Prediction of Passive Membrane Permeability of Linagliptin

Authors

  • Chinwe Onah Department of pharmaceutical and medicinal Chemistry University of Nigeria Nsukka Enugu state Nigeria
  • Chika Mbah Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences University of Nigeria, Nsukka, Enugu State. NIGERIA.
  • Chibuike Iloabuchi Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences University of Nigeria, Nsukka, Enugu State. NIGERIA.

DOI:

https://doi.org/10.47957/ijpda.v11i2.540

Keywords:

Linagliptin, partition coefficient, salts (electrolytes), passive diffusion

Abstract

Linagliptin is a highly selective inhibitor of dipeptidyl peptidase-4 and therefore clinically utilized to treat adults with type 2 diabetes mellitus. The objective of this study was to predict how the ions normally found in extracellular or intracellular fluids within the body system will influence the linagliptin’s rate of passive diffusion across a cell membrane. The methodology involved measuring linagliptin partition coefficient in a chloroform-water system containing the salts at 25 oC by the shake flask method. The results indicate that at the highest concentration (0.5 M) of the salts studied, sodium chloride was found to give the highest partition coefficient value when compared to the control. In conclusion, physiological ions would have little or no effect on the drug’s molecular state within extracellular or intracellular fluid as the salts failed to significantly alter the partition coefficient of the drug, hence will not alter passive membrane permeability of linagliptin.

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Author Biographies

Chinwe Onah, Department of pharmaceutical and medicinal Chemistry University of Nigeria Nsukka Enugu state Nigeria

Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University Of Nigeria, Nsukka, Enugu State. Nigeria

Chika Mbah, Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences University of Nigeria, Nsukka, Enugu State. NIGERIA.

Professor, Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University Of Nigeria, Nsukka, Enugu State. Nigeria

Chibuike Iloabuchi, Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences University of Nigeria, Nsukka, Enugu State. NIGERIA.

Department of Pharmaceutical and Medicinal Chemistry, Faculty of Pharmaceutical Sciences, University Of Nigeria, Nsukka, Enugu State. Nigeria

References

Boer GA, Holst JJ. Incretin hormones and type 2 diabetes-Mechanistic insights and therapeutic approaches. Biology. 2020;9(12): 473-478.

Retlich S, Duval V, Ring A. Pharmacokinetics and pharmacodynamics of single rising intravenous dose (0.5 mg-0 mg) and determination of absolute bioavailability of dipeptidyl peptidase-4 inhibitor linagliptin (B 1 1356) in healthymale patients.

Clinical Pharmacokinetics. 2010;49: 829-840.

Deeks ED. Linagliptin. Drugs. 2012;72(13): 1793-1824.

Blech S, Ldwig-Schwellinger E, Grafe-Mody EU. The metabolism and disposition of the oral dipeptidyl peptidase-4 inhibitor, linagliptin in humans.

Drug Metabolism Disposition. 2010;38(4): 667-678.

Agrò FE, Vennari M. Physiology of Body Fluid Compartments and Body Fluid Movements. In: Agrò FE Body Fluid Management. Milano, Italy, Springer, 2013, pp. 1-25..

Wolak DJ, Thorne RG. Diffusion of macromolecules in the brain: implications for drug delivery. Molecular pharmaceutics. 2013;10(5): 1492-1504.

Liu X, Testa B, Fahr A. Lipophilicity and its relationship with passive drug permeation. Pharmaceutical research. 2011;28(5): 962-77.

Shuo S, Shu-zhi L, Mao-bo D, Ke-ya G, Lihua S, Zu-guang Y. Determination of equilibrium solubility and apparent oil/water partition coefficient of artesunate. Chinese Journal of Experimental Traditional Medical Formulae. 2013;19: 9-12.

Johansen M, Bundgaard H. Prodrugs as drug delivery systems XI. Solubility, dissolution and partition behaviour of n-mannich bases and n-hydroxymethyl derivatives.

Archives Pharmaceutical Chemistry Science Education 1980;8: 141-151.

Pallicer JM, Rosés M, Ràfols C, Bosch E, Pascual R, Adriana PA. Evaluation of log Po/w values of drugs from some molecular structure calculation software.

ADMET & DMPK 2014;2(2): 107-114.

Published

2023-08-10
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How to Cite

Onah, C., C. . Mbah, and C. . Iloabuchi. “Prediction of Passive Membrane Permeability of Linagliptin”. International Journal of Pharmaceutics and Drug Analysis, vol. 11, no. 2, Aug. 2023, doi:10.47957/ijpda.v11i2.540.

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