In which rounds were the most rotations of key players made, and how did this affect physical activity? Analysis of the eight best teams of the 2018 FIFA world cup Russia.

BACKGROUND: Team management, especially player selection, rotation, and availability, are critical issues when dealing with the high demands of modern training and gameplay. As such, research continuously seeks ways to improve these actions or implement new ideas to gain a competitive advantage through the rotation of players in the starting line-up. The current study aimed to examine the rounds of the 2018 FIFA World Cup Russia in which the most rotations of key players were made and how this affected physical activity. METHODS: The sample consisted of 110 players from the top eight teams in the 2018 World Cup Russia who played entire matches for up to 90 min in seven consecutive games. All players were divided into key players (KPs, n = 58) and non-key players (NKPs, n = 52). The analysis used data collected by an advanced motion analysis system known as STATS®, with physical activity variables analyzed, including total distance covered (TDC), distance covered with high intensity over 20 km/h (HIR), and the number of sprints undertaken. In statistical analysis, differences between categories and consecutive matches were calculated using the Kruskal-Wallis H test, and if a significant effect size was found, a multiple comparisons p values test was performed. RESULTS: The best teams at the 2018 FIFA World Cup Russia used the most KP rotations with NKPs in the third match of the group stage. In addition, this was even more visible among more successful teams than less successful teams. The rotation strategy among the best eight teams allowed them to maintain the physical activity of KPs and NKPs in all rounds of the tournament. CONCLUSIONS: Coaches and coaching staff should incorporate squad rotation that includes a large group of players in their team management to improve their success. Team management expertise in player rotation during matches played over congested schedules at top tournaments maintains high levels of physical activity indicators (TDC, HIR, and sprints).

Do players competing in the UEFA Champions League maintain running performance until the end of the match? Positional analysis between halves and 5-minute intervals.

BACKGROUND: This investigation aimed to analyze differences in running performances amongst playing positions between the first and second halves of soccer matches and at 5-minute intervals during matches. METHODS: Data were collected from 179 soccer players during 20 UEFA Champions League (UCL) 2020/2021 group stage matches. Data were examined using the InStat Fitness semi-automatic video system. Eight variables were selected to quantify players' running performance (RP). Players were categorized based on positional groups: central defenders (CD), fullbacks (FB), central midfielders (CM), wide midfielders (WM), and forwards (FW). Univariate differences in RP were analyzed using ANOVA and the t-test for dependent samples and multivariate differences were identified using canonical discriminant analysis. RESULTS: The main findings were that all positions achieved significantly higher average speeds and walking distances in the first half of the match than in the second half. Furthermore, analysis of positions showed that CM covered more distance than CD in all 5-minute intervals. In addition, WM performed more high-intensity running than CD in all 5-minute intervals and FW performed more high-intensity running than all other playing positions. CONCLUSIONS: The findings from the present study should help coaches design training exercises that are specific to parts of a match. Moreover, the findings can help provide better understanding of match demands and individualization of training. Analysis of 5-minute intervals may also help coaches understand the stages of a match where player substitutions will be most effective.

Long-Acting Injectable Antipsychotics-A Review on Formulation and In Vitro Dissolution.

Long-acting injectable (LAI) neuroleptics constitute an effective therapeutical alternative for individuals suffering from persistent mental illness. These injectable pharmaceuticals help patients manage their condition better and improve long-term outcomes by preventing relapses and improving compliance. This review aims to analyse the current formulation aspects of LAI neuroleptics, with particular emphasis on analysis of drug release profiles as a critical test to guarantee drug quality and relevant therapeutical activity. While there is no officially approved procedure for depot parenteral drug formulations, various dissolution tests which were developed by LAI manufacturers are described. In vitro dissolution tests also possess a critical function in the estimation of the in vivo performance of a drug formulation. For that reason, thorough inspection of the in vitro-in vivo correlation (IVIVC) is also discussed.

The Effect of Squad Rotation on Physical Activity at the 2018 World Cup in Russia. Analysis the Most Exploited Players of the 4 Best Teams.

