DEVELOPMENT OF NITROFURAN DERIVATIVE: COMPOSITION AND TECHNOLOGY OF EFFERVESCENT TABLETS WITH SOLID DISPERSIONS

Taking into account the current Product specification file, the aim of the work was to develop the composition and technology for obtaining effervescent tablets based on solid dispersions of furazolidone in the form of an aqueous solution for external use.Materials and methods. The used substances were: furazolidone, anhydrous sodium carbonate (chemically pure), polyvinylpyrrolidone-24000±2000 (chemically pure), malic acid (analytically pure), tartaric acid (chemically pure), citric acid (chemically pure), sodium benzoate (chemically pure), ethyl alcohol 96% (chemically pure), purified water. Preparation of granulates is separate wet granulation in a fluidized bed (Mycrolab, BOSCH, Germany). Obtaining tablets is the process of pressing on a manual hydraulic test press ("PRG", VNIR, Russia). The dependence of disintegration, abrasion capacity and crushing resistance on compacting pressure was investigated. Technological parameters of granulates, еру obtained effervescent tablets, shelf life and storage conditions were investigated according to the State Pharmacopoeia of the Russian Federation XIVth ed.Results. Two compositions of effervescent tablets containing solid dispersions of furazolidone as an active substance were obtained, which, when dissolved in 100 ml of water at room temperature (20°C), form a solution of furazolidone with a concentration of 0.004% in less than 5 minutes. The method of quantitative determination of the furazolidone content in the effervescent tablets was validated. A complex of physicochemical methods for the analysis of tablets was carried out. Quality standards have been developed. The developed compositions stability of instant tablets during storage during accelerated and long-term tests has been experimentally confirmed. The preliminary shelf life and storage conditions have been determined.Conclusion. The result of technological and chemical-pharmaceutical research is the creation and evaluation of the quality of a new instant furazolidone dosage form as effervescent tablet formulations

Development of Composition and Technologies of Dental Gel of Meloxicam

BACKGROUND: Dental gels have several advantages over other oral dosage forms. Being a viscoplastic dosage form, the gel, when applied to the damaged area of the gum or mucous membrane, creates a protective film, preventing mechanical irritation, and providing a localized effect of the drug components. AIM: The aim of this work was to develop the composition and technology of the dental gel of meloxicam, the study of the main technological and consumer characteristics, as well as the local irritating effect of the dosage form. METHODS: Dental gels were prepared using purified water, alcohol, glycerol, and buckthorn oil as solvents, gelling agents used were: Hydroxyethylcellulose Natrosol® 250 HHX Pharm, Carbopol® 974P NF Polymer, and solubilizer Poloxamer 407 (Lutrol® F 127). The bioadhesive component and Noveon® Polycarbophil component were used for dental gel preparation. Aspartame was used as sweetener. Menthol and ascorbic acid were used to correct the organoleptic properties of the pharmaceutical composition. The formulated dental gel of meloxicam at a concentration of 7.5% was evaluated for organoleptic properties, pH, rheological characteristics, bioadhesive properties, and stability under the accelerated aging period. The in vivo local irritant effect was evaluated using ten rabbits by cutaneous, subcutaneous, subconjunctival administration, as well as application to the upper palate. RESULTS: Based on the results of studying technological and organoleptic properties, the optimal composition based on the Natrosol® 250 HHX hydroxyethylcellulose gelling agent, glycerol solvent, and purified water in the ratio 1/5 was selected, the composition contains Noveon® bioadhesive in an amount of 2%. The composition has good taste, pH close to pH of saliva has high bioadhesive properties, satisfactory rheological characteristics. The shelf life of the experimental series by accelerated aging was 2 years. The selected composition does not have a local irritant effect. CONCLUSION: A new dosage form of meloxicam was developed – a gel for use in dental practice

Synthesis, structure, and antimicrobial activity of (carboxyalkyl)dimethylsulfonium halides

