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Kajian Teknik Modifikasi Metformin HCl Oral dalam Upaya Peningkatan Permeabilitas Yerisy, Linggih Elra; Fitrianti Darusman; Hanifa Rahma
Jurnal Riset Farmasi Volume 5, No. 2, Desember 2025, Jurnal Riset Farmasi (JRF)
Publisher : UPT Publikasi Ilmiah Unisba

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.29313/jrf.v5i2.8343

Abstract

Abstract. Metformin HCl is a biguanide-class antidiabetic drug widely used as a first-line therapy for patients with type 2 diabetes mellitus. Although it has high solubility, metformin is classified as a BCS Class III drug due to its low permeability, which limits its oral bioavailability. This study aims to review various formulation modification techniques developed to enhance the permeability of metformin HCl. The review was conducted through literature analysis of scientific articles obtained from major databases such as Sciencedirect, MDPI, PubMed, and Scopus. Based on the findings, strategies to improve metformin’s permeability include the use of ionic salts, lipid matrices, permeation enhancers, nanoparticles, microparticles and solid dispersions. Each technique demonstrates distinct mechanisms and effectiveness in overcoming permeability limitations. Therefore, selecting the appropriate formulation modification approach has the potential to significantly enhance the oral therapeutic efficacy of metformin. Abstrak. Metformin HCl merupakan obat antidiabetes golongan biguanida yang secara luas digunakan sebagai terapi lini pertama pada pasien diabetes melitus tipe 2. Meskipun memiliki kelarutan tinggi, metformin termasuk dalam  BCS kelas III karena permeabilitasnya yang rendah, yang membatasi bioavailabilitas oralnya. Penelitian ini bertujuan untuk mengkaji berbagai teknik modifikasi formulasi yang telah dikembangkan guna meningkatkan permeabilitas metformin HCl. Kajian dilakukan dengan metode telaah pustaka terhadap artikel-artikel ilmiah dari berbagai database terkemuka seperti Sciencedirect, MDPI, PubMed, dan Scopus. Berdasarkan hasil penelusuran, strategi peningkatan permeabilitas metformin mencakup penggunaan garam ionik, matriks lipid, permeation enhancer, nanopartikel, mikropartikel dan solid dispersion. Masing-masing metode menunjukkan mekanisme dan efektivitas yang berbeda dalam mengatasi keterbatasan permeabilitas metformin. Dengan demikian, pemilihan metode modifikasi formulasi yang tepat berpotensi meningkatkan efikasi terapi oral metformin secara signifikan.
In Silico Activity Identification of Cyclo Peptide Alkaloids from Zizyphus Spina-Christi Species Against Sars-Cov-2 Main Protease Fakih, Taufik Muhammad; Ramadhan, Dwi Syah Fitra; Darusman, Fitrianti
Jurnal Biodjati Vol 6 No 1 (2021): May
Publisher : UIN Sunan Gunung Djati Bandung

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.15575/biodjati.v6i1.10603

Abstract

The COVID-19 has spread worldwide and become an international pandemic. The promising target for drug discovery of COVID-19 was SARS-CoV-2 Main Protease (Mpro), that has been successfully crystallized along with its inhibitor. The discovery of peptide-based inhibitors may present better options than small molecules for inhibitor SARS-CoV-2 Mpro. Natural compounds have such a wide potential and still few explored, Zizyphus spina-christi is one of the medicinal plants that have many pharmacological activities and contains a peptide compound from alkaloids class, i.e. cyclopeptide alkaloids, that is interesting to explore as SARS-CoV-2 Mpro inhibitor. The compound structure was drawn and optimized using density functional theory 3-21G method. The protein chosen was the high resolution of SARS-CoV-2 MPro receptor (1.45 Å) with PDB ID: 6WNP, in complex with boceprevir. Molecular docking simulation was performed using Autodock4 with 100 numbers of GA run, the validation methods assessed by RMSD calculation. Furthermore, the prediction of pharmacological activity spectra was carried out using the PASS Prediction server. The results showed RMSD value was 1.98 Å, this docking method was valid. The binding energy of all compounds showed better results than the native ligand (Boceprevir). The in silico PASS prediction results indicated that all compounds showed antiviral activity. Some compounds showed protease inhibitory activity, i.e Ambiphibine-H, Franganine, and Mauritine-A, and the highest Pa (Predicted activity) value showed by Mauritine-A compounds. It can be concluded that the cyclopeptide compounds of Zizyphus spina-christi were indicated to have a potential as COVID-19 therapy targeting SARS-CoV-2 Mpro.
Co-Authors Amila Amila Amila Amila, Amila Anan Suparman Anan Suparman Annisa Meilani Aprian Dwiatama Aprian Dwiatama Astrid Feinisa Khairani Aulia Fikri Hidayat Azyyati Adzhani Budi Prabowo Soewondo Cepy Hadiansyah Cepy Hadiansyah, Cepy Dara Azalea Wahdah Debby Prihasti Ayustine Dewi, Mentari Luthfika Dinnanda Yussepina Wulansari Dinnanda Yussepina Wulansari Dwi Oktariani Dwi Syah Fitra Ramadhan Dwiatama, Aprian Endah Rahayu Endah Rahayu, Endah Fia Siti Nopalia Firda Aulia Jannati Frida Anggita Amalia Gina Fuji Nurfarida Gita Cahya Eka Darma Hamdi Azwir, Hery Hanifa Rahma Hanifa Rahma Hilda Aprilia, Hilda Hirawati Oemar Inayah Fitri Wulandari Inayah Fitri Wulandari Indra Topik Indra Topik, Indra Jihan Sahira Khodimul Haramain Khuza’i, Rodliyah Larasati Sofiyandini Legina Ayu Kusumah, Dea Marillia, Viola Mega Suryani Putri Mentari Lutfika Dewi Mentari Luthfika Dewi Millati Hanifa Suparno Muhamad Rizqy Maulana Muhammad Sultan Ramadhan Mutiara Haifania Nadya Azzahra Nawang Wulan Rachmatillah Prastowo Putri Niken Fitria Yuliar Nurrayyan Nurrayyan Nurrayyan, Nurrayyan Nyayu Ista Yulita Putri, Nawang Wulan Rachmatillah Prastowo Rachmat Mauludin Rachmat Mauludin Ratih Aryani Riza Ramadhan Saadiya Noerman Sani Ega Priani Shannie Megaliane Silvi Sandi Putri Soewandhi, Sundani N Sundani N Soewandhi Syafanisa Alifia Rahma Syifa Nur Oktaviani Syifa Siti Fatimah Azzahro Syilfiana Anwar Taufik Muhammad Fakih Teti Sofia Yanti Tia Aulia Silvianti Triandri Permana Uci Ary Lantika Uci Ary Lantika Ulfa Siti M Viola Marillia Widad Aghnia Shalannandia Widad Aghnia Shalannandia Yan Orgianus Yerisy, Linggih Elra Yukeu Fazriah Yukeu Fazriah, Yukeu Zalfa Ainun Rozak