The purpose of this study was to examine how the four best teams in the 2018 Football Men's World Cup rotate by squad and how this impact the physical activity of the teams in consecutive rounds. The study sample consisted of the 31 players of the 4 best teams, who played in every tournament match, except for the third game of the group stage. The analysis included 186 observations and was carried out on the most exploited players (MEP) excluding goalkeepers, who played at least 450 mins (5 full matches) in the tournament. The analysis was conducted using data collected by an advanced motion analysis system known as STATS®. The selected physical activity parameters analyzed included: total distance covered (m/min), distance covered at various intensity ranges (m/min), top speed (km/h), and number of sprints performed. It was found that all four teams in the third match of the group stage have performed the largest number of rotations with most exploited players and introduced the highest number of rested players (7.75 ± 2.06). A significant increase was observed between the second and fourth match in the 0-7 km/h distance covered (37.99 ± 3.19-39.23 ± 3.35 m/min) and the top speed (28.12 ± 2.22-29.21 ± 2.64 km/h)-p < 0.05. Furthermore, MEPs in the knockout stage, used pacing strategies by increasing the amount of low-intensity running to maintain high intensity during the game. From a practical point of view, this investigation shows that squad rotation can be a valuable support to a pacing strategy by players.

How did three consecutive matches with extra time affect physical performance? A case study of the 2018 football Men's World Cup.

The purpose of this study was to ascertain the effect of playing three consecutive matches with extra time (ET) on the physical performance of selected Croatian players in their subsequent match, the final of the 2018 Men's World Cup in Russia. The case study consisted of 4 players on the Croatian national team (16 observations) who had played in all three matches up to 120 min. The consecutive full time matches (90 minutes) and extra time (30 minutes) were compared. The analysis was conducted using data collected by an advanced motion analysis system known as STATS and from interviews with the strength and conditioning coach of the Croatian national team. The recorded variables used were: total distance covered [m], distances covered [m] at intensity ranges of 20-25 km/h and above 25 km/h, and number of sprints performed. All the studied parameters systematically increased in each match up to 90 minutes of play, reached their maximum values in the semi-final and then decreased in the final match. Compared to the first extra time period, in the third extra time period the players covered twice as much distance with an intensity of 20-25 km/h and above 25 km/h, and recorded twice as many sprints. This investigation shows that players in central positions on the pitch are able to maintain or even increase high and very high intensity activity in three consecutive matches with extra time. These data complement the developing body of literature relating to the influence of accumulation of match play with extra time periods on high level players.

Characteristic of Cyclodextrins: Their Role and Use in the Pharmaceutical Technology.

About 40% of newly-discovered entities are poorly soluble in water, and this may be an obstacle in the creation of new drugs. To address this problem, the present review article examines the structure and properties of cyclodextrins and the formation and potential uses of drug - cyclodextrin inclusion complexes. Cyclodextrins are cyclic oligosaccharides containing six or more D-(+)- glucopyranose units linked by α-1,4-glycosidic bonds, which are characterized by a favourable toxicological profile, low local toxicity and low mucous and eye irritability; they are virtually non-toxic when administered orally. They can be incorporated in the formulation of new drugs in their natural form (α-, ß-, γ-cyclodextrin) or as chemically-modified derivatives. They may also be used as an excipient in drugs delivered by oral, ocular, dermal, nasal and rectal routes, as described in the present paper. Cyclodextrins are promising compounds with many beneficial properties, and their use may be increasingly profitable for pharmaceutical scientists.

[Applications of synthetic and semisynthetic polymers (Kollidon K25, Kollidon K90 and Hydroksyethylocellulose) as carriers of ketoprofen in solid oral prolonged release dosage forms. The impact of selected non-ionic surfactants (Tween 80 and Rofam 70) on the release kinetics].

