Skip to main content
SpringerLink
Log in

Preparation and Bioavailability Evaluation of Micronized Steroidal Mecigestone Drug Substance

  • DRUG SYNTHESIS METHODS AND MANUFACTURING TECHNOLOGY
  • Published:
Pharmaceutical Chemistry Journal Aims and scope

Microcrystals of 6α-methyl-16α,17α-cyclohexapregn-4-ene-3,20-dione (mecigestone) that differed from the starting drug substance by decreased sizes and altered morphologies were produced using a Nano Spray Dryer B-90 (Buchi, Switzerland) that allowed operation with organic solvents in a closed cycle. The bioavailability of starting crystalline and micronized mecigestone drug substance was studied by oral administration to laboratory white rats. Mecigestone was extracted from rat blood serum using solvent extraction. The extraction coefficient was 64%. The detection limit of the drug substance was 0.08 ng/mL. The content of unaltered mecigestone in the extracts was determined using HPLC with high-resolution mass spectrometric detection. Micronized mecigestone was 7.5 times more bioavailable than the starting drug substance.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5

Similar content being viewed by others

References

  1. K. P. Madauss, E. L. Stewart, and S. P. Williams, Med. Res. Rev., 27, 374 – 400 (2007).

    Article  CAS  PubMed  Google Scholar 

  2. A. V. Kamernitskii and I. S. Levina, Bioorg. Khim., 31, 115 – 129 (2005).

    CAS  PubMed  Google Scholar 

  3. A. V. Kamernitskii and I. S. Levina, Bioorg. Khim., 31, 227 – 238 (2005).

    CAS  PubMed  Google Scholar 

  4. N. L. Shimanovskii, A. V. Semeikin, T. A. Fedotcheva, et al., Byull. Eksp. Biol. Med., No. 10, 447 – 450 (2002).

  5. S. V. Emshanova, Khim.-farm. Zh., 42(2), 38 – 43 (2008); Pharm. Chem. J., 42(2), 89 – 94 (2008).

  6. N. V. Efremova and I. N. Topchieva, Biokhimiya, 58(7), 1071 – 1076 (1993).

    CAS  Google Scholar 

  7. J. L. Benifia, M. Dumont, M. Levardion, et al., Contracept. Fertil. Sex., 25, 165 – 169 (1997).

    Google Scholar 

  8. N. Rasenack, H. Streckel, and B. W. Muller, J. Pharm. Sci., 92(1), 35 – 44 (2003).

  9. Y. P. Sun, M. J. Meziani, P. Pathak, et al., Chem. Eur. J., 11(5), 1366 – 1373 (2005).

    Article  CAS  PubMed  Google Scholar 

  10. K. Moribe, S. Tsutsumi, S. Morishita, et al., Chem. Pharm. Bull., 53(8), 1025 – 1028 (2005).

    Article  CAS  PubMed  Google Scholar 

  11. N. Schafroth, C. Arpagaus, U. Y. Jadhav, et al. Colloids Surf., B, 90, 8 – 15 (2012).

  12. A. S. Kashin and V. P. Ananikov, Izv. Akad. Nauk, Ser. Khim., No. 12, 2551 – 2556 (2011).

Download references

Acknowledgments

We thank the Division of Structural Research, Inst. Org. Chem., RAS, for performing the electron microscope studies.

Author information

Authors and Affiliations

  1. Zelinsky Institute of Organic Chemistry, Russian Academy of Sciences, Leninskii Prosp., 47, Moscow, 119991, Russia

    A. K. Nazarov, I. V. Zavarzin, G. V. Nazarov, A. V. Aksenov & I. S. Levina

Authors
  1. A. K. Nazarov
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. I. V. Zavarzin
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. G. V. Nazarov
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. A. V. Aksenov
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. I. S. Levina
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to A. K. Nazarov.

Additional information

Translated from Khimiko-Farmatsevticheskii Zhurnal, Vol. 49, No. 10, pp. 44 – 48, October, 2015.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Nazarov, A.K., Zavarzin, I.V., Nazarov, G.V. et al. Preparation and Bioavailability Evaluation of Micronized Steroidal Mecigestone Drug Substance. Pharm Chem J 49, 706–710 (2016). https://doi.org/10.1007/s11094-016-1357-6

Download citation

  • Received:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s11094-016-1357-6

Keywords

Search

Navigation