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Kajian Pembentukan Dispersi Padat Atenolol Menggunakan Metode Freeze Drying Maulita, Arina Swastika; Winantari, Agnes Nuniek; Rani, Karina Citra; Pradana, Aditya Trias; Kesuma, Dini
MPI (Media Pharmaceutica Indonesiana) Vol. 7 No. 1 (2025): JUNE
Publisher : Fakultas Farmasi, Universitas Surabaya

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.24123/mpi.v7i1.7334

Abstract

Atenolol merupakan obat golongan β1-adrenoblocker selektif yang digunakan untuk mengobati kondisi kardiovaskular seperti hipertensi dan angina pektoris. Namun, atenolol memiliki kelarutan dan permeabilitas yang rendah hal ini dapat membatasi bioavailabilitas oralnya. Salah satu metode yang efektif untuk meningkatkan kelarutan dan laju disolusi obat dengan kelarutan rendah adalah melalui pembentukan dispersi padat. Dispersi padat melibatkan pembawa obat dalam matriks yang bersifat inert dalam keadaan padat, yang dapat meningkatkan kelarutan dan stabilitas obat. Metode freeze drying (liofilisasi) digunakan dalam pembuatan dispersi padat atenolol untuk menghindari dekomposisi termal dan menghasilkan dispersi molekuler yang homogen. Karakterisasi dispersi padat yang dihasilkan meliputi analisis morfologi, identifikasi gugus fungsi, sifat kristalinitas, analisis termal, ukuran partikel, distribusi ukuran partikel, dan potensi zeta. Pada berbagai penelitian sebelumnya menunjukkan bahwa dispersi padat dapat meningkatkan kelarutan dan laju disolusi atenolol secara signifikan. Atenolol is a selective β1-adrenoblocker drug used to treat cardiovascular conditions such as hypertension and angina pectoris. However, atenolol has low solubility and permeability, which can limit its oral bioavailability. One effective method to increase the solubility and dissolution rate of drugs with low solubility is through the formation of solid dispersions. Solid dispersions involve drug carriers in an inert matrix in the solid state, which can increase the solubility and stability of the drug. The freeze drying (lyophilization) method is used in the preparation of atenolol solid dispersions to avoid thermal decomposition and produce homogeneous molecular dispersions. Characterization of the resulting solid dispersions includes morphological analysis, identification of functional groups, crystallinity properties, thermal analysis, particle size, particle size distribution, and zeta potential. Various previous studies have shown that solid dispersions can significantly increase the solubility and dissolution rate of atenolol. Submitted: 05-02-2025, Revised: 10-04-2025, Accepted: 16-05-2025, Published regularly: June 2025
KOKRISTALISASI HESPERIDIN – NIKOTINAMIDA DENGAN SLURRY METHOD Winantari, Agnes Nuniek; Tjioe, Felicia Reynaldo; Rizky , Astridani
JURNAL FARMASI GALENIKA Vol 8 No 1 (2021): Jurnal Farmasi Galenika Vol 8 No 1
Publisher : Universitas Bhakti Kencana

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.70410/jfg.v8i1.184

Abstract

Penelitian ini dilakukan untuk membentuk kokristal hesperidin-nikotinamida (1:1) menggunakan metode slurry. Metode slurry merupakan metode yang sederhana dengan menambahkan aquadem ke campuran hesperidin dan nikotinamida sampai membentuk massa bubur/lumpuran atau suspensi pada kecepatan 200 rpm. Kokristal dikarakterisasi menggunakan instrument PXRD, DSC, FTIR dan SEM. Difraktogram menunjukkan empat puncak baru pada sudut 2? yaitu 21,26?; 22,21?; 23,28?; 25,35?. Termogram memperlihatkan puncak endotermik pada 240,56?C. Spektrum FTIR menunjukkan adanya pergeseran dan hilangnya puncak pada kokristal. Fotomikrograf SEM memperlihatkan adanya perubahan bentuk permukaan menjadi lebih porous. Kesimpulan penelitian ini adalah kokristal hesperidin-nikotinamida (1;1) dapat terbentuk
Enhancing In Vitro Dissolution of Ferulic Acid Through Co-Crystal Formation Using Malonic Acid and Nicotinamide Co-formers Setyawan, Dwi; Soraya, Yasmin; Ekowati, Juni; Winantari, Agnes Nuniek; Rani, Karina Citra; Kanzaffa, Firly Afnauriza Tedja; Pujiono, Ferry Eko
Science and Technology Indonesia Vol. 10 No. 4 (2025): October
Publisher : Research Center of Inorganic Materials and Coordination Complexes, FMIPA Universitas Sriwijaya

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.26554/sti.2025.10.4.1255-1269

Abstract

Ferulic acid is categorized as a Biopharmaceutical Classification System (BCS) class II drug, which exhibits low solubility in water (0.91 mg/mL). The formation of a co-crystal using malonic acid and nicotinamide as co-formers by the microwave irradiation method is an approach to enhance its solubility and dissolution. This study aims to evaluate the effect of co-crystal formation using these two co-formers at a 1:1 molar ratio on the solubility and dissolution of ferulic acid. The result emphasizes the formation of new peaks and peak shifting compared to the pure materials characterized from the Fourier Transform Infrared (FT-IR) spectrum. Moreover, the Differential Scanning Calorimetry (DSC) thermogram exhibits the differences in the co-crystal melting point compared to the pure drug and co-former, indicating the alteration of molecular structure on the crystal lattice of ferulic acid caused by the strong interaction between supramolecular homomer and heteromeric synthon. The formation of a new crystalline phase is also observed from the X-ray Diffraction (XRD) diffractogram, suggesting the formation of a different phase from its co-crystal component. The morphology characterization using Scanning Electron Microscope (SEM) revealed that the ferulic acid crystal habit changes into different forms, which is acclaimed as a co-crystal formation. The results of this study also disclosed that the co-crystal formation of ferulic acid significantly enhances ferulic acid solubility and dissolution characteristics compared to the pure drug and physical mixture (p < 0.05). The enhancement of solubility is 11.85% and 10.39% for ferulic acid–malonic acid and ferulic acid–nicotinamide co-crystal, respectively. Moreover, the dissolution rate of ferulic acid increases 3.50-fold and 3.61-fold from the formation of those co-crystals. Therefore, the formation of ferulic acid–malonic acid as well as ferulic acid–nicotinamide co-crystals in a 1:1 molar ratio by the microwave irradiation method is effective in improving ferulic acid solubility and dissolution.