Mathematical modeling of pH-surfactant-mediated solubilization of nimesulide
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2009
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Aim: The equilibrium-based mathematical model was used to describe the pH-surfactant-mediated solubilization of weakly acidic electrolyte, nimesulide, in buffer solutions. This model assumed that the total drug solubility could be expressed as a sum of the solubilities of four different species: unionized and ionized form in solution and their corresponding micellar forms. Sucrose-laurate, new synthetic surfactant, and polysorbate 80 were investigated for their benefits in the testing of poorly soluble acidic model drug. Method: Two sets of solubility data, determined at pH values 4.5 and 9.0 in media containing different surfactant concentrations, were used to calculate solubilization slopes and corresponding micellar equilibrium constants for the unionized (K(n)) and ionized (K(i)) drug. These values were used to estimate drug solubilization in media considered to represent physiologically relevant conditions. Results: Predicted solubility values were in good agreement with the exper...imental data, suggesting that the impact of pH and surfactant on nimesulide solubility could be well characterized by the equilibrium model described in this article. Conclusions: Obtained results indicated that the extent of solubilization was significantly dependent on the surfactant used.
Ključne reči:
Nimesulide / pH effect / polysorbate 80 / solubilization / sucrose-laurate / surfactantIzvor:
Drug Development and Industrial Pharmacy, 2009, 35, 7, 852-856Izdavač:
- Taylor & Francis Inc, Philadelphia
Finansiranje / projekti:
- Razvoj i primena in vitro i in silico metoda u biofarmaceutskoj karakterizaciji lekova BSK grupe 2 i 3 (RS-MESTD-MPN2006-2010-23015)
DOI: 10.1080/03639040802680230
ISSN: 0363-9045
PubMed: 19347760
WoS: 000268182100010
Scopus: 2-s2.0-70350686569
Institucija/grupa
PharmacyTY - JOUR AU - Grbić, Sandra AU - Parojčić, Jelena AU - Đurić, Zorica AU - Ibrić, Svetlana PY - 2009 UR - https://farfar.pharmacy.bg.ac.rs/handle/123456789/1286 AB - Aim: The equilibrium-based mathematical model was used to describe the pH-surfactant-mediated solubilization of weakly acidic electrolyte, nimesulide, in buffer solutions. This model assumed that the total drug solubility could be expressed as a sum of the solubilities of four different species: unionized and ionized form in solution and their corresponding micellar forms. Sucrose-laurate, new synthetic surfactant, and polysorbate 80 were investigated for their benefits in the testing of poorly soluble acidic model drug. Method: Two sets of solubility data, determined at pH values 4.5 and 9.0 in media containing different surfactant concentrations, were used to calculate solubilization slopes and corresponding micellar equilibrium constants for the unionized (K(n)) and ionized (K(i)) drug. These values were used to estimate drug solubilization in media considered to represent physiologically relevant conditions. Results: Predicted solubility values were in good agreement with the experimental data, suggesting that the impact of pH and surfactant on nimesulide solubility could be well characterized by the equilibrium model described in this article. Conclusions: Obtained results indicated that the extent of solubilization was significantly dependent on the surfactant used. PB - Taylor & Francis Inc, Philadelphia T2 - Drug Development and Industrial Pharmacy T1 - Mathematical modeling of pH-surfactant-mediated solubilization of nimesulide VL - 35 IS - 7 SP - 852 EP - 856 DO - 10.1080/03639040802680230 ER -
@article{ author = "Grbić, Sandra and Parojčić, Jelena and Đurić, Zorica and Ibrić, Svetlana", year = "2009", abstract = "Aim: The equilibrium-based mathematical model was used to describe the pH-surfactant-mediated solubilization of weakly acidic electrolyte, nimesulide, in buffer solutions. This model assumed that the total drug solubility could be expressed as a sum of the solubilities of four different species: unionized and ionized form in solution and their corresponding micellar forms. Sucrose-laurate, new synthetic surfactant, and polysorbate 80 were investigated for their benefits in the testing of poorly soluble acidic model drug. Method: Two sets of solubility data, determined at pH values 4.5 and 9.0 in media containing different surfactant concentrations, were used to calculate solubilization slopes and corresponding micellar equilibrium constants for the unionized (K(n)) and ionized (K(i)) drug. These values were used to estimate drug solubilization in media considered to represent physiologically relevant conditions. Results: Predicted solubility values were in good agreement with the experimental data, suggesting that the impact of pH and surfactant on nimesulide solubility could be well characterized by the equilibrium model described in this article. Conclusions: Obtained results indicated that the extent of solubilization was significantly dependent on the surfactant used.", publisher = "Taylor & Francis Inc, Philadelphia", journal = "Drug Development and Industrial Pharmacy", title = "Mathematical modeling of pH-surfactant-mediated solubilization of nimesulide", volume = "35", number = "7", pages = "852-856", doi = "10.1080/03639040802680230" }
Grbić, S., Parojčić, J., Đurić, Z.,& Ibrić, S.. (2009). Mathematical modeling of pH-surfactant-mediated solubilization of nimesulide. in Drug Development and Industrial Pharmacy Taylor & Francis Inc, Philadelphia., 35(7), 852-856. https://doi.org/10.1080/03639040802680230
Grbić S, Parojčić J, Đurić Z, Ibrić S. Mathematical modeling of pH-surfactant-mediated solubilization of nimesulide. in Drug Development and Industrial Pharmacy. 2009;35(7):852-856. doi:10.1080/03639040802680230 .
Grbić, Sandra, Parojčić, Jelena, Đurić, Zorica, Ibrić, Svetlana, "Mathematical modeling of pH-surfactant-mediated solubilization of nimesulide" in Drug Development and Industrial Pharmacy, 35, no. 7 (2009):852-856, https://doi.org/10.1080/03639040802680230 . .