ScienceRise: Pharmaceutical Science

Optimization of HPLC method for control of propranolol hydrochloride impurities in liquid medicine for oral use in pediatrics

Thu, 30 Apr 2026 00:00:00 +0300

Propranolol hydrochloride is approved in Ukraine as one of the drugs for the treatment of infantile hemangiomas in pediatrics, however, there are no industrially produced drugs, which necessitates the development and small-scale production. To ensure their proper quality, it is important to implement high-precision analytical control methods, to determine accompanying impurities that may affect the safety and effectiveness of therapy in children.

Aim. To optimize the liquid chromatography method for determining impurities of the active pharmaceutical ingredient in the drug "Propranolol hydrochloride, 4.28 mg/ml, oral solution", manufactured by pharmacy No. 2 CHEMOTEKA of the Pharmaceutical Department of PE "Infusia", intended for use in pediatrics.

Materials and methods. The study was carried out as part of the development of the medicinal product “Propranolol hydrochloride, 4.28 mg/ml, solution for oral administration” (pharmacy No. 2 CHEMOTEKA, PE "Infusia"). Impurities were controlled by liquid chromatography according to the US Pharmacopoeia method “Propranolol hydrochloride for injection”. Method verification was carried out considering the requirements of international standards and the SPhU.

Results. The proposed method for determining the content of related impurities is characterized by high specificity, linearity in the range of 0.5 - 1.6 mg/ml, accuracy, precision, confirmed reproducibility and reporting limit at the level of no more than 0.1%. Additionally, the stability of solutions for 24 hours has been established, which ensures the convenience of its use in routine pharmaceutical analysis.

Conclusions. The optimized liquid chromatography technique provides reliable determination of impurities in the medicinal product "Propranolol hydrochloride, 4.28 mg/ml, oral solution", meets international validation requirements and can be used in routine quality control. The results obtained confirm the feasibility of its use to improve the safety and effectiveness of therapy with the study drug

Structural modification of the 1,2,4-triazole core as a strategy for the design of biologically active compounds (Literature Review)

Thu, 30 Apr 2026 00:00:00 +0300

The aim. The aim of this review article is to systematize and summarize current literature data on methods of chemical modification of 1,2,4-triazole derivatives, as well as to analyze the impact of structural transformations on their biological activity and pharmacological potential.

Materials and methods. The analysis was based on scientific publications by domestic and international authors devoted to the synthesis, functionalization, and biological evaluation of 1,2,4-triazole derivatives. Data generalization was carried out using methods of systematic analysis, comparative assessment of synthetic approaches, and analysis of the results of in silico, in vitro, and in vivo studies (molecular docking, ADME analysis, SAR evaluation).

Results. It has been shown that 1,2,4-triazole derivatives are characterized by high chemical lability and the ability to undergo modification at the sulfur atom, amino group, and nitrogen atoms of the heterocyclic core. Alkylation and acylation reactions, salt formation, hybridization with other pharmacophoric fragments, as well as the application of microwave-assisted synthesis enable the development of compounds with a wide spectrum of biological activity. Among the studied derivatives, compounds exhibiting antioxidant, antimicrobial, antitumor, anti-inflammatory, neuroprotective, and hypoglycemic activities have been identified. A correlation between the chemical structure of the compounds, the nature of substituents, and their pharmacological properties has been established.

Conclusions. 1,2,4-Triazole derivatives represent a promising pharmacophoric platform for the development of new biologically active compounds. Further targeted investigation of their chemical modification pathways and structure–activity relationships offer broad opportunities for the design of potential therapeutic agents

Study of the effect of the microstructure of combined aggregates of nonionic surfactant and cetostearyl alcohol on the rheological properties of hydrophilic cream bases and the release of active substances in experiments in vitro

Thu, 30 Apr 2026 00:00:00 +0300

The aim. To study the effect of the microstructure of mixed aggregates and adsorption layers of non-ionic surfactant and cetostearyl alcohol (CSA) on the rheological characteristics of hydrophilic cream bases and the release of certain active substances in experiments in vitro.