BACKGROUND: Hydrophilic matrices used as oral forms of sustained release drugs are a suitable application medium for short-acting nonsteroidal anti-inflammatory drugs (NSAID) - ketoprofen. A properly selected hydrophilic matrix in oral preparations may significantly increase efficacy and application safety of ketoprofen. OBJECTIVES: The aim of the research was to analyze the usefulness of polymers (synthetic Kollidon K25 and K90, semi-synthetic hydroxyethylcellulose) and calcium hydrogen phosphate dihydrate (as an inorganic filler) in manufacturing solid oral matrix forms of ketoprofen and to study of the effect of non-ionic surfactants (Tween 80, Rofam 70) on release kinetics. MATERIAL AND METHODS: Ketoprofen, HEC, Kollidon K25, and K90, calcium hydrogen phosphate, magnesium stearate. Incorporation. Studies on the tablet mass. Direct tableting. Studies on the pharmacopoeial parameters and pharmaceutical availability. Approximation of the results. RESULTS: The results of the granulometric studies on tablet mass were in accordance with pharmacopoeial standards. The results of morphological and biopharmaceutical studies of the obtained matrices (tablets) were consistent with the pharmacopoeial standards for formulations with HEC, K25 and K90. The release results most closely related to row 0 kinetics were obtained for the matrix containing HEC and K25. Tween 80 added to 0.1N HCl accelerated the release of ketoprofen, while Rofam 70 decelerated it. Tween 80 and Rofam 70 added to the pH 7.4 buffer accelerated the release of ketoprofen. CONCLUSIONS: The presented model system of preformulation studies showed the usefulness of HEC and Kolidon K25 in the technology of hydrophilic matrices with ketoprofen. Surfactants added to the medium do not affect the release rate of ketoprofen.

Diclofenac in the treatment of pain in patients with rheumatic diseases.

Diclofenac, a phenylacetic acid derivative, is a drug demonstrating high efficacy after oral administration in the treatment of pain and physical disability in rheumatic diseases. In view of the adverse effects associated with using diclofenac, it is necessary to consider all known drug safety information before the drug is selected for therapy and the dosage regimen is set for individual patients. Selecting an oral dosage form with specific properties determined by excipients is a method to improve the availability of the drug substance and, at the same time, minimize adverse drug reactions. An alternative to tablet or capsule dosage forms is diclofenac application to the skin. The proven efficacy of this method is further improved through the use of transdermal penetration enhancers and vehicle ingredients which provide dosage forms with specific physical properties.

The biomechanical characteristics of elite deaf and hearing female soccer players: comparative analysis.

PURPOSE: The aim of this study was to examine the differences in body composition, strength and power of lower limbs, height of jump measured for the akimbo counter movement jumps, counter movement jump and spike jumps between deaf and hearing elite female soccer players. METHODS: Twenty deaf (age: 23.7±5.0 years, hearing loss: 96±13.9 dB) and 25 hearing (age: 20.3±3.8 years) participated in the study. Their WHR and BMI were calculated. Body fat was measured using the BIA method. The maximal power and height of jump were measured by force plate. Biodex dynamometer was used to evaluate isokinetic isometric strength of the hamstrings and quadriceps. RESULTS: Significant differences between hearing and deaf soccer players in anthropometric values were for the waist and calf circumferences and the WHR index ( p < 0.01, effect size 0.24-0.79). Statistically significant differences were observed for flexion of the lower limb in the knee joint for the relative joint torque and relative power obtained for the angular velocity of 300 degˑs-1 for both lower limbs (p < 0.01, effect size 0.19-0.48) and for 180 degˑs-1 during flexion of the left limb (p = 0.02, effect size 0.13). The hearing female football players developed significantly greater MVC in all the cases. Statistically significant differences between deaf and hearing athletes were found for spike jump for maximal power (1828.6 ± 509.4 W and 2215.2 ± 464.5 W, respectively; p = 0.02, effect size 0.14). CONCLUSIONS: Hearing impairment does not limit the opportunities for development of physical fitness in the population of deaf women.

New Biopolymer Nanoparticles Improve the Solubility of Lipophilic Megestrol Acetate.

