REVIEW: AN EFFORTS TO INCREASE THE SOLUBILITY AND DISSOLUTION OF ACTIVE PHARMACEUTICAL INGREDIENTS

The most significant aspect of a drug's physicochemical nature is its solubility. If the medicine is in a dissolved form, it can dissolve and enter the membrane, resulting in a therapeutic effect. The pharmacokinetic phase of the drug in the body, which includes absorption, distribution, metabolism, and excretion, will be correlated with solubility. Some medications, however, have a low solubility. To obtain a therapeutic impact, an effort must be made to increase the drug's solubility. Based on the literature research, the goal of this paper is to explain approaches that can be utilized to improve solubility. In general, physical, chemical, and micelle formation efforts can all be used it to enhance solubility. Particle size reduction, crystal shape modification, and the utilization of matrices in the disperse phase are examples of physical alterations. pH adjustment, buffering, salt formation, complexation, and derivatization all are examples of chemical alterations. The employment of supercritical processes in solutions and also excipients such as surfactants, cosolvents, stabilizing solutions, and others are examples of how micelle formation can be modified.

Distribution of Selected Dissolved and Particulate Heavy Metals in Lake Kenyir, Malaysia

This study was conducted to determine the concentration and possible sources of dissolved and particulate heavy metals in Lake Kenyir, Terengganu, Malaysia. The heavy metals studied included Cd, Fe, Pb, Zn and Cu. The findings indicated that the mean concentrations found in the dissolved form for surface waters were in decreasing order of Fe>Zn>Pb~Cu>Cd. A similar trend was also recorded for the particulate form i.e., Fe>Zn>Pb~Cu>Cd. In terms of vertical distribution, most of the heavy metals showed a trend of increasing concentrations from the surface to the bottom waters. The main sources of heavy metals were from anthropogenic activities such as discharge of untreated sewage, surface runoff and boat activity. However, the levels of dissolved heavy metals were still lower compared to other study areas in Malaysia. The dissolved heavy metal concentrations were equivalent with Class II based on the National Water Quality Standard for Malaysia.

Detection of contamination by some trace elements in the muscles of Carassius auratus (Linnaeus) collected from the Euphrates River / Central Iraq

The study involved measuring the concentration of seven trace elements (Cd , Pb , Zn , Fe , Mn , Se and Ni) In edible tissues of three classes of different weight and height of Carassius auratus (Linnaeus) collected from three sites of the Euphrates River, which Al- Hindiya barrage (first site) and Touirij (second location) and the Kifil (third site), for the period from Spring 2015 to Winter 2016 , and included also The study also estimated the concentrations of the trace elements studied in river water, in both dissolved and particular form , as well as exiamining of some physio- chemical properties of water river , which variations depended on the different both sites and seasons The Findings of the present study indicated seasonal changes in the concentration of trace elements studied in both water forms (dissolved and particular form) and in fish muscle in the three locations of the current study. These were noticed that the level of trace elements in the third group, the contrast of the first and second categories was strong, and the finding found a clear link between the length and weight of the fish and the concentration of the fish as elements of concentration increases with increasing length and weight . The results founded that the concentrations of trace elements studied the particular form of higher compared to dissolved form as well as to the effective of certain physical and chemical properties of water such as Temperature, pH, Electrical conductivity and salinity on the concentration of these trace elements.

Chemical and algological composition of the snow cover at the mouth of the Onega river (White Sea basin)

In the study, the content and speciation of Mn, Pb, Cd, Zn, Cr, Ni, Co, Cu, and Fe in the snow cover at the mouth of the Onega river (White Sea basin) at the end of the winter periods in 2018, 2019 and 2020 were determined. Winter 2019 year was the snowiest, as the maximum values of the snow cover depth and water equivalent were almost two times higher than in all other years. The total content of suspended matter in the snow cover was 0.2–5.5 μg/L. Increased concentrations of suspended solids were identified near highways. Mn, Cr and Ni were present in the snow cover mainly in their dissolved form, while Fe, Pb and Co were mostly contained as solids. The algological composition of the snow cover was also studied.

Herbal Infusions as a Valuable Functional Food

Herbal infusions are an underestimated and easy to intake a source of biologically active natural compounds (polyphenols), which, in the dissolved form, are more easily absorbed. Therefore, this study aimed to assess the potential of herbal infusions as a functional food to reduce postprandial hyperglycemia (inhibition of α-amylase and α-glucosidase) and to reduce the effects of increased blood glucose level (antioxidant effect-DPPH, CUPRAC, and Fe2+ chelating assays, as well as anti-inflammatory activity-inhibition of collagenase). We showed that polyphenols are present in the examined aqueous herbal infusions (including chlorogenic and gallic acids). Subsequently, our research has shown that herbal infusions containing cinnamon bark, mulberry leaves, and blackberry fruits most strongly inhibit glucose release from complex carbohydrates, and that all herbal infusions can, to different degrees, reduce the effects of elevated blood sugar. In conclusion, infusions prepared from herbal blends could be recommended to prevent type II diabetes.

