G.O. Nifontova (1, 2), S.P. Krechetov (1), MD; O.V. Dolotova (1), PhD; A.R. Akhmetzyanova (3); Professor I.I. Krasnyuk (2), PhD 1-Center of Living Systems, Moscow Institute of Physics and Technology; 9, Institutsky Lane, Build. 7, Dolgoprudnyi, Moscow Region 141701, Russian Federation; 2-I.M. Sechenov First Moscow State Medical University; 8, Trubetskaya St., Build. 2, Moscow 119991, Russian Federation; 3-Farmzashchita (Pharmprotection) Research-and-Production Center, Federal Biomedical Agency of Russia; 11, Vashutinskoe Shosse, Khimki, Moscow Region 141402, Russian Federation

Introduction. The unsatisfactory technological characteristics of powder of the pharmaceutical substance (PS) proroxane indicate that the latter should undergo wet granulation when solid dosage forms are manufactured. Objective: to substantiate wet granulation technology to obtain floating extended-release proroxane tablets. Material and methods. The tablets were obtained by wet pregranulation of the PS. Proroxane and its impurities were quantified using high performance liquid chromatography. The release of proroxane from tablets was assessed from dissolution test results. The time of tablet floating lag-time and floating was determined using video recordings. Results. The tablets manufactured using wet granular materials have required proroxane release kinetics, but have poor floatability (the long-term emergence of tablets and the time of their floating is substantially shorter than that of full PS release). The elevated levels of gas-forming agents make it possible to reduce the time of emergence, but to fail to ensure optimal floating duration. Conclusion. Wet granulation of proroxane using an aqueous solution of citric acid improves the technological properties of a granular material and ensures PS stability.

floating tablets
extended release
wet granulation
citric acid

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