Materials and methods. Cream bases with a dispersion medium of water and propylene glycol (9:1) were studied. The ratio of surfactant to CSA was varied within the base formulations. The rheological properties of the bases were analysed using rotational viscometry, and the microstructure of the aggregates was examined by the spin probe method employing four probes based on fatty acids. The release of active substances from the bases and solutions was tested in vitro; the content of active substances in the dialysate was determined by liquid chromatography.

Results. The apparent viscosity of the bases was observed to reach its maximum at certain ratios of surfactant to CSA, when coagulation structures were formed. The structural arrangement of mixed aggregates of surfactant and CSA was dependent on their ratio. It was demonstrated that a higher specific fraction of CSA in aggregates/adsorption layers contributed to lateral phase separation at the interface with the dispersion medium. This process led to the formation of solid CSA domains and liquid surfactant domains. The mixed aggregates of surfactant and CSA possessed a non-spherical configuration. The hydration of aggregates was ensured by non-ionic surfactant domains. These factors contributed to the formation of coagulation structures at certain concentrations of surfactant and CSA. An increase in the specific fraction of surfactant led to a tendency towards a homogeneous distribution of surfactant and CSA in their aggregates. This was accompanied by a decrease in the apparent viscosity of dispersed systems and a transition from creams to liquids. A decrease in the surfactant fraction resulted in a decline in the hydration of aggregates/adsorption layers, consequently leading to a decrease in the apparent viscosity of the bases. The release of ofloxacin or dexpanthenol was significantly retarded from the bases where coagulation structures were formed.

Conclusions. The rheological characteristics of hydrophilic cream bases are contingent on the microstructure of mixed aggregates or adsorption layers formed by nonionic surfactant and CSA. These properties can be modified by adjusting the mass ratios between these emulsifiers. In the case of cream bases, where a coagulation structure has formed, the release of active ingredients is found to be significantly retarded.

Comparative analysis of biologically active compounds in Tagetes patula L. and Tagetes erecta L.

Thu, 30 Apr 2026 00:00:00 +0300

The aim. The aim of this study was to conduct a comparative analysis of biologically active compounds accumulated in two species – Tagetes patula L. and Tagetes erecta L. – in order to identify the most promising plant material for pharmaceutical development. The research focused on evaluating the qualitative and quantitative composition of free amino acids, water-soluble vitamins, flavonoids, and polysaccharides, as well as assessing their structural characteristics using titrimetric and phytochemical methods.

Methods. Plant raw materials consisting of inflorescences (flowers) of Tagetes patula L. and Tagetes erecta L., collected during the flowering period, were used for analysis. Free amino acids were identified and quantified using chromatographic methods. Water-soluble vitamins were determined spectrophotometrically. The flavonoid profile was established through chromatographic identification of dihydroquercetin, luteolin, rutin, rosavin, quercetin, salidroside, and cynaroside. Polysaccharides, pectic substances, and hemicelluloses were isolated, and their monosaccharide composition was assessed. Titrimetric analysis was used to determine free and methoxylated carboxyl groups and to calculate the degree of esterification of pectic substances. Comparative evaluation between the two species was carried out for all analyzed parameters.

Results. A total of 20 free amino acids were identified in both species, including eight essential amino acids. The total amino acid content was significantly higher in T. patula (57.053 mg/g) compared with T. erecta (38.020 mg/g). Both species contained equivalent qualitative sets of water-soluble vitamins–thiamine, riboflavin, pyridoxine, folic, nicotinic, and ascorbic acids–while T. patula demonstrated considerably higher quantitative levels. The flavonoid composition of both species was identical qualitatively; however, the total flavonoid content was markedly higher in T. patula. Polysaccharide analysis showed that pectic substances and hemicelluloses predominated in both species, with lower levels of water-soluble polysaccharides. The degree of esterification indicated highly esterified pectins, with T. patula containing higher levels of both free and methoxylated carboxyl groups.

Discussion. The results indicate that Tagetes patula L. contains substantially higher quantities of key biologically active substances–including amino acids, vitamins, flavonoids, and structurally active polysaccharides–compared to Tagetes erecta L. The richer phytochemical profile of T. patula supports its greater pharmacological potential, including anti-inflammatory, antioxidant, antimicrobial, gastroprotective, and anthelmintic properties traditionally attributed to Tagetes species. Structural analysis of polysaccharides further demonstrates their suitability for use as bioactive excipients in dosage forms.