As many substances are poorly soluble in water and thus possess decreased bioavailability, creating orally administered forms of these substances is a challenge. The objective of this study was to determine whether the solubility of megestrol acetate, a Biopharmaceutical Classification System (BCS) class II drug, can be improved by using a newly-synthesized surfactant (Rofam 70: a rapeseed methyl ester ethoxylate) and compare it with two references surfactants (Tween 80, Pluronic F68) at three different pH values. Spectrophotometry was used to compare the solubility profiles in the presence of three tested surfactants at pH 5.0, 7.4 and 9.0. Rapeseed methyl ester ethoxylate was found to improve the solubility of the BCS Class II drug and increase its bioavailability; It increased drug solubility more effectively than Pluronic F68. Its cytotoxicity results indicate its possible value as a surfactant in Medicine and Pharmacy.

[Application of synthetic and semisynthetic polymers (Kollidon K30 and hydroxypropylmethylcellulose) as carriers of ketoprofen in solid oral prolonged-release dosage forms].

BACKGROUND: One of the most important challenges of the modern technology of solid oral dosage forms is to increase the effectiveness of the drug, reduce side effects and improve the comfort of use. One way to obtain such effects are prolonged release dosage forms. OBJECTIVES: The aim of the study was to investigate the suitability of polymers (synthetic - Kollidon K30 and semisynthetic - hydroxypropyl methylcellulose), and calcium hydrogen phosphate dihydrate - as an inorganic insoluble filler - in the construction of the matrices of the solid oral dosage forms containing non-steroidal anti-inflammatory drugs (NSAIDs). We used ketoprofen as a model active ingredient. MATERIAL AND METHODS: Ketoprofenum, hydroxypropylmethylcellulose, calcium hydrogen phosphate, kollidon K30, magnesium stearate. Incorporation. Studies of the tablet mass. Direct tabletting. Studies of the pharmacopoeial parameters and pharmaceutical availability. Measurements of the viscosity of 1% solution of HPMC and Kollidon K30. Approximation of the results. RESULTS: We obtained three versions (formulations) of the matrices. The results of the granulometric research on tablet formulations were consistent with the standards. The results of morphological studies and pharmacopoeial tablets were consistent with the standards. The best results were obtained for the release formulations containing HPMC and calcium hydrogenphoshate. Kollidon K30 accelerated the release of ketoprofen from tablets of formulation I. CONCLUSIONS: The model system of preformulation studies showed the usefulness of HPMC and Kollidon K30 in the technology of hydrophilic matrices with ketoprofen.

Nuclear factor κB inhibitor BAY 11-7082 suppresses oxidative stress induced by endothelin-1 (ET-1) in rat kidney.

AIM: The aim of the study was to evaluate the effect of BAY 11-7082, an NF-κB inhibitor, on basal and ET-1-induced production of reactive oxygen species (ROS), TNF-α and p65 protein in rat kidney. MATERIAL/METHODS: The experimental animals were divided into five groups (n=7) receiving: 1) saline (control); 2 and 3) ET-1 in a dose of 3 µg/kg body weight (b.w.) or 12.5 µg/kg b.w.; 4) BAY 11-7082 (10 mg/kg b.w.); 5) BAY 11-7082 (10 mg/kg b.w.) and ET-1 (12.5 µg/kg b.w.), respectively. In kidney homogenates the concentration of thiobarbituric acid reactive substances (TBARS), H2O2, TNF-α, p65 protein and GSH/GSSG ratio were determined. RESULTS: ET-1 resulted in a dose-dependent increase in TBARS and hydrogen peroxide (H2O2) levels, and a decrease in GSH/GSSG ratio when compared to the controls. BAY 11-7082 administered 1 h before ET-1 administration at a dose of 12.5 µg/kg resulted in a decrease (P<0.001) in TBARS and H2O2 levels and an increase (P<0.001) in GSH/GSSG ratio compared to the ET-1 groups. The level of TNF-α was increased (P<0.001) in the presence of ET-1, while BAY 11-7082 reduced the TNF-α level (P<0.001). The rats receiving BAY 11-7082 showed a decrease in NF-κB p65 protein level in the nuclear fraction and an increase in the cytoplasmic fraction. CONCLUSIONS: The results suggest that BAY 11-7082 plays a protective role against ET-1 induced oxidative stress in kidney tissue. These actions of BAY 11-7082 may result from reduced activity of NF-κB signaling pathways. Inhibition of the NF-κB pathway may be a promising strategy for preventing the progression of kidney damage.

