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Preparation and Characterization of a Novel Cocrystal of Atorvastatin Calcium with Succinic Acid Coformer Yudi Wicaksono; Dwi Setyawan; Siswandono Siswandono; Tri Agus Siswoyo
Indonesian Journal of Chemistry Vol 19, No 3 (2019)
Publisher : Universitas Gadjah Mada

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (21.219 KB) | DOI: 10.22146/ijc.35801

Abstract

Preparation and characterization of a novel cocrystal of atorvastatin calcium with succinic acid coformer were successfully performed. This research aims to modify the crystalline form of atorvastatin calcium through cocrystallization with succinic acid coformer. The cocrystal was prepared by a solvent evaporation method and characterized by Powder X-Ray Diffraction (PXRD), Differential Scanning Calorimetry (DSC), Fourier Transform Infrared Spectroscopy (FTIR) and Scanning Electron Microscopy (SEM). The atorvastatin calcium-succinic acid cocrystal has new crystalline peaks at 2θ of 12.9, 18.2 and 26.7° indicating the formation of a new crystalline phase. The cocrystal showed the melting point at 205.7 °C with an enthalpy of fusion 30.2 J/g which is different from the initial components. The FTIR spectra of cocrystal showed the shifting of absorption peaks of groups of initial components indicating of formation of atorvastatin calcium-succinic acid cocrystal through acid–amide intermolecular hydrogen bond interactions. The solubility and dissolution test showed that the cocrystal has solubility and dissolution rate significantly higher than the solubility and dissolution rate of pure atorvastatin calcium.
Preparation of Atorvastatin Calcium-Dipicolinic Acid Multicomponent Solids by Liquid-Assisted Grinding Method to Increase Solubility Yudi Wicaksono; Shafira Faradiba Tsaniyah; Budipratiwi Wisudyaningsih; Kuni Zu''aimah Barikah; Lusia Oktora Ruma Kumala Sari
Molekul Vol 17 No 3 (2022)
Publisher : Universitas Jenderal Soedirman

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.20884/1.jm.2022.17.3.5946

Abstract

Atorvastatin calcium is a cholesterol-lowering drug that is very potent but difficult to dissolve in water, so its bioavailability is low. In this study, atorvastatin calcium-dipicolinic acid multicomponent solids were prepared using the liquid-assisted grinding method to improve atorvastatin calcium's solubility. Characterization of multicomponent solids was carried out using powder x-ray diffraction (PXRD), differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). Solubility test was carried out by shaking method using distilled water media. The results showed that the particles of atorvastatin calcium - dipicolinic acid multicomponent solids had an irregular shape with rough and porous surface topography. The multicomponent solids have a diffractogram with specific peaks of 2θ at 8.8, 9.9, 11.5, 16.7, 19.1, 21.2, 22.4, 23.4, and 27.7°. The DSC thermogram of multicomponent solids showed a sharp endothermic peak at 181.9 °C (∆H=17.69 J/g), indicating its melting point. The FTIR spectra of atorvastatin calcium-dipicolinic acid multicomponent solids indicated an intermolecular interaction that was thought to be a hydrogen bond between the molecules of atorvastatin calcium and dipicolinic acid. The results of the solubility test showed that the atorvastatin calcium-dipicolinic acid multicomponent solids had a significantly increased solubility (p<0.05) compared to the solubility of pure atorvastatin calcium.
Effect of Hydrophilic Polymers on Solubility Properties of Ketoprofen - 2,5-Dihydroxybenzoic Acid Multicomponent Solids Wicaksono, Yudi; Wisudyaningsih, Budipratiwi; Priyadi, Karina Priyadi Devi Wahyu; Laily, Aisyah Prida; Putri, Salsabila Bara
Molekul Vol 18 No 3 (2023)
Publisher : Universitas Jenderal Soedirman