Conclusions. Comparative phytochemical evaluation of Tagetes patula L. and Tagetes erecta L. demonstrated that T. patula accumulates significantly higher levels of biologically active compounds. Based on the obtained data, Tagetes patula L. can be considered the optimal species for use as medicinal plant raw material in the development of modern phytopharmaceuticals with pronounced therapeutic activity

Research on the use of medicinal plant materials and herbal-based medicines in the treatment of children, pregnant and breastfeeding women

Ain Raal, Elen Nikker, Tetiana Ilina, Alla Kovalyova, Oleh Koshovyi — Thu, 30 Apr 2026 00:00:00 +0300

Plants have been the primary therapeutic agents for humanity for millennia. Parents are increasingly seeking alternative treatments that appear safer to improve their children's health, utilizing Herbal Medicine Substances (HMS).

The aim of the study was to provide evidence-based information for physicians and the public on the most commonly used medicinal plant materials and herbal remedies for treating children, pregnant women, and breastfeeding mothers, and to assess potential risks.

Materials and Methods. Data were collected about 713 children under the age of 12, represented by 678 respondents, and 383 of them about pregnancy and 385 women about breastfeeding. The study analyzed information on the herbal remedies used, their frequency of application, indications for use, treatment efficacy, and potential side effects of herbal preparations. The study examined seven specific objects: linden flowers (Tiliae flos), garlic bulbs (Allii sativi bulbus), chamomile flowers (Matricariae flos), calendula flowers (Calendulae flos), aloe leaves (Aloe folium), mint leaves (Menthae piperitae folium), and blueberry fruits (Myrtilli fructus). The analysis of the current state of HMS research was conducted based on data from PubMed, Embase, Best Evidence, EMA, and the British Medical Journal.

Results. Within the studied continuum, 81% of children used medicinal plant materials or herb-based preparations. The predominant indications for use were respiratory infections (colds) and digestive disorders. It was established that the use of herbal remedies only partially complied with the recommendations of the European Medicines Agency (EMA). For instance, 54% of children used aloe leaves to treat skin inflammation, which the EMA does not recommend for this age group. The study also revealed the use of medicinal plant materials not recommended by the EMA, specifically coltsfoot leaves, St. John's wort herb, and ginkgo biloba leaves. Side effects were recorded in 2.6% of children, most frequently associated with the use of garlic bulbs and mint leaves. Furthermore, the use of raw materials not recommended during pregnancy and lactation, such as motherwort herb, was identified. The systematized data served as the basis for recommendations for physicians and the public regarding the core criteria of phytotherapy in pediatrics, and for pregnant and breastfeeding women.

Conclusions. Since medicinal plant materials and herb-based preparations play a significant role in pediatric treatment, as well as during pregnancy and lactation, and study results indicate the use of products not recommended by the EMA, there is an urgent need to inform physicians and the general public about the correct application of herbal remedies and the potential risks associated with their use

The frigoprotective effects of etoricoxib and diclofenac sodium in a model of acute general cooling in rats: the role of leukotrienes, interleukins, and nitric oxide synthase

Sergiy Shtrygol’, Olesia Kudina, Dmytro Lytkin, Andrii Taran, Tetiana Yudkevych — Thu, 30 Apr 2026 00:00:00 +0300

The aim: The aim of the study was to evaluate the role of leukotrienes, interleukins, and nitric oxide synthase in frigoprotective effect of etoricoxib and diclofenac sodium in a model of acute general cooling in rats.

Material and methods: Acute general cooling was induced by exposing rats to −18 °C for 2 hours without animal mobility restriction. 30 min before cold exposure animals were treated with etoricoxib (5 mg/kg) or diclofenac sodium (7 mg/kg). Body temperature was measured before and after acute general cooling modeling. In rat liver the following parameters were determined: 5-lipoxygenase (5-LOX), leukotriene B4 (LTB4), total leukotrienes (LTs), interleukins (IL-1β, IL-4, IL-6, IL-10), tumor necrosis factor-α (TNF-α), and nitric oxide synthase (NOS).

