Use of Solid Dispersions and Inclusion Complexation for Enhancing Oral Bioavailability of Ziprasidone in Treating Schizophrenia

Poonam Mogal; Deeliprao Derle

doi:doi:10.11648/j.jddmc.20170303.12

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Use of Solid Dispersions and Inclusion Complexation for Enhancing Oral Bioavailability of Ziprasidone in Treating Schizophrenia

Poonam Mogal, Deeliprao Derle

Published in Journal of Drug Design and Medicinal Chemistry (Volume 3, Issue 3)

Received: 19 May 2017 Accepted: 21 June 2017 Published: 25 July 2017

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Abstract

In modern times, people are suffering from many mental health disorders like schizophrenia, bipolar disorders and many psychoses. Hence, it is essential to treat these mental disorders using medications as well as with assistance from caregivers for the social well being of person. This study was focussed on improving solubility & dissolution of poorly soluble drug Ziprasidone using different formulation approaches like solid dispersion & inclusion complexation. Different solubility enhancing techniques like physical mixing, solvent evaporation, microwave irradiation, lyophilization & spray drying were used for the along with four different polymers i.e Kollidon, Soluplus, Pluronic and HPβCD. The prepared formulations were evaluated for saturated solubility, dissolution, ATR, SEM, XRD, pharmacodynamic and pharmacokinetic in vivo study. The prepare formulations showed increment in solubility as well as dissolution. The order of solubility enhancement for the studied polymers was found to be of following order: Soluplus >HPβCD >Kollidon >Pluronic. In the pharmacodynamic study, the optimized solid dispersion showed the calming effect on mice when compared to pure Ziprasidone. The pharmacokinetic study demonstrated the increase in oral absorption of Ziprasidone in all prepared formulations and it followed the same order as that solubility & dissolution enhancement. The Soluplus-solid dispersion prepared by spray drying technique was found to be suitable in enhancing oral absorption with significant (p < 0.05) enhancement in Cmax & AUC than pure Ziprasidone. Hence, comparative study was helpful in increasing oral bioavailability Of Ziprasidone in choosing the suitable polymer with decreasing the dose and increasing patient adherence to therapy.

Published in	Journal of Drug Design and Medicinal Chemistry (Volume 3, Issue 3)
DOI	10.11648/j.jddmc.20170303.12
Page(s)	37-48
Creative Commons	This is an Open Access article, distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution and reproduction in any medium or format, provided the original work is properly cited.
Copyright	Copyright © The Author(s), 2017. Published by Science Publishing Group

Keywords

Ziprasidone, Solubility, Kollidon, Soluplus, Pluronic, HPβCD, Solid Dispersion

References

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APA Style

Poonam Mogal, Deeliprao Derle. (2017). Use of Solid Dispersions and Inclusion Complexation for Enhancing Oral Bioavailability of Ziprasidone in Treating Schizophrenia. Journal of Drug Design and Medicinal Chemistry, 3(3), 37-48. https://doi.org/10.11648/j.jddmc.20170303.12

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Poonam Mogal; Deeliprao Derle. Use of Solid Dispersions and Inclusion Complexation for Enhancing Oral Bioavailability of Ziprasidone in Treating Schizophrenia. J. Drug Des. Med. Chem. 2017, 3(3), 37-48. doi: 10.11648/j.jddmc.20170303.12

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AMA Style

Poonam Mogal, Deeliprao Derle. Use of Solid Dispersions and Inclusion Complexation for Enhancing Oral Bioavailability of Ziprasidone in Treating Schizophrenia. J Drug Des Med Chem. 2017;3(3):37-48. doi: 10.11648/j.jddmc.20170303.12

