Accepted Manuscript Formulation of risperidone in floating microparticles to alleviate its extrapyramidal side effects Hussein O. Ammar, Mahmoud M. Ghorab, Azza A. Mahmoud, Shereen H. Noshi PII:
S2314-7245(16)30034-6
DOI:
10.1016/j.fjps.2016.08.001
Reference:
FJPS 16
To appear in:
Future Journal of Pharmaceutical sciences
Received Date: 31 March 2016 Revised Date:
27 July 2016
Accepted Date: 10 August 2016
Please cite this article as: Ammar HO, Ghorab MM, Mahmoud AA, Noshi SH, Formulation of risperidone in floating microparticles to alleviate its extrapyramidal side effects, Future Journal of Pharmaceutical sciences (2016), doi: 10.1016/j.fjps.2016.08.001. This is a PDF file of an unedited manuscript that has been accepted for publication. As a service to our customers we are providing this early version of the manuscript. The manuscript will undergo copyediting, typesetting, and review of the resulting proof before it is published in its final form. Please note that during the production process errors may be discovered which could affect the content, and all legal disclaimers that apply to the journal pertain.
ACCEPTED MANUSCRIPT
Title: Formulation of risperidone in floating microparticles to alleviate its
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extrapyramidal side effects
Hussein O. Ammar1,2, Mahmoud M. Ghorab3, Azza A. Mahmoud1,2, and Shereen H. Noshi4
Department of Pharmaceutical Technology, National Research Center,
Dokki, Cairo, Egypt,
2
SC
1
Department of Pharmaceutical Technology,
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Faculty of Pharmaceutical Sciences and Pharmaceutical Industries, Future University in Egypt, Cairo, Egypt, 3Department of Pharmaceutics, Faculty of Pharmacy, Cairo University, Cairo, Egypt, 4Department of
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Pharmaceutics, Faculty of Pharmacy, MSA University, Cairo, Egypt.
Corresponding author:
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Shereen Hamdi Nosi E-mail:
[email protected] Tel.: +201002520902 / +201223862466
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Keywords: Gastroretentive, Eudragit, Compritol 888 ATO and cyclodextrin.
ACCEPTED MANUSCRIPT
Formulation of risperidone in floating microparticles to alleviate its extrapyramidal side effects
Hussein O. Ammar1,2, Mahmoud M. Ghorab3, Azza A. Mahmoud1,2, and
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Shereen H. Noshi4
SC
Abstract
Risperidone is effective in the treatment of positive as well as negative
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symptoms of schizophrenia. But, there is a strong correlation between plasma levels of risperidone and its adverse effects. This study aimed to develop risperidone in floating microparticles to overcome its extrapyramidal side effects. Floating microparticles were prepared using Eudragit S100, hydroxypropyl methyl cellulose (HPMC), Gelucires
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(Gelucire 43/01 pellets, Gelucire 44/14 and Gelucire 50/13), Geleol mono & diglyceride NF, glyceryl monostearate, Compritol 888 ATO, Methylbetacyclodextrin
(MβCD)
and
hydroxypropyl-beta-cyclodextrin
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(HPβCD), by emulsion solvent diffusion technique. In-vitro experiments were conducted to optimize formulation parameters regarding floating
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ability, yield value, drug loading and in-vitro release properties. The best formula was investigated for its in-vivo floating ability and for its pharmacokinetics as well as its extrapyramidal side effects in human volunteers. The optimized floating microparticles showed promising invitro experiment performance with floating ability up to 95.93% for 12 hr. Also, this floating ability was confirmed using in-vivo x-ray studies. Pharmacokinetics studies revealed significant (p
