Propranolol degradation through processes based on the generation of hydroxyl free radical

Pharmaceutical substances such as propranolol (PRO) are an emerging class of aquatic contaminants that have increasingly been detected in ground and surface water. For this reason, the aim of this study was to evaluate the efficiency of advanced oxidation systems for the PRO degradation. The tests started with anodic oxidation (AO), using 0.01, 0.05, and 0.1 M Na2SO4 as the supporting electrolyte and 16, 32, 48, and 64 mA cm−2 as current density. Under the best conditions obtained in AO, the electro-Fenton (EF) process was reviewed, where the effect of Fe2+ was analyzed with 5, 10, 15, and 20 mg Fe2+ L−1. The Fenton reaction (FR) was studied using the Fe2+ concentration that promoted the highest percentage of PRO removal and initial concentration of 16 mg L−1 of H2O2, in addition to these conditions, in the photo-Fenton (PF) system, the effect of UV light with wavelengths 254 and 365 nm were evaluated. The results obtained showed that the degradation efficiency of the EF > AO > PF > FR system along with a percent removal of 94.52, 90.4, 25.97, and 4.4%, respectively. The results showed that PRO can be removed through the studied systems, with the EF system being the most efficient.

NUCLEOPHILIC SUBSTITUTION OF NITRO GROUP IN 1-METHYL- 5-NITRO-1,2,4-TRIAZOLE BY DIAMINOGLYOXIME

Изучен процесс взаимодействия 1-метил-5-нитро-1,2,4-триазола с многоцентровым бифункциональным О-нуклеофилом – диаминоглиоксимом. Показано, что исходный субстрат вступает в реакцию SNipso-замещения нитрогруппы с гидроксильными группами О-нуклеофила с образованием биологически активного соединения, объединяющего в единой молекуле фармакофорные фрагменты различного типа – 1,2,4-триазоловые гетероциклы и NH2-группы. Процесс сопровождается конкурентными реакциями образования триазолона и продукта его дальнейшего взаимодействия с исходным субстратом. С помощью веб-ресурса PASS Online осуществлен компьютерный скрининг, показано, что исходный субстрат и продукты реакции могут выступать потенциальными фармацевтическими субстанциями. The reaction between 1-methyl-5-nitro-1,2,4-triazome and a concerted bifunctional О-nucleophile – diaminoglyoxime was explored herein. The starting substrate was shown to engage into the SNipso-substitution of the nitro group by the О-nucleophile hydroxyls to furnish a bioactive compound whose single molecule combines different-type pharmacophoric moieties – 1,2,4-triazole heterocycles and NH2groups. The process came amid competitive reactions to form triazolone and a product from its subsequent reaction with the starting substrate. The PASS Online web-resource was used to perform computer-aided screening, demonstrating that the starting substrate and the reaction products can serve as potential pharmaceutical substances.

QUALITATIVE CONTENT AND SOME PHYSICAL AND CHEMICAL PROPERTIES OF POLYSACCHARIDES FROM ONOPORDUM ACANTHIUM L. HERB

Natural polymers are interesting as independent pharmaceutical substances also as complex drugs including herbal drugs. The aim of this work was determination of the main features of water-soluble polysaccharides (WSPS) and pectinic substances (PS) isolated from Onopordum acanthium L. herb for using as pharmaceutical substances. The following tasks were set to achieve this aim: determination of qualitative content of monosaccharides after previous acidic hydrolysis of fractions by paper chromatography, determination of molecular weight, isoelectric point, distribution coefficient, superficial activity these fractions by physical and chemical methods. It was found that WSPS consist of xylose and rhamnose, PS – galacturonic acid. WSPS have molecular weighs 783.96 g/mol, PS – 17351.37 g/mol. Molecules WSPS are neutralize in buffer solution with pH 5.2 and PS – pH 4.7. Also WSPS and PS have similar distribution activity with distribution coefficient 2.97 and 2.59, respectively. But WSPS and PS are superficially inactive substances. Determinate features including well distribution activity may be used for development complex herbal drugs containing herb of Onopordum acanthium L. Also sorption activity should be detected in the future.

Removal of Meropenem by using Lemna minor

In this paper we presented a case study about the removal of a pharmaceutical contamination (in this case Meropenem) from the environment using organic natural substance (in this case study is Lemna minor). The study proved the efficiency of the used material to remove the contamination of three specific contamination levels of Meropenem. The experimental testing proved the concept, the effect on two vital measures (the chemical oxygen demand – COD, and the root length), which showed improvement in both measures. The degradation mechanism was proven to be not arbitrary by testing the degradation behavior measured practically to four kinetic models. The practical work was found to fit perfectly with the Grau second order model as the simulation work included in the paper shows. Based on this study it can be proven that the dangerous chemicals resulted from the residue of a pharmaceutical substances can be removed efficiently using a totally natural environmental friendly material.

Cardiovascular comorbidity of osteoarthritis: clinical significance and therapy strategies

The comorbidity of osteoarthritis and cardiovascular disease is the most frequent and typical polymorbidity in older patients. The identity of risk factors, low intensity pathogenetic effect of systemic inflammation, dyslipidemia define a greater degree and progression of both osteoarthritis and cardiovascular diseases in patients with a combination thereof. There is a significant decline in physical functioning and loss of autonomy. There is a higher risk of cardiovascular mortality in osteoarthritis patients. Only comprehensive programs involving physical rehabilitation, nutraceutical support, and pharmaceutical substances of chondroitin sulfate and glucosamine sulfate can supply effective and safe treatment in patients with osteoarthritis and cardiovascular disease.

PHARMACEUTICAL DEVELOPMENT OF A FIXED DOSE COMBINATION FORM OF MEMANTINE AND CYTICOLINE WITH MODIFIED RELEASE: RESEARCH OF TECHNOLOGICAL PROPERTIES OF SUBSTANCES

The pharmaceutical development of a fixed dose combination form of citicoline and memantine for the treatment of cognitive disorders, which will improve compliance is a topical area of research. Purpose: to investigate the technological properties of the active pharmaceutical ingredients: memantine hydrochloride and citicoline monosodium salt in the framework of the development of a fixed dose combination modified release. The samples of pharmaceutical substances citicoline "Kyowa Hakko Bio Co., Ltd." (Japan) and memantine hydrochloride - Hetero Drags Limited (India) were used. Technological studies of the substances were carried out in accordance with the requirements of the State Pharmacopoeia of the RF XIV edition. It was revealed that the particles of the investigated substances show an anisodiametric shape, the anisodiametric shape of the analyzed particles indicates possible poor flowability of APIs, which predicts difficulties in dosing during the tablet compression process. The following characteristics were studied: the ability of the powder to compaction, the bulk density and compressibility index, Hausner ratio were established. It was found that, according to the USP classification, the flowability of substances can be characterized as very, very poor. Pharmaceutical substances of memantine hydrochloride and citicoline monosodium salt have unsatisfactory technological properties, which can complicate the processes of die filling and dosing of pharmaceutical substances during tableting tablet compression. To prevent these disadvantages, it is further recommended to provide research on the possibility of using wet granulation, or the usage in the composition of the tablet mass of excipients with a high bulk density and good flowability. Thus, within the framework of pharmaceutical development, the physicochemical properties of the pharmaceutical substances memantine hydrochloride and citicoline monosodium salt were investigated.