Advertisement

AAPS PharmSciTech

, Volume 19, Issue 3, pp 1337–1343 | Cite as

Effect of Moisture Content of Chitin-Calcium Silicate on Rate of Degradation of Cefotaxime Sodium

  • Suhair S. Al-Nimry
  • Khouloud A. Alkhamis
Research Article
  • 78 Downloads

Abstract

Assessment of incompatibilities between active pharmaceutical ingredient and pharmaceutical excipients is an important part of preformulation studies. The objective of the work was to assess the effect of moisture content of chitin calcium silicate of two size ranges (two specific surface areas) on the rate of degradation of cefotaxime sodium. The surface area of the excipient was determined using adsorption method. The effect of moisture content of a given size range on the stability of the drug was determined at 40°C in the solid state. The moisture content was determined at the beginning and the end of the kinetic study using TGA. The degradation in solution was studied for comparison. Increasing the moisture content of the excipient of size range 63–180 μm (surface area 7.2 m2/g) from 3.88 to 8.06% increased the rate of degradation of the drug more than two times (from 0.0317 to 0.0718 h−1). While an opposite trend was observed for the excipient of size range < 63 μm (surface area 55.4 m2/g). The rate of degradation at moisture content < 3% was 0.4547 h−1, almost two times higher than that (0.2594 h−1) at moisture content of 8.54%, and the degradation in solid state at both moisture contents was higher than that in solution (0.0871 h−1). In conclusion, the rate of degradation in solid should be studied taking into consideration the specific surface area and moisture content of the excipient at the storage condition and it may be higher than that in solution.

KEY WORDS

moisture content chitin calcium silicate degradation kinetics cefotaxime sodium surface area 

Notes

Acknowledgments

The authors thank the Jordanian Manufacturing Co. (Amman, Jordan) for kindly donating chitin. Also, they thank the deanship of scientific research at Jordan University of Science and Technology for their financial support (grant number 148/2015).

Compliance with Ethical Standards

Conflict of Interest

The authors declare that they have no conflict of interest.