[The Use of Synthetic Polymers (Superdisintegrants) in Technology Tablets Containing Ethanol Dry Extract from Asparagus officinalis]. / Zastosowanie syntetycznych polimerów (superdezintegrantów) w technologii tabletek zawierajacych etanolowy suchy wyciag z Asparagus officinalis.

BACKGROUND: Dry extracts are now frequently used in medicine as an alternative to synthetic drugs. In the case of tablet technology with dry plant extracts, the proper selection of disintegrants (superdisintegrants) is particularly important. Objectives. The aim of this study was to evaluate the usefulness of the polymers constituting superdisintegrants (Vivasol®, Vivastar®, Polyplasdone XL) in uncoated tablet formulation of alcoholic extracted from Asparagus officinalis. MATERIAL AND METHODS: Dry the ethanol extract of Asparagus officinalis, Vivasol®, Vivastar®, Vivapur®, Kollidon VA64, Polyplasdone XL, magnesium stearate. Direct compression. Paddle method was carried out to study pharmacopoeial parameters and pharmaceutical availability. The calculation of equivalency factors: similarity [f2] and the difference [f1]. Approximation results. RESULTS: Tablets brownish-green, with a smooth and uniform surface, without stains, chipping and damage. The determined average weight of the tablets compiled with the standards. The test friability and crushing strength revealed that the most mechanically strong tablets contained Vivasol, Vivastar, Polyplasdone XL. These tablets also have a longer disintegration and dissolution time compared with tablets containing only Vivasol. These differences are also confirmed by the calculated f2 and f1. CONCLUSIONS: The addition of a mixture of Polyplasdone XL and Vivastar to Vivasol significantly increases the mechanical strength of the tablets (crushing strength, resistance to crushing). The addition of a mixture of Polyplasdone XL and Vivastar to Vivasol paradoxically increases the disintegration time of tablets (11.1 min). Single superdisintegrant breaks up the tablet more effectively than a mixture of superdisintegrants.

The role of endothelin-1 and endothelin receptor antagonists in inflammatory response and sepsis.

Endothelin-1 (ET-1) is a potent endogenous vasoconstrictor, mainly secreted by endothelial cells. It acts through two types of receptors: ETA and ETB. Apart from a vasoconstrictive action, ET-1 causes fibrosis of the vascular cells and stimulates production of reactive oxygen species. It is claimed that ET-1 induces proinflammatory mechanisms, increasing superoxide anion production and cytokine secretion. A recent study has shown that ET-1 is involved in the activation of transcription factors such as NF-κB and expression of proinflammatory cytokines including TNF-α, IL-1, and IL-6. It has been also indicated that during endotoxaemia, the plasma level of ET-1 is increased in various animal species. Some authors indicate a clear correlation between endothelin plasma level and morbidity/mortality rate in septic patients. These pathological effects of ET-1 may be abrogated at least partly by endothelin receptor blockade. ET-1 receptor antagonists may be useful for prevention of various vascular diseases. This review summarises the current knowledge regarding endothelin receptor antagonists and the role of ET-1 in sepsis and inflammation.

Usefulness of Rosen's postulate for studying the relationship between the structure of cholic acid oxyethylation products and the process of solubilization of lipophilic therapeutic agents (BCS class II and IV) in aqueous solutions in equilibrium.

