Advertisement

Pharmaceutical Chemistry Journal

, Volume 52, Issue 9, pp 786–789 | Cite as

Analgesic Rectal Suppositories Containing a Nonsteroidal Anti-Inflammatory Drug in Combination with a Tricyclic Antidepressant and Transmucosal Conductor

  • I. G. ZyryanovaEmail author
  • L. P. Larionov
  • E. V. Shadrina
  • M. V. Ivanenko
  • T. G. Khonina
Article
  • 118 Downloads

A composition and preparation method for new analgesic rectal suppositories containing a nonsteroidal anti-inflammatory drug (ketorolac), tricyclic antidepressant (amitriptyline), and transmucosal conductor (silicon glycerolates) as the active ingredients in a poly(ethylene glycol) (PEG-4000) base were proposed. The acute toxicity was determined and showed they were safe to use. The high analgesic activity of the suppositories was confirmed using electrical stimulation. Their high transmucosal activity in vitro was revealed by measuring the degree of diffusion of one of the active ingredients (amitriptyline) through a natural biological membrane. The results indicated that the developed suppositories could be recommended for further investigations of future medical use to relieve pain of various etiologies.

Keywords

analgesia nonsteroidal anti-inflammatory drugs tricyclic antidepressants rectal suppositories transmucosal conductors 

Notes

Acknowledgments

The work was financially supported by RFBR Project No. 15-03-01770 a.

References

  1. 1.
    A. E. Karateev, L. I. Alekseeva, E. G. Filatova, et al., Analgesic Preparations in Therapeutic Practice [in Russian], OOO IMA-PRESS, Moscow (2013).Google Scholar
  2. 2.
    A. E. Karateev, E. L. Nasonov, N. N. Yakhno, et al., Sovrem. Revmatol., No. 1, 4 – 23 (2015).Google Scholar
  3. 3.
    G. R. Abuzarova, Diagnostics and Differentiated Pharmacotherapy of Chronic Pain Syndrome in Oncological Patients [in Russian], GEOTAR-Media, Moscow (2015).Google Scholar
  4. 4.
    V. A. Malakhov and E. S. Romelashvili, Nevrologiya, No. 4 (360), 39 – 42 (2011).Google Scholar
  5. 5.
    N. V. Chichasova, G. R. Imametdinova, A. E. Karateev, et al., Nauchno-Prakt. Revmatol., No. 1, 46 – 52 (2001).Google Scholar
  6. 6.
    T. V. Orlova, T. A. Pankrusheva, M. V. Pokrovskii, et al., Nauchn. Vedom. Ser. Med. Farm., No. 4, 198 – 202 (2012).Google Scholar
  7. 7.
    E. V. Kompantseva, A. P. Kuznetsov, et al., RU Pat. 2,292,201, Jan. 27, 2007; Ref. Zh. Khim., 07.14–19O.240P (2007).Google Scholar
  8. 8.
    T. G. Khonina, L. P. Larionov, et al., RU Pat. 2,255,939, Feb. 20, 2005; Ref. Zh. Khim., 05.23–19O.219P (2005).Google Scholar
  9. 9.
    T. G. Khonina, O. N. Chupakhin, L. P. Larionov, et al., Khim.-farm. Zh., 42(11), 30 – 34 (2008); Pharm. Chem. J., 42(11), 609 – 613 (2008).Google Scholar
  10. 10.
    State Pharmacopoeia of the Russian Federation, XIIIth Ed., Vol. 2, Ministry of Health of the Russian Federation, Moscow (2015), pp. 224 – 243; http: // www.femb.ru (accessed May 27, 2016).
  11. 11.
    A. N. Mironov (ed.), Handbook for Preclinical Drug Trials [in Russian], Grif i K, Moscow (2012).Google Scholar
  12. 12.
    I. G. Zyryanova, Zdorov’e Obraz. XXI Vek., 16(4), 282 – 284 (2014).Google Scholar
  13. 13.
    E. G. Filatova, Russ. Med. Zh., No. 4, 256 – 260 (2009).Google Scholar
  14. 14.
    A. E. Karateev, Nevrol., Neiropsikhiatr. Psikhosom., No. 4, 81 – 89 (2011).Google Scholar
  15. 15.
    T. G. Khonina, O. N. Chupakhin, L. P. Larionov, et al., Khim.-farm. Zh., 43(2), 26 – 32 (2009); Pharm. Chem. J., 43(2), 95 – 100 (2009).Google Scholar

Copyright information

© Springer Science+Business Media, LLC, part of Springer Nature 2018

Authors and Affiliations

  • I. G. Zyryanova
    • 1
    Email author
  • L. P. Larionov
    • 1
  • E. V. Shadrina
    • 2
  • M. V. Ivanenko
    • 2
  • T. G. Khonina
    • 2
  1. 1.Ural State Medical University, Ministry of Health of the RFEkaterinburgRussia
  2. 2.I. Ya. Postovsky Institute of Organic SynthesisUral Branch, Russian Academy of SciencesEkaterinburgRussia

Personalised recommendations