References

  1. 1.
    Harbir K. Processing technologies for pharmaceutical tablets: a review. Int Res J Pharm. 2012;3(7):20–3.Google Scholar
  2. 2.
    Saha S, Shahiwala AF. Multifunctional coprocessed excipients for improved tabletting performance. Expert Opin Drug Deliv. 2009;6(2):197–208.  https://doi.org/10.1517/17425240802708978.CrossRefPubMedGoogle Scholar
  3. 3.
    Al-Shaikh Hamid R, Al-Akayleh F, Shubair M, RashidI, Al Remawi M, Badwan A. Evaluation of three chitin metal silicate co-precipitates as a potential multifunctional single excipient in tablet formulations. Mar Drugs. 2010;8(5):1699–715.  https://doi.org/10.3390/md8051699.CrossRefGoogle Scholar
  4. 4.
    Rashid I, Daraghmeh N, Al-Remawi M, Leharne SA, Chowdhry BZ, Badwan A. Characterization of chitin–metal silicates as binding superdisintegrants. J Pharm Sci. 2009;98(12):4887–901.  https://doi.org/10.1002/jps.21781.CrossRefPubMedGoogle Scholar
  5. 5.
    Connors KA, Amidon GL, Stella VJ. Chemical stability of pharmaceuticals: a handbook for pharmacists. 2nd ed. United States: John Wiley & Sons; 1986.Google Scholar
  6. 6.
    Berge SM, Henderson NL, Frank MJ. Kinetics and mechanism of degradation of cefotaxime sodium in aqueous solution. J Pharm Sci. 1983 Jan;72(1):59–63.  https://doi.org/10.1002/jps.2600720114.CrossRefPubMedGoogle Scholar
  7. 7.
    Fabre H, Eddine NH, Berge G. Degradation kinetics in aqueous solution of cefotaxime sodium, a third-generation cephalosporin. J Pharm Sci. 1984;73(5):611–8.  https://doi.org/10.1002/jps.2600730508.CrossRefPubMedGoogle Scholar
  8. 8.
    Cupta V. Stability of cefotaxime sodium as determined by high-performance liquid chromatography. J Pharm Sci. 1984;73(4):565–7.CrossRefGoogle Scholar
  9. 9.
    Lerner DA, Bonnefond G, Fabre H, Mandrou B, Simeon de Buochberg M. Photodegradation paths of cefotaxime. J Pharm Sci. 1988;77(8):699–703.  https://doi.org/10.1002/jps.2600770812.CrossRefPubMedGoogle Scholar
  10. 10.
    Byrn SR, Xu W, Newman AW. Chemical reactivity in solid-state pharmaceuticals: formulation implications. Adv Drug Deliv Rev. 2001;48(1):115–36.  https://doi.org/10.1016/S0169-409X(01)00102-8.CrossRefPubMedGoogle Scholar
  11. 11.
    Bharate SS, Bharate SB, Bajaj AN. Interactions and incompatibilities of pharmaceutical excipients with active pharmaceutical ingredients: a comprehensive review. J. Excipients and Food Chem. 2010;1(3):3–26.Google Scholar
  12. 12.
    Zhou D. Understanding physicochemical properties for pharmaceutical product development and manufacturing II: physical and chemical stability and excipient compatibility. J Val Tech. 2009;15(3):36–47.Google Scholar
  13. 13.
    Rowe RC, Sheskey PJ, Quinn ME, editors. Handbook of pharmaceutical excipients. 6th ed. United Kingdom: Pharmaceutical press; 2009.Google Scholar
  14. 14.
    Gana FZ, Rashid I, Badwan A, Alkhamis KA. Determination of solid state acidity of chitin metal silicates and their effect on the degradation of cephalosporin antibiotics. J Pharm Sci. 2012;101(7):2398–407.  https://doi.org/10.1002/jps.23142.CrossRefPubMedGoogle Scholar
  15. 15.
    Mwesigwa E, Basit AW. An investigation into moisture barrier film coating efficacy and its relevance to drug stability in solid dosage forms. Int J Pharm. 2016;497(1-2):70–7.  https://doi.org/10.1016/j.ijpharm.2015.10.068.CrossRefPubMedGoogle Scholar
  16. 16.
    Al-Nimry SS, Alkhamis KA, Alzarieni KZ. The effect of specific surface area of chitin metal silicate coprocessed excipient on the chemical decomposition of cefotaxime sodium. J Pharm Sci. 2017;106(2):570–8.  https://doi.org/10.1016/j.xphs.2016.10.012.CrossRefPubMedGoogle Scholar
  17. 17.
  18. 18.
    Rashid I, Daraghmeh NH, Al Omari MM, Chowdhry BZ, Leharne SA, Hodali HA, et al. Magnesium silicate. In: Brittain HG, editor. Profiles of drug substances, excipients and related methodology. San Diego: Academic press; 2011. p. 241–85.Google Scholar
  19. 19.
    McClellan AL, Harnsberger HF. Cross-sectional areas of molecules adsorbed on solid surfaces. J Colloid Interface Sci. 1967;23(4):577–99.  https://doi.org/10.1016/0021-9797(67)90204-4.CrossRefGoogle Scholar
  20. 20.
    Sinko PJ, Allen LV Jr, Popovich NG, Ansel HC. Martin’s physical pharmacy and pharmaceutical sciences. 5th ed. United States: Lippincott Williams & Wilkins; 2006.Google Scholar
  21. 21.
    Adamson A, Gast A. Physical chemistry of surfaces. 6th ed. New York: John Wiley and Sons, Inc; 1997.Google Scholar
  22. 22.
    Lowell S, Shields JE, Thomas MA, Thommes M. Characterization of porous solids and powders: surface area, pore size and density. New York: Springer Science Business Media; 2004.CrossRefGoogle Scholar
  23. 23.
    Vega-Baudrit J, Sibaja-Ballestero M, Vázquez P, Torregrosa-Maciá R, Martín-Martínez JM. Properties of thermoplastic polyurethane adhesives containing nanosilicas with different specific surface area and silanol content. Int J Adhes Adhes. 2007;27(6):469–79.  https://doi.org/10.1016/j.ijadhadh.2006.08.001.CrossRefGoogle Scholar
  24. 24.
    Gana FZ. The effect of solid state acidity of chitin metal silicates on the degradation and dissolution of cefotaxime sodium and ketoconazole. MSc dissertation, Irbid, Jordan, Jordan University of Science and Technology; 2011.Google Scholar
  25. 25.
    Weng HL, Parrott EL. Solid-solid reaction between sulfacetamide and phthalic anhydride. J Pharm Sci. 1984;73(8):1059–63.  https://doi.org/10.1002/jps.2600730810.CrossRefPubMedGoogle Scholar

Copyright information

© American Association of Pharmaceutical Scientists 2018

Authors and Affiliations

  1. 1.Pharmaceutical Technology Department, Faculty of PharmacyJordan University of Science and TechnologyIrbidJordan

Personalised recommendations