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Introduction: Common ivy (Hedera helix) is a plant used successfully in the treatment of various ailments. This is possible owing to the unique set of substances contained in it such as large amount of saponins, flavonoids, phenolic acids and phytosterols as well as polyacetylenes and coumarins. All these substances have been used in the production of cosmetic and medicinal preparations. Clinical trials on the efficacy and safety of dry ivy leaf extract have shown its high efficacy, comparable to synthetic medications, and better tolerance of herbal drugs.

Preformulation studies were carried out to estimate the solubilization capacity of products of catalytic oxyethylation of triglyceride fractions extracted from the pharmacopoeial lard (Adeps suillus, PP XI). There were determined basic viscosity ([η], Mη and hydrodynamic (Ro, Robs., O) values of micellar solutions of oxyethylated derivatives as well as their surface activity - γcmc25. Critical micellar concentration (cmc) was used to calculate the thermopotential for the formation of micelles (ΔGom). Model studies on micellar solubilization of gemfibrozil, loratadine and valsartan from the solid body surface (phase boundary) were performed under equilibrium conditions at the surfactant concentration of cexp >> cmc. The amount of dissolved lipophilic therapeutic agents with qualitative and quantitative involvement of micellar solubilization was determined by spectrophotometry: (UV) method - cΙsΙ (mg/100 mL) as well as by calculating the solubilization indices - nΙsΙ (mol/mol). The research study has identified structures of oxyethylated derivatives of triglyceride fractions which selectively and effectively solubilize gemfibrozil, loratadine and valsartan from the solid surface in the equilibrium system. The obtained results are a technological inspiration to create a model form of the drug (tablet) with continuous dispersion of lipophilic therapeutic agents (gemfibrozil, loratadine and valsartan), obtained on the basis of the liquefied surfactant structure. [ABSTRACT FROM AUTHOR]

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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).

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).

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).

The catalytic oxyethylation products of Lard's fractions and Tweens--as a reference products, were analised by chromatographic analysis HPLC and GPC. The above part was determination average molecular weights dispersion (Mw I Mn) and the content of polyethylene glycols (PEG), which are obtained during catalytic oxyethylation, and determination iodine value of the product (L(J2)). Viscosity measurements were carried out by Ubelohde method and enabled determination of basic viscosity and hydrodynamic parameters. The obtained results indicate that, comparing reference products--polysorbates, Tweens, products of triglycerides oxyethylation contain significantly less, in some cases very small amount of polyethylene glycols (PEG), and also maintained a high amount of unsaturated fatty acids (oleic acid), which is proven by the iodine value. Numerical value n(s) /H2O/ confirms important disparity of micells palisad structure, which are created based on oxyethylated triglycerides nTE = 40. That indicates significant solubilization possibilities of their aqueous solutions Cexp < or = Cmc.

Various methods of chromatographic analysis (GPC, HPLC, TLC) were used to estimate qualitatively and quantitatively the product of oxyethylation of rapeseed oil acid methyl esters (RME). The investigation enabled to evaluate PEG content in the product. The method of eliminating insignificant quantity of PEG found in oxyethylation products of n(TE) < or = 20 was presented. The data of thin-layer chromatography obtained in the course of research constitute a point of departure for calculating n(TE) content and HLB level.

Research was conducted into the properties and identity of the oxyethylenation products of triglycerides derived from Lard (Adeps suillus) using original, stereoselective catalyst K-4. Determined of drop-point temperature -Tk (273.15 + t degrees C) allowed for calculation coefficients of volumetric dilatability--alpha (v0), linear dilatability--alpha(l0) as well as structural viscosity of the product (eta) in the state of equilibrium liquefaction. The solubility parameter delta(1/2) and the required numerical value of HLB(R )were calculated for oxyethylated product's fractions. The number of oxyethylated segments -n(TE) was determined by 1HNMR method, it made possible to estimate the weight-average molecular mass Mw, and also structural (m. Griffin) and analitycal (m. 1HNMR) level of hydrophilic/lipophilic balance--HLB. The results obtained in the course of research served as a basis for determine application properties of oxyethylated products of triglycerides fractions, in particular for the purpose of examination them for using as a transdermal passage promotors and micellar solubilizers for lipophilic therapeutic agents belonging to BCS Class II and III.