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.20884/1.jm.2023.18.3.7292

Abstract

Ketoprofen is a medicinal compound derivative of phenyl alkanoic acid that works as an anti-inflammatory, antipyretic, and analgesic. In the Biopharmaceutical Classification Systems, ketoprofen is a class II drug with high permeability but low solubility. Due to its low solubility, the absorption and bioavailability of ketoprofen are very limited, which can affect its therapeutic effectiveness. This study aimed to increase ketoprofen's solubility by forming multicomponent solids using 2,5-dihydroxybenzoic acid coformer with adding hydrophilic polymers ((hydroxypropyl)methylcellulose, polyvinylpyrrolidone K90, and polyethylene glycol 4000). The results showed that ketoprofen with 2,5-dihydroxybenzoic acid coformer prepared using the solvent evaporation method formed a eutectic mixture. Adding hydrophilic polymers to the ketoprofen - 2,5-dihydroxybenzoic acid multicomponent solid increased the crystallinity and decreased the melting point of the multicomponent solids. The multicomponent solids of ketoprofen - 2,5-dihydroxybenzoic acid with the addition of hydrophilic polymers had solubility and dissolution efficiency significantly higher (p<0.05) than the ketoprofen - 2,5-dihydroxybenzoic acid multicomponent solids without hydrophilic polymers.
Phase Diagram and Thermodynamic Properties of Ketoprofen-Succinic Acid Binary Mixtures Wicaksono, Yudi; Setyawan, Dwi; Siswandono, S.
Jurnal ILMU DASAR Vol 19 No 2 (2018)
Publisher : Fakultas Matematika dan Ilmu Pengetahuan Alam Universitas Jember

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (373.972 KB) | DOI: 10.19184/jid.v19i2.5521

Abstract

The equilibrium phase diagram and thermodynamic properties of a mixture of drugs and additives are information related to various possible interaction processes between components. Therefore, we conducted a study of the phase diagrams and thermodynamic properties of binary mixtures of ketoprofen-succinic acid to estimate the types of interactions that may occur between these materials. The solid-liquid phase diagram of ketoprofen-succinic acid binary mixtures was determined by differential scanning calorimetry and composition of eutectic system was determined accurately using a Tamman diagram. The measurement of binary mixtures of ketoprofen-succinic acid with differential scanning calorimeter obtained the value of melting temperature and heat of fusion of ketoprofen- succinic acid system. The solid-liquid phase diagram of ketoprofen- succinic acid showed the formation of eutectic type phase diagram. The Tamman diagram showed accurately composition of the eutectic system of the Kp-SA binary mixtures at the mole fraction of Kp 0.87 and temperature 96.9oC.Keywords: ketoprofen, phase diagram, eutectic system, Tamman diagram
Quercetin-Glycolic Acid Cocrystalization Using Solvent Evaporation and Slurry Methods Barikah, Kuni Zu'aimah; Wicaksono, Yudi; Wisudyaningsih, Budipratiwi
Indonesian Journal of Pharmaceutical Science and Technology Vol 11, No 3 (2024)
Publisher : Indonesian Journal of Pharmaceutical Science and Technology

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.24198/ijpst.v11i3.43596

Abstract

Quercetin is a flavonoid compound with the highest antioxidant activity and has the potential to treat various diseases. However, quercetin has poor solubility in water which causes low bioavailability of the drug in the body. One of the modifications that can be made to improve the solubility of a drug is solid modification, for example cocrystals. Cocrystal is a crystalline system between drug and coformer which interacts through hydrogen bonding. Glycolic acid is a compound that can function as a coformer because it has functional groups that have the potential to interact through hydrogen bonds with quercetin molecules. Quercetin-glycolic acid cocrystals were prepared in two molar ratios, namely 1:1 and 1:2, and through two methods of preparation, namely solvent evaporation and slurry. The results of the crystallinity analysis and thermal analysis of the sample indicated that a new solid phase was formed in the sample that was specific and different from the two constituent components. Samples with a molar ratio of 1:2 and the slurry preparation method are known to be samples with the most optimal new crystalline phase formation.
PENGARUH PENAMBAHAN EKSTRAK DAUN MANGGA MANALAGI TERHADAP MUTU FISIK DAN EFEKTIVITAS TABIR SURYA EMULGEL KOMBINASI OCTINOXATE-AVOBENZONE Lidya Ameliana; Viddy Agustian Rosyidi; Dwi Nurahmanto; Yudi Wicaksono; Lita Putri Ayu Lestari
Jurnal Ilmiah Manuntung: Sains Farmasi Dan Kesehatan Vol. 9 No. 2 (2023): Jurnal Ilmiah Manuntung: Sains Farmasi Dan Kesehatan
Publisher : Sekolah Tinggi Ilmu Kesehatan Samarinda