Strengthening hair growth Карр (Dent. med. Woch., 1921, №11)

In the past, to enhance hair growth, they were limited exclusively to the use of chemical, thermal and electrical stimuli on the skin, with the aim of encouraging the hair papillae to intensify activity. Zuptz for the first time went to this goal in a different way, by introducing into the body, in a dissolved form, keratin, which is necessary for hair growth.

TYPES OF CHITOZAN MODIFICATION BY USING VARIOUS DERIVATIVE AGENTS

The prevalence of the study of chitosan is associated with favorable biological properties of the polymer: low toxicity, biodegradability, and biocompatibility with cells of the human body. Chitosan is a complex aminopolysaccharide consisting of two types of monosaccharaides: 2-acetamide-D-glucose and 2-amino-D-glucose connected by a 1,4-β-glycosidic bond, obtained by chitosan by chitin deacetylation. Chitosan has hemostatic, hypolipedymic and antimicrobial activity against gram-positive and gram-negative microorganisms. However, the preparation of various drugs based on it is accompanied by difficulties in the development of biodegradable compositions that are related to the field of application. For the immobilization of various compounds used as drugs for the treatment of complications associated with damage to the skin, it is possible to use chitosan in dissolved form, converted into a salt form. However, salt forms of chitosan are water-soluble polymers, which leads to the rapid degradation of the matrix and the release of the drug from it, due to hydrophilicity. Additional lipophilization is required to obtain insoluble chitosan structures. Therefore, various modified chitosan structures are used that have suitable properties for the manufacture of a medicament. In addition, lipophilization of the chitosan structure allows the immobilization of more lipophilic structures. The purpose of this work was to study the literature and patent data sources for conducting information-analytical search of the approach. That led to the choice of a modified chitosan structure for its use in the pharmaceutical development of finished dosage forms. The article considers various types of derivatizing agents and the properties of modified chitosan structures.

Behavior of 129I in the Abukuma River water during two high-flow events in 2018

<p>Radioiodine is one of the most important radionuclides released by the accidents of Fukushima Dai-ichi nuclear power plant (FDNPP). Iodine-131 elevated ambient radiation dose rate immediately after the accident, but it is extinguished due to its short half-life. The long-lived <sup>129</sup>I can be used as a tracer to retrospectively infer the level of <sup>131</sup>I. Understanding of environmental behavior of <sup>129</sup>I is important for preparedness against nuclear disaster. This study presents sampling campaigns on the Abukuma River during two high flow events, and discusses riverine <sup>129</sup>I behavior based on comparisons with that of <sup>137</sup>Cs. The study site was the Kuroiwa site locating at midstream of the Abukuma river. Its catchment area was 2886 km<sup>2 </sup>and mean <sup>129</sup>I inventory in the catchment was 0.041 Bq m<sup>-2</sup>. Five and seven river water samples were taken during high-flow events in July 2018 (JUL18) and October 2018 (OCT18), respectively. Suspended sediment and filtrate samples were obtained by decantation and subsequent filtration with 0.45 μm-mash membrane filter, respectively. The suspended sediment and filtrate samples were measured for <sup>137</sup>Cs activity concentrations with HPGe detector and then measured for <sup>129</sup>I/<sup>127</sup>I ratio with accelerator mass spectrometer and for <sup>127</sup>I concentration with ICP-QQQ-MS. Mean <sup>129</sup>I activity concentration in suspended sediment during JUL18 and OCT18 were 1.0 and 0.43 mBq kg<sup>-1</sup>, respectively. In terms of temporal trends, <sup>129</sup>I activity concentration in suspended sediment lowered in the peak water discharge phase, contrastive to those of <sup>137</sup>Cs which were the highest at peak water discharge phase. Mean dissolved <sup>129</sup>I activity concentrations during JUL18 and OCT18 were 0.18 and 0.067 μBq L<sup>-1</sup>, respectively. Both <sup>129</sup>I and <sup>137</sup>Cs activity concentrations in dissolved form tended to decrease with time during two high-flow events. Mean apparent distribution coefficient (Kd) during JUL18 and OCT18 were 4.3 ×10<sup>4</sup> and 6.1 ×10<sup>3</sup> L kg<sup>-1</sup>, respectively. The Kd values of <sup>129</sup>I were lower than those of <sup>137</sup>Cs and it reveal relatively-high solubility of <sup>129</sup>I. Total exportation of <sup>129</sup>I from the catchment during JUL18 and OCT18 were estimated as 1.0 × 10<sup>4</sup> and 2.3 × 10<sup>4</sup> Bq, respectively. Exported <sup>129</sup>I in dissolved form accounted for 80 and 27% of total exportations, respectively. By contrast, more than 95% of <sup>137</sup>Cs was exported in particulate form in the events. These results indicated an importance of dissolved form for understanding environmental behavior of radioiodine.</p>

