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Formulation self nano emulsifying drug delivery system glimepiride using oleic acid as oil phase Sani Ega Priani; Nurrayyan Nurrayyan; Fitrianti Darusman
Pharmaciana Vol 7, No 2 (2017): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (357.782 KB) | DOI: 10.12928/pharmaciana.v7i2.7387

Abstract

Glimepiride is a third generation sulphonylurea antidiabetic drug. Glimepiride is poorly water soluble drug that may cause poor dissolution and unpredicted bioavailability. Self nanoemulsifying drug delivery systems (SNEDDS) have become a popular formulation option as nanocarriers for poorly water-soluble drugs. The objective of this research was to develop SNEDDS formulation of glimepiride to improve oral dissolution and bioavailability. Glimepiride SNEDDS  was formulated using oleic acid as oil phase, tween 80 as surfactant, and transcutol as co-surfactant due to their higher solubilization effect. The formulated SNEDDS were evaluated for % transmittance, dispersibility, thermodynamic stability, dissolution, globule size and morphology analysis. The results showed that the glimepiride SNEDDS was rapidly formed clear emulsion and stabile based on thermodynamic test. Transmission electron microscopy demonstrated the spherical droplets morphology in nanometer range. The globule average diameter size was 45 nm. The SNEDDS formulation significantly increase dissolution of glimepiride compared with pure drug.
Identification of the molecular mechanism of christinin compounds from Arabian bidara leaves (Ziziphus spina-christi L.) on microorganisms that cause female genital problems through computational approaches Fitrianti Darusman; Taufik Muhammad Fakih
Pharmaciana Vol 10, No 3 (2020): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.12928/pharmaciana.v10i3.18177

Abstract

Arabian bidara leaves (Ziziphus spina-christi, L.) are known to have strong antimicrobial activity against microorganisms that cause infection in the female genital area, namely Staphylococcus aureus bacteria and Candida albicans fungi. They contain main secondary metabolites such as flavonoids, alkaloids, and saponins. Christinin is a saponin glycoside derivative compound which consists of four types, namely christinin-A, B, C, and D. The role of computational studies in the discovery of new drugs is crucial and interesting nowadays because it is relatively cheap, effective, fast, and precise with a reliable level of accuracy. This computational study result will later be used to confirm in vitro test results which are carried out using experimental microbiological testing methods in the laboratory. This study identified, evaluated, and explored the interactions between christinin-A, B, C, and D compounds with Penicillin Binding Protein (PBP) from Staphylococcus aureus and Dihydrofolate Reductase from the fungus Candida albicans using computational study were carried out using the molecular docking. The christinin-A, B, C, and D compounds were modeled into 3D conformation using GaussView 5.0.8 and Gaussian09 software. The best conformation was selected for molecular interaction studies on Penicillin Binding Protein (PBP) from Staphylococcus aureus bacteria and Dihydrofolate Reductase from Candida albicans using MGLTools 1.5.6 software with AutoDock 4.2. The molecular interactions that occurred were further observed using the BIOVIA Discovery Studio 2020 software. Based on the molecular docking results, the christinin-B compound had the highest affinity for Penicillin Binding Protein (PBP) from Staphylococcus aureus bacteria, with a binding-free energy value of −7.67 kcal/mol. Meanwhile, the christinin-A compound has the highest affinity for Dihydrofolate Reductase from the fungus Candida albicans, with a binding-free energy value of −8.38 kcal/mol. Thus, it is predicted that christinin compounds can be chosen as the main component in feminine hygiene preparations to maintain the female genital area's health. 
The effect of particle size on dissolution rate of fast dissolving oral film containing diclofenac sodium Fitrianti Darusman; Nyayu Ista Yulita; Gita Cahya Eka Darma
Pharmaciana Vol 10, No 2 (2020): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.12928/pharmaciana.v10i2.15988

