2017
|
Cascone, Sara Modeling and comparison of release profiles: Effect of the dissolution method Journal Article European Journal of Pharmaceutical Sciences, 106 , pp. 352-361, 2017, ISSN: 0928-0987. Abstract | Links | BibTeX | Tags: drug release, In silico, In vitro, Pharmacokinetics @article{Cascone2017,
title = {Modeling and comparison of release profiles: Effect of the dissolution method},
author = {Sara Cascone},
url = {http://www.sciencedirect.com/science/article/pii/S092809871730355X},
doi = {10.1016/j.ejps.2017.06.021},
issn = {0928-0987},
year = {2017},
date = {2017-08-30},
journal = {European Journal of Pharmaceutical Sciences},
volume = {106},
pages = {352-361},
abstract = {During the last decades, the study of the in vitro dissolution of pharmaceuticals has been strongly encouraged by the FDA in order to determine its relationship with the in vivo bioavailability of a drug. In this work immediate and extended release formulations containing diclofenac, a BCS class II drug, were studied using different dissolution methods. The release profiles obtained in USP Apparatus II and USP Apparatus IV were evaluated and compared to determine the effect of the fluid dynamic conditions on the release. The influence of the mixing conditions (i.e. the paddle rotation speed in USP Apparatus II or the inlet flow rate in USP Apparatus IV) on the drug release were evaluated, finding that, for the extended release formulations, they do not affect significantly the release profile. An in vitro device simulating the peristaltic contractions of the stomach during the digestion was used to simulate fluid dynamics closer to the real physiology. The tablets were found to behave in a completely different way if tested in the artificial stomach.
Both model-independent and model-dependent approaches were used to compare and fit the dissolution profiles, respectively. Fit factors were used as indicators of similarity of two dissolution profiles; model equations (such as zero-order, first-order, or Korsmeyer-Peppas equations) were used to fit the experimental data. With the identification of the best fitting model by the use of correlation factors and Akaike Information Criterion, the transport phenomena that determine the behavior of each formulation were identified.},
keywords = {drug release, In silico, In vitro, Pharmacokinetics},
pubstate = {published},
tppubtype = {article}
}
During the last decades, the study of the in vitro dissolution of pharmaceuticals has been strongly encouraged by the FDA in order to determine its relationship with the in vivo bioavailability of a drug. In this work immediate and extended release formulations containing diclofenac, a BCS class II drug, were studied using different dissolution methods. The release profiles obtained in USP Apparatus II and USP Apparatus IV were evaluated and compared to determine the effect of the fluid dynamic conditions on the release. The influence of the mixing conditions (i.e. the paddle rotation speed in USP Apparatus II or the inlet flow rate in USP Apparatus IV) on the drug release were evaluated, finding that, for the extended release formulations, they do not affect significantly the release profile. An in vitro device simulating the peristaltic contractions of the stomach during the digestion was used to simulate fluid dynamics closer to the real physiology. The tablets were found to behave in a completely different way if tested in the artificial stomach.
Both model-independent and model-dependent approaches were used to compare and fit the dissolution profiles, respectively. Fit factors were used as indicators of similarity of two dissolution profiles; model equations (such as zero-order, first-order, or Korsmeyer-Peppas equations) were used to fit the experimental data. With the identification of the best fitting model by the use of correlation factors and Akaike Information Criterion, the transport phenomena that determine the behavior of each formulation were identified. |
2016
|
Lamberti, Gaetano; Cascone, Sara; Marra, Francesco; Titomanlio, Giuseppe; D'Amore, Matteo; Barba, Anna Angela Gastrointestinal behavior and ADME phenomena: II. in silico simulation Journal Article Journal of Drug Delivery Science and Technology, 35 , pp. 165-171, 2016, ISSN: 1773-2247. Abstract | Links | BibTeX | Tags: In silico, Pharmacokinetics @article{Lamberti2016,
title = {Gastrointestinal behavior and ADME phenomena: II. in silico simulation},
author = {Gaetano Lamberti and Sara Cascone and Francesco Marra and Giuseppe Titomanlio and Matteo D'Amore and Anna Angela Barba},
url = {http://www.sciencedirect.com/science/article/pii/S1773224716302118},
doi = {10.1016/j.jddst.2016.06.014},
issn = {1773-2247},
year = {2016},
date = {2016-07-04},
journal = {Journal of Drug Delivery Science and Technology},
volume = {35},
pages = {165-171},
abstract = {The main goal of the pharmacokinetic modeling is the prediction of the drug concentration in the blood, tissues, and organs. The approaches to the modeling of physiological phenomena can be different on the basis of the details used to describe the Adsorption, Distribution, Metabolism, and Excretion (ADME) phenomena.
