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Susanto, Sharon
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Arts Humanities Biochemistry, Genetics & Molecular Biology Chemistry Education Environmental Science Health Professions Immunology & microbiology Languange, Linguistic, Communication & Media Mathematics Medicine & Pharmacology Public Health Social Sciences Other

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Journal : Jurnal Ilmiah Medicamento

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Kombinasi Teknik Pembentukan Kokristal dan Ball milling untuk Peningkatan Disolusi Etoricoxib Susanto, Sharon; Wikarsa, Saleh; Nugraha, Yuda Prasetya
Jurnal Ilmiah Medicamento Vol 10 No 1 (2024): Jurnal Ilmiah Medicamento
Publisher : Fakultas Farmasi Universitas Mahasaraswati Denpasar

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.36733/medicamento.v10i1.7561

Abstract

Etoricoxib (ETX) is a selective COX-2 anti-inflammatory drug classified in BCS class II. This study aims to enhance the dissolution rate of etoricoxib through a combination of co-crystal formation and ball milling conducted in-situ and ex-situ. Optimization was done by varying milling times and types of stabilizers, including Tween 80 (ETX-OXA-BM-T), Poloxamer 188 (ETX-OXA-BM-P), and a combination of Tween 80-sodium lauryl sulfate (SLS) (ETX-OXA-BM-T-S). In-situ experiments yielded a very low yield (<10%) and failed to produce co-crystals, thus deeming them unsuitable for continuation. Meanwhile, the ex-situ process showed more potential, leading to further evaluation using Differential Scanning Calorimetry (DSC), Powder X-Ray Diffractometry (PXRD), and Scanning Electron Microscope (SEM). DSC analysis showed endothermic peaks at 130°C for ETX and around 179 - 180°C for ETX-OXA and its derivatives. PXRD diffractograms for ETX-OXA and its derivatives exhibited similar peaks, differing from ETX. SEM analysis indicated that ETX-OXA-BM-T with 60 minutes of milling resulted in nanometer-sized particles, while the use of Poloxamer 188 and the combination of Tween 80-SLS produced particle sizes > 1 µm. ETX-OXA-BM-T showed the highest increase in solubility in all media. The dissolution results of ETX-OXA-BM-T showed improvement in phosphate buffer pH 6.8, while no significant differences were observed in pH 1.2 and 4.5 buffers. This study demonstrates that the combination of co-crystal formation and ex-situ ball milling is a potential approach to enhancing the dissolution rate of etoricoxib.
Co-Authors Alwi, Felisca Emmalyn Chaineyla, Florencia Christian, Yulius Evan Gunawan, Untung Ishariyanto, Riski Laurensia Nababan, Agnes Aditia Nugraha, Yuda Prasetya Putri, Fadhilla Sivana Saleh Wikarsa, Saleh Septiana, Rita Susanto, Michael Darell