Abstract

Diclofenac sodium is a Non-Steroidal Anti Inflammatory Drugs that if being taken orally have the side effects of peptic ulcers and undergone the first pass metabolism, and also included in the Biopharmaceutics Classification System class 2 which resulted in the low rate of dissolution. This study aims to determine the influence of particle size reduction on the dissolution rate of diclofenac sodium in the form of an FDOF dosage. The formation of diclofenac sodium nanoparticles is carried out by ionic gelation method using chitosan and sodium tripolyphosphate as a crosslinker in various ratios characterized by Particle Size Analyzer and Scanning Electron Microscopy, then it is incorporated into the form of an FDOF that were prepared by solvent casting method at a dose of 12.5 mg using variations concentration of SSG as superdisintegrant and PEG 400 as plasticizer. From the research results, diclofenac sodium nanoparticles are formed in the ratio of chitosan-sodium tripolyphosphate 6:1, have a size of 804 nm and spherical-shaped. The best FDOF dosage formula is F8 containing HPMC E5 LV 35% as the film forming agent, SSG 8% as superdisintegrant and PEG 400 10% as plasticizer.  FDOF formula containing diclofenac sodium nanoparticles has a slightly bitter taste, disintegration time less than one minute, surface pH around 7 (neutral), drug content that meets the requirements of the range of determination which is 93.24 ± 0.96, the cumulative amount of drug dissolved in the 28th minute is higher by 88.45% compared to FDOF containing diclofenac sodium raw material, which is only 70.0%.
Effect of carboxymethylcellulose sodium addition as stabilizer for physicochemical characteristic of purple sweet potato fortified yogurt (Ipomoea batatas L.) Uci Ary Lantika; Fitrianti Darusman; Widad Aghnia Shalannandia; Astrid Feinisa Khairani
Pharmaciana Vol 11, No 1 (2021): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.12928/pharmaciana.v11i1.18088

Abstract

The yoghurt consisted of low-fat milk, three bacterial strains starter, which included: L. bulgaricus ATCC 11842, L. plantarum ATCC 8014, and B. longum (1:1:1); purple sweet potato puree (Ipomoea batatas, L.) and carboxymethylcellulose sodium with the concentration of 0.6%, 1.2%, and 1.8%. Purple sweet potato fortification in yogurt can prevent hypercholesterolemic conditions because it inhibits lipid and sugar absorption in the intestine. Unfortunately, there is one shortcoming in the production of yogurt which affects the final product quality. This shortcoming is in the decrease in the air holding capacity (whey off) during the production due to the pH level within the isoelectric point of casein. This causes precipitation and phase separation. This study will add a stabilizer to the formula to overcome it. The stabilizer used is carboxymethylcellulose sodium, which is semi-synthetic water-soluble ester polymer cellulose. This study aimed to determine the optimal concentration of carboxymethylcellulose sodium and its effect on purple sweet potato yogurt's physicochemical and organoleptic properties. The product quality evaluations were on organoleptic evaluation, density, viscosity, and pH level. Centrifugation and freeze-thaw tests were also performed to evaluate product stability. The results showed that carboxymethylcellulose sodium could maintain the stability of purple sweet potato yogurt by binding the air content, increasing consistency, and smoothing the texture even though it did not affect the freezing point of the product. This study gave the best results for purple sweet potato yogurt with 1.2% carboxymethylcellulose sodium concentration.
In-vitro diffusion study of caffeine from microemulsion gel system containing grape seed oil Sani Ega Priani; Dinnanda Yussepina Wulansari; Fitrianti Darusman
Pharmaciana Vol 11, No 1 (2021): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.12928/pharmaciana.v11i1.18048

Abstract

Cellulite was identified by the orange-peel appearance of skin surface that presents in 80-90% of post-pubertal women. Caffeine and grape seed oil were known can be used as an anti-cellulite agent. Microemulsion systems are known could enhance the diffusion rate of drugs through the skin. This study was conducted to develop a microemulsion gel containing caffeine and grape seed oil and determine the effect of caffeine's in vitro diffusion profile. Microemulsion gel was prepared using tween 80 as a surfactant, glycerin as cosurfactant, viscolam mac 10 as a gelling agent. The preparations were evaluated by organoleptic, pH, viscosity, rheology, spreadability, globule size, and thermodynamic stability tests. In vitro diffusion tests were performed by Franz diffusion cell. The result showed that microemulsion containing 1 % of caffeine and 5% of grapeseed oil has good physical characteristics and stability with an average globule size 126 ±17 nm. Microemulsion gel system could enhance the cumulative release amount of caffeine through synthetic membrane compared with gel system. Drug release kinetics of caffeine from microemulsion gel system follows the Higuchi model.
In-vitro diffusion study of ibuprofen--cyclodextrin inclusion complex nanogel Fitrianti Darusman; Debby Prihasti Ayustine; Saadiya Noerman; Sani Ega Priani; Widad Aghnia Shalannandia
Pharmaciana Vol 11, No 2 (2021): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | DOI: 10.12928/pharmaciana.v11i2.20024