We verified the usefulness of "Rosen's postulate", i.e., the logarithm of reciprocal concentration of surfactant--log(1/cPi=20) by which the surface tension of a solution can be decreased by 20 mJ/m2 in relation to water (physiological value gamma25 = 48-52 mJ/m2) in the evaluation of the applicatory properties of cholic acid oxyethylation products. Moreover, the values of deltaG0m for solubilizers and their micellar adducts with diclofenac, naproxen, and loratadine constituted the basis for estimating the thermodynamic value of "Rebinder's effect", associated with change in the state of matter of therapeutic agent. We determined critical micellar concentration for the aqueous products of oxyethylation and for micellar adducts with diclofenac, naproxen, and loratadine, and used these values to calculate (thermodynamic potential of micelle formation).

[Endothelin receptor antagonists--a brief description of the new class of drugs]. / Antagonisci receptorów endotelinowych (ERA)--krótka charakterystyka nowej grupy leków.

Endothelins are endothelial peptides, the properties of which have been investigated for over 25 years. They play a special role in the pathophysiology of many diseases of the cardiovascular system. Endothelin-1, which is the most explored one, is a potent vasoconstrictor. It increases renal water and sodium excretion, augments cell growth and proliferation and has proinflammatory activity, by intensifying the production of reactive oxygen and nitrogen species (ROS and RNS). ET-1 takes part in the progression of such diseases as hypertension, atherosclerosis, heart and renal failure. The physio- and pathological effects of endothelins are mediated through ETA and ETB receptors. Blocking these receptors, in particular the ETA receptor, can prevent negative effects of endothelins. Long-term efforts to create drugs which act like that have brought relevant results. Endothelin receptor antagonists (ERA) are a new class of medicines, which are indicated in the treatment of pulmonary arterial hypertension. There are also optimistic results of trials with ERA administered in other disorders. On the basis of these data we may conclude that there will be more indications for this group of drugs. This review discusses properties and new research directions of ERA registered in pharmacotherapy.

Surface activity of novel surface active compounds, products of catalytic oxyethylation of cholic acid and their micellar adducts with selected lipophilic therapeutic agents.

The aim of this study was to determine the surface activity parameters of novel surface active compounds, products of catalytic oxyethylation of cholic acid, and their micellar adducts with selected lipophilic therapeutic agents (diclofenac, loratadine, naproxen and rutin). High solubility of lipophilic naproxen was observed in the environment of aqueous solutions of the cholic acid oxyethylation products as suggested by determined factual solubility and the value of micellar partition coefficient (K(w)(m)). Determined surface activity of surfactants described by various physicochemical characteristics (gamma(cmc)(25), cmc, deltaG(m)(o) and A(m)) suggested their compatibility with physiological values of the surface activity of plasma (48.0-52.0 mJ/m2) and lacrimal fluid (46.0-52.0 mJ/m2). Calculated values of HLB(1)(HNMR) and n(TE) of the micellar adduct in solid phase (solid dispersion) corresponded to an increase in its hydrophilicity, and, therefore, suggested possible mechanisms and site of diclofenac, loratadine, naproxen and rutin solubilization in the micellar structure (core or palisadic layer).

[The use of semi-synthetic polymers in the formulation of sucking and chewable tablets containing sage extract and zinc gluconate]. / Zastosowanie pólsyntetycznych polimerów w formulacji tabletek do ssania i zucia zawierajacych ekstrakt z szalwii i glukonian cynku.

