PROSPECTS FOR USING SOLID METHYLURACIL DISPERSIONS IN MEDICINE AND PHARMACY

DOI: https://doi.org/None
Issue: 
5
Year: 
2016

V.V. Grikh, I.I. Krasnyuk, Jr., PhD; Professor I.I. Krasnyuk, PhD; A.V. Be-lyatskaya, PhD; O.I. Stepanova; T.M. Kosheleva; L.V. Ovsyannikova; O.N. Plakhotnaya, PhD; L.A. Korol, PhD; A.N. Galaiko I.M. Sechenov First Moscow State Medical University; 8, Trubetskaya St., Build. 2, Moscow 119991

Methyluracil dosage forms are commonly used in different fields of medicine. The oral route is the most effective route of administration for this drug substance. However, methyluracil is slightly soluble in water, which re-duces the biopharmaceutical characteristics of its based drugs. Analysis of the data available in the literature has shown that the preparation of solid disper-sions with methyluracil is a promising technology that can enhance the bioavailability of slightly soluble methyluracil, shorten its dissolution time, and improve its pharmaceutical parameters. The development of synthetic chemis-try, polymer chemistry in particular, provides possibilities to search for novel polymer combinations and to design solid dispersions.

Keywords: 
methyluracil
solid dispersions
polymers
solubility
bioavailability

References: 
  1. Guzev K.S., Arhapchev V.I., Nozdrin V.I., Vliyanie mazevoy osnovy na farmakokinetiku metiluracila. Farmaciya, 2008; 6: 47–51.
  2. Mashkovskiy M.D., Lekarstvennye sredstva.2006; 706–7.
  3. Gosudarstvennaya farmakopeya Rossiyskoy Federacii XII izd., chast` 1.2007; 588–9.
  4. Gus`kov V.Yu., Ivanov S.P., Kudasheva F.H., Murinov Yu.I. Sposob polucheniya sorbenta. Patent RF № 2452562. Izobreteniya i poleznye modeli. Oficial`nyy byulleten` federal`noy sluzhby po intellektual`noy sobstvennosti (Rospatent). 2012;16.
  5. Svetlakova E.N., Mandra Yu.V., Larionov L.P., Honina T.G.i dr. Sredstvo dlya mestnogo lecheniya zabolevaniy parodonta. Patent RF № 2491061. Izobreteniya i poleznye modeli. Oficial`nyy byulleten` federal`noy sluzhby po intellektual`noy sobstvennosti (Rospatent). 2013; 24.
  6. Nozdrin V.I, Belousova T.A., Yackovskiy A.N. Morfologicheskie aspekty dermatotropnogo deystviya metiluracila v usloviyah nakozhnogo primeneniya. Morfologiya, 2002; 122 (5): 74–8.
  7. Popova O.I. Vliyanie 6-metiluracila na obmen svobodnyh nukleotidov v normal`noy i regeneriruyushhey pecheni krys Avtoref. dis. kand. biol. na-uk. M., 1980; 23.
  8. Germanovich M.L. Lechebnoe deystvie metacila (4-metiluracila) pri povrezhdeniyah slizistyh obolochek u bol`nyh, podvergayushhihsya luchevoy terapii po povodu zlokachestvennyh opuholey. Materialy Konferencii po primeneniyu pirimidinovyh proizvodnyh v onkologii i drugih oblastyah mediciny. 1963; 17–20.
  9. Lazurina L.P., Losickaya O.S., Basareva O.I., Bukreeva E.M., Samohvalova I.V. Farmacevticheskaya antibakterial`naya
  10. kompoziciya dlya mestnogo primeneniya na osnove aktivnyh biometallokompleksov. Patent RF № 2489147. Izobreteniya poleznye modeli. Oficial`nyy byulleten` federal`noy sluzhby
  11. po intellektual`noy sobstvennosti (Rospatent). 2013; 22.
  12. Khosro Adibkia, Alireza Mohajjel Nayebi, Mohammad Barzegar- Jalali1, Siavash Hosseinzadeh, Saeed Ghanbarzadeh3, Afshin Shivai, Comparison of the Analgesic Effect of Diclofenac Sodium-Eudragit® RS100 Solid Dispersion and Nanoparticles Using Formalin Testinthe Rats. Adv. Farm. Bjull., 2015, 5(1): 77–81.
