IIUM Repository (IREP)

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

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

[img]
Preview
PDF - Published Version
Download (1MB) | Preview

Abstract

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.

Item Type: Article (Journal)
Additional Information: 6923/67672
Uncontrolled Keywords: Key words: Solid dispersion, Gliclazide, Soluplus®, Improved dissolution, Amorphous.
Subjects: R Medicine > RS Pharmacy and materia medica > RS192 Materia Medica-Pharmaceutical Technology
Kulliyyahs/Centres/Divisions/Institutes: Kulliyyah of Pharmacy
Kulliyyah of Pharmacy > Department of Pharmaceutical Technology
Depositing User: Dr Bappaditya Chatterjee
Date Deposited: 07 Dec 2018 15:28
Last Modified: 07 Dec 2018 15:28
URI: http://irep.iium.edu.my/id/eprint/67672

Actions (login required)

View Item View Item

Downloads

Downloads per month over past year