Development of Dosage Forms Containing a Solid Dispersion of Diclofenac

Krasnyuk, I. I.; Ovsyannikova, L. V.; Степанова, О. И.; Belyatskaya, A. V.; Grikh, V. V.; Kosheleva, T. M.; Skovpen, Y. V.; Kozin, Dmitry

doi:10.1007/s11094-018-1821-6

Cited by 3 publications

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“…В виду того, что полученные данные позднее планируется использовать при разработке твёрдых быстрорастворимых лекарственных форм метронидазола, в качестве актуальных объектов исследования были выбраны именно ПЭГ твёрдой консистенции с массами 1500, 2000 и 3000 г/моль. Выбранные полимеры часто используются, как вспомогательные вещества при производстве таблеток и гранул [5].…”

Section: результаты и обсуждениеunclassified

“…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

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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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Preparation and In Vitro/Vivo Evaluation of New Celecoxib Solid Dispersions with Co-Carrier Containing Aerosil and Poloxamer 188

et al. 2021

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Prospects of Methods of Solid Dispersed Systems in the Development of Innovative Medicinal Forms

G.Z.,

E.F.

2024

Mediko-farmacevtičeskij žurnal "Pulʹs"

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. Expansion of the range of drugs with high therapeutic efficacy of the domestic market, including original dosage forms, are the priority tasks of the Ministry of Health within the framework of the state program of the Government of the Russian Federation "Development of Pharmaceutical and Medical Industry" dated December 29, 2021 with a term until 2030. One of the solutions to this problem at the stage of development of innovative dosage forms is the use of solid dispersions technology, which can provide prolonged action and sufficient stability. This is evidenced by the results of scientific research and obtaining solid dispersed systems based on various drug substances. The review is devoted to types of solid dispersions, general advantages of their application in pharmaceutical practice, evaluation of disadvantages and possibility of their correction. The list of polymers and substances of non-polymeric nature acting as carriers of solid dispersions is presented. The main methods of their preparation are reviewed, including industrial production: melt extrusion, used for drugs with not very high melting points; spray drying for drugs soluble in at least one volatile solvent and co-precipitation, used for drugs with high melting points and low solubility in common organic solvents. The use of a combination of preparation methods allows choices to be made regarding the optimal use of solid dispersions in dosage forms. Recent advances in the field of solid dispersions are described, as well as pharmaceuticals based on them, registered with the Ministry of Health of Russia.

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Development of Dosage Forms Containing a Solid Dispersion of Diclofenac

Cited by 3 publications

References 2 publications

Effect of Solid Dispersions on the Solubility of Metronidazole

Effect of Solid Dispersions on the Solubility of Metronidazole

Preparation and In Vitro/Vivo Evaluation of New Celecoxib Solid Dispersions with Co-Carrier Containing Aerosil and Poloxamer 188

Prospects of Methods of Solid Dispersed Systems in the Development of Innovative Medicinal Forms

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