This review is focused on the state of the art in the pharmacokinetic modeling, on the different approaches used to describe the drug fate once it is administered. In particular, the early and the recent developments in the pharmacokinetic and in the gastrointestinal behavior modeling are discussed, together with some case histories of their applications.},
keywords = {In silico, Pharmacokinetics},
pubstate = {published},
tppubtype = {article}
}
The main goal of the pharmacokinetic modeling is the prediction of the drug concentration in the blood, tissues, and organs. The approaches to the modeling of physiological phenomena can be different on the basis of the details used to describe the Adsorption, Distribution, Metabolism, and Excretion (ADME) phenomena.
This review is focused on the state of the art in the pharmacokinetic modeling, on the different approaches used to describe the drug fate once it is administered. In particular, the early and the recent developments in the pharmacokinetic and in the gastrointestinal behavior modeling are discussed, together with some case histories of their applications. |
2015
|
Cascone, Sara; Piazza, Ornella; Lamberti, Gaetano; Barba, Anna Angela; Abbiati, Roberto Andrea; Manca, Davide PHARMACOKINETICS OF REMIFENTANIL: METABOLISM AND MODELING Inproceedings 1st International Congress of Controlled Release Society - Greek Local Chapter, 2015. BibTeX | Tags: In silico, Pharmacokinetics @inproceedings{Cascone:aa,
title = {PHARMACOKINETICS OF REMIFENTANIL: METABOLISM AND MODELING},
author = {Sara Cascone and Ornella Piazza and Gaetano Lamberti and Anna Angela Barba and Roberto Andrea Abbiati and Davide Manca},
year = {2015},
date = {2015-05-27},
booktitle = {1st International Congress of Controlled Release Society - Greek Local Chapter},
keywords = {In silico, Pharmacokinetics},
pubstate = {published},
tppubtype = {inproceedings}
}
|
2013
|
Cascone, Sara; Lamberti, Gaetano; Titomanlio, Giuseppe; Piazza, Ornella Pharmacokinetics of Remifentanil: a three-compartmental modeling approach Journal Article Translational Medicine @ UniSa, 7 , pp. 18–22, 2013, ISSN: 2239-9747. Abstract | Links | BibTeX | Tags: In silico, Pharmacokinetics @article{Cascone2013,
title = {Pharmacokinetics of Remifentanil: a three-compartmental modeling approach},
author = { Sara Cascone and Gaetano Lamberti and Giuseppe Titomanlio and Ornella Piazza},
url = {http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3829787/},
issn = {2239-9747},
year = {2013},
date = {2013-09-01},
journal = {Translational Medicine @ UniSa},
volume = {7},
pages = {18--22},
publisher = {Universit},
abstract = {Remifentanil is a new opioid derivative drug characterized by a fast onset and by a short time of action, since it is rapidly degraded by esterases in blood and other tissues. Its pharmacokinetic and pharmacodynamics properties make remifentanil a very interesting molecule in the field of 0anesthesia. However a complete and versatile pharmacokinetic description of remifentanil still lacks. In this work a three-compartmental model has been developed to describe the pharmacokinetics of remifentanil both in the case in which it is administered by intravenous constant-rate infusion and by bolus injection. The model curves have been compared with experimental data published in scientific papers and the model parameters have been optimized to describe both ways of administration. The ad hoc model is adaptable and potentially useful for predictive purposes.},
keywords = {In silico, Pharmacokinetics},
pubstate = {published},
tppubtype = {article}
}
Remifentanil is a new opioid derivative drug characterized by a fast onset and by a short time of action, since it is rapidly degraded by esterases in blood and other tissues. Its pharmacokinetic and pharmacodynamics properties make remifentanil a very interesting molecule in the field of 0anesthesia. However a complete and versatile pharmacokinetic description of remifentanil still lacks. In this work a three-compartmental model has been developed to describe the pharmacokinetics of remifentanil both in the case in which it is administered by intravenous constant-rate infusion and by bolus injection. The model curves have been compared with experimental data published in scientific papers and the model parameters have been optimized to describe both ways of administration. The ad hoc model is adaptable and potentially useful for predictive purposes. |
2012
|
