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. 2013 Dec 3:2013:131358.
doi: 10.1155/2013/131358. eCollection 2013.

Pharmacokinetic delivery and metabolizing rate of nicardipine incorporated in hydrophilic and hydrophobic cyclodextrins using two-compartment mathematical model

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Pharmacokinetic delivery and metabolizing rate of nicardipine incorporated in hydrophilic and hydrophobic cyclodextrins using two-compartment mathematical model

Sergey Shityakov et al. ScientificWorldJournal. .

Abstract

The dispersion routes of cyclodextrin complexes with nicardipine (NC), such as hydrophilic hydroxypropyl-β-cyclodextrin (NC/HPβCD) and hydrophobic triacetyl-β-cyclodextrin (NC/TAβCD), through the body for controlled drug delivery and sustained release have been examined. The two-compartment pharmacokinetic model described the mechanisms of how the human body handles with ingestion of NC-cyclodextrin complexes in gastrointestinal tract (GI), distribution in plasma, and their metabolism in the liver. The model showed that drug bioavailability was significantly improved after oral administration of cyclodextrin complexes. The mathematical significance of this study to predict nicardipine delivery using pharmacokinetic two-compartment mathematical model with linear ordinary differential equations (ODE) approach represents a valuable tool to emphasize its effectiveness and metabolizing rate and diminish the side effects.

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Figures

Figure 1
Figure 1
Loading of long-range GI and plasma concentration-time profiles from a dosage regime for NC (a), NC/HPβCD (b), and NC/TAβCD (c) compounds after oral administration.
Figure 2
Figure 2
{x(t), y(t)} with limit cycle for NC, NC/HPβCD, and NC/TAβCD substances.
Figure 3
Figure 3
Short-range GI (a) and plasma concentration (b) levels for NC, NC/HPβCD, and NC/TAβCD and their metabolizing rates (c) as functions of time using refined rate constants.
Algorithm 1
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Algorithm 2

References

    1. Marques Fernandes C, Ramos P, Celta Falcão A, Baptista Veiga FJ. Hydrophilic and hydrophobic cyclodextrins in a new sustained release oral formulation of nicardipine: in vitro evaluation and bioavailability studies in rabbits. Journal of Controlled Release. 2003;88(1):127–134. - PubMed
    1. Watson CA, Vine KL, et al. The antiangiogenic properties of sulfated beta-cyclodextrins in anticancer formulations incorporating 5-fluorouracil. Anticancer Drugs. 2013;24(7):704–714. - PubMed
    1. Koester LS, Ortega GG, Mayorga P, Bassani VL. Mathematical evaluation of in vitro release profiles of hydroxypropylmethylcellulose matrix tablets containing carbamazepine associated to β-cyclodextrin. European Journal of Pharmaceutics and Biopharmaceutics. 2004;58(1):177–179. - PubMed
    1. McIntosh MP, Rajewski RA. Comparative canine pharmacokinetics-pharmacodynamics of fospropofol disodium injection, propofol emulsion, and cyclodextrin-enabled propofol solution following bolus parenteral administration. Journal of Pharmaceutical Sciences. 2012;101(9):3547–3552. - PubMed
    1. Langenbucher F. Linearization of dissolution rate curves by the Weibull distribution. Journal of Pharmacy and Pharmacology. 1972;24(12):979–981. - PubMed

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