Study on the Solubility of Ketoprofen From Solid Dispersions with Polyvinylpyrrolidone

Belyatskaya, A. V.; Krasnyuk, I. I.; Степанова, О. И.; Abgaryan, Z. A.; Kudinova, T. P.; Vorob’yov, A. N.; Nesterenko, I. S.

doi:10.3103/s0027131419020056

Cited by 4 publications

(3 citation statements)

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“…Анализ патентной и научной литературы не выявил информации о применении ПЭГ в технологии твердых лекарственных форм в качестве полимеров-носителей для получения ТД с метронидазолом с целью повышения его растворимости в воде. Из анализа научной литературы и предварительно собственных исследований, определен диапазон оптимальных соотношений метронидазол: ПЭГ -от 1:1 до не более 1:5 (по массе) [1][2][3][4][5][6][7][8][9]. С учётом физико-химических свойств ПЭГ (как вспомогательного вещества) и его влияния на технологические характеристики твёрдых лекарственных форм (например, на их прочность), указанный диапазон соотношений является оптимальным для будущего включения ТД метронидазола с ПЭГ в состав твёрдых лекарственных форм.…”

Section: результаты и обсуждениеunclassified

“…Сеченова получены и изучены твёрдые дисперсии более 30 малорастворимых лекарственных субстанций из разных фармакологических групп: альбендазол, Volume IX, Issue 3, 2021 амоксициллина тригидрат, ампициллина тригидрат, анестезин, ацетомепрегенол, ацикловир, бензонал, диклофенак (кислотная форма), индометацин, кверцетин, кетопрофен, левомицетин, липоевая кислота, мезапам, метилурацил, нафтифина гидрохлорид, нифидепин, нозепам, пармидин, протионамид, рибофлавин, рифампицин, рутин, синтомицин, стрептоцид, сульфадиметоксин, феназепам, фуразолидон, фурацилин, эритромицин, и т.д. [1][2][3][4][5][6][7][8][9][10].…”

Section: Introductionunclassified

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Effect of Solid Dispersions on the Solubility of Metronidazole

Krasnyuk

Naryshkin

Краснюк

et al. 2021

Farm. farmakol. (Pâtigorsk)

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The aim of the work is to study the effect of solid dispersions using polyethylene glycols of various molecular weights on the solubility of metronidazole in water. Metronidazole is an antimicrobial and antiprotozoal drug. Its low solubility in water limits the use of metronidazole, causing technological difficulties and reducing its bioavailability. The solubility and release of the active substance from dosage forms can be increased using the solid dispersion methods. Solid dispersions are bi- or multicomponent systems consisting of an active substance and a carrier (a highly dispersed solid phase of the active substance or molecular-dispersed solid solutions) with a partial formation of complexes of variable compositions with the carrier material.Materials and methods. The substance of metronidazole used in the experiment, was manufactured by Hubei Hongyuan Pharmaceutical Technology Co., Ltd. (China). To obtain solid dispersions, polyethylene glycols of various molar masses – 1500, 2000 and 3000 g/mol – were used. The solid dispersions were prepared by “the solvent removal method”: metronidazole and the polymer were dissolved in a minimum volume of 96% ethyl alcohol (puriss. p.a./analytical grade) at 65±2°C, and then the solvent was evaporated under vacuum to the constant weight. A vacuum pump and a water bath were used at the temperature of 40±2°C. The dissolution of the samples was studied using a magnetic stirrer with heating, and a thermostatting device. The concentration of metronidazole was determined on a spectrophotometer using quartz cuvettes at the wavelength of 318±2 nm. To filter the solutions, syringe nozzles were used, the pores were 0.45 μm, the filter was nylon. Microcrystalloscopy was performed using a microscope with a digital camera. The optical properties of the solutions were investigated using a quartz cuvette and a mirror camera (the image exposure – 20 sec).Results. Obtaining solid dispersions increases the completeness and rate of the metronidazole dissolution. The solubility of metronidazole from solid dispersions increases by 14–17% in comparison with the original substance. The complex of physical-chemical methods of the analysis, including UV spectrophotometry, microcrystalloscopy and the study of the optical properties of the obtained solutions, makes it possible to suggest the following. The increase in the solubility of metronidazole from solid dispersions is explained by the loss of crystallinity and the formation of a solid solution of the active substance and the solubilizing effect of the polymer with the formation of colloidal solutions of metronidazole at subsequent dissolution of the solid dispersion in water.Conclusion. The preparation of solid dispersions with polyethylene glycols improves the dissolution of metronidazole in water. The results obtained are planned to be used in the development of rapidly dissolving solid dosage forms of metronidazole with an accelerated release and an increased bioavailability.

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Section: результаты и обсуждениеunclassified

Section: Introductionunclassified

Effect of Solid Dispersions on the Solubility of Metronidazole

Krasnyuk

Naryshkin

Краснюк

et al. 2021

Farm. farmakol. (Pâtigorsk)

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“…Одним из приоритетных методов, позволяющих повысить растворимость и скорость растворения ДВ II класса БКС, является метод твердых дисперсий (ТД). ТД -это би-или многокомпонентные системы, состоящие из ДВ и носителя, представляющие собой высокодиспергированную твердую фазу ДВ или молекулярно-дисперсные твердые растворы с частичным образованием комплексов переменного состава с материалом носителя [9][10][11].…”

Section: Introductionunclassified

Development of Nitrofuran Derivative: Composition and Technology of Effervescent Tablets With Solid Dispersions

Elagina

Belyatskaya

Krasnyuk

et al. 2022

Farm. farmakol. (Pâtigorsk)

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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.

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