The study of base and surface-active substances influence on biopharmaceutical characteristics of suppository with praziquantel

Authors

  • D. M. Romanina Zaporizhzhia State Medical University,
  • V. V. Gladishev Zaporizhzhia State Medical University,
  • G. P. Lisyanska Zaporizhzhia State Medical University,
  • I. L. Kechin Zaporizhzhia State Medical University,

DOI:

https://doi.org/10.14739/2409-2932.2016.3.77928

Keywords:

Praziquantel, Suppository, Demodicosis, Base, Surface-Active Substance, Releasing

Abstract

Acne dermatoses (rosacea, perioral dermatitis, seborrheic dermatitis etc.) are one of the most actual problems in dermatology. Praziquantel is an antiparasitic medication effective towards trematodes, cestodes. Investigations developed by domestic scientists revealed antidemodicosis activity of praziquantel. Use of semisolid dosage forms for rectal administration will allow to increase its efficacy and minimize the risks of adverse reactions.

The aim of this work is the study of influence of excipients (bases and surfactants) use in suppository manufacturing on the biopharmaceutical characteristics of praziquantel rectal dosage form.

Methods and results. As excipients for praziquantel rectal dosage form we have investigated suppository bases and surfactants, which are widely used in manufacturing and compounding of semisolid dosage forms and are described in literature. Suppositories were made by the fusion method. Concentration of surfactants in all compositions was 2%, praziquantel – 0,6 g on one suppository. Investigation was carried out by the 2-factors dispersive analysis with repeated observations.

Suppository compounding was carried out by the suspension type. After thorough pulverization of praziquantel, it was mixed with some part of the base and then obtained mixture was added to the all melted base.

As optimization parameter the praziquantel releasing was chosen as the first step of bioavailability investigation. Praziquantel releasing from suppository was studied by the equilibrium dialysis by Kruvchinsky. Ethyl alcohol was chosen as a dialysis medium considering the solubility of praziquantel. Concentration of released praziquantel after 30 minutes of the dialysis was determined by spectrophotometric analysis.

Conclusion. It has been established that the sort of the base and surfactant have significant influence on praziquantel releasing from rectal suppository. It has been revealed that sort of base has the greatest influence on praziquantel releasing from rectal suppository. Variance analysis has shown optimal praziquantel releasing from rectal suppository with composition of factory fatty base and distilled monoglycerides.

References

Khilkevich, M. D., Kachuk, M. V., Muzichenko, A. P., Kruk, N. V., Vetohina, E. L. (2012). Demodekoz kak dermatologicheskaya problema [Demodecosis as a dematological problem]. Voennaya medicina, 3, 151–153. [in Belarus].

Kogan, B. G., & Golovchenko, D. Ya. (2011). Sovremennye podkhody v kompleksnom lechenii pacientov s demodikozom i rozovymi ugryami [Modern approaches in treatment of patients with demodex and pink acne]. Klinichna imunolohiia. Alerholohia. Infektolohiia: vudannia dlia likaria-praktyka, 1, 38–43. [in Ukrainian].

Sulym, A.G. (2010). Prazykvantel u likuvanni khvorykh na rozatsea, demodykoz ta perioralnyi dermatyt [Praziquantel to treat Rosacea, perioral dermatitis and demodicosis]. Visnyk Sumskoho derzhavnoho universyitetu. Seriia Medytsyna, 1, 158–161. [in Ukrainian].

Kechyn, I. L., Romanina, D. M., Hladyshev, V. V., & Diudiun, A. D. (2015). Vyvchennia hostroi toksychnosti prazykvantelu za riznykh shliakhiv vvedennia [Study of acute toxicity of praziquantel for different routes of administration]. Farmatsevtychnyi zhurnal, 6, 91–95. [in Ukrainian].

Orlova, T. V. (2014). Sovremennye rekta´lnye, vaginal´nye i uretral´nye lekarstvennye formy [Modern rectal, vaginal and urethral medicinal forms] (2014). Vestnik Voronezhskogo gosudarstvennogo universisteta. Seriyja: Himiya. Biologiya. Farmaciya, 1, 126–133. [in Russian].

Simonyan, E. V., Shikova, Yu. V., Likhoded, V. A., Ushkova, V. A., Nozhkina, N. N., Klimantova, M. S., & Yumaguzhina, A. T. (2014). Obosnovanie sostava i biofarmacevticheskie issledovaniya suppozitoriev, soderzhashchikh kislotu glutaminovuyu i e´kstrakt propolisa [Rationale composition biopharmaceutical research and suppositories containing glutamic acid and propolis extract]. Nauchnye vedomosti Belgorodskogo gosudarstvennogo universiteta. Seriya: Medicina. Farmacia, 11, 255–257. [in Russian].

Kuchina, L. K., Gladyshev, V. V., Kechin, I. L., & Pukhal´skaya, I. A. (2014). Vliyanie vspomogate´lnykh veshchestv na vysvobogdaemost´ diltiazema iz rektal´nykh suppositoriev [Effect of Adjuvants on the releasability of diltiazem rectal suppository]. Nauchnye vedomosti Belgorodskogo gosudarstvennogo universiteta. Seriya: Medicina. Farmacia, 18, 234–237. [in Russian].

Hroshovyi, T. A., Martseniuk, V. P., Kucherenko, L. I., et al. (2008). Matematychne planuvannia eksperymentu pry provedenni naukovykh doslidzhen v farmatsii [Mathematical planning experiment in scientific research in pharmacy] Ternopil: TDMU. [in Ukrainian].

Fadi, Al Zedan, Hladyshev, V. V., Burlaka, B. S., & Kechyn, I. L. (2011). Rozrobka i biofarmatsevtychni doslidzhennia supozytoriiv z amlodypinom [Development and biopharmaceutical studies of suppositories with amlodipine]. Medychna khimiia,, 2, 72–75. [in Ukrainian].

Monaikina, Yu. V., Vasiuk, S. O., Romanina, D. M., & Pukhalska, I. A. (2014). Kilkisne vyznachennia prazykvantelu v likarskii formi spektrofotometrychnym metodom [Assay praziquantel in the dosage form by spectrophotometric method]. Aktualni pytannia farmatsevtychnoi i medychnoi nauky ta praktyky, 1, 62–64. [in Ukrainian].

How to Cite

1.
Romanina DM, Gladishev VV, Lisyanska GP, Kechin IL. The study of base and surface-active substances influence on biopharmaceutical characteristics of suppository with praziquantel. Current issues in pharmacy and medicine: science and practice [Internet]. 2016Sep.22 [cited 2024Nov.13];9(3). Available from: http://pharmed.zsmu.edu.ua/article/view/77928

Issue

Section

Pharmaceutical manufacturing