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Current Issues in Pharmacy and Medical Sciences

Formerly Annales UMCS Sectio DDD Pharmacia

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Influence of the dissolution medium on the release of dehydroepiandrosterone from lipophilic suppositories

Regina Kasperek1
  • Corresponding author
  • Chair and Department of Applied Pharmacy, Medical University of Lublin, Chodzki 1, 20-093 Lublin, Poland
  • Email
  • Other articles by this author:
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/ Krzysztof Galczynski / Magdalena Nalesniak
  • Chair and Department of Applied Pharmacy, Medical University of Lublin, Chodzki 1, 20-093 Lublin, Poland
  • Other articles by this author:
  • De Gruyter OnlineGoogle Scholar
/ Karol Iwaniak
  • Chair and Department of Applied Pharmacy, Medical University of Lublin, Chodzki 1, 20-093 Lublin, Poland
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  • De Gruyter OnlineGoogle Scholar
/ Ewa Poleszak
  • Chair and Department of Applied Pharmacy, Medical University of Lublin, Chodzki 1, 20-093 Lublin, Poland
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  • De Gruyter OnlineGoogle Scholar
Published Online: 2014-05-30 | DOI: https://doi.org/10.2478/cipms-2014-0012

Abstract

Suppositories with cocoa butter containing dehydroepiandrosterone (DHEA) without and with the addition of Span 80 and Tween 80 as surfactants with low and high HLB values were prepared. The physical properties and the drug content of all prepared suppositories were in accordance with the pharmacopoeial requirements. The release study tests in three dissolution media such as water, lactic acid solution at pH 4.2 and phosphate buffer at pH 7.4 were carried out. In acidic and alkalic media only about 10% and 27% of DHEA were released, respectively. The addition of Span 80 to the suppository mass did not improve the release process, but the addition of Tween 80 caused the increase in the amount of DHEA released in the acidic medium to about 35%. The data showed that rectal administration of suppositories with DHEA based on cocoa butter caused about 30% availability and after vaginal administration, only topical activity can be expected. By the addition of Tween 80 to the suppository mass availability of DHEA of about 35% from vaginal suppositories can be achieved.

Keywords: dehydroepiandrosterone; suppositories; release; dissolution medium

References

  • 1. Azarmi S. et al.: Current perspectives in dissolution testing of conventional and novel dosage forms. Int. J. Pharm., 328(1), 12, 2007.Web of ScienceGoogle Scholar

  • 2. Babar A., Fares H. M., Plakogiannis F. M.: In vitro release of testosterone from suppository bases and in vivo absorption studies in human males. J. Pharm. Sci., 82(4), 389, 1993.CrossrefGoogle Scholar

  • 3. Beral V., Bull D., Reeves G.: Endometrial cancer and hormonereplacement therapy in the Million Women Study. Lancet, 365, 1543, 2005.Google Scholar

  • 4. Bergogne-Bérézin E., Bryskier A.: The suppository form of antibiotic administration: pharmacokinetics and clinical application.J. Antimicrob. Chemother., 43(2), 177, 1999.CrossrefGoogle Scholar

  • 5. Buster J.E., Casson P.R. (2000). Biology and use in therapeutic intervention. in Menopause: Biology and Pathobiology. Lobo R. A., Kelsey J. and Marcus R. (editors). San Diego: Academic Press; p 628.Google Scholar

  • 6. Casson P. R. et al.: Dehydroepiandrosterone (DHEA) replacement in postmenopausal women: Present status and future promise.Menopause, 4, 225, 1997.CrossrefGoogle Scholar

  • 7. Casson P. R. et al.: Oral dehydroepiandrosterone in physiologic doses modulates immune function in postmenopausal women. Am.J. Obstet. Gynecol., 169, 1536, 1993.Google Scholar

  • 8. Casson P. R. et al.: Replacement of dehydroepiandrosterone enhances T-lymphocyte insulin binding in postmenopausal women. Fertil Steril, 63(5), 1027, 1995.CrossrefGoogle Scholar

  • 9. Castelo-Branco C. et al.: Management of post-menopausal vaginal atrophy and atrophic vaginitis. Maturitas, 52(Suppl. 1), 46, 2005.CrossrefGoogle Scholar

  • 10. Chicco D. et al.: Correlation of in vitro and in vivo paracetamol availability from layered excipient suppositories. Int. J. Pharm., 189, 147, 1999.Google Scholar

  • 11. Czarnecki W., Kasperek R.: Patent RP Nr P337979 z 21.01.2000r.Biomed Wytwórnia Surowic i Szczepionek w Lublinie.Google Scholar

  • 12. Dal Zorro M. et al.: Effect of the surfactant on the availability of piroxicam as a poorly hydrosoluble drug from suppositories.Pharmazie, 67(1), 37, 2012.Google Scholar

