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Mathematical modeling of pH-surfactant-mediated solubilization of nimesulide

Authorized Users Only
2009
Authors
Grbić, Sandra
Parojčić, Jelena
Đurić, Zorica
Ibrić, Svetlana
Article (Published version)
Metadata
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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 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.

Keywords:
Nimesulide / pH effect / polysorbate 80 / solubilization / sucrose-laurate / surfactant
Source:
Drug Development and Industrial Pharmacy, 2009, 35, 7, 852-856
Publisher:
  • Taylor & Francis Inc, Philadelphia
Funding / projects:
  • Razvoj i primena in vitro i in silico metoda u biofarmaceutskoj karakterizaciji lekova BSK grupe 2 i 3 (RS-23015)

DOI: 10.1080/03639040802680230

ISSN: 0363-9045

PubMed: 19347760

WoS: 000268182100010

Scopus: 2-s2.0-70350686569
[ Google Scholar ]
3
2
URI
https://farfar.pharmacy.bg.ac.rs/handle/123456789/1286
Collections
  • Radovi istraživača / Researchers’ publications
Institution/Community
Pharmacy
TY  - 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 . .

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