Impact of typhoons on particulate and dissolved ¹³⁷Cs activities in seawater off the Fukushima Prefecture: results from the SOSO 5 Rivers cruise (October 2014)

Cruise SoSo 5 Rivers took place during October 2014 off the coast of Fukushima Prefecture shortly after the passage of two typhoons. Detection of dissolved 134Cs and 137Cs in all samples reflected contamination caused by accidental releases of radiocaesium from the Fukushima Dai-ichi Nuclear power plant (FNPP1) accident. The dissolved activities were generally higher at coastal sites and decreased with distance from shore, and they were higher in the surface than in the bottom water. The tendency of 137Cs activities to decrease with distance from the coast reflected mixing of coastal water and open-ocean water of which 137Cs activity concentration was ~1.5 Bq m−3. At stations very close to the coast, we observed high particulate 137Cs activity concentration that exceeded dissolved 137Cs activity concentration. 137Cs activities were generally 1–2 orders of magnitudes lower in organic particles than in dissolved form, and the ratios of 137Cs activity concentration in organic particles to 137Cs activity concentration in dissolved form ranged from 0.01 ± 0.00 to 0.12 ± 0.01. The ratio of 137Cs to 134Cs activity concentrations in organic particles did not change with distance from shore or with 137Cs activity concentration and generally remained around 1, even in samples collected far from the coast. This pattern indicated that the organic particles had come from rivers or a source very close to the coast. The 137Cs / 134Cs activity ratio in dissolved form north of FNPP1 region was estimated to be 1.074 ± 0.015, a ratio that is in good agreement with the 137Cs / 134Cs activity ratio in the core of Unit 1 of the FNPP1 while the 137Cs / 134Cs activity ratio at Tomioka port which located south of FNPP1 was 0.998 ± 0.017. Therefore we can conclude the source of radiocaesium in seawater in the coastal region north of FNPP1 was deposited radiocaesium released from the core of Unit 1 of FNPP1, while the source of radiocaesium observed in the coastal region south of FNPP1 was a mixture of deposited radiocaesium released from the core of Unit 2 and the core of Unit 1 of FNPP1. During September–October of each year, the typhoon season in Japan, the 137Cs activity concentration generally increased at Ukedo port, Tomioka port, FNPP1, and Iwasawa beach, and showed a good relationship with the 7-day modified antecedent precipitation index (API) while there is less correlation between the modified API and 137Cs activity concentration near the outlet of canal from unit 5 and 6 of FNPP1 to the sea.

Geochemical composition of ice wedges in the Batagay yedoma

The subject of this research is the syngenetic ice wedges stripped in the Batagaika crater (67°34 '49" N, 134°46 ' 19 " E), located 10 km southeast of the Batagay settlement. The assessment of macroelement composition of ice was conducted using “Stayer” ion chromatograph (Russia), the chloride ion detection limit is 0.02 mg/l. The article examines the ionic and macroelement composition of ice in suspended and dissolved forms in the Late Pleistocene syngenetic ice wedge of the Batagay yedoma. A comprehensive geochemical research of the Batagaika crater is carried out for the first time. The author explores the upper and lower ice wedges of different age. The main conclusions are as follows: 1) mineralization of Late Pleistocene ice wedge of the Batagay yedoma ranges from 66.56 to 424.8 mg/l, from ultra-fresh to slightly salted; by ionic composition, the ice is bicarbonate-calcium and corresponds to the snow formed under the influence of continental air masses; 2)  the share of Ca contained in the dissolved form does not exceed 20-30%’ as far as other elements, the share of Mg, K, Na, Al, Fe, Mn in the suspended form is over  90%; 3) by mineralization, the Pleistocene ice of Batagay yedoma coincides with the previously studied Pleistocene ice wedges of Yakutia and the Interior Alaska.