© 2017, Pleiades Publishing, Ltd. Reactions of a series of ω-halocarboxylic acids (2-bromo-, 2-chloroethanoic, 3-bromo- and 3-chloropropanoic) with dimethyl sulfide resulted in the formation of stable (carboxylalkyl)dimethylsulfonium bromides and chlorides. Composition and structure of the salts obtained were established by a complex of chemical, physical and physicochemical methods. The sulfonium salts obtained showed high antibacterial and antimycotic activities with respect to the pathogenic microflora of humans and animals

Development of composition and technologies of dental film with ketorolac trometamine

The report presents the results of the development of dental films with ketorolac trometamine based on the natural biodegradable polymers from the groups of sodium alginates and xanthan gums in combination with lightly crosslinked acrylic polymer carbopo

Effect of Solid Dispersions on the Dissolution of Ampicillin

© 2016, Springer Science+Business Media New York.In this work, we studied water solubility of ampicillin trihydrate and its solid dispersions (SD) with polyethylene glycol-1500, polyvinylpyrrolidone-10000, and β-cyclodextrin. It was found that SD formation increases the solubility by a factor of 1.34–1.73 and the rate of ampicillin dissolution by a factor of 3.43–7.40. The results of complex physicochemical studies suggest that the improved release of ampicillin from SD is due to its micronization and solubilization by the polymer

Тhe Viscosity Study of Naftifine Hydrochloride Solution with a Combination of Polyethylene Glycols

Introduction. Naftifin hydrochloride is an antifungal drug from the allylamine group, which is used as a drug for external use in the treatment of onychomycosis. Quickly penetrates the skin and nails. It has antifungal, antibacterial and anti-inflammatory effects. It has a wide range of actions against many fungi that cause onychomycosis (dermatophytes, molds and yeast). In addition, it has an antibacterial effect in the ratio of gram-positive and gram-negative bacteria, reduces the risk of complicated course of the disease. It has a pronounced anti-inflammatory effect. Polyethylene glycols belong to the class of organic polymers of ethylene glycol. Polyethylene glycols are safe and widely used in pharmaceutical production, due to the variety of applications. The object of the study is a number of solutions of naftifin hydrochloride in different combinations and with different ratios of polyethylene glycols.Aim. The purpose of the work is to choose the optimal composition of the solution of naftifin hydrochloride. Achieve due to the viscosity of the prolonging action of the solution. Depending on the molecular weight of polyethylene glycol to determine the flow time of solutions. Choose among a number of samples with different ratios of polyethylene glycols, a solution with maximum viscosity.Materials and methods. To determine the viscosity of this solution, a capillary viscometry method was used on the vpzh-2 apparatus. «Exoderil» solution was chosen as a reference formulation.Results and discussion. Alternating different combinations of polyethylene glycol, we have increased the viscosity of the fluid naftifine hydrochloride, which has achieved a more accurate method of application of medicinal substances. During the study, it was determined that the solution «Exoderil» has a minimum viscosity, compared with all samples of the studied solutions.Сonclusion. The optimal viscosity of the solution of naftifin hydrochloride provides a prolonged action of the drug, due to a longer stay on the nail plate. Viscosity allows for more accurate application to the damaged nail, and reduces the loss of concentration of the active substance. Moisturizing properties of polyethylene glycols will help to reduce the severity of side effects (dryness, rarefaction), and provide a longer and more comfortable treatment of onychomycosis

THE USE OF NAFTIFINI HYDROCHLORIDE AND ITS ADVANTAGES IN THE TREATMENT OF VARIOUS TYPERS OF FUNGAL DISEASES

Studying the susceptibility of dermatophyte strains to naftifine revealed that the range of inhibitory concentrations (MIC) is 0,1-0,2 μg/ml. The naftifine spectrum is very wide and includes almost all mycotic pathogens. Testing the strains of Trichophyton rubrum, Trichophyton mentagrophytes, Microsporum canis and Epidermophyton floccosum in comparison with clotrimazole and 4-imidazole antimycotics has shown that naftifine is the most active drug affecting dermatophytes. In concentrations of no more than 1,0 μg/ml, naftifine inhibited 98,75% of dermatophyte strains. Naftifine hydrochloride can find a worthy use in the treatment of skin diseases against the background of infectious and inflammatory processes associated with mycoses