Cascone, Sara; Lamberti, Gaetano; Paolucci, Fabio; Titomanlio, Giuseppe In vitro and in silico approaches to reproduce pharmacokinetic relevant phenomena Inproceedings Proceedings of 8th World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology, pp. 1–2, PBP 2012, Istanbul, Turkey, 2012. BibTeX | Tags: In silico, In vitro, Pharmacokinetics @inproceedings{s.2012,
title = {In vitro and in silico approaches to reproduce pharmacokinetic relevant phenomena},
author = { Sara Cascone and Gaetano Lamberti and Fabio Paolucci and Giuseppe Titomanlio},
year = {2012},
date = {2012-03-01},
booktitle = {Proceedings of 8th World Meeting on Pharmaceutics, Biopharmaceutics and Pharmaceutical Technology},
pages = {1--2},
publisher = {PBP 2012},
address = {Istanbul, Turkey},
keywords = {In silico, In vitro, Pharmacokinetics},
pubstate = {published},
tppubtype = {inproceedings}
}
|
Lamberti, Gaetano; Cascone, Sara; Titomanlio, Giuseppe An engineering approach to biomedical sciences: advanced testing methods and pharmacokinetic modeling Journal Article Translational Medicine@ UniSa, 4 , pp. 34–38, 2012. Abstract | BibTeX | Tags: In silico, in-silico, in-vitro, in-vivo, Pharmacokinetics, testing methods @article{Lamberti2012b,
title = {An engineering approach to biomedical sciences: advanced testing methods and pharmacokinetic modeling},
author = { Gaetano Lamberti and Sara Cascone and Giuseppe Titomanlio},
year = {2012},
date = {2012-01-01},
journal = {Translational Medicine@ UniSa},
volume = {4},
pages = {34--38},
publisher = {Universit},
abstract = {In this paper, the philosophy of a research in pharmacology field, driven by an engineering approach, was described along with some case histories and examples. The improvement in the testing methods for pharmaceutical systems (in-vitro techniques), as well as the proposal and the testing of mathematical models to describe the pharmacokinetics (in-silico techniques) are reported with the aim of pointing out methodologies and tools able to reduce the need of expensive and ethical problematic in-vivo measurements.},
keywords = {In silico, in-silico, in-vitro, in-vivo, Pharmacokinetics, testing methods},
pubstate = {published},
tppubtype = {article}
}
In this paper, the philosophy of a research in pharmacology field, driven by an engineering approach, was described along with some case histories and examples. The improvement in the testing methods for pharmaceutical systems (in-vitro techniques), as well as the proposal and the testing of mathematical models to describe the pharmacokinetics (in-silico techniques) are reported with the aim of pointing out methodologies and tools able to reduce the need of expensive and ethical problematic in-vivo measurements. |
2011
|
Grassi, Mario; Lamberti, Gaetano; Cascone, Sara; Grassi, Gabriele Mathematical modeling of simultaneous drug release and in vivo absorption. Journal Article International journal of pharmaceutics, 418 (1), pp. 130–41, 2011, ISSN: 1873-3476. Abstract | Links | BibTeX | Tags: Absorption, Administration, Area Under Curve, Biological, Drug Delivery Systems, Humans, In silico, Models, Oral, Pharmacokinetics, Solubility, Theoretical @article{Grassi2011,
title = {Mathematical modeling of simultaneous drug release and in vivo absorption.},
author = { Mario Grassi and Gaetano Lamberti and Sara Cascone and Gabriele Grassi},
url = {http://www.sciencedirect.com/science/article/pii/S0378517311000275},
doi = {10.1016/j.ijpharm.2010.12.044},
issn = {1873-3476},
year = {2011},
date = {2011-10-01},
journal = {International journal of pharmaceutics},
volume = {418},
number = {1},
pages = {130--41},
abstract = {The attention of this review is focussed on the mathematical modeling of the simultaneous processes of drug release and absorption/distribution/metabolism/elimination (ADME processes) following different administration routes. Among all of them, for their clinical importance, the oral, transdermal and local delivery are considered. The bases of the presented mathematical models are shown after the discussion of the most relevant phenomena characterising the particular administration route considered. Then, model performances are compared to experimental evidences in order to evaluate their reliability and soundness. The most important conclusion of this review is that despite the complexity of the problem involved in the description of the fate of the drugs after their administration, the scientific community is close to the solution as witnessed by the various interesting and promising approaches here presented about the oral, transdermal and local administration routes.},