  13. Krasnyuk I.I. (ml.), Krasnyuk I.I., Koval`skiy I.V., Belyackaya A.V., Nikulina O.I, Haritonov Yu.Ya. i dr. Sposob polucheniya tabletok rutina. Patent RF № 2523562. Izobreteniya i poleznye modeli. Oficial`nyy byulleten` federal`noy sluzhby po intellektual`noy sobstvennosti (Rospatent). 2014; 20.
  14. Koval`skiy I.I., Krasnyuk I.I., Krasnyuk I.I. (ml.), Nikulina O.I., Belyackaya A.V. Izuchenie rastvorimosti rutina iz tverdyh dispersiy. Him.-farm. zhurn., 2013; 47 (11): 42–5.
  15. Laxmikant Ramvallabh Zawar, Sanjay Baburao Bari, Preparation, Characterization and in Vivo Evaluation of Antihyperglycemic Activity of Microwave Generated Repaglinide Solid DispersionHim. Farm. Bjulleten', 2012; 60 (4): 482–7.
  16. Pozharickaya O.N., Vaynshteyn V.A., Strelkova L.F., Kalinina N.A. Izuchenie mehanizma vysvobozhdeniya nifedipina iz tverdyh dispersnyh sistem na osnove polie`tilenglikolya 1500. Farmaciya, 1999; 2: 18–20.
  17. Krasnyuk I.I. (ml.), Belyackaya A.V., Nikulina O.I, Haritonov Yu.Ya., Grih V.V. Biofarmacevticheskie aspekty primeneniya tverdyh dispersiy. V sb.: A.I. Tencova. «E`poha v farmacii». M., 2014; 62–5.
  18. Mohammad Reza Siahi-Shadbad, Saeed Ghanbarzadeh, Mohammad Barzegar-Jalali, Hadi Valizadeh, Alireza Taherpoor,
  19. Ghobad Mohammadi, Azim Barzegar-Jalali, Khosro Adibkia. Development and Characterization of Solid Dispersion for Dissolution Improvement of Furosemide.Adv. Farm. Bjull., 2014; 4(4): 391-9.
  20. Atsushi Sakurai, Toshiro Sakai, Kazuhiro Sako, Yoshie Maitani. Polymer Combination Increased Both Physical Stability and Oral Absorption of Solid Dispersions Containing a Low Glass Transition Temperature Drug: Physicochemical Characterization and in Vivo Study. Him.Farm.Bjulleten', 2012; 60 (4): 459–64.
  21. Krasnyuk I.I. (ml.), Stepanova O.I., Belyackaya A.V., Korol` L.A. Razrabotka sostava i tehnologii bystrorastvorimyh lekarstvennyh form furacilina. Farmaciya, 2015;3: 36–9.
  22. Krasnyuk I.I. (ml.), Krasnyuk I.I., Popkov V.A., Reshetnyak V.Yu., Shvecova A.S. Sposob polucheniya tabletok e`ritromicina. Patent RF № 2403049. Byulleten` federal`nogo instituta promyshlennoy sobstvennosti. Izobreteniya i poleznye modeli. 2010; 31 (III ch.):583.
  23. Ovsyannikova L.V., Krasnyuk I.I. (ml.), Belyackaya A.V., Nikulina O.I., Grih V.V. Rol` tverdyh dispersiy s polimerami v izmenenii opticheskih svoystv rastvorov i kristallicheskogo stroeniya diklofenaka. Voprosy biologicheskoy, medicinskoy i
  24. farmacevticheskoy himii, 2014; 12: 59–60.
  25. Koval`skiy I.I., Krasnyuk I.I., Nikulina O.I., Belyackaya A.V. i dr. Sposob vvedeniya tverdyh dispersiy flavonoidov v
  26. tabletirovannye lekarstvennye formy. Materialy mezhdunarodnoy nauchno-prakticheskoy konferencii Obshhestv nauki i tvorchestva. Kazan`, 2013; 60–3.
  27. Habriev R.U., Popkov V.A., Reshetnyak V.Yu., Krasnyuk I.I., Manahova O.V. Povyshenie rastvorimosti angioprotektora metodom tverdyh dispersiy. Him.-farm. zhurn., 2009; 43 (8): 45–9.
  28. Alekseev K.V., Grickova I.A., Kedik S.A. Polimery dlya farmacevticheskoy tehnologii. M.: 2011; 511.
  29. Noushin Bolourchian, Mohammad Mehdi Mahboobian, SiminDadachzadeh, The Effect of PEG Molecular Weights on Dissolution Behavior of Simvastatin in Solid. Dispertions.Iran.farm. issled. zhurnal, 2013; 12: 11–20.