The production technology of powder cellulose (Arbocel) and microcrystaline cellulose (Vivapur) and their application in the composition of direct compression tablet mass was provided. The function of silicified microcrystaline cellulose type Prosolv in the direct compression process of dry plant extract was discussed. An analysis of the chemical structure of cellulose fiber (Vitacel) enabled determining its properties and applications in the manufacture of diet supplement, pharmaceutical and food products.

The morphological and structural properties of basic types of starch used as excipients in solid drug form technology with reference to its bioadhesive properties with fully polymer biodegradation. The production technology and application of: carboxymethyl starch (CMS), pregelled starch, hydroxyethyl starch (HES), hydroxypropyl starch (HPS) and the share of modified starch in technology of selected food products is provided. The authors focus on hydroxyethyl starch, which is used not only as blood and plasma substitution but also as drug camouflage agent in sports competition. In papers were presented based on literature data actually used types of starch and their chemical modifications products in drug forms and food technology.

A metod of refininig technical Rokopols, products of copolymerization of ethylene oxide and propylene oxide of 30p160, 30p27 and 30p10 type was developed. The course of the relation between R(f)(R(m)) and the number of oxyethylene segments n(TE) in the molecule of the homological series ofpolyethyleneglycols (PEG) was used to examine the content of n(TE) in the refined fractions of Rokopols. For the aqueous solutions of Rokopols weight-average molecular mass M(w) was calculated and the surface tension coefficient gamma25 was determined on the basis of the stalgmometric method. The value of the critical micellar concentration (cmc) and the thermodynamic potential for micelle formation (DeltaG(m)(0)), which facilitates the assessment of the solubilizing abilities of the investigated class of copolymers, were estimated.

Research was conducted into the properties and identity of the products oxyethylenation of cholesterol, which were obtained with the use of a selective catalyst (K-4) and standard alkaline catalyst (Na/NaOH). The 1HNMR method was employed to assess the content of oxyethylated segments and the analytic level of hydrophilic--lipophilic balance (HLB). Basic viscosity and hydrodynamic values were determined for the solubilizers and their micellar adduct with ibuprofen, ketoprofen, naproxen and cholesterol. In addition, the amount of solubilized therapeutic agents and cholesterol as well as the micellar partition coefficient--K(m)w. was estimated. The results obtained in the course of research served as a basis for determining the solubilization mechanism and the stability of the micellar adduct for the purpose of application.

The aim of the carried out investigations was to establish relation between rheological parameters of market hydrogels containing ibuprofen and therapeutic agent diffusion coefficient dependent on their prescription. An attempt was made to estimate rheological parameters (structural viscosity, kinetics of volatile components loss) effect on pharmaceutical availability Q and the order of the process of mass exchange through artificial and natural phase boundary. Designed for skin anti-inflammatory hydrogels containing ibuprofen in the form of hydrotropic adduct with lysine (Ibufen, Dolofast), in the form of sodium salt (Nurofen) and in the form of molecular fragmentation of acidic form (Dolgit) were tested. The rate of volatile components loss was estimated with gravimetric method, viscosity measurements of therapeutic agents aqueous solutions were performed with Ubbelohde viscosimeter, while hydrogels rheological parameters - with cone-plate digital rheometer. The rate of ibuprofen penetration through phase boundary (Viscing dialysis membrane and pig perimastoid dermis) into dialysis fluid was determined in vitro. The kinetics of this process was monitored by measuring electric conduction Deltalambda = f(t) of model dialysis fluid. Viscometric measurements of aqueous solutions of ibuprofen lysine salt and ibuprofen sodium salt, by determining boundary viscosity gradient GLL(eta) and calculation of hydrodynamic radius Robs, enabled the applicative solution of Einstein-Smoluchowski equation (D = kT/6Pi r eta) and the estimation of structural value of therapeutic agent diffusion coefficient. Tracing the dependence between diffusion coefficient and shear rate enabled to recognize the preferences of preparations to the process of mass exchange on the phase boundary. An association was confirmed between the determined and calculated rheological parameters and the process of mass exchange on phase boundary through selected dialysis membranes. Mass exchange on phase boundary was found to be the derivative of the process of diffusion and its quantitative aspect depends on the kind of the applied membrane (it is the function of the quantity of statistically distributed pores on the unit of its surface [cm2]). Ibuprofen penetration through an artificial and natural phase boundary is complex. Its mechanism is between the kinetics of "0" and "II" order. The quantitative differentiation of the process of mass exchange between hydrotropic ibuprofen forms: ibuprofen lysine salt > ibuprofen sodium salt > ibuprofen in the form of acid molecule results from the carried out experimental study.

