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Solid dispersion of quercetin-PVP K-30 and its effects on the antioxidant activity Zahara Gayo; Henny Lucida; Erizal Zaini
Jurnal Ilmiah Farmasi Vol. 16 No. 2 (2020): Jurnal Ilmiah Farmasi
Publisher : Universitas Islam Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.20885/jif.vol16.iss2.art6

Abstract

AbstractBackground: Quercetin (3,3’,4’,5,7-pentahydroxil-flavon) is a flavone and secondary metabolite known as flavonoid. Quercetin belongs to class II BCS that has low solubility and high permeability. The poor solubility of quercetin restricts the accessibility and bioavailability.Objectives: To increase the solubility, dissolution, and antioxidant activity in a solid dispersion system.Methods: Preparation of quersetin-PVP K-30 solid dispersion was conducted using the freeze-drying method at -96 degree C for 24 hours with a ratio of 1:1, 1:0.5, and 0.5:1 and a 1:1 physical mixture of quercetin-PVP K-30. The solid dispersion of quercetin-PVP K-30 was characterized by Scanning Electron Microscopy (SEM), X-Ray Diffraction (XRD) analysis, and FT-IR spectrophotometric analysis. Solubility test was analyzed using a UV-Vis spectrophotometer, dissolution test was done using a paddle-type dissolution tester, dissolved quercetin concentrations were analyzed using a UV-Vis spectrophotometer, and antioxidant activity was determined using the DPPH method in a UV-Vis spectrophotometer.Results: SEM analysis showed the formation of quercetin-PVP K-30 solid dispersion using the freeze-drying method, and the form changed into anhydrate as seen from the XRD results with the presence of new crystalline peaks in solid dispersion, which were not seen in pure quercetin and PVP K-30. Quercetin-PVP K-30 solid dispersion could increase the solubility by 54-fold at a ratio of 0.5:1 with 94.36%±0.85 quercetin dissolved in 120 minutes. The formation of this solid dispersion affected the antioxidant activity which was observable from the IC50 value at the best ratio of 0.5:1 reaching 0.714 microgram/mL while the IC50 value of pure quercetin is 1.102 microgram/mL.Conclusion: The formation of quercetin solid dispersion could increase the solubility and dissolution and affect the antioxidant activity.Keywords: solid dispersion, freeze-drying, quercetin, antioxidantIntisariLatar Belakang: Kuersetin (3,3’,4’,5,7-pentahydroxil flavon) adalah flavon dan merupakan metabolit sekunder yang dikenal dengan flavonoid. Kuersetin tergolong dalam BCS kelas II yaitu memiliki kelarutan rendah dan permeabilitas tinggi (low solubility and high permeability drugs), kelarutan kuersetin yang buruk membatasi aksesibilitas dan bioavailabilitasnya.Tujuan: Untuk meningkatkan kelarutan dan disolusi kuersetin serta melihat pengaruhnya terhadap aktivitas antioksidan kuersetin.Metode: Pembuatan dispersi padat menggunakan metode freeze dry pada suhu -96 derajat C selama 24 jam.Hasil: Dengan pembuatan disepersi padat kuersetin-PVP K-30 dapat meningkatkan kelarutan, disolusi dan dapat meningkatkan aktivitas antioksidan kuersetin.Kesimpulan: Uji statistik menggunakan ANOVA dua arah menunjukkan uji kelarutan dan disolusi pada pembentukan dispersi padat kuersetin-PVP K-30 terdapat perbedaan yang signifikan (p= 0,000 (Sig<0,05)).Kata Kunci: Dispersi padat, Freeze Dry, Kuersetin, Antioksidan
KARAKTERISASI FISIKOKIMIA DAN LAJU DISOLUSI DISPERSI PADAT IBUPROFEN DENGAN PEMBAWA POLIETILENGLIKOL 6000 Erizal Zaini; Rahmi x Rahmi Nofita; Salman -; Irna Kurniati
Jurnal Riset Kimia Vol. 4 No. 1 (2010): September
Publisher : Universitas Andalas

