Osmotic Activity of Drugs is an Important Factor of Their Local Action at the Injection Site: What We Don't Use to Prevent Post-Injection Abscesses

It is established that very few modern high-quality drugs in the dosage form "Solution for injection" have isoosmotic activity in the range of 280-300 mosmol/l of water. The main part of solutions for injection is hypotonic or hypertonic solutions, which can have osmotic activity in the range of 0 - 4000 mosmol/l of water. The reason for this was that the osmotic activity of drugs is not included in the list of controlled indicators of drugs quality, so it is not subject to control. It is shown that the osmotic activity of drug solutions increases with an increase in the total concentration of all dissolved ingredients present in the solution. It was found that an excessively high concentration of the drug in the solution gives it an excessively large hyperosmotic activity, which can cause a local irritant and cauterizing effect at the injection sites due to dehydration of the cells. Therefore, to exclude post-injection abscesses, it is proposed to dilute the hypertonic drug with water for injection until it is given isotonic activity.

Prediction of the Osmotic/activity Coefficients of Alkali Hydroxide Electrolytes

<div><div><div><p>The osmotic/activity coefficients are one of the most fundamental and important properties of electrolyte solutions. There is currently no reliable means of predicting them from first principles without relying on extensive fitting to experimental measure- ments. The alkali hydroxide aqueous electrolytes are a particularly important class of solutions due to the crucial role they play in a vast range of applications. Here, for the first time we predict the osmotic/activity coefficients of these solutions without any fitting using a previously developed continuum solvent model of ion–ion interactions with no modifications. The feasibility of making these predictions with first princi- ples molecular simulation is also assessed. This demonstrates the reliability of this continuum solvent model and provides a plausible pathway to the fast and accurate prediction of these important properties for a wide range of electrolyte solutions.</p></div></div></div>

APPROACHES TO THE SELECTION OF EXCIPIENTS FOR DENTAL GEL WITH CETYLPYRIDINIUM CHLORIDE

The aim of the study was to determine the excipients influence on the characteristics of gels with cetylpyridinium chloride and to select the dental gel formulation gelation agents promising for the development of dental gel compositions. Hereby, the properties of the active pharmaceutical ingredient, characteristics of the specific gelation agents, as well as their influence on stability, biopharmaceutical and application properties of gels, were taken into account. Materials and methods. In this study, polymers with various gelation mechanisms were considered. Their compatibility with cetylpyridinium chloride as well as storing kinetic and colloid kinds of stability, pH of aqueous solutions, spreadability and textural properties, a penetration ability by the agar diffusion method, an osmotic activity and rheological properties of the gels, were examined. For a complex evaluation of gel compositions study results, a desirability function was used.Results. Stable homogenous dental gels with cetylpyridinium chloride can be obtained by using 25% poloxamer 407 and 5.0% high molecular weight chitosan as the basis.The addition of poloxamer 188 to high molecular weight chitosan gels can produce stable systems with improved textural characteristics as well as increase their osmotic activity. Agar and low molecular weight chitosan addition significantly decrease, whereas poloxamer188 and various molecular weight polyethyleneglycol increase the osmotic activity of 25 % poloxamer 407 gels which are also characterized by a high penetration ability.Conclusion. A complex evaluation of biopharmaceutical, physicochemical and application properties of the gels made it possible to establish that combinations of poloxamer 407 with polyvinylpyrrolidone, agar, and low molecular weight chitosan, can be recommended as a base for a dental gel with cetylpyridinium chloride.

THE DEVELOPMENT OF BISCHOFITE ANTI-SCAR GEL COMPOSITION

The development of an external gel containing purified bischofite will allow the scars treatment in the stage of prevention and formation due to the effect on various links of pathological wound healing. This study’s aim was the development of a gel with bischofite for the scars prevention and treatment. Bischofite brine from the purified Volgograd deposit was selected as the active pharmaceutical substance. Polymer gelling agents: methylcellulose-100, sodium carboxymethyl cellulose, hydroxymethyl cellulose, aerosil, Tizol®. The QTPP requirements for developed bischofite gel are aimed at effective wound healing and prevention of pathological scarring, which corresponds to the ointments used at the III stage of the wound process. Comprehensive technological studies of model samples of gels with bischofite were carried out: determination of external signs and the application to the skin, smearing, thermal stability and pH, study of osmotic activity and release of bischofite (in terms of magnesium ions). The maximum amount (8 points) was observed in the composition using the Tizol® gel-forming agent, the model sample based on it provided the maximum degree of release, minimal osmotic activity, and good smearing. In addition, Tizol® possesses anti-inflammatory activity. The optimal concentration of the aqueous phase is justified by the assessment of the consistency properties, the spreadability and rheological properties. Thus, as a result the composition of the bischofite gel was developed using Tizol® as a base, containing glycerin as a plasticizer and a moisture agent, the preservative sodium benzoate and purified water.

On the Issue of Creating a Cream of Reparative Action for the Treatment and Prevention of Cheilitis