BACKGROUND: Halitosis and gingivitis are most common pathologies (15-60% of population) which, if left untreated, lead to periodontal diseases and tooth loss. OBJECTIVES: The aim of this study was to develop, based on polymers of dry sage extract and zinc gluconate, tablets intended for sucking and chewing that can be applied in the treatment of halitosis and gingivitis. MATERIAL AND METHODS: Dried aqueous sage extract, zinc gluconate, Pharmagum M, Prosolv SMCC90 and SMCCHD90, Vivapur 102, sorbitol, mannitol, ludipress. Direct tableting. Testing pharmacopeial parameters and pharmaceutical availability (using basket and rotating disk methods) of tablets intended for sucking and chewing. Approximation of the obtained results. RESULTS: Grey and green color tablets were obtained with smooth and uniform surface, without stains, spalls or mechanical damage. The determined average mass (weight) of a tablet complied with the standard. The friability and crushing strength test revealed that tablets containing Prosolv SMCCHD90, Vivapur 102 and mannitol demonstrated the highest mechanical strength. Tablets containing these substances and intended for sucking had prolonged disintegration and release time. Tablets intended for chewing had a hardness at the level of 124 N.They demonstrated compressibility, low friability and prolonged release. The release profiles of tablets intended for sucking (v2) and those for chewing, obtained by basket and rotating disk methods, were similar. CONCLUSIONS: The addition of Prosolv SMCCHD90, Vivapur 102 and mannitol increased significantly the mechanical strength (higher hardness, lower friability), prolonged the disintegration time and slowed the release from the obtained tablets intended for sucking and chewing. The application of Prosolv SMCCHD90 in the formulation of tablets for chewing carries the risk for sorption of active components to the polymer structure. This process takes place in the early stage of the release. Rotating disk method used in pharmaceutical availability testing gives better results while analyzing the phenomenon than the standard basket method. The suggested and tested formulations of tablets intended for sucking and chewing may be used as an alternative to formulations containing dried titrated extracts from plants of antimicrobial activity (sage - Salvia officinalis) in combination with substances binding volatile sulfur compounds (zinc gluconate).

Surface-active agents from the group of polyoxyethylated glycerol esters of fatty acids. Part III. Surface activity and solubilizing properties of the products of oxyethylation of lard (Adeps suillus, F.P. VIII) in the equilibrium system in relation to lipophilic therapeutic agents (class II and III of BCS).

Research was conducted into the solubilization processes of diclofenac, ibuprofen, ketoprofen and naproxen in equilibrium conditions in the environment of aqueous solutions of oxyethylated lard's fractions (Adeps suillus, Polish Pharmacopoeia VIII). The determined thermodynamic (cmc, deltaGm(0)) and hydrodynamic (R0, R(obs), omega, M(eta)) parameters characterizing the micelle of the solubilizer and the adduct demonstrate that lipophilic therapeutic agents are adsorbed in a palisade structure of the micelle due to a topologically created so-called "lipophilic adsorption pocket". This shows that the hydrophilicity of the micelle and the adsorption layer decreases at the phase boundary, which is confirmed by the calculated values of coefficients A(m) and r x (a). The results obtained indicate the possibility of making use of the class of non-ionic surfactants which are not ksenobiotics for the modification of the profile of solid oral dosage forms with lipophilic therapeutic agents from the II class of Biopharmaceutics Classification System (BCS).

Solubilizing properties of new surface-active agents, products of catalytic oxyethylation of cholic acid.

Solubilizing properties of aqueous solutions of a series of surface-active agents, products of oxyethylation of cholic acid, were examined in the present study. The content of oxyethylated segments determined by means of the 1H NMR method enabled the verification of the molecular mass of surfactants along with the calculation of the structural hydrophilic-lipophilic balance (HLB), the solubility parameter delta1/2, and the required solubility level of balance HLB(R). Viscosimetric measurements enabled the calculation of the limiting viscosity number, the content-average molecular mass, the effective volume, the hydrodynamic radius of the surfactant micelle and their equilibrium adducts with rutin, diclofenac and loratadine (BCS Class II and III). By means of the spectrophotometric method (UV) the amount of the solubilized diclofenac, loratadine and rutin (rutoside) was determined in the equilibrium system (saturated solution) in the environment of aqueous solutions of cholic acid derivatives of n(TE) = 20-70. The obtained results serve as a basis for determining the solubilization mechanism of lipophilic therapeutic products and indirectly for estimating the influence of the above process on pharmaceutical as well as biological availability of a micellar adduct from model drug forms (Lindbladt lithogenolitic index).