Results: activation of the lipoxygenase pathway of arachidonic acid metabolism was characterized by a significant increase in leukotriene levels (total and leukotriene B4) without substantial changes in proinflammatory cytokines (IL-1β, IL-6, TNF-α) but with a significant decrease in anti-inflammatory cytokines (IL-4, IL-10) in the liver. Etoricoxib and diclofenac sodium similarly reduced the severity of hypothermia, prevented the increase in leukotriene levels without affecting 5-LOX content. Etoricoxib and particularly diclofenac sodium significantly reduced IL-1β levels without substantial changes in the other cytokines. Both studied medicines restored NOS levels to those observed in the intact control group.

Conclusions: obtained results experimentally substantiate the possibility of diclofenac sodium and etoricoxib to decrease the severity of acute general cooling, while also demonstrating certain differences in the mechanisms underlying their frigoprotective effects

Assessment of the implementation status of medical information systems in pharmacy institutions of Ukraine based on the results of a questionnaire survey

Thu, 30 Apr 2026 00:00:00 +0300

Digital transformation of the healthcare system is one of the key areas of reforming the sector in Ukraine and involves the active implementation of an electronic healthcare system and medical information systems in the activities of pharmacy institutions. However, along with the regulatory technical requirements for the functioning of medical information systems, the issue of their practical effectiveness from the perspective of direct users - pharmaceutical workers - remains insufficiently researched.

The aim of the work. To assess the status of the implementation and functioning of MIS in pharmacy institutions in Ukraine based on the results of a questionnaire survey of specialists involved in their use in practical activities.

Methods. A descriptive cross-sectional questionnaire survey was applied with a combination of normative and user-oriented approaches. The survey was conducted among 76 pharmacy specialists. The results were processed using descriptive statistics, comparative analysis, and qualitative interpretation.

Results. It was established that the implementation of medical information systems in pharmacies in Ukraine is at the stage of formed basic integration with the electronic health care system and ensures the implementation of key digital processes, in particular work with electronic prescriptions. The uneven implementation of individual functional modules, the fragmentation of administrative and accounting functionality, as well as the heterogeneity of the level of technical support were revealed. Most respondents supported the need for further expansion of the functionality of medical information systems and the implementation of a comprehensive multi-criteria approach to assessing their effectiveness.

Conclusions. The results obtained justify the feasibility of further unification and standardization of the functionality of medical information systems, as well as the development of a single methodology for assessing their effectiveness for pharmacies in Ukraine, considering technical, organizational, information and communication, social and economic criteria

Pharmacological action of thick extract of common tansy (Tanacetum vulgare L.) flowers in an experimental model of estrogen-induced cholestasis

Thu, 30 Apr 2026 00:00:00 +0300

The aim. To study the protective effect of thick extract of Tanacetum vulgare L. flowers (TETVF) in an experimental model of estrogen-induced cholestasis (EIC).

Materials and methods. EIC was reproduced by subcutaneous administration of 7α-ethinylestradiol (E) (5 mg/kg) to rats. TETVF and the reference preparation (RP) cholelesan (ChL) were administered to animals intragastrically once a day for 3 days before and 5 days of the modeling period. One day after the last E administration, the animals were anesthetized (thiopental sodium, 50 mg/kg, intraperitoneally), the volume of bile secreted in 60 min was determined, and the bile secretion rate (BSR) was calculated. The activity of alanine aminotransferase (ALT), alkaline phosphatase (ALP), gamma-glutamyl transpeptidase (GTT), the content of TBA-active products (TBA-AP) and reduced glutathione (RG) was determined in the blood serum. For histological examination, prepared liver sections were stained with hematoxylin, eosin and sudan IV to identify lipids. A semi-quantitative assessment of EIC signs was performed.

