Development of nitrofuran derivative: composition and technology of effervescent tablets with solid dispersions

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Abstract

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.

Abbreviations: FZ – furazolidone; SD – solid dispersions; AS – active substance; DF – dosage form; PVP – polyvinylpyrrolidone; SP RF XIV – State Pharmacopoeia of the Russian Federation XIV edition; Es – excipients; PSF – Product Specification File; GL – granulation liquid.

About the authors

Anastasia O. Elagina

Sechenov First Moscow State Medical University

Email: a.o.elagina@gmail.com
ORCID iD: 0000-0001-5255-3991

post-graduate student, Department of Pharmaceutical Technology, Institute of Pharmacy n. a. A.P. Nelyubin

Russian Federation, Bldg. 2, 8, Trubetskaya St., Moscow, 119991

Anastasiya V. Belyatskaya

Sechenov First Moscow State Medical University

Email: av.beliatskaya@mail.ru
ORCID iD: 0000-0002-8214-4483

Candidate of Sciences (Pharmacy), Associate Professor, Associate Professor of the Department of Pharmaceutical Technology, Institute of Pharmacy n. a. A.P. Nelyubin

Russian Federation, Bldg. 2, 8, Trubetskaya St., Moscow, 119991

Ivan I. (Jr) Krasnyuk

Sechenov First Moscow State Medical University

Email: krasnyuk.79@mail.ru
ORCID iD: 0000-0001-8557-8829

Doctor of Sciences (Pharmacy), Professor, Professor of the Department of Analytical, Physical and Colloidal Chemistry, Institute of Pharmacy n. a. A.P. Nelyubin

Russian Federation, Bldg. 2, 8, Trubetskaya St., Moscow, 119991

Ivan I. Krasnyuk

Sechenov First Moscow State Medical University

Email: krasnyuki@mail.ru
ORCID iD: 0000-0002-7242-2988

Doctor of Sciences (Pharmacy), Professor, Professor of the Department of Pharmaceutical Technology, Institute of Pharmacy n. a. A.P. Nelyubin

Russian Federation, Bldg. 2, 8, Trubetskaya St., Moscow, 119991

Olga I. Stepanova

Sechenov First Moscow State Medical University

Email: o.i.nikulina@mail.ru
ORCID iD: 0000-0002-9885-3727

Candidate of Sciences (Pharmacy), Associate Professor, Associate Professor of the Department of Pharmacology, Institute of Pharmacy n. a. A.P. Nelyubin

Russian Federation, Bldg. 2, 8, Trubetskaya St., Moscow, 119991

Tatyana V. Fateeva

All-Russian Research Institute of Medicinal and Aromatic Plants

Email: fateeva2151@mail.ru
ORCID iD: 0000-0002-8231-0621

Head of the Laboratory of Microbiological Research

Russian Federation, Bldg. 7, Grin St., Moscow, 117216

Elena A. Smolyarchuk

Sechenov First Moscow State Medical University

Email: smolyarchuk@mail.ru
ORCID iD: 0000-0002-2615-7167

Candidate of Sciences (Medicine), Associate Professor, Head of the Department of Pharmacology, Institute of Pharmacy n. a. A.P. Nelyubin

Russian Federation, Bldg. 2, 8, Trubetskaya St., Moscow, 119991

Sergey V. Kozin

Sechenov First Moscow State Medical University

Email: enfadado@yandex.ru
ORCID iD: 0000-0002-4722-8315

Candidate of Sciences (Biology), Associate Professor, Department of Pharmacology, Institute of Pharmacy n. a. A.P. Nelyubin

Russian Federation, Bldg. 2, 8, Trubetskaya St., Moscow, 119991

Olga N. Plakhotnaya

Sechenov First Moscow State Medical University

Email: plahotnaya.o@mail.ru
ORCID iD: 0000-0001-7266-2933

Candidate of Sciences (Chemistry), Associate Professor, Associate Professor of the Department of Analytical, Physical and Colloidal Chemistry, Institute of Pharmacy n. a. A.P. Nelyubin

Russian Federation, Bldg. 2, 8, Trubetskaya St., Moscow, 119991

Olga V. Rastopchina

Sechenov First Moscow State Medical University

Email: rastop0309@yandex.ru
ORCID iD: 0000-0002-5443-6980

Candidate of Sciences (Pharmacy), Associate Professor, Associate Professor of the Department of Pharmaceuticals, Institute of Pharmacy n. a. A.P. Nelyubin

Russian Federation, Bldg. 2, 8, Trubetskaya St., Moscow, 119991

Julietta V. Rau

Sechenov First Moscow State Medical University; Istituto di Struttura della Materia, Consiglio Nazionale delle Ricerche (ISM-CNR)

Author for correspondence.
Email: giulietta.rau@ism.cnr.it
ORCID iD: 0000-0002-7953-1853

Doctor of Sciences (Philosophy), Professor, Istituto di Struttura della Materia; Associate Professor, Associate Professor of the Department of Analytical, Physical and Colloidal Chemistry. Institute of Pharmacy n. a. A.P. Nelyubin

Russian Federation, Bldg. 2, 8, Trubetskaya St., Moscow, 119991; Via del Fosso del Cavaliere, 100-00133 Rome

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Supplementary files

Supplementary Files
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1. JATS XML
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2. Figure 1 – Furazolidone structural chemical formula

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3. Figure 2 – Ultraviolet absorption spectra of substance furazolidone aqueous solutions (1), effervescent FZ tablets (2) and excipients (3)

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4. Figure 3 – Regression line for quantitative determination of furazolidone content by spectrophotometry

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5. Figure 4 – Dependence of the effect of compacting pressure values on the disintegration of furazolidone effervescent tablets

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6. Figure 5 – Dependence of the effect of compacting pressure value on crushing resistance of furazolidone effervescent tablets

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7. Figure 6 – Dependence of the effect of compacting pressure on the аbrasion capacity of furazolidone effervescent tablets

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8. Figure 7 – Effervescent tablets containing a solid furazolidone dispersion as an active substance

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Copyright (c) 2022 Elagina A.O., Belyatskaya A.V., Krasnyuk I., Krasnyuk I.I., Stepanova O.I., Fateeva T.V., Smolyarchuk E.A., Kozin S.V., Plakhotnaya O.N., Rastopchina O.V., Rau J.V.

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