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.51352/jim.v9i2.683

Abstract

Avobenzone and octinoxate are often used as a combination of organic UV filters in sunscreen. At high exposure to UV light, these UV filters can be degraded so that their sunscreen’s effectiveness is reduced. Several studies reported that the combination of plant extracts with synthetic UV filters could increase sunscreen's SPF. Mango leaves contain high levels of flavonoids and in several studies have been shown to have photoprotective activity with good Sun Protection Factor (SPF) values. The Manalagi mango plant is a type of mango that is widely planted in yards, so it's easy to get the raw materials. This study aims to determine the effect of manalagi mango leaf extract with a concentration of 1, 3, and 5% on the physical quality (pH, viscosity, spreadability) and sunscreen activity (SPF, %TE, %TP) of sunscreen emulgel containing avobenzone and octinoxate. This study showes that increasing the concentration of manalagi mango leaf extract reduced the pH and viscosity of the preparation, and significantly increased the spreadability of all formulas. Besides that, it can also increase the SPF value and decrease the %TE and %TP values. The emulgel formula that had the highest sunscreen activity was F3 with an extract concentration of 5%, had an SPF value of 30.597 ± 0.600, %TE 0.0001 ± 0.0001, and %TP 0.0038 ± 0.0016.
Optimasi Quercetin Kombinasi Avobenzone dalam Sediaan Spray Lotion Tabir Surya Budipratiwi Wisudyaningsih; Elok Rimadani; Lidya Ameliana; Lusia Oktora Ruma Kumala Sari; Yudi Wicaksono; Kuni Zu’aimah Barikah
Jurnal Ilmu Farmasi dan Farmasi Klinik No 1 (2024): JIFFK Special Edition Suppl. 2
Publisher : Universitas Wahid Hasyim Semarang

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.31942/jiffk.v2i1.9230

Abstract

Excessive exposure to ultraviolet radiation can cause various skin problems. This problem can be prevented by using cosmetic products that contain sunscreen ingredients. In this study, optimization of the combination of quercetin and avobenzone in sunscreen spray lotion was carried out using the factorial design method. The aim of this study was to determine the optimum concentrations of avobenzone and quercetin which could provide optimum physicochemical properties and effectiveness of in vitro sunscreen spray lotion. The formula is made with a low concentration of 0.5% quercetin and an upper limit of 3%, while avobenzone has a low level of 2% and an upper level of 4%. Based on the research that has been done, the optimum formula prediction is obtained with a concentration of 0.934% quercetin and 4% avobenzone. The optimum formula has a desirability value of 0.958 and shows the predicted value of software to have an SPF in vitro value of 33.311, a %TE 0.058%, a %TP 0.002%, a viscosity of 10 dPa.s, and a pH of 5.689. The results of the analysis using the t-test (one sample t-test) with a 95% level of confidence between the software prediction results and the observation results showed a value of > 0.05, which means that there was no significant difference between the software prediction results and the observation group.
Interaksi Padatan dan Pembentukan Eutektik dalam Campuran Biner Gemfibrozil-Nikotinamida Prihandini , Khairinna; Wisudyaningsih , Budipratiwi; Wicaksono, Yudi
Journal of Pharmaceutical and Sciences JPS Volume 8 Nomor 3 (2025)
Publisher : Fakultas Farmasi Universitas Tjut Nyak Dhien

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.36490/journal-jps.com.v8i3.986

