Formulation of dispersed gliclazide powder in polyethylene glycol–polyvinyl caprolactam– polyvinyl acetate grafted copolymer carrier for capsulation and improved dissolution

Background: Oral bioavailability of gliclazide, a hypoglycemic drug, is hindered by its low aqueous solubility. Improvement of solubility will enhance dissolution rate and in turn the bioavailability. This research aimed to formulate the solid dispersed gliclazide using a novel polyethylene glycol–p...

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Main Authors:	Ahmed Mahdi Dukhan, Ather, Mohamad Yusoff, Nursazreen Amalina, Kyaw Oo, May, Sengupta, Pinaki, Doolaanea, Abd Almonem, Aljapairai, Khater Ahmed Saeed, Chatterjee, Bappaditya
Format:	Article
Language:	English
Published:	Association of Pharmaceutical Teachers of India 2018
Subjects:	RS192 Materia Medica-Pharmaceutical Technology
Online Access:	http://irep.iium.edu.my/67672/ http://irep.iium.edu.my/67672/ http://irep.iium.edu.my/67672/ http://irep.iium.edu.my/67672/1/IJPER_4_18-QC-RD.pdf

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recordtype	eprints
spelling	iium-676722019-07-15T02:04:06Z http://irep.iium.edu.my/67672/ Formulation of dispersed gliclazide powder in polyethylene glycol–polyvinyl caprolactam– polyvinyl acetate grafted copolymer carrier for capsulation and improved dissolution Ahmed Mahdi Dukhan, Ather Mohamad Yusoff, Nursazreen Amalina Kyaw Oo, May Sengupta, Pinaki Doolaanea, Abd Almonem Aljapairai, Khater Ahmed Saeed Chatterjee, Bappaditya RS192 Materia Medica-Pharmaceutical Technology Background: Oral bioavailability of gliclazide, a hypoglycemic drug, is hindered by its low aqueous solubility. Improvement of solubility will enhance dissolution rate and in turn the bioavailability. This research aimed to formulate the solid dispersed gliclazide using a novel polyethylene glycol–polyvinyl caprolactam–polyvinyl acetate grafted copolymer (Soluplus®) as carrier to enhance in-vitro dissolution and to study drug-carrier physical interaction. Method: Final solid dispersion (SDGLC) containing drug:carrier (1:8 w/w) was prepared by solvent evaporation after drug-polymer miscibility study. The SDGLC powder was characterized by differential scanning calorimetry (DSC), attenuated total reflectance infra-red spectroscopy (ATR-IR), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). SDGLC powder was filled in gelatin capsule after flowability and moisture analysis followed by assay, disintegration and in-vitro dissolution study. Results: Miscibility study showed negative values of free energy transfer indicating spontaneous solubilization of drug with increase in carrier concentration. Absence of sharp melting peak in SDGLC was observed by DSC. Reduced peak intensity at specific 2θ values in PXRD indicates loss of crystallinity in solid dispersion. Interaction to form H-bond between gliclazide and Soluplus® was evidenced by ATR-IR. SDGLC filled capsule resulted in 20% improved dissolution (approximately 20% higher) in 0.1(N) HCl and phosphate buffer pH 7.4 compared to physical mixture (gliclazide-Soluplus®) containing capsule. Conclusion: Soluplus® effectively enhanced gliclazide solubility in solid dispersed state and SDGLC powder filled capsules could provide pH independent and improved in-vitro dissolution for gliclazide. Association of Pharmaceutical Teachers of India 2018-11 Article PeerReviewed application/pdf en http://irep.iium.edu.my/67672/1/IJPER_4_18-QC-RD.pdf Ahmed Mahdi Dukhan, Ather and Mohamad Yusoff, Nursazreen Amalina and Kyaw Oo, May and Sengupta, Pinaki and Doolaanea, Abd Almonem and Aljapairai, Khater Ahmed Saeed and Chatterjee, Bappaditya (2018) Formulation of dispersed gliclazide powder in polyethylene glycol–polyvinyl caprolactam– polyvinyl acetate grafted copolymer carrier for capsulation and improved dissolution. Indian Journal of Pharmaceutical Education and Research, 52 (4). S210-219. ISSN 0019-5464 http://ijper.org/sites/default/files/IndJPhaEdRes_52_4-s210_0.pdf 0.5530/ijper.52.4s.100
repository_type	Digital Repository
institution_category	Local University
institution	International Islamic University Malaysia
building	IIUM Repository
collection	Online Access
language	English
topic	RS192 Materia Medica-Pharmaceutical Technology
