The influence of salt formation on electrostatic and compression properties of flurbiprofen salts

Article English OPEN
Šupuk, Enes ; Ghori, Muhammad U. ; Asare-Addo, Kofi ; Laity, Peter R. ; Panchmatia, Pooja M. ; Conway, Barbara R (2013)

Salt formation is an effective method of improving physicochemical properties of acidic and basic drugs. The selection of a salt form most suitable for drug development requires a well-designed screening strategy to ensure various issues are addressed in the early development stages. Triboelectrification of pharmaceutical powders may cause problems during processing such as segregation of components due to the effects of particle adhesion. However, very little work has been done on the effect of salt formation on triboelectrification properties. In this paper, salts of flurbiprofen were prepared by combining the drug with a selection of closely related amine counter ions. The aim of the work was to investigate the impact of the counter ion on electrostatic charge of the resultant salts to inform the salt selection process. The experimental results show the magnitude of charge and polarity of the flurbiprofen salts to be highly dependent on the type of counter ion selected for the salt formation. Furthermore, particle adhesion to the stainless steel surface of the shaking container and the salts’ compression properties were measured. The formed salts had lower electrostatic charges, improved tabletability, and resulted in reduced adhesion of these powders compared with the parent drug.
  • References (20)
    20 references, page 1 of 2

    Bastin, R.J., Bowker, M. J., Slater, B.J., 2000. Salt selection and optimisation for pharmaceutical new chemical entities.Org. Proc. Res. Dev., 4, 427-435.

    Chow, S.F., Chen, M., Shi, L., Chow, A.H. Sun, C.C., 2012. Simultaneously improving the Gould, P.L., 1986. Salt selection for basic drugs. Int. J. Pharm., 33, 201-217.

    Greason, W., 2000, Investigation of a Test Methodology for Triboelectrification, J. Electrostat., 49, 245-256.

    Heckel, , R.W., 1961. An analysis of powder compaction phenonmenon T.Metllac Soc. AIME, 221, 1001-1008.

    Heckel, R.W., 1961a. Desity pressure relationship in powder compaction. T.Mettall Soc. AIME 221, 671-675.

    Kawakita, K., Ludde, K.H., 1970-1971. Some consideration on powder compression equations.

    Powder Tech.,4, 61-68.

    Khankari, R., Grant, D., 1995. Pharmaceutical Hydrates. ThermochimActa., 248, 61-79.

    Kumar, L., Amin, A., Bansal, A.K., 2008.Salt selection in drug development. Pharm.Technol., 3(32), 128-146.

    Lacoulonche, F., Chauvet, A., Masse, J., 1997, An investigation of flurbiprofen polymorphism by thermoanalytical and spectroscopic methods and a study of its interactions with poly-(ethylene glycol) 6000 by differential scanning calorimetry and modelling, Int. J. Pharm., 153 (2), 167-179.

  • Metrics
    0
    views in OpenAIRE
    0
    views in local repository
    192
    downloads in local repository

    The information is available from the following content providers:

    From Number Of Views Number Of Downloads
    University of Huddersfield Repository - IRUS-UK 0 192
Share - Bookmark