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.25077/jrk.v4i1.63

Abstract

 Solid dispersions of the antiinflamation drug ibuprofen and polyethylene glycol 6000 (PEG 6000) were prepared by the melting method in order to increase the dissolution rates of this poorly water-soluble compound. The temperature/composition phase diagram of binary system was analyzed by termal analysis hot-stage microscopy, showing an eutectic formation. Polarized light hot stage microscopy and X-ray-powder diffraction confirmed, that solid dispersion technique decrease the crystalliny of ibuprofen after melting and solidifying of a 4/6 (w/w) mixture of ibuprofen and polyethylene glycol 6000 respectively, which the results enhanced dissolution rates compared to the physical mixtures and ibuprofen intact. However, no such chemical interactions in the solid state were confirmed by FTIR spectra which showed the presence of ibuprofen crystalline in solid dispersion.   
MANUFACTURE OF PLASTICS FILM CONTAINING OF POLYSTIRENE, POLYCAPROLACTONE, POLY(3-HIDROKSIBUTYRATE-CO-3- HIDROXYVALERATE) AND BIODEGRADATION STUDY IN OCEAN WATER Asiska Permata Dewi; Erizal Zaini; Akmal Djamaan
Jurnal Riset Kimia Vol. 7 No. 2 (2014): March
Publisher : Universitas Andalas

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.25077/jrk.v7i2.167

Abstract

 ABSTRACTThe manufacture of a biodegradable plastics film containing of polymer synthetic polystyrene(PS) and biopolymer of polycaprolactone (PCL), poly(3-hydroxybutyrate-co-3-hydroxyvalerate)[P(3HB-ko-3HV)] and biodegradation study in ocean water has been carried out. Plastics filmcontaining of PS/PCL/P(3HB-ko-3HV) produced by blending techniques followed by solventcasting with ratios were of 100/0/0, 95/5/0, 95/0/5, 90/5/5, 85/10/5, 85/5/10. This testing wasconducted based on immersion test method recommend by American Society for Testing andMaterials. Poly blend plastics film PS/PCL/P(3HB-ko-3HV) were characterized by tensilestrength, thermal properties and SEM analysis. The profiles of the rate biodegradation view byweight reduction of the tested plastic film for 1-7 weeks period. Tensile strength analysisshowed the decreasing of tensile strength with the addition of P(3HB-ko-3HV). Thermalanalysis showed a decreasing in the melting point with the addition of PCL and P(3HB-co-3HV). SEM micrograph showed the destruction occurred and erosion at surface of plastic filmduring observation time. The rate of biodegradation showed that increasing of PCL and P (3HBco-3HV) in a mixture of plastic film, so biodegradation increased.Keywords: polystyrene, polycaprolactone, poly(3-hidroxybutyrate-co-3-hydroxyvalerate),biodegradation, film plastic.
Identification of physical interaction between trimethoprim and sulfamethoxazole by contact method koflerand crystallization reaction Erizal Zaini; Yeyet C. Sumirtapura; Sundani N. Soewandhi; Auzal Halim
Indonesian Journal of Pharmacy Vol 21 No 1, 2010
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (734.118 KB) | DOI: 10.14499/indonesianjpharm0iss0pp32-39

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Identification  of  solid  state  interaction  between  TMP  and  SMZ  by  hot contact  method Kofler and  crystallization  reaction  had  been  carried  out.  The results of hot contact method Koflershown formation a new crystalline habit as long  and thin needle  shaped  on  contact  zone  (mixing  zone) between Solid  TMP and SMZ. It had a different melting point in compared to its single component. Crystallization  reaction  between  two  of  supersaturated  solution  of  component TMP and  SMZ  in methanol  solvent  also  indicated  the  growth  of crystal  habit  as similar as   hot contact method Kofler.  Solid  state  interaction between  TMP  and SMZ  was confirmed  by  microscopic  SEM, powder  X-ray diffraction,  and  thermal DSC.  Microscopic  analysis by  SEM  showed significantly  the  change  of habit and morphology  of   crystal  as  long  and  thin  needle  shaped.  New  powder  X-ray diffraction  (PXRD)  interferences  peaks  were  observed  in  addition  to  PXRD interference  peaks  of  each  component  that  proved  formation  of  cocrystalline phase.  Thermogram  DSC  indicated  a  new   endothermic  peak  corresponding  to melting point of a new cocrystalline phase at temperature 178,82 °C.Key words : trimethoprim, sulfamethoxazole, physical interaction, cocrystalline phase
Peningkatan Laju Disolusi Trimetoprim dengan Teknik Co-Grinding Menggunakan Polimer Polivinilpirolidon K-30 AUZAL HALIM; SYUKRAN HAMDENI; ERIZAL ZAINI
JURNAL ILMU KEFARMASIAN INDONESIA Vol 11 No 1 (2013): JIFI
Publisher : Fakultas Farmasi Universitas Pancasila