The state pharmacopoeia in the system of higher education

The article provides with a brief historical background for the editions of the State Pharmacopoeia. It characterizes the Russian State Pharmacopoeia of the XIII edition. It was shown that the Russian State Pharmacopoeia, being an essential part of the drug standardization system, also carries an important educational function. Guality standards and methods of analysis, systematization of knowledge, definitions and classifications regulated by the Pharmacopoeia, not only form the knowledge base, but also define the scientific veiw for future experts

Evaluation of the Possibility of Using the Method of UV Spectrophotometry for the Development of Quantitative Determination of Naftifine Hydrochloride in its Solution with a Combination of PEG for the Treatment of Fungal Infections

Introduction. An innovative antifungal agent based on hydrochloride with combination of PEG-400 and PEG-1000 has been developed based at the chairs of Sechenov University. This solution is designated for external application as an antifungal agent. Naftifine hydrochloride has a broad spectrum of action against various fungi capable of causing onychomycosis. PEGs, forming part of the developed dosage form, bring about necessary viscosity of the solution (for retention in application area) and do not prevent drug product performance. Naftifine hydrochloride has an apparent UV absorption band with maximum of 256 ± 2 mn, in connection with this, it is supposed to use the UV spectrophotometry method for further development of quantitation method of naftifine hydrochloride detection in tested oral liquid.Aim. To evaluate the feasibility of using the UV spectrophotometry method for development of quantitation of naftifine hydrochloride in its solution with a combination of PEG for mycotic infection treatment.Materials and methods. The substance of naftifine hydrochloride, PEG-400 and PEG-1000, ethyl alcohol 96 %, UV spectrophotometry, «Millipore» filter.Results and discussion. A set of operations was carried out with UV spectrophotometer, including trials of solutions of initial substance of naftifine hydrochloride, PEG solutions, a solution of developed prolonged antimycotic drug and its placebo. The identity of UV spectra of the actual substance in various media was determined, maximum absorption of actual substance and dependence preservation between specified concentration and optical density of the solution were proved. It was found that auxiliary substances included in liquid dosage form do not affect the main characteristics of the UV spectrum of actual substance.Conclusion. The possibility in principle of using the UV spectrophotometry method for quantitative and qualitative analysis of innovative prolonged antimycotic drug – liquid dosage form of naftifine hydrochloride with a combination of PEG has been established

Nitrofurans for External Use (Review)

Introduction. Aspects of the use of nitrofurans for external use (nitrofural, furazolidone and furazidin) are described in the article. Review of current research that is dedicated to development of drugs containing nitrofuran derivatives has been carried out. The prospects for creating dosage forms of furaсillin and furazolidone containing their solid dispersions with polymers are considered.Text. The group of nitrofurans is widely in demand in the modern pharmaceutical market. The most common active ingredients – furacillin, furazolidone and furazidin are represented by various dosage forms for both internal and external use. All nitrofuran derivatives have a wide spectrum of antimicrobial action and a specific mechanism of action on bacterial cells. The low level of development of antimicrobial resistance allows nitrofurans to remain one of the most effective chemotherapeutic groups of antimicrobial compounds for many decades. The review shows a numerous current developments carried out by both Russian and foreign authors about use of furacillin, furadonin and furazidin to develop the composition of new drugs, including combination drugs, as well as promising treatment methods. Currently, on the basis of Sechenov University, research is actively conducted to increase the solubility and dissolution rate of nitrofurans in water using the method of solid dispersions. Also, work is underway to develop the composition and technology of solid (instant) dosage forms granules and tablets, and soft dosage forms gels containing furacillin and furazolidone as active substances.Conclusion. Despite the use of active substances from the nitrofuran group in pharmaceutical practice for more than half a century and their low solubility in water, research on the development of complex drugs for external use and mono-preparations of nitrofurans have not lost their relevance and are actively conducted to this day