EXPLOITING THE DESIGN OF EXPERIMENTS FOR PREPARING EXTENDED-RELEASE DOSAGE FORM OF GLICLAZIDE USING THE HOT-MELT EXTRUSION TECHNIQUE

IBRAHIM HASHIM; ALIA KH. ALSUWAIS; ALAA ABU ALHAIJA; AHMAD ALJABERI

doi:10.22159/ijap.2025v17i1.52367

Authors

IBRAHIM HASHIM Department of Pharmaceutical Sciences and Pharmaceutics, Faculty of Pharmacy, Applied Science Private University. Amman, Jordan https://orcid.org/0009-0008-7149-4411
ALIA KH. ALSUWAIS Department of Pharmaceutical Sciences and Pharmaceutics, Faculty of Pharmacy, Applied Science Private University. Amman, Jordan https://orcid.org/0009-0006-1190-0049
ALAA ABU ALHAIJA Department of Pharmaceutical Sciences and Pharmaceutics, Faculty of Pharmacy, Applied Science Private University. Amman, Jordan. Registration and R and D Department, Ram Pharmaceutical industries, Sahab Industrial city, Amman, Jordan
AHMAD ALJABERI Department of Pharmaceutical Sciences and Pharmaceutics, Faculty of Pharmacy, Applied Science Private University. Amman, Jordan https://orcid.org/0000-0001-7657-7357

DOI:

https://doi.org/10.22159/ijap.2025v17i1.52367

Keywords:

Gliclazide, Diamicron, Hot melt extrusion, Hydrophilic matrices, Polyethylene oxide, Design of experiments, Response surface methodology

Abstract

Objective: Polyethylene Oxide (PEO) is an amphiphilic polymer available in various grades, allowing manipulation of drug release rates. This work hypothesized the attempt to combine Hot-Melt Extrusion (HME) and Design of Experiments (DoE) with mixtures of various PEO grades to efficiently produce a dosage form with tailored drug release.

Methods: MODDE software recommended sixteen runs. A D-optimal mixture design evaluated the effects of gliclazide, PEO 303, and PEO 205 on the release profile of extrudates containing, as well, fixed amounts of Polyethylene Glycol (PEG) 8000 and Colloidal Silicon Dioxide (CSD). The formulations were extruded at a screw speed of 20 rpm using a vertical lab-scale single screw with four heating zones set at 85, 90, 90, and 95°C. The most discriminative dissolution method was used to generate release profiles of extrudate containing 30 mg of the drug. Factors affecting the drug release rate at 1, 3, 4, and 6 hours were identified and modeled.

Results: The goodness of fit (R²) and prediction (Q²) for release responses were 0.969 and 0.830 at 1 hr, 0.983 and 0.760 at 3 hrs, 0.987 and 0.687 at 4 hrs, and 0.947 and 0.786 at 6 hrs, respectively. The optimal design space for PEO 303 as a release-retarding polymer and PEO 205 as a release modifier at each gliclazide level (10–30%) was successfully constructed by Response Surface Modeling (RSM).

Conclusion: This work produced an extended-release profile of gliclazide that mimics the innovator by leveraging HME and DoE.

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