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (1085.687 KB)

Abstract

Improvement of the dissolution rate of trimethoprim (TMP) as a model for a poorly water-soluble drug by solid state co-grinding technique with hydrophilic polymer polyvinylpyrrolidone K-30 (PVP K-30) using ball milling apparatus have been investigated. The ratios of drug to hydrophilic polymer were 1:1, 1:3 and 1:5. The solid state interaction of co-ground and physical mixture were characterized by powder X-ray diffraction, thermal DTA, SEM and FT-IR spectroscopy analysis. The dissolution studies were carried out in USP type I apparatus. The result of powder X-ray diffraction analysis showed that the co-grinding of TMP with PVP K-30 decreased the drug’s crystalinity. The endothermic peak of TMP of co-ground products shifted to lower temperature and peak intensity decreased significantly. Powder X-ray diffraction and DTA analysis indicated transformation of crystalline state of TMP to amorphous form by co-grinding with PVP K-30. FT-IR Spectra indicated that no chemical interaction between TMP and PVP K-30 in the co-grounds. Significant enhancement in dissolution rates were observed with the co-ground products of TMP and PVP K-30 as compared to the intact TMP and its physical mixture. In general, the dissolution rates of TMP in the co-grounds were enhanced as the polymer ratio increased.
PEMBENTUKAN MULTIKOMPONEN KRISTAL PIPERIN DAN KUERSETIN Adhitya Jessica; Rifka Naura; Uswatul Hasanah; Erizal Zaini; Lili Fitriani
JURNAL FARMASI DAN MAKANAN Vol 4 No 2 (2021): Journal Of Pharmacy and Science
Publisher : LPPM Universitas Abdurrab

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.36341/jops.v4i2.1881

Abstract

Penggunaan klinis piperin masih terbatas karena memiliki kelarutan rendah di dalam air. Kuersetin dikenal sebagai bioenhancer yang dapat meningkatkan bioavailibilitas senyawa lain. Penelitian ini bertujuan untuk meningkatkan kelarutan piperin dengan memodifikasinya menjadi bentuk multikomponen kristal bersama kuersetin. Pembentukan multikomponen kristal piperin-kuersetin dilakukan menggunakan metode solvent drop grinding (SDG). Multikomponen dikarakterisasi dengan Differential Scanning Calorimetry (DSC), Powders X-Ray Diffraction (PXRD) dan spektroskopi FTIR.Evaluasi multikomponen dilakukan dengan uji kelarutan dan hasilnya dianalisis menggunakan KCKT.Termogram DSC menunjukkan tidak adanya puncak endotermik baru yang berbeda nyata dari kedua komponen. Pola difraksi sinar-X multikomponen kristal piperin-kuersetin menunjukkan difraktogram yang serupa dengan komponen penyusun, yang mengindikasikan tidak terbentuknya fase kokristalin. Karakterisasi menggunakan FTIR menunjukkan hampir tidak ada pergeseran puncak serapan gugus fungsi piperin pada multikomponen kristal. Uji kelarutan dilakukan terhadap senyawa tunggal piperin, campuran fisik piperin-kuersetin dan multikomponen piperin-kuersetin (1:1) yang dibuat dengan metode SDG. Campuran fisik dan multikomponen piperin-kuersetin yang dibuat dengan metode SDG meningkatkan kelarutan piperin sebesar 1,475 kali lipat dan 1,389 kali lipat jika dibandingkan dengan piperin murni.
Studi Sistem Dispersi Padat Asam Mefenamat Menggunakan Polivinilpirolidon K-30 Maria Dona Octavia; Erizal Zaini; Vina Oktavia
Jurnal Farmasi Higea Vol 7, No 2 (2015)
Publisher : STIFARM Padang

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (670.647 KB) | DOI: 10.52689/higea.v7i2.128