keywords = {Absorption, Administration, Area Under Curve, Biological, Drug Delivery Systems, Humans, In silico, Models, Oral, Pharmacokinetics, Solubility, Theoretical},
pubstate = {published},
tppubtype = {article}
}
The attention of this review is focussed on the mathematical modeling of the simultaneous processes of drug release and absorption/distribution/metabolism/elimination (ADME processes) following different administration routes. Among all of them, for their clinical importance, the oral, transdermal and local delivery are considered. The bases of the presented mathematical models are shown after the discussion of the most relevant phenomena characterising the particular administration route considered. Then, model performances are compared to experimental evidences in order to evaluate their reliability and soundness. The most important conclusion of this review is that despite the complexity of the problem involved in the description of the fate of the drugs after their administration, the scientific community is close to the solution as witnessed by the various interesting and promising approaches here presented about the oral, transdermal and local administration routes. |
Cascone, Sara; Santis, Felice De; Lamberti, Gaetano; Titomanlio, Giuseppe The influence of dissolution conditions on the drug ADME phenomena. Journal Article European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft für Pharmazeutische Verfahrenstechnik e.V, 79 (2), pp. 382–91, 2011, ISSN: 1873-3441. Abstract | Links | BibTeX | Tags: ADME, Dissolution, Enteric coated, In silico, In vitro, Pharmacokinetic modeling, Pharmacokinetics @article{Cascone2011,
title = {The influence of dissolution conditions on the drug ADME phenomena.},
author = { Sara Cascone and Felice De Santis and Gaetano Lamberti and Giuseppe Titomanlio},
url = {http://www.sciencedirect.com/science/article/pii/S093964111100141X},
doi = {10.1016/j.ejpb.2011.04.003},
issn = {1873-3441},
year = {2011},
date = {2011-10-01},
journal = {European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft f\"{u}r Pharmazeutische Verfahrenstechnik e.V},
volume = {79},
number = {2},
pages = {382--91},
abstract = {In this work, a review of the apparatuses available to mimic what happens to a drug (or to foodstuffs) once ingested is presented. Similarly, a brief review of the models proposed to simulate the fate of a drug administered to a living body is reported. Then, the release kinetics of extended release of diclofenac from a commercial enteric-coated tablet was determined both in a conventional dissolution tester (USP Apparatus 2, Method A) as well as in an apparatus modified to reproduce a given pH evolution, closer to the real one than the one suggested by USP. The two experimental release profiles were reported and discussed; therefore, they were adopted as input functions for a previously proposed pharmacokinetic model. The obtained evolutions with time of plasma concentration were presented and used to assess the effectiveness of the commercial pharmaceutical products. The importance of a correct in vitro simulation for the design of pharmaceutical dosage systems was thus emphasized.},
keywords = {ADME, Dissolution, Enteric coated, In silico, In vitro, Pharmacokinetic modeling, Pharmacokinetics},
pubstate = {published},
tppubtype = {article}
}
In this work, a review of the apparatuses available to mimic what happens to a drug (or to foodstuffs) once ingested is presented. Similarly, a brief review of the models proposed to simulate the fate of a drug administered to a living body is reported. Then, the release kinetics of extended release of diclofenac from a commercial enteric-coated tablet was determined both in a conventional dissolution tester (USP Apparatus 2, Method A) as well as in an apparatus modified to reproduce a given pH evolution, closer to the real one than the one suggested by USP. The two experimental release profiles were reported and discussed; therefore, they were adopted as input functions for a previously proposed pharmacokinetic model. The obtained evolutions with time of plasma concentration were presented and used to assess the effectiveness of the commercial pharmaceutical products. The importance of a correct in vitro simulation for the design of pharmaceutical dosage systems was thus emphasized. |