Results of the study. In animals with EIC TETVF contributed to the normalization of bile volume and BSR to the level of intact control (IC), a significant (p < 0.05) decrease in the studied parameters: ALT, LF and GTT, a decrease in lipid peroxidation (LPO) processes and an increase in liver antioxidant defense, as evidenced by a significant decrease in the level of TBA-AP (30.98±0.90 μmol/g vs. 44.87±4.26, p < 0.05) and a 1.9-fold increase in RG (4.11±0.36 μmol/g vs. 2.19±0.16, p < 0.05) compared to the control pathology (CP). In general, TETVF showed a normalizing effect like RP, but was inferior to it in terms of its effect on BER and on ALT activity and TBA-AP level. After the introduction of TETVF the severity of ductal proliferation significantly decreased by 1.6 times (p < 0.05), periductal inflammation by 3.8 times (p < 0.05), and fatty degeneration of hepatocytes of the periductal zones by 2.3 times (p < 0.05) compared to CP.

Conclusion. The ability of TETVF to improve impaired liver function under conditions of EEIS and reduce pathological manifestations was established

Formulation and characterization of ezetimibe nanoparticles for hyperlipidemia treatment

Asmaa Abdelaziz Mohamed, Olla Maan, Firas Aziz Rahi, Doaa Zakaria Elkashif — Thu, 30 Apr 2026 00:00:00 +0300

The aim of the work. Ezetimibe (EZ) is categorized as a Biopharmaceutics Classification System class II (BCS II) agent that possesses poor solubility and is highly permeable. This work aimed to incorporate EZ into nanoparticles (NPs) to accelerate release and to enhance its bioavailability.

Materials and Methods. A stability-indicating method for the computation of EZ was developed to compute EZ in NPs in fresh and stored samples. Nine formulations of EZ-NPs were developed by solvent evaporation using HPMC 6 cps, sodium alginate, and Tween 80 in various proportions. A HPLC method was designed to estimate EZ in NPs. EZ-NPs were tested chemically and characterized.

Results. The developed method was fully validated, and EZ NPs comprising HPMC and tween 80 had zeta potential (ZP) ranging from -21.6 mV to -30.1 mV, higher than other formulae, and their release was enhanced. The formulation (HP4) had an elevated ZP (-30.1 mV) and released about 91% of EZ within 20 min. HP4 was chosen for stability assessment and proved to be stable.

Conclusion. The formulation (HP4), including 0.1:0.5:0.4 ratios of the EZ: HPMC: sodium alginate, was the optimized EZ-NPs formulation. Microencapsulation of EZ with HPMC: sodium alginate in a 0.1:0.5:0.4 ratio could enhance the release and achieve stability

TiO2-catalyzed synthesis of a primary amine NONOate

Thu, 30 Apr 2026 00:00:00 +0300

HNO induces vascular and myocardial activities, exhibits anticancer and antioxidant activities and inhibits platelet aggregation. However, the mechanism by which it functions is still poorly understood. Primary amine NONOates are HNO donors that can be used to study and understand the chemical properties and physiological effects of HNO. However, its synthesis involves very high pressure and low temperature conditions and requires specialized glassware and equipment.

The aim. In this study, a method for the synthesis of an HNO donor, a primary amine NONOate based on cyclohexylamine, that does not involve specialized glassware and high pressure is developed.

Materials and methods. The synthesis of primary amine NONOate was performed through the reaction of cyclohexylamine and NO gas, in the presence of sodium methoxide and TiO₂, for 24 h. The resulting product was isolated and characterized spectrophotometrically to determine its identity, decomposition kinetics, and HNO release profile at physiological pH. The synthesis method was further optimized based on reaction time, solvent, catalyst loading, and temperature.

Results. The TiO₂-catalyzed method yielded the desired product which was characterized spectrophotometrically. The product shows typical electronic spectrum of a NONOate (λ_max = 250 nm), followed first-order decomposition kinetics, and released both HNO and NO at physiological pH, which are characteristics of primary amine NONOate. The method yielded 5.98 mg cyclohexylamine NONOate which is equivalent to a percent yield of 0.0550%. The yield of the method was low but comparable to the yield from conventional method (1-20%) which requires -78 °C and 50 psi NO. Furthermore, the yield of this method is sufficient for chemical and biological assays.

Conclusion. This study proposed a possible alternative method for synthesizing cyclohexylamine NONOate using TiO₂ catalysis at ambient conditions. Although the yield is lower than that of conventional method, the result is quite sufficient for chemical and biological assays. This approach eliminates the requirement of using specialized high-pressure and low-temperature equipment, making the study of HNO donors more feasible.