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Mefenamic acid was categorized as Non-Steroidal Anti-Inflamatory Drugs (NSAIDs) which has useful as analgesic, anti inflammatory, and antypiretic effect but it has poor solubility in water. The aim of this study was to increase the dissolution rate of mefenamic acid in a solid dispersion system which made by solvent method. Solid dispersion and physical mixture prepared with ratio 1:1, 1:3, and 1:5. Solid dispersion was prepared by solvent method Preparation of solid dispersion mefenamat acid – PVP-K30 in formula 1:3 was increased of dissolution significantly.  Characterization of Solid dispersion Mefenamic Acid with Polyvinylpyrrolidone used Scanning Electron Microscopy (SEM), X-Ray, Spectroscopy IR, Differentyal Thermal Analysis (DTA). The result of X-ray diffraction characterization the dissolution Mefenamic Acid-Polyvinylpyrrolidone in which the intensity is visible. The characterization with DTA showed a change in the peak of Mefenamic Acid where the endoterm, the characterization using infrared spectroscopy shows no functional group interaction between Mefenamic Acid and Polyvinylpyrrolidone.
Studi Sistem Dispersi Padat Meloksikam Menggunakan Hiroksipropil Metilselulosa (HPMC) 6 Centipoise (CPS) Erizal Zaini; Maria Dona Octavia; Kiki Rizky Wirza
Jurnal Farmasi Higea Vol 4, No 2 (2012)
Publisher : STIFARM Padang

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (574.196 KB) | DOI: 10.52689/higea.v4i2.63

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The solid dispersion system of meloxicam-hydroxypropyl methylcelluloce (HPMC) 6 centipoise (cps) had been studied. The solid dispersion system was prepared by solvation method with several combination of meloxicam and HPMC were 1:1, 1:3 and 1:5. The physical mixture of meloxicam and HPMC with similar composition were used as standard. The powder of solid dispersion system and physical mixture were evaluated by X-ray powder diffraction, thermal (DTA), SEM and FT-IR spectroscopy analysis. The dissolution studies were carried out in USP type II apparatus. The result of X-ray powder diffraction analysis showed that the solid dispersion of  meloxicam with HPMC decreased the drug crystallinity. The endothermic peak of meloxicam from solid dispersion products shifted to lower temperature and peak intensity decreased significantly. X-ray powder diffraction and DTA indicated transformation of crystalline state of meloxicam to amorphous one by solid dispersion with HPMC. SEM results showed the solid dispersion of meloxicam and HPMC has agglomerates form. FT-IR spectra indicated no chemical interaction between meloxicam and HPMC in the solid dispersion. The highest in dissolution rate was observed with solid dispersion products of meloxicam and HPMC with ratio 1:5 (94,083 %) compared to pure meloxicam and its physical mixture.
Peningkatan Laju Disolusi Sistem Dispersi Padat Ibuprofen – PEG 6000 Auzal Halim; Elvi Rahma Yulisman; Erizal Zaini
Jurnal Farmasi Higea Vol 5, No 2 (2013)
Publisher : STIFARM Padang

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (786.399 KB) | DOI: 10.52689/higea.v5i2.83

Abstract

It has done research on increasing the dissolution rate of solid dispersion system Ibuprofen with polymer Polyethylenglycols 6000 (PEG 6000). Solid dispersion system prepared by melting method with a ratio of raw materials Ibuprofen - PEG 6000, namely : 6:4, 7:3, 8:2, and 9:1. As a comparison was made with the physical mixture of the same composition. The powder mixture of physics and solid dispersion system properties of solids characterized by spectroscopic analysis, SEM analysis, DTA analysis, and X-ray diffraction analysis. Dissolution test method is determined by a basket. The results showed that the powder solid dispersion system can improve the physicochemical properties of Ibuprofen. Dissolution profiles showed that the 7:3 solid dispersion system powder in the 45th minute to increase the dissolution rate compared to the powder mixture of physics.
Pelepasan Ibuprofen dari Gel Karbomer 940 Kokristal Ibuprofen-Nikotinamida Rini Agustin; Novica Sari; Erizal Zaini
Jurnal Sains Farmasi & Klinis Vol 1, No 1 (2014): J Sains Farm Klin 1(1), November 2014
Publisher : Fakultas Farmasi Universitas Andalas