Research was conducted into the properties and identity of the products of Croda-type hypoallergenic lanolin, which were obtained with the use of a selective catalyst (K-4) and a standard alkaline catalyst (Na/NaOH). The 1HNMR method was employed to assess the content of oxyethylated segments and the analytic level of hydrophilic-lipophilic balance (HLB). Surface activity of products soluble in water with n(TE) > or = 40 was examined and the thermodynamic potential for micelle formation deltaGm(o) was calculated. Basic viscosity and hydrodynamic values were determined for the solubilizers and their micellar adduct with ibuprofen, ketoprofen and naproxen. In addition, the amount of solubilized therapeutic agents c/s/ was examined by means of the spectroscopic method and the micellar partition coefficient--Kw(m) was estimated. The results obtained in the course of research served as a basis for determining the solubilization mechanism and the stability of the micellar adduct for the purpose of application. This enabled the commencement of technological work on the design and manufacture of a model dosage form administered to the skin and containing the products of lanolin oxyethylation.

A new class of non-ionic surface-active agents were synthesized by means of oxyethylation of ursodeoxycholic acid (UDOCh acid) with the application of modified generation of catalysts in the form of a model prodrug. Basic viscosity values ([eta], Meta, Ro, Robs., Omga) as well as the analytic level of hyrohilic-lipophilic balance HLB in the notation of Griffin, Davies and 'HNMR method were determined. In the state of equilibrium the solubilizing properties of aqueous solutions of the products of oxyetyenation of UDOCh acid x nTE were estimated with respect to non-steroidal therapeutic agents such as diclofenac, ibuprofen, ketoprofen, and naproxen. The surface activity of solubilizers of UDOCh acid > or = nTE = 30 type and the thermodynamic stability deltaGm of an adduct emerging in the state of equilibrium were determined.

The process of the equilibrium solubilization of nonsteroidal anti-inflammatory drugs (NSAID), viz. diclofenac and naproxen, by Rofams, ie. the products of the oxyethylenating of the rape oil fatty acid methyl esters, in the environment of water solutions NaCl 9 g/l, H3BO3 19 g/l, KNO3 16 g/l, was tested. The solubilization activity of Rofam aqueous solutions was estimated with the use of the spectrophotometric method by means of the determination of the amount of the solubilized NSAID. The calculated apparent solubility of Rofam aqueous solutions was the basis for the estimation of the micellar partition coefficient K(w)m. The course of the ratio of the solubilized naproxen and diclofenac in the function of the solubilizer (Rofam R-13, R-15, R-17) exposure concentration was described by means of approximative equations with a high correlation coefficient.

The process of equilibrium solubility of sterols (cholesterol, cholic acid, hydrocortisone) by aqueous solutions of Rokanols was investigated. Critical micellar concentration (cmc) and thermodynamic potential of micellarization (deltaG(m)0) were determined for aqueous solutions of Rokopols RF-55, RF-33, TG-500 and R-330. The solubility activity of aqueous solutions of Rokopols was defined by calculation from the viscosity measurements of solubility index n(sol) for cholesterol, cholic acid and hydrocortisone. The amount of solubilized hydrocortisone by Rokopol micelles was determined by a spectrophotometric method.

Systematic research has been conducted on the products of catalytic oxyethylenation of lanolin. The level of hydrophilic-lipophilic balance HLB and the amount of oxyethylene segments nTE in homologous series of products were determined by means of the 1HNMR method. Viscosity and spectrophotometry measurements were used to determine solubilization indices n/s/, the micellar partition coefficient K(m)w, and the solubility quotient i25(r) of diclofenac in aqueous solutions of surfactants. The determination of basic viscosity values enabled identification of the solubilization site of diclofenac molecules. For the purpose of application, the relationship between the amount of oxyethylene segments nTE and K(m)w of diclofenac determined in an equilibrium system was defined.