Abstract

Background: Gemfibrozil is an antihyperlipidemic drug that effectively lowers cholesterol and triglyceride levels in the blood. However, it has limitations, primarily low solubility and compactibility. Objective: The objective of this study was to analyze the solid interactions in a binary mixture of gemfibrozil and nicotinamide, which is useful for modifying the physicochemical properties of gemfibrozil through the formation of multicomponent solids. Methods: The method employed for solid-state interaction analysis was differential scanning calorimetry (DSC), which involved constructing solid-liquid phase diagrams, accompanied by Fourier transform infrared spectroscopy (FTIR) analysis to identify any hydrogen bonding interactions between the components. Results: The results revealed that the gemfibrozil-nicotinamide binary mixture formed a solid-liquid phase diagram characterized by a V-type solid curve. A eutectic mixture was observed at a molar ratio of 8:2, with a eutectic melting point of 59.3 °C. FTIR analysis revealed no hydrogen bonding interactions between gemfibrozil and nicotinamide. Conclusion: It was concluded that gemfibrozil in the binary mixture system did not form a solid interaction with nicotinamide but was a eutectic mixture. These findings can be used to design strategies for improving the physicochemical properties of gemfibrozil through the formation of multicomponent solids.
Stability Improvement and Solid-State of Sauropus androgynus Leaf Extract Solid Dispersion Using a Carrier of Polyvinylpyrrolidone Jingga, Mutiara Dara; Barikah, Kuni Zuaimah; Wicaksono, Yudi
Indonesian Journal of Applied Research (IJAR) Vol. 6 No. 2 (2025): Indonesian Journal of Applied Research (IJAR)
Publisher : Universitas Djuanda

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.30997/ijar.v6i2.682

Abstract

The Sauropus androgynus leaf contains various phytochemical compounds with various pharmacological activities. However, phytochemical compounds in plant extracts are generally unstable during storage or formulation. This study aimed to prepare S. androgynus leaf extract solid dispersions and evaluate the solid-state properties and stability. Solid dispersions were produced through solvent evaporation using polyvinylpyrrolidone (PVP) as the carrier. Solid dispersions were characterized by powder X-ray diffractometer (PXRD), differential scanning calorimeter (DSC), and scanning electron microscope (SEM). Solid dispersions were stored at a temperature of 60 °C for 30 days, and the stability was determined by measuring the total flavonoid content. The preparation results showed that solid dispersions of S. androgynus leaf extract with PVP K30 and PVP K90 carriers were amorphous solids with a glass transition temperature of 160-170 °C. The phytochemical content of the extract in solid dispersion showed degradation at a temperature of 175.3 - 188.3 °C. At a temperature of 60 °C for 30 days, the decrease of total flavonoid content in solid dispersion was lower than in pure extract. Thus, the formation of solid dispersion of S. androgynus leaf extract with PVP K30 and PVP K90 carriers can increase the stability of phytochemical compounds in S. androgynus leaf extract.
Potensi Antimalaria Fraksi-Fraksi Daun Kembang Bulan (Tithonia diversifolia [Hemsley] A. Gray) Nuri; Wicaksono, Yudi; Rahardi, Verdian; Utami, Wiwien Sugih; Armiyanti, Yunita
Journal of Agropharmacy Vol. 1 No. 1 (2024)
Publisher : Faculty of Pharmacy, University of Jember

Show Abstract | Download Original | Original Source | Check in Google Scholar

Abstract

Kembang bulan (Tithonia diversifolia [Hemsley] A. Gray) has been used in traditional medicine to treat malaria. Previous research results showed that the ethanol extract of kembang bulan leaves had antimalarial activity in vivo with an ED50 of 113.39 mg/kgBW. Until now, the compounds with antimalarial activity in vivo are unknown. The initial stage that can be done to separate the compounds in the extract is fractionation. This study aims to separate the extract into fractions and test its antimalarial activity. Fractionation was carried out using a vacuum liquid chromatography method using a stationaryphase of silica gel GF254 and a mobile phase of n-hexane, chloroform and methanol in a gradient. In vivo antimalarial activity was tested using the Peter test method. Fractionation produces 5 fractions, each yield is 1.9; 2.1; 17.6; 60.8, and 17.6% respectively for fractions 1-5. The results of the antimalarial activity test for fractions 1-5 with a dose of 2 mg/kgBW showed inhibition of the growth of Plasmodium berghei respectively at 52.3 ± 1.4; 83.5±1.4; 74.6±1.2; 69.5±0.9; 44.8 ± 0.3%. Fraction 2 with the greatest resistance was tested further and showed an ED50 value of 0.52 mg/kgBW.