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Biopharmaceutical Characterization of Ciprofloxacin HCl-Ferrous Sulfate Interaction

Parojčić, Jelena; Stojković, Aleksandra; Tajber, Lidia; Cvijić, Sandra; Paluch, Krzysztof J.; Đurić, Zorica; Corrigan, Owen I.

(Wiley-Blackwell, Malden, 2011)

TY  - JOUR
AU  - Parojčić, Jelena
AU  - Stojković, Aleksandra
AU  - Tajber, Lidia
AU  - Cvijić, Sandra
AU  - Paluch, Krzysztof J.
AU  - Đurić, Zorica
AU  - Corrigan, Owen I.
PY  - 2011
UR  - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1512
AB  - The ciprofloxacin-iron interaction, resulting in a lower bioavailability, is well documented in vivo; however, a mechanistic explanation supported by experimental data of this interaction is missing. In the present study, ciprofloxacin hydrochloride (HCl) and ferrous sulfate interaction was simulated in vitro by performing solubility and dissolution studies in the reactive media containing ferrous sulfate. Characterization of the precipitate formed indicated its probable chemical structure as Fe(SO(4)(2-))(2)(Cl(-))(2)(ciprofloxacin)(2) x (H(2)O)(n), where n is up to 12 molecules of water. The solubility of this complex in water was estimated to be approximately 2mg/mL, being about 20-fold lower than the solubility of ciprofloxacin HCl. The solubility of the complex was used as input parameter for an in silico modeling by GastroPlus (TM) and the resulting predicted plasma time curves were in good agreement with the in vivo data. These results strongly indicate that ciprofloxacin-iron interaction in vivo is caused by the formation of a low soluble complex. This interaction was also simulated by in vitro dissolution, in which a mini scale apparatus provided more biorelevant results than the standard dissolution apparatus, probably because the drug concentrations in the mini apparatus were higher and, thus, closer to the conditions encountered in vivo.
PB  - Wiley-Blackwell, Malden
T2  - Journal of Pharmaceutical Sciences
T1  - Biopharmaceutical Characterization of Ciprofloxacin HCl-Ferrous Sulfate Interaction
VL  - 100
IS  - 12
SP  - 5174
EP  - 5184
DO  - 10.1002/jps.22707
ER  - 
@article{
author = "Parojčić, Jelena and Stojković, Aleksandra and Tajber, Lidia and Cvijić, Sandra and Paluch, Krzysztof J. and Đurić, Zorica and Corrigan, Owen I.",
year = "2011",
abstract = "The ciprofloxacin-iron interaction, resulting in a lower bioavailability, is well documented in vivo; however, a mechanistic explanation supported by experimental data of this interaction is missing. In the present study, ciprofloxacin hydrochloride (HCl) and ferrous sulfate interaction was simulated in vitro by performing solubility and dissolution studies in the reactive media containing ferrous sulfate. Characterization of the precipitate formed indicated its probable chemical structure as Fe(SO(4)(2-))(2)(Cl(-))(2)(ciprofloxacin)(2) x (H(2)O)(n), where n is up to 12 molecules of water. The solubility of this complex in water was estimated to be approximately 2mg/mL, being about 20-fold lower than the solubility of ciprofloxacin HCl. The solubility of the complex was used as input parameter for an in silico modeling by GastroPlus (TM) and the resulting predicted plasma time curves were in good agreement with the in vivo data. These results strongly indicate that ciprofloxacin-iron interaction in vivo is caused by the formation of a low soluble complex. This interaction was also simulated by in vitro dissolution, in which a mini scale apparatus provided more biorelevant results than the standard dissolution apparatus, probably because the drug concentrations in the mini apparatus were higher and, thus, closer to the conditions encountered in vivo.",
publisher = "Wiley-Blackwell, Malden",
journal = "Journal of Pharmaceutical Sciences",
title = "Biopharmaceutical Characterization of Ciprofloxacin HCl-Ferrous Sulfate Interaction",
volume = "100",
number = "12",
pages = "5174-5184",
doi = "10.1002/jps.22707"
}
Parojčić, J., Stojković, A., Tajber, L., Cvijić, S., Paluch, K. J., Đurić, Z.,& Corrigan, O. I.. (2011). Biopharmaceutical Characterization of Ciprofloxacin HCl-Ferrous Sulfate Interaction. in Journal of Pharmaceutical Sciences
Wiley-Blackwell, Malden., 100(12), 5174-5184.
https://doi.org/10.1002/jps.22707
Parojčić J, Stojković A, Tajber L, Cvijić S, Paluch KJ, Đurić Z, Corrigan OI. Biopharmaceutical Characterization of Ciprofloxacin HCl-Ferrous Sulfate Interaction. in Journal of Pharmaceutical Sciences. 2011;100(12):5174-5184.
doi:10.1002/jps.22707 .
Parojčić, Jelena, Stojković, Aleksandra, Tajber, Lidia, Cvijić, Sandra, Paluch, Krzysztof J., Đurić, Zorica, Corrigan, Owen I., "Biopharmaceutical Characterization of Ciprofloxacin HCl-Ferrous Sulfate Interaction" in Journal of Pharmaceutical Sciences, 100, no. 12 (2011):5174-5184,
https://doi.org/10.1002/jps.22707 . .
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