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (398.538 KB) | DOI: 10.29208/jsfk.2014.1.1.15

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One of the methods to increase the solubility is co-crystalization. As Ibuprofen can be used in topical application for rheumatoid arthritis, a study about formulation and release of ibuprofen-nicotinamide co-crystal in carbomer gel had been conducted. Co-crystal was obtained from a dissolve method, which ibuprofen and nicotinamida were mixed with equimol composition (1:1). Gel consisted of two formulas with the same amount of ibuprofen (5%). The first formula was gel co-crystal ibuprofen-nicotinamide and the second formula was pure ibuprofen. The basis used was carbormer 940. The release test was done using the horizontal type of Franz diffusion cell and measured using HPLC (High Performance Liquid Chromatography) with mobile phase of methanol: aquabidest (80:20) pH 3.5 with orthophosphate acid. The results showed both formulas were not stable in homogeneity aspect for several storage days. Separation was occurred at low and high temperatures. The result of release profiles at the 120th minutes was 4.4793 % and 4.4293 % and the release efficiencies were 3.8891 and 3.8612. The statistic analysis showed that release efficiencies of both formulas were not significantly different (p>0.05) using One-Way ANOVA. In a conclusion, the process of making gel of co-crystal ibuprofen-nicotinamide did not influenced ibuprofen release in gel preparation.
Co-Authors -, Salman Adhitya Jessica Agusri Boestari Agustina, Annisa Akmal Djamaan Amri Bakhtiar Andarifera, Alya Zahira Annisa Agustina Aprilianti, Hizra Dwi Arif, Zhafira Asiska Permata Dewi Asiska Permata Dewi Asiska Permatadewi Auzal Halim Auzal Halim Azzahra, Cindy Maynia Ben, Elfi Sahlan Deni Anggraini Deni Noviza Dhea Sultana Lutfiyah DINI HANIFA, DINI Dwi Setyawan Ellyza Nasrul Elpa Giovana Zola Elsa Badriyya Elvi Rahma Yulisman Elvita Sari Fadhila, Muthia Fauzi Saputra Fifi Harmely Friardi Ismed Gaesari, Sherly Rahmah Gaesari, Sherly Rahmah Gumala, Azhoma Habibie Deswilyaz Ghiffari Hansen Nasif Haq AH, Ahdi Dinil Hasmiwati Helen Sonita Henny Lucida Hulwa Salsabila Ihsan, Ikhwanul Ima Kurniati Irna Kurniati Jessica, Adhitya Kiki Rizky Wirza Kurniati, Irna Lili Fitriani Mai Efdi Maria Dona Octavia Melanny Ika Sulistyowaty Melisa Melisa Melzi Octaviani Mohd Amin, Mohd Cairul Iqbal Muhammad Taher Muthia Fadhila Mutiara Zulkarnaini Najmi Hilaliyati Netty Novitasari Nova Syafni Novica Sari Prameswari, Putu Pradnya Mimba Raden Joko Kuncoroningrat Susilo Rahmadasmi, Nola Rahmadevi Rahmi Nofita Rahmi Yosmar Rahmi Yosmar Resva Meinisasti Revila, Gusti Reza Safitri Rifka Naura Rini Agustin Rini Agustin Rizky, Fattihatul Rosaini, Henni Rose Intan Perma Sari Rustini Rustini Rustini Rustini S, Agnes Saafrida Saafrida Saafrida Saafrida Saafrida Salman - Salman - Salman Salman Salman Umar Sari, Elvita Sayyidina, Fasqina Simbolon, Clara Alverina Sundani N. Soewandhi Sundani N. Soewandhi, Sundani N. Syofyan Syofyan SYUKRAN HAMDENI Syukriati Chaira Tahta Amrillah Trisfa Augia Try Andy Sahputra Try Andy Sahputra Usman, Hendrizal Uswatul Hasanah Uswatul Hasanah, Uswatul Verlia Nisrina Putri Vike Zulia Putri Vina Oktavia Yeni Novita Sari Yeyet C. Sumirtapura Yufri Aldi Yuliza, Sukma Yuska Noviyanty Zahara Gayo Zidan, Sabry A. H. Zulhadjri Zulhadjri