum and urinary creatinine, total protein, albumin, serum urea, blood urea nitrogen (BUN) and uric acid in diabetic animals as compared to the control rats. CoQ10 and/or NAC effectively alleviated the disturbances in renal function. Diabetic rats showed increased MDA, decreased SOD and CAT activities and decreased GSH along with a significant increase in MPO activity and nitrite content. Treatment with the aforementioned antioxidants and their combination ameliorated the kidney damage as indicated by the reduced OS with improved renal function.</p> </sec> <sec><title style='display:none'>Conclusion</title> <p>The investigation suggests that the chronic hyperglycaemia-induced OS leads to the development and progression of DN. The combined treatment with CoQ10 and NAC has shown a remarkable nephroprotective effect suggesting that combined antioxidant therapy with CoQ10 and NAC may be useful in the attenuation of DN.</p> </sec> </abstract>ARTICLE2021-06-18T00:00:00.000+00:00Study of the solubilisation process of bacterial model membranes induced by DDAO<abstract> <title style='display:none'>Abstract</title> <p>Solubilisation of two bacterial model membranes induced by <italic>N,N-</italic>dimethyl-1-dodecanamine-<italic>N-</italic>oxide (DDAO) was studied. The first model membrane consisted of a mixture of palmitoyloleoylphosphatidylethanolamine (POPE) and palmitoyloleoylphosphatidylglycerol (POPG) in a molar ratio 0.6:0.4 mol/mol, and a second model membrane was enriched with tetraoleoylcardiolipin (TOCL) with a composition POPE-POPG-TOCL = 0.67:0.23:0.1 mol/mol/mol. Solubilisation of these model membranes was studied by static light scattering (nephelometry). Effective ratio R<sub>e</sub> (the amount of DDAO integrated into the bilayer to the amount of lipid) at different steps of the solubilisation process was determined. The molar partition coefficient of DDAO was calculated – in case of the POPE-POPG membrane, K<sub>p</sub> = 5,300 ± 400, for the POPE-POPG-TOCL membrane, K<sub>p</sub> = 6,500 ± 500.</p> </abstract>ARTICLE2021-05-11T00:00:00.000+00:00Iridoids from K. Koch (Lamb's Ears) and L. (Downy Woundwort)<abstract> <title style='display:none'>Abstract</title> <p>Iridoids are a class of secondary metabolites found in a wide variety of plants. Iridoids are typically found in plants as glycosides, most often found to glucose. The genus <italic>Stachys</italic> L. is one of the largest genera of the Lamiaceae family, containing iridoids.</p> <sec><title style='display:none'>Aim</title> <p>The aim of this study was the isolation and identification of iridoids from the aerial parts of <italic>Stachys byzantina</italic> K. Koch and <italic>Stachys germanica</italic> L.</p> </sec> <sec><title style='display:none'>Methods</title> <p>For the isolation and identification of the iridoids, different chromatographic methods (NP-TLC, CPC and RP-HPLC) were used. The structures were established by one- and two-dimensional NMR and mass spectrometry, also.</p> </sec> <sec><title style='display:none'>Results</title> <p>Iridoids (aucubin, harpagide, ajugoside and harpagoside) were isolated and identified by combination of different chromatographic methods from <italic>S. byzantina</italic> and <italic>S. germanica</italic>.</p> </sec> <sec><title style='display:none'>Conclusion</title> <p><italic>Stachys</italic> species may also be used as a potential source of iridoids.</p> </sec> </abstract>ARTICLE2021-07-25T00:00:00.000+00:00en-us-1