  • 13. Ghorab D., Refai H., Tag R.: Preparation and evaluation of fenoterol hydrobromide suppositories. Drug Discov. Ther., 5(6), 311, 2011.Google Scholar

  • 14. Hargoli S. et al.: Preparation and In vitro Evaluation of Naproxen Suppositories. Indian J. Pharm. Sci., 75(2), 143, 2013.Google Scholar

  • 15. Kalmár É. et al.: Novel sample preparation method for surfactant containing suppositories: effect of micelle formation on drug recovery. J. Pharm. Biomed. Anal., 83, 149, 2013.Web of ScienceGoogle Scholar

  • 16. Karavana S. Y. et al.: Dissolution and histological studies on ordidazole vaginal formulation. Acta Pharma. Sci., 52, 430, 2010.Google Scholar

  • 17. Labrie F. et al.: Effect of intravaginal dehydroepiandrosterone (Prasterone) on libido and sexual dysfunction in postmenopausal women. Menopause, 16(5), 923, 2009.CrossrefWeb of ScienceGoogle Scholar

  • 18. Labrie F. et al.: Intravaginal dehydroepiandrosterone (prasterone), a highly efficient treatment of dyspareunia. Climacteric, 14(2), 282, 2011.Web of ScienceCrossrefGoogle Scholar

  • 19. Labrie F. et al.: Intravaginal dehydroepiandrosterone (Prasterone), a physiological and highly efficient treatment of vaginal atrophy.Menopause, 16(5), 907, 2009.Web of ScienceCrossrefGoogle Scholar

  • 20. Labrie F. et al.: Is Dehydroepiandrosterone a hormone? J. Endocrinol., 187,169, 2005.Google Scholar

  • 21. Labrie F. et al.: Marked decline in serum concentrations of adrenal C19 sex steroid precursors and conjugated androgen metabolites during aging. J. Clin. Endocrinol. Metab., 82, 2396, 1997.Google Scholar

  • 22. Lynch C.: Vaginal estrogen therapy for the treatment of atrophic vaginitis. J. Womens Health (Larchmt), 18(10), 1595, 2009.Web of ScienceCrossrefGoogle Scholar

  • 23. Nestler J. E. et al.: Dehydroepiandrosterone reduces serum low density lipoprotein levels and body fat but does not alter insulin sensitivity in normal men. J. Clin. Endocrinol. Metab., 66, 57, 1988.Google Scholar

  • 24. Niraj et al.: Effect of Adjuvants on the Release Pattern of Suppositories Containing Paracetamol. RJCES, 1(1), 19, 2013.Google Scholar

  • 25. Odeniyi M. A., Jaiyeoba K. T.: Effects of interacting variables on the release properties of chloroquine and aminophylline suppositories.Trop. J. Pharm. Res., 3(1), 285, 2004.Google Scholar

  • 26. Panjari M., Davis S.R.: DHEA for postmenopausal women: a review of the evidence. Maturitas, 66(2), 172, 2010.Web of ScienceCrossrefGoogle Scholar

  • 27. Panjari M., Davis S.R.: Vaginal DHEA to treat menopause related atrophy: a review of the evidence. Maturitas, 70(1), 22, 2011.CrossrefWeb of ScienceGoogle Scholar

  • 28. Polish Pharmacopoeia IXth ed., vol. I, PTF Warsaw (2011).Google Scholar

  • 29. Realdon N. et al.: Effects of surfactant characteristics on drug availability from suppositories. Pharmazie, 63(6), 459, 2008.Web of ScienceGoogle Scholar

  • 30. Sah M. L., Saini T.R.: Formulation development and release studies of indomethacin suppositories. Indian J. Pharm. Sci., 70(4), 498, 2008.Web of ScienceGoogle Scholar

  • 31. Varshney H. M., Chatterjee A.: Formulation, evaluation and in-vitro release characteristics of zaltoprofen suppositories. Asian J. Pharm.Clin. Res., 5(4), 235, 2012.Google Scholar

  • 32. Varshney H. M., Tanwar Y. S.: Effect of different surfactants on the release pattern of cocoa butter suppositories containing flurbiprofen sodium. Acta Pharm. Sci., 52, 129, 2010.Google Scholar

  • 33. Verma P. et al.: Routes of drug administration. Int. J. Pharm. Studies Res., 1(1), 54, 2010.Google Scholar

About the article

Received: 2014-02-18

Accepted: 2014-03-04

Published Online: 2014-05-30

Published in Print: 2014-06-01


Citation Information: Current Issues in Pharmacy and Medical Sciences, Volume 27, Issue 1, Pages 46–50, ISSN (Online) 2300-6676, ISSN (Print) 2084-980X, DOI: https://doi.org/10.2478/cipms-2014-0012.

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© 2014. This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License. BY-NC-ND 3.0

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