spellingShingle	RS192 Materia Medica-Pharmaceutical Technology Ahmed Mahdi Dukhan, Ather Mohamad Yusoff, Nursazreen Amalina Kyaw Oo, May Sengupta, Pinaki Doolaanea, Abd Almonem Aljapairai, Khater Ahmed Saeed Chatterjee, Bappaditya Formulation of dispersed gliclazide powder in polyethylene glycol–polyvinyl caprolactam– polyvinyl acetate grafted copolymer carrier for capsulation and improved dissolution
description	Background: Oral bioavailability of gliclazide, a hypoglycemic drug, is hindered by its low aqueous solubility. Improvement of solubility will enhance dissolution rate and in turn the bioavailability. This research aimed to formulate the solid dispersed gliclazide using a novel polyethylene glycol–polyvinyl caprolactam–polyvinyl acetate grafted copolymer (Soluplus®) as carrier to enhance in-vitro dissolution and to study drug-carrier physical interaction. Method: Final solid dispersion (SDGLC) containing drug:carrier (1:8 w/w) was prepared by solvent evaporation after drug-polymer miscibility study. The SDGLC powder was characterized by differential scanning calorimetry (DSC), attenuated total reflectance infra-red spectroscopy (ATR-IR), powder X-ray diffraction (PXRD), and scanning electron microscopy (SEM). SDGLC powder was filled in gelatin capsule after flowability and moisture analysis followed by assay, disintegration and in-vitro dissolution study. Results: Miscibility study showed negative values of free energy transfer indicating spontaneous solubilization of drug with increase in carrier concentration. Absence of sharp melting peak in SDGLC was observed by DSC. Reduced peak intensity at specific 2θ values in PXRD indicates loss of crystallinity in solid dispersion. Interaction to form H-bond between gliclazide and Soluplus® was evidenced by ATR-IR. SDGLC filled capsule resulted in 20% improved dissolution (approximately 20% higher) in 0.1(N) HCl and phosphate buffer pH 7.4 compared to physical mixture (gliclazide-Soluplus®) containing capsule. Conclusion: Soluplus® effectively enhanced gliclazide solubility in solid dispersed state and SDGLC powder filled capsules could provide pH independent and improved in-vitro dissolution for gliclazide.
format	Article
author	Ahmed Mahdi Dukhan, Ather Mohamad Yusoff, Nursazreen Amalina Kyaw Oo, May Sengupta, Pinaki Doolaanea, Abd Almonem Aljapairai, Khater Ahmed Saeed Chatterjee, Bappaditya
author_facet	Ahmed Mahdi Dukhan, Ather Mohamad Yusoff, Nursazreen Amalina Kyaw Oo, May Sengupta, Pinaki Doolaanea, Abd Almonem Aljapairai, Khater Ahmed Saeed Chatterjee, Bappaditya
author_sort	Ahmed Mahdi Dukhan, Ather
title	Formulation of dispersed gliclazide powder in polyethylene glycol–polyvinyl caprolactam– polyvinyl acetate grafted copolymer carrier for capsulation and improved dissolution
title_short	Formulation of dispersed gliclazide powder in polyethylene glycol–polyvinyl caprolactam– polyvinyl acetate grafted copolymer carrier for capsulation and improved dissolution
title_full	Formulation of dispersed gliclazide powder in polyethylene glycol–polyvinyl caprolactam– polyvinyl acetate grafted copolymer carrier for capsulation and improved dissolution
title_fullStr	Formulation of dispersed gliclazide powder in polyethylene glycol–polyvinyl caprolactam– polyvinyl acetate grafted copolymer carrier for capsulation and improved dissolution
title_full_unstemmed	Formulation of dispersed gliclazide powder in polyethylene glycol–polyvinyl caprolactam– polyvinyl acetate grafted copolymer carrier for capsulation and improved dissolution
title_sort	formulation of dispersed gliclazide powder in polyethylene glycol–polyvinyl caprolactam– polyvinyl acetate grafted copolymer carrier for capsulation and improved dissolution
publisher	Association of Pharmaceutical Teachers of India
publishDate	2018
url	http://irep.iium.edu.my/67672/ http://irep.iium.edu.my/67672/ http://irep.iium.edu.my/67672/ http://irep.iium.edu.my/67672/1/IJPER_4_18-QC-RD.pdf
first_indexed	2023-09-18T21:36:03Z
last_indexed	2023-09-18T21:36:03Z
_version_	1777412827839987712

Formulation of dispersed gliclazide powder in polyethylene glycol–polyvinyl caprolactam– polyvinyl acetate grafted copolymer carrier for capsulation and improved dissolution

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