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@article{10.11648/j.jddmc.20170303.12,
  author = {Poonam Mogal and Deeliprao Derle},
  title = {Use of Solid Dispersions and Inclusion Complexation for Enhancing Oral Bioavailability of Ziprasidone in Treating Schizophrenia},
  journal = {Journal of Drug Design and Medicinal Chemistry},
  volume = {3},
  number = {3},
  pages = {37-48},
  doi = {10.11648/j.jddmc.20170303.12},
  url = {https://doi.org/10.11648/j.jddmc.20170303.12},
  eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.jddmc.20170303.12},
  abstract = {In modern times, people are suffering from many mental health disorders like schizophrenia, bipolar disorders and many psychoses. Hence, it is essential to treat these mental disorders using medications as well as with assistance from caregivers for the social well being of person. This study was focussed on improving solubility & dissolution of poorly soluble drug Ziprasidone using different formulation approaches like solid dispersion & inclusion complexation. Different solubility enhancing techniques like physical mixing, solvent evaporation, microwave irradiation, lyophilization & spray drying were used for the along with four different polymers i.e Kollidon, Soluplus, Pluronic and HPβCD. The prepared formulations were evaluated for saturated solubility, dissolution, ATR, SEM, XRD, pharmacodynamic and pharmacokinetic in vivo study. The prepare formulations showed increment in solubility as well as dissolution. The order of solubility enhancement for the studied polymers was found to be of following order: Soluplus >HPβCD >Kollidon >Pluronic. In the pharmacodynamic study, the optimized solid dispersion showed the calming effect on mice when compared to pure Ziprasidone. The pharmacokinetic study demonstrated the increase in oral absorption of Ziprasidone in all prepared formulations and it followed the same order as that solubility & dissolution enhancement. The Soluplus-solid dispersion prepared by spray drying technique was found to be suitable in enhancing oral absorption with significant (p < 0.05) enhancement in Cmax & AUC than pure Ziprasidone. Hence, comparative study was helpful in increasing oral bioavailability Of Ziprasidone in choosing the suitable polymer with decreasing the dose and increasing patient adherence to therapy.},
 year = {2017}
}

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TY  - JOUR
T1  - Use of Solid Dispersions and Inclusion Complexation for Enhancing Oral Bioavailability of Ziprasidone in Treating Schizophrenia
AU  - Poonam Mogal
AU  - Deeliprao Derle
Y1  - 2017/07/25
PY  - 2017
N1  - https://doi.org/10.11648/j.jddmc.20170303.12
DO  - 10.11648/j.jddmc.20170303.12
T2  - Journal of Drug Design and Medicinal Chemistry
JF  - Journal of Drug Design and Medicinal Chemistry
JO  - Journal of Drug Design and Medicinal Chemistry
SP  - 37
EP  - 48
PB  - Science Publishing Group
SN  - 2472-3576
UR  - https://doi.org/10.11648/j.jddmc.20170303.12
AB  - In modern times, people are suffering from many mental health disorders like schizophrenia, bipolar disorders and many psychoses. Hence, it is essential to treat these mental disorders using medications as well as with assistance from caregivers for the social well being of person. This study was focussed on improving solubility & dissolution of poorly soluble drug Ziprasidone using different formulation approaches like solid dispersion & inclusion complexation. Different solubility enhancing techniques like physical mixing, solvent evaporation, microwave irradiation, lyophilization & spray drying were used for the along with four different polymers i.e Kollidon, Soluplus, Pluronic and HPβCD. The prepared formulations were evaluated for saturated solubility, dissolution, ATR, SEM, XRD, pharmacodynamic and pharmacokinetic in vivo study. The prepare formulations showed increment in solubility as well as dissolution. The order of solubility enhancement for the studied polymers was found to be of following order: Soluplus >HPβCD >Kollidon >Pluronic. In the pharmacodynamic study, the optimized solid dispersion showed the calming effect on mice when compared to pure Ziprasidone. The pharmacokinetic study demonstrated the increase in oral absorption of Ziprasidone in all prepared formulations and it followed the same order as that solubility & dissolution enhancement. The Soluplus-solid dispersion prepared by spray drying technique was found to be suitable in enhancing oral absorption with significant (p < 0.05) enhancement in Cmax & AUC than pure Ziprasidone. Hence, comparative study was helpful in increasing oral bioavailability Of Ziprasidone in choosing the suitable polymer with decreasing the dose and increasing patient adherence to therapy.
VL  - 3
IS  - 3
ER  -

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Author Information

Poonam Mogal

Department of Pharmaceutics, M. V. P. S’ College of Pharmacy, Nashik, India
Deeliprao Derle

Department of Pharmaceutics, M. V. P. S’ College of Pharmacy, Nashik, India

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Poonam Mogal, Deeliprao Derle. (2017). Use of Solid Dispersions and Inclusion Complexation for Enhancing Oral Bioavailability of Ziprasidone in Treating Schizophrenia. Journal of Drug Design and Medicinal Chemistry, 3(3), 37-48. https://doi.org/10.11648/j.jddmc.20170303.12

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ACS Style

Poonam Mogal; Deeliprao Derle. Use of Solid Dispersions and Inclusion Complexation for Enhancing Oral Bioavailability of Ziprasidone in Treating Schizophrenia. J. Drug Des. Med. Chem. 2017, 3(3), 37-48. doi: 10.11648/j.jddmc.20170303.12

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AMA Style

Poonam Mogal, Deeliprao Derle. Use of Solid Dispersions and Inclusion Complexation for Enhancing Oral Bioavailability of Ziprasidone in Treating Schizophrenia. J Drug Des Med Chem. 2017;3(3):37-48. doi: 10.11648/j.jddmc.20170303.12