BACKGROUND: Cheilitis is an inflammatory disease of the lips, its red border, mucous membranes, and skin. There are meteorological, actinic, hypo-, and avitaminosis cheilitis, according to medical indications. Classification of cheilitis includes many types of diseases and is somewhat conditional. For these types of cheilitis treatment are most appropriate to use biologically active substances, in particular lipophilic extract of bee pollen. Lipophilic extract of bee pollen is a complex, concentrated plant-bee product with unique consumer and medicinal qualities. It should be noted that experiments have shown that the bee pollen lipophilic extract has a reparative effect higher than the widespread sea buckthorn oil. AIM: The aim of the work is to create therapeutic and prophylactic cream with lipophilic extract of bee pollen for the cheilitis treatment and prevention. MATERIALS AND METHODS: Cream preparation was conducted by phase inversion. Thermal and colloidal stability, pH values, the quantitative content of carotenoids, viscosity, osmotic activity, and microbiological purity were determined by generally accepted methods. RESULTS: Samples of the cream containing lipophilic extract of bee pollen are a homogeneous mass of soft consistency with light yellow color and pleasant specific odor. In estimating, the thermal stability cream samples cheilitis curing were successfully tested and proved to be stable. When centrifuging, the absence of stratification of the cream into fatty and aqueous phases after the test has showed the stability of the cream. The pH of the cream samples corresponds to the pH of the skin. During a qualitative test green color indicates the presence of carotenoids. Quantitative determination of the carotenoids amount in the cream for treatment and prevention cheilitis (in recalculation to β-carotene) corresponds to the set content of carotenoids in the cream of 5.4 mg. The viscosity of the developed cream at 16.2 s−1 is 68.38 ± 0.21 Pa x s, that fully corresponds to the viscosity of creams. In the study of osmotic activity, it was found that the cream with a glycerol content of 7% provides moderate osmotic activity of the drug for 8 h, which may indicate the absence of overdrying and irritating effect. In terms of microbiological purity, the investigated cream with lipophilic extract of bee pollen meets the requirements of the State Pharmacopoeia for finished medicines for topical use (category 2). CONCLUSION: For the cheilitis treatment and prevention has suggested the composition of the cream which contains biologically active substance – lipophilic extract of bee pollen. The technology of the cream with lipophilic extract of bee pollen was developed. Thermal and colloidal stability, pH values were studied; the quantitative content of carotenoids, viscosity, osmotic activity, and microbiological purity was determined. The research carried out made it possible to make sure of the correctness and rationality of the developed technology of the cream for the treatment and prevention of cheilitis.

Study of the kinetics of benzidamine hydrochloride release from topical sprays in an in vitro experiment

Inflammatory processes accompanied by a sore throat are a widespread symptom of both infectious and non-infectious genesis. In this case, topical therapy with medications that combine anti-inflammatory and analgesic effects, in the form of comfortable dosage forms — sprays, is the most effective. In this case, the used drug has a complex effect on contact tissues, due to both the actual pharmacological activity of the pharmaceutical substance and the physico-chemical properties of the excipients forming the dosage form. A study of the release of the active substance from sprays in the perspective of their topical application, as well as their osmotic activity in an in vitro experiment that simulates the process of application to the throat mucosa, was carried out. The real influence of the osmotic activity of the dosage form on the degree of release of the active substance due to the multidirectional nature of the resulting diffusion flows is shown.

Prediction of the Osmotic/activity Coefficients of Alkali Hydroxide Electrolytes

<div><div><div><p>The osmotic/activity coefficients are one of the most fundamental and important properties of electrolyte solutions. There is currently no reliable means of predicting them from first principles without relying on extensive fitting to experimental measure- ments. The alkali hydroxide aqueous electrolytes are a particularly important class of solutions due to the crucial role they play in a vast range of applications. Here, for the first time we predict the osmotic/activity coefficients of these solutions without any fitting using a previously developed continuum solvent model of ion–ion interactions with no modifications. The feasibility of making these predictions with first princi- ples molecular simulation is also assessed. This demonstrates the reliability of this continuum solvent model and provides a plausible pathway to the fast and accurate prediction of these important properties for a wide range of electrolyte solutions.</p></div></div></div>

Prediction of the Osmotic/activity Coefficients of Alkali Hydroxide Electrolytes

<div><div><div><p>The osmotic/activity coefficients are one of the most fundamental and important properties of electrolyte solutions. There is currently no reliable means of predicting them from first principles without relying on extensive fitting to experimental measure- ments. The alkali hydroxide aqueous electrolytes are a particularly important class of solutions due to the crucial role they play in a vast range of applications. Here, for the first time we predict the osmotic/activity coefficients of these solutions without any fitting using a previously developed continuum solvent model of ion–ion interactions with no modifications. The feasibility of making these predictions with first princi- ples molecular simulation is also assessed. This demonstrates the reliability of this continuum solvent model and provides a plausible pathway to the fast and accurate prediction of these important properties for a wide range of electrolyte solutions.</p></div></div></div>

Hydrogen peroxide discolors blood in the cavity of the hematoma under the nail and in the skin over the bruise

Purpose. Modern medical standards do not contain information about the urgent bleaching of nail hematomas and bruises. The aim of this work is developing of new ways and means for blood bleaching of the bruising and subungual hematomas for its immediate discoloration. Materials and methods. The peculiarities of hydrogen peroxide effect on blood color alteration in different environment have been studied in laboratory, by experiment and in clinical conditions. We studied the peroxide effect on liquid and dry venous blood in a Petri dishes, in bloody gauze bandages, on the surface of the skin, in hematoma under the nail in humans and in the skin over the bruise created by intradermal injection of pig blood. The studies take into account the role of local interaction such factors as the duration of interaction, the concentration of ingredients, local temperature, the value of alkaline and osmotic activity of the studied solutions. The results were recorded by color photo and video. Results. In laboratory and experimental conditions the red and blue blood as well as red, brown and/or blue stained tissues were shown to be urgently bleached by alkaline solutions of hydrogen peroxide. Hemoglobin was found to be the «dye» of blood-stained tissues. We listed the inventions to the intradermal bruising discoloration, subungual hematomas, and fresh and dried blood. The main ingredients of the inventions for intradermal and subungual hematomas bleaching are reported. The essence of the invented methods of skin and nail hematomas discoloration is presented. Conclusion. The alkaline solution of hydrogen peroxide can be used for emergency discoloration subungual hematoma, the skin in the area of bruise and the bandage stained with blood.