Abstract

The inclusion complex is one way to enhance active substance solubility, affecting medicine dissolution and penetration. The inclusion complex is formed by utilizing b-cyclodextrin as the host of the active compounds. The Ibuprofen (2-(4-isobutyl-phenyl)propionate) is a propionate acid derivative and classified in class II of the Biopharmaceutic Classification System, which has low dissolutions and high permeability. This study aims to develop a nanogel containing ibuprofen-β-cyclodextrin inclusion complex with the ratio of 1:1, 1:2 and 2:1; and to compare the in-vitro diffusion profile with pure ibuprofen gel. The inclusion complex of ibuprofen-β-cyclodextrin was prepared using the coprecipitation method with the three molar comparison ratio of 1:1, 1:2, and 2:1. The in-vitro study was performed using the gel-based viscolam, comparing the three formulas of ibuprofen-β-cyclodextrin with pure ibuprofen gel. The ibuprofen concentration of each gel tested in the experiment was 1%. The particle size characterization of ibuprofen-β-cyclodextrin inclusion complex gel resulted in having nanoparticle size (510 nm). This characteristic indicates that the inclusion complex gel could enhance the cumulative release amount of ibuprofen compared with pure ibuprofen gel with a relatively smaller particle size (156 nm). Pure ibuprofen and inclusion complex powder size measured to be 763 nm and 957 nm, respectively. The ibuprofen-b-cyclodextrin inclusion complex gel with a molar ratio of 2:1 demonstrated an increase in in-vitro diffusion profile of ibuprofen with a cumulative release amount of 740.3 µg.cm-2. Meanwhile, pure ibuprofen gel had the cumulative release amount of 294.74 µg.cm-2. The gel containing ibuprofen-β-cyclodextrin inclusion complex could enhance the cumulative release amount of ibuprofen compared to pure ibuprofen gel. The ibuprofen-β-cyclodextrin inclusion complex gel at a ratio of 2:1 exhibited an increase in the diffusion of ibuprofen in-vitro.
Pengaruh Jenis Penyalut Terhadap Stabilitas Likopen Dalam Bentuk Sediaan Mikrokapsul Amila, Amila; Hadiansyah, Cepy; Fazriah, Yukeu; Darusman, Fitrianti; Topik, Indra
Indonesian Journal of Pharmaceutical Science and Technology Vol 3, No 3 (2016)
Publisher : Indonesian Journal of Pharmaceutical Science and Technology

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (308.673 KB) | DOI: 10.15416/ijpst.v3i3.9558

Abstract

Berbagai penelitian membuktikan bahwa likopen dapat menurunkan resiko berbagai penyakit seperti gangguan kardiovaskular, diabetes,  hiperkolesterolemia dan kanker. Akan tetapi, likopen sangat mudah mengalami reaksi isomerisasi dan oksidasi selama proses pengolahan maupun penyimpanan karena memiliki banyak ikatan tak jenuh, sehingga aktivitasnya jadi menurun. Oleh sebab itu, untuk meningkatkan stabilitas likopen dilakukan teknik mikroenkapsulasi. Tujuan dari penelitan ini adalah mengetahui pengaruh jenis penyalut terhadap stabilitas likopen hasil mikroenkapsulsi dengan metode spray dry. Jenis penyalut yang digunakan adalah Hidroksi propil β-siklodekstrin (M1) dan kombinasi Whey protein-Maltodekstrin (M2). Mikrokapsul yang diperoleh dievaluasi meliputi Efisiensi Enkapsulasi (EE), kandungan lembab dan sifat organolpetis, lalu dilanjutkan dengan pengujian stabilitas pada suhu kamar dengan dua kondisi yang berbeda yaitu  terpapar cahaya dan tidak terpapar cahaya. Hasil evaluasi menunjukan nilai EE untuk M1 dan M2 adalah 7,6 % dan 8,2 %, Kandungan lembab 5,4 % (M1) dan 5,09% (M2), dan semua formula menunjukan sifat organolpetis yang hampir sama yaitu berbentuk serbuk berwarna jingga dengan bau khas. Hasil uji stablitas menunjukan bahwa baik M1 maupun M2 tidak mengalami penurunan kadar selama 4 minggu penyimpanan pada tempat tidak terpapar cahaya, sedangkan pembanding dalam bentuk serbuk likopen bebas mengalami penurunan kadar sebesar 40,9%. Pada penyimpanan terpapar cahaya M1 dan M2 mengalami penurunan kadar masing masing sebesar 48,7% dan 43,37%, sedangkan pembanding 96,75%. Kesimpulan yang didapat adalah bahwa kedua jenis penyalut tidak mempengaruhi stabilitas likopen dalam bentuk mikrokapsul. 
Peningkatan Kelarutan dan Laju Disolusi Glimepirid Melalui Metode Kokristalisasi Mauludin, Rachmat; Soewandhi, Sundani N; Darusman, Fitrianti
Indonesian Journal of Pharmaceutical Science and Technology Vol 4, No 1 (2017)
Publisher : Indonesian Journal of Pharmaceutical Science and Technology

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (1448.815 KB) | DOI: 10.15416/ijpst.v4i1.9008

