Improving drug solubility is necessary for formulations of poorly water-soluble drugs, especially for oral administration. Amorphous solid dispersions (ASDs) are widely used in the pharmaceutical industry to improve the physical stability and solubility of drugs. Therefore, this study aims to characterize interaction between a drug and polymer in ASD, as well as evaluate the impact on the physical stability and dissolution of alpha-mangostin (AM). AM was used as a model of a poorly water-soluble drug, while polyvinylpyrrolidone (PVP) and eudragit were used as polymers. The amorphization of AM-eudragit and AM-PVP was confirmed as having a halo pattern with powder X-ray diffraction measurements and the absence of an AM melting peak in the differential scanning calorimetry (DSC) curve. The solubility of amorphous AM increased in the presence of either eudragit or PVP due to amorphization and interactions of AM-polymer. Furthermore, FT-IR spectroscopy and in silico studies revealed hydrogen bond interactions between the carbonyl group of AM and the proton of eudragit as well as PVP. AM-eudragit with a ratio of 1:1 recrystallized after 7 days of storage at 25 °C and 90% RH, while the AM-PVP 1:4 and 1:10 samples retained the X-ray halo patterns, even under humid conditions. In a dissolution test, the presence of polymer in ASD significantly improved the dissolution profile due to the intermolecular interaction of AM-polymer. AM-eudragit 1:4 maintained AM supersaturation for a longer time compared to the 1:1 sample. However, a high supersaturation was not achieved in AM-PVP 1:10 due to the formation of large agglomerations, leading to a slow dissolution rate. Based on the results, interaction of AM-polymer in ASD can significantly improve the pharmaceutical properties of AM including the physical stability and dissolution.
Ketombe merupakan salah satu penyakit kulit akibat infeksi jamur yang banyak diderita terutama di Indonesia yang merupakan negara tropis. Prevalensi ketombe di dunia mencapai 50% pada usia pubertas dari seluruh populasi penduduk dunia. Pityrosporum ovale diduga merupakan penyebab utama dari penyakit ketombe. Saat ini masyarakat banyak menggunakan tanaman herbal untuk pengatasi ketombe. Tinjaun pustaka ini dibuat dengan tujuan agar dapat mengetahui tanaman herbal mana saja yang memiliki daya antipungal yang berpengaruh pada pertumbuhan jamur Pityroporum ovale. Metode penelitian ini dilakukan dengan Systematic Literature Review, situs yang digunakan dalam penelusuran literatur yaitu Google Scholar dan NCBI. Kata kunci yang digunakan adalah “tanaman terhadap jamur Pityrosporum Ovale”, “tanaman untuk ketombe”, “Herbs for dandruff”. Literatur yang digunakan pada tinjauan pustaka ini yaitu 15 jurnal. Hasil didapat tanaman yang berpengaruh terhadap pertumbuhan jamur pytirosporum ovale penyebab ketombe, dengan kategori zona hambat sangat kuat, kuat, sedang dan lemah. Tanaman dengan katedori tersebut secara berturut-turut daun alamanda (Allamanda cathartica L.) 301,28 mm; daun karuk (Piper sarmentosum Roxb) 19,4 mm. kangkung air (Ipomoea aquatica) 10,0 mm dan daun belingbing wuluh (Averrhoa bilimbi L.) 3,07 mm.
Diabetes mellitus tipe 2 disebabkan oleh ekspresi PTP1B yang tinggi dan mempengaruhi aktivitas PTKs, yang menyebabkan insulin gagal berikatan dengan reseptor insulin dan menginduksi resistensi insulin. Senyawa xanton dan benzofenon merupakan senyawa yang telah diketahui memiliki aktivitas farmakologi sebagai antidiabetes. Salah satu tanaman dengan kandungan senyawa tersebut adalah Garcinia cowa. Penelitian ini dilakukan dengan tujuan untuk mengetahui afinitas dan mekanisme inhibisi PTP1B oleh senyawa turunan xanton, benzofeno, dan triterpenoid dalam Garcinia cowa antara lain garcinia cowone K, guttiferone I, 1,7-dihydroxyxanthone, 1-hydroxyl-7-methoxyxanthone, mangostinone, ?-mangostin, cowanol, gacibiphenyl C, friedelin, ?-friedelinol, dan oleanane-12-ol secara in silico dengan molecular docking serta melakukan studi pre-ADMET terhadap senyawa tersebut. Molecular docking dilakukan melalui beberapa tahap diantaranya preparasi dan optimasi struktur 3D senyawa uji, preparasi struktur 3D reseptor PTP1B, validasi metode, dan docking senyawa uji dengan PTP1B. Hasil yang diperoleh dari docking senyawa uji dengan reseptor PTP1B berupa energi ikatan, konstanta inhibisi (KI), dan ikatan hidrogen. Semakin rendah nilai energi ikatan menunjukkan ikatan antara protein dan ligan yang dihasilkan semakin stabil. Hasil penelitian menunjukkan energi ikatan dan KI PTP1B dengan native ligand berturut-turut sebesar -10,07 kkal/mol dan 0,0417 ?M. Sementara dengan senyawa ?-mangostin berturut-turut sebesar -8,91 kkal/mol dan 0.29317 ?M. Hal tersebut menunjukkan bahwa senyawa ?-mangostin memiliki potensi sebagai antidiabetes mellitus tipe 2 dengan menghambat PTP1B. Selain itu, senyawa ?-mangostin juga memiliki profil ADMET yang baik. Kata kunci: antidiabetes, diabetes mellitus tipe 2, penambatan molekuler, PTP1B, Xanton Type 2 diabetes mellitus is caused by high PTP1B expression and affects the activity of PTKs, which causes insulin to fail to bind to insulin receptors, and induces insulin resistance. Xanthones and benzophenones are compounds that have been known to have pharmacological activity as antidiabetic. One of the plants containing these compounds is Garcinia cowa. This study aims to know the affinity and inhibition mechanism of PTP1B by xanthones, benzophenones, and triterpenoid in Garcinia cowa, including garcinia cowone K, guttiferone I, 1,7-dihydroxyxanthone, 1-hydroxyl-7 methoxyxanthone, mangostinone, ?-mangostin, cowanol, gacibiphenyl C, friedelin, ?-friedelinol, and oleanane-12-ol in silico by molecular docking and conducted a pre-ADMET study of these compounds. Molecular docking is carried out in several steps including preparation and optimization of the 3D structure of the compound, preparation of the PTP1B receptor 3D structure, method validation, and docking of the compound with PTP1B. The results obtained from the docking of the compound with the PTP1B receptor appears in the form of bond energies, inhibition constant (IC), and hydrogen bonds. The lower the bond energy value, the more stable the bond between the protein and the resulting ligand is. The results showed that the bond energy and IC value of PTP1B with the native ligand is -10,07 kcal/mol and 0,0417 ?M. Meanwhile the ?-mangostin compound is -8,91 kcal/mol and 0,29317 ?M. It shows that the ?-mangostin has potential as an antidiabetic mellitus type 2 agent by inhibiting PTP1B. In addition, ?-mangostin also shows a good ADMET profile. Keywords: antidiabetic, molecular docking, PTP1B, type 2 diabetes mellitus, xanthones
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