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@article{10.11648/j.jddmc.20170303.12,
  author = {Poonam Mogal and Deeliprao Derle},
  title = {Use of Solid Dispersions and Inclusion Complexation for Enhancing Oral Bioavailability of Ziprasidone in Treating Schizophrenia},
  journal = {Journal of Drug Design and Medicinal Chemistry},
  volume = {3},
  number = {3},
  pages = {37-48},
  doi = {10.11648/j.jddmc.20170303.12},
  url = {https://doi.org/10.11648/j.jddmc.20170303.12},
  eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.jddmc.20170303.12},
  abstract = {In modern times, people are suffering from many mental health disorders like schizophrenia, bipolar disorders and many psychoses. Hence, it is essential to treat these mental disorders using medications as well as with assistance from caregivers for the social well being of person. This study was focussed on improving solubility & dissolution of poorly soluble drug Ziprasidone using different formulation approaches like solid dispersion & inclusion complexation. Different solubility enhancing techniques like physical mixing, solvent evaporation, microwave irradiation, lyophilization & spray drying were used for the along with four different polymers i.e Kollidon, Soluplus, Pluronic and HPβCD. The prepared formulations were evaluated for saturated solubility, dissolution, ATR, SEM, XRD, pharmacodynamic and pharmacokinetic in vivo study. The prepare formulations showed increment in solubility as well as dissolution. The order of solubility enhancement for the studied polymers was found to be of following order: Soluplus >HPβCD >Kollidon >Pluronic. In the pharmacodynamic study, the optimized solid dispersion showed the calming effect on mice when compared to pure Ziprasidone. The pharmacokinetic study demonstrated the increase in oral absorption of Ziprasidone in all prepared formulations and it followed the same order as that solubility & dissolution enhancement. The Soluplus-solid dispersion prepared by spray drying technique was found to be suitable in enhancing oral absorption with significant (p < 0.05) enhancement in Cmax & AUC than pure Ziprasidone. Hence, comparative study was helpful in increasing oral bioavailability Of Ziprasidone in choosing the suitable polymer with decreasing the dose and increasing patient adherence to therapy.},
 year = {2017}
}

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TY  - JOUR
T1  - Use of Solid Dispersions and Inclusion Complexation for Enhancing Oral Bioavailability of Ziprasidone in Treating Schizophrenia
AU  - Poonam Mogal
AU  - Deeliprao Derle
Y1  - 2017/07/25
PY  - 2017
N1  - https://doi.org/10.11648/j.jddmc.20170303.12
DO  - 10.11648/j.jddmc.20170303.12
T2  - Journal of Drug Design and Medicinal Chemistry
JF  - Journal of Drug Design and Medicinal Chemistry
JO  - Journal of Drug Design and Medicinal Chemistry
SP  - 37
EP  - 48
PB  - Science Publishing Group
SN  - 2472-3576
UR  - https://doi.org/10.11648/j.jddmc.20170303.12
AB  - In modern times, people are suffering from many mental health disorders like schizophrenia, bipolar disorders and many psychoses. Hence, it is essential to treat these mental disorders using medications as well as with assistance from caregivers for the social well being of person. This study was focussed on improving solubility & dissolution of poorly soluble drug Ziprasidone using different formulation approaches like solid dispersion & inclusion complexation. Different solubility enhancing techniques like physical mixing, solvent evaporation, microwave irradiation, lyophilization & spray drying were used for the along with four different polymers i.e Kollidon, Soluplus, Pluronic and HPβCD. The prepared formulations were evaluated for saturated solubility, dissolution, ATR, SEM, XRD, pharmacodynamic and pharmacokinetic in vivo study. The prepare formulations showed increment in solubility as well as dissolution. The order of solubility enhancement for the studied polymers was found to be of following order: Soluplus >HPβCD >Kollidon >Pluronic. In the pharmacodynamic study, the optimized solid dispersion showed the calming effect on mice when compared to pure Ziprasidone. The pharmacokinetic study demonstrated the increase in oral absorption of Ziprasidone in all prepared formulations and it followed the same order as that solubility & dissolution enhancement. The Soluplus-solid dispersion prepared by spray drying technique was found to be suitable in enhancing oral absorption with significant (p < 0.05) enhancement in Cmax & AUC than pure Ziprasidone. Hence, comparative study was helpful in increasing oral bioavailability Of Ziprasidone in choosing the suitable polymer with decreasing the dose and increasing patient adherence to therapy.
VL  - 3
IS  - 3
ER  -

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