Abstract

Telah dilakukan kokristalisasi glimepirid (GMP) dengan asam oksalat (AO) menggunakan metode penggilingan dan pelarutan (menggunakan pelarut aseton). Diagram fase sistem biner GMP-AO digunakan untuk identifikasi awal pembentukan interaksi antar kedua komponen serta ditegaskan kembali dengan analisis mikroskopik menggunakan alat pemanas (hot stage) yang dihubungkan dengan mikroskop polarisasi. Padatan hasil kokristalisasi dikarakterisasi dengan metode analisis termal (Differential Scanning Calorymetry), difraktometri sinar-X serbuk (Powder X-Ray Diffraction), spektrofotometri inframerah (Fourier Transform-Infra Red) dan mikroskopi (Scanning Electron Microscope). Hasil identifikasi dan karakterisasi menunjukkan interaksi eutektik antara kedua fase kristalin GMP-AO dalam keadaan padat pada perbandingan molar 3:7, dengan titik eutektik pada temperatur 128,7°C. Selanjutnya, uji kelarutan dan laju disolusinya menggunakan media dapar fosfat pH 7,4. Kelarutan dan laju disolusi GMP hasil kokristalisasi meningkat dibandingkan dengan campuran fisika dan senyawa tunggalnya.Kata kunci : glimepirid, kokristalisasi, eutektik, kelarutan dan laju disolusi.
Penentuan Parameter Termodinamika Pembentukan Kompleks Inklusi Glimepirid-Betasiklodekstrin Darusman, Fitrianti; Rahayu, Endah
Indonesian Journal of Pharmaceutical Science and Technology Vol 4, No 3 (2017)
Publisher : Indonesian Journal of Pharmaceutical Science and Technology

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (327.298 KB) | DOI: 10.15416/ijpst.v4i3.13858

Abstract

Glimepirid merupakan obat antidiabetika oral golongan sulfonilurea generasi ketiga yang termasuk dalam Biopharmaceutical Classification System (BCS) kelas II dengan sifat kelarutan praktis tidak larut dalam air sehingga dapat ditingkatkan kelarutannya dengan pembentukan kompleks inklusi menggunakan senyawa turunan siklodekstrin yaitu betasiklodekstrin yang memiliki rongga toroidal dengan bagian dalam bersifat hidrofobik dan bagian luar bersifat hidrofilik. Penelitian ini dilakukan untuk menentukan harga tetapan stabilitas kompleks berdasarkan parameter termodinamika (ΔH, ΔG, dan ΔS) pada proses pembentukan kompleks inklusi glimepirid-betasiklodekstrin. Penelitian dilakukan dalam dapar asetat pH 6,2 dan dapar fosfat pH 7,4 pada suhu 32°, 37° dan 42°C. Hasil penelitian menunjukkan bahwa glimepirid dapat berinteraksi membentuk kompleks inklusi dengan betasiklodekstrin. Interaksi antara glimepirid dengan betasiklodekstrin pada pH 6,2 berlangsung secara eksotermik (ΔH<0), proses terjadi secara spontan (ΔG<0) dan terjadi peningkatan ketidakteraturan sistem (ΔS positif). Pada pH 7,4 interaksi berlangsung secara eksotermik, proses terjadi secara spontan (ΔG<0) dan terjadi penurunan ketidakteraturan sistem (ΔS negatif).Kata kunci : glimepirid, betasiklodesktrin, kompleks inklusi, termodinamika.
Formulation self nano emulsifying drug delivery system glimepiride using oleic acid as oil phase Nurrayyan, Nurrayyan; Priani, Sani Ega; Darusman, Fitrianti
Pharmaciana Vol 7, No 2 (2017): Pharmaciana
Publisher : Universitas Ahmad Dahlan

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (357.782 KB) | DOI: 10.12928/pharmaciana.v7i2.7387

Abstract

Glimepiride is a third generation sulphonylurea antidiabetic drug. Glimepiride is poorly water soluble drug that may cause poor dissolution and unpredicted bioavailability. Self nanoemulsifying drug delivery systems (SNEDDS) have become a popular formulation option as nanocarriers for poorly water-soluble drugs. The objective of this research was to develop SNEDDS formulation of glimepiride to improve oral dissolution and bioavailability. Glimepiride SNEDDS  was formulated using oleic acid as oil phase, tween 80 as surfactant, and transcutol as co-surfactant due to their higher solubilization effect. The formulated SNEDDS were evaluated for % transmittance, dispersibility, thermodynamic stability, dissolution, globule size and morphology analysis. The results showed that the glimepiride SNEDDS was rapidly formed clear emulsion and stabile based on thermodynamic test. Transmission electron microscopy demonstrated the spherical droplets morphology in nanometer range. The globule average diameter size was 45 nm. The SNEDDS formulation significantly increase dissolution of glimepiride compared with pure drug.