Biopharmaceutical Characterization of Ciprofloxacin HCl-Ferrous Sulfate Interaction
Samo za registrovane korisnike
2011
Autori
Parojčić, JelenaStojković, Aleksandra
Tajber, Lidia
Cvijić, Sandra
Paluch, Krzysztof J.
Đurić, Zorica
Corrigan, Owen I.
Članak u časopisu (Objavljena verzija)
Metapodaci
Prikaz svih podataka o dokumentuApstrakt
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 i...nteraction 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.
Ključne reči:
bioavailability / Biopharmaceutics Classification System (BCS) / ciprofloxacin HCl / dissolution / drug interaction / in silico modeling / ferrous sulfate / oral absorption / solubilityIzvor:
Journal of Pharmaceutical Sciences, 2011, 100, 12, 5174-5184Izdavač:
- Wiley-Blackwell, Malden
Finansiranje / projekti:
- Razvoj proizvoda i tehnologija koje obezbeđuju željeno oslobađanje lekovitih supstanci iz čvrstih farmaceutskih oblika (RS-34007)
- Solid State Pharmaceutical Cluster
DOI: 10.1002/jps.22707
ISSN: 0022-3549
PubMed: 21789771
WoS: 000297425600008
Scopus: 2-s2.0-80054921557
Institucija/grupa
PharmacyTY - 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 . .