Number №1, 2019 - page 32-42

Chemical-pharmaceutical analysis of original and generic tamsulosin preparations DOI: 10.29188/2222-8543-2019-11-1-32-42

Moskalev A.V., Ogienko A.G., Myz' S.A., Ogienko A.A., Gladkih V.S.
Information about authors:
  • Moskalev A.V. – «EOL Labs» Ltd, e-mail: andrei.v.moskalev@gmail.com
  • Ogiyenko A.G. – Novosibirsk State University; A.V. Nikolaev Inorganic Chemistry Institute of Siberian Branch of Russian Academy of Sciences; Translational Medicine Laboratory, Novosibirsk State Medical University
  • Myz S.A. – Novosibirsk State University; Institute of Solid State Chemistry and Mechanochemistry of Siberian Branch of Russian Academy of Sciences
  • Ogiyenko A.A. – Novosibirsk State University; Institute of Molecular and Cell Biology of Siberian Branch of Russian Academy of Sciences
  • Gladkikh V.S. – «EOL Labs» Ltd

Drugs based on α1-adrenergic blockers are currently used as a first line of treatment for lower urinary tract symptoms (LUTS). Blockage of α1a-adrenergic receptors leads to relaxation of smooth muscles in prostatic stroma which leads to a decrease in obstruction symptoms. Tamsulosin blocks α1a- and α1d-adrenergic receptors, which allows it to effectively diminish all LUTS, while circulatory adverse events are rare because of its low activity towards α1b-adrenergic receptors.

However, therapeutic efficacy of drugs belonging to this group is possible only when required serum drug concentration is reached and maintained for a necessary period of time. These characteristics are defined by properties of a pharmaceutical form no less, or sometimes even more than by properties of an active ingredient itself. They are influenced by a choice of excipients which define drug release profile. Properties of a pharmaceutical form may radically change after substitution of one excipient by another, after substitution of solvent used for this pharmaceutical form, due to altered temperature regimen without following optimization of composition or manufacturing flaws.

The aim of this research was to perform a comparative study of physical, chemical, pharmaceutical and technological characteristics of drugs based on tamsulosin hydrochloride currently prescribed and used in Russia (capsules: «Omnic», «Proflosin», «Focusin», «Tamsulosin-OBL», «Tamsulosin Vertex», «Tamsulosin Canon», «Omsulosin» and «Tulosin»; tablets: «Omnic Ocas», «Tamsulosin Retard»). General characteristics of tablets and capsules (comparison of composition, fillers and carriers, authenticity, mean mass of tablets and capsule contents, homogenicity, resistance to crushing, disintegration) were studied, as well as morphology of film coating, core material of tablets and capsule contents, chemical and phase composition of tablets and capsules and tamsulosin release profile.

It was shown that modifications made to composition of certain generic drugs led to significant changes in their physical and chemical properties when compared to original drug, which correlated with significant changes in tamsulosin release profile.

An observed difference may potentially influence therapeutic activity of a pharmaceutical form and requires further in vivo studies.

Authors declare lack of the possible conflicts of interests

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tamsulosin hydrochloride, alpha-blockers, benign prostatic hyperplasia, urodynamicscorrector, instrumental methods ofresearch, original and reproduced drugs, equivalence

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