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Peningkatan Laju Disolusi Ketokonazol Dengan Teknik Dispersi Padat Asyarie, Sukmadjaja; Mauludin, Rachmat; Utami, Ratna A.; Narsa, Angga Cipta
Acta Pharmaceutica Indonesia Vol 38, No 4 (2013)
Publisher : School of Pharmacy Institut Teknologi Bandung

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

Abstract

Ketokonazol merupakan zat antijamur sintetik golongan azol yang merupakan turunan imidazol. Ketokonazol praktis tidak larut dalam air dan ketersediaan hayati melalui rute oral sangat beragam tergantung dari kondisi pH saluran pencernaan. Penelitian ini bertujuan untuk meningkatkan kelarutan dan laju disolusi ketokonazol dengan cara pembuatan dispersi padat mengunakan Eudragit® E 100, PEG 6000, serta gliserol. Dispersi padat di evaluasi dengan uji kelarutan, uji disolusi, kristalinitas, dan morfologinya. Uji disolusi juga dilakukan pada tablet yang mengandung dispersi padat. Formula terbaik yang diperoleh pada penelitian ini dengan peningkatan kelarutan tertinggi dihasilkan oleh dispersi padat dengan perbandingan ketokonazol - Eudragit® E 100 - gliserol (1:8:0,5). Hasil uji disolusi ketokonazol murni, dispersi padat ketokonazol - Eudragit® E 100 - gliserol 1:8:0,5 dan campuran fisiknya dalam media dapar fosfat pH 6,8 selama 360 menit secara berurutan yaitu 22,88, 28,41 dan 58,71%. Terjadi peningkatan persen terdisolusi pada campuran fisik dan dispersi padatnya dengan persen terdisolusi terbesar ditunjukkan oleh dispersi padatnya. Uji disolusi juga dilakukan pada sediaan tablet yang mengandung dispersi padat formula optimum dan campuran fisiknya yang dibuat dengan metode kempa langsung. Sediaan tablet yang mengandung dispersi padat juga menunjukkan peningkatan persen terdisolusi. Pengujian difraksi sinar-X menunjukkan adanya perubahan kristalinitas ketokonazol yaitu sama seperti Eudragit® E 100. Hasil ini juga didukung oleh hasil pengujian spetkrofotometer infra merah dan puncak endotermik differential scanning calorimetry. Berdasarkan hasil scanning electron microscopy terlihat morfologi dari Eudragit® E 100 murni dan dispersi padatnya yang hampir sama. Proses tabletasi mempengaruhi disolusi dispersi padat sehingga terjadi penurunan jumlah yang terdisolusinya. Pembentukan dispersi padat ketokonazol dengan Eudragit® E 100 dan gliserol dapat meningkatkan kelarutan dan disolusi ketokonazol. Pembuatan dispersi padat yang dilakukan tidak efektif untuk meningkatkan disolusi ketokonazol dari sediaan tablet.Kata Kunci: ketokonazol, dispersi padat, Eudragit® E 100.AbstractKetoconazole is an antifungal azole synthetic which derivatived from imidazole. Ketoconazole is practically insoluble in water and its bioavailability depend on pH condition of the gastrointestinal tract. The purpose of the research is to increase the solubility and dissolution rate of ketoconazole by solid dispersion method using Eudragit® E 100, PEG 6000, and glycerol. Solid dispersion was evaluated with respect to solubility, dissolution rate, cristalinity and morphology of solid dispersion. Dissolution test was also performed on tablets loaded solid dispersion. The optimum formulation with the highest solubility was resulted by solid dispersion with ratio ketoconazole - Eudragit® E 100 - glycerol of 1:8:0.5. Dissolution test was performed by pure ketoconazole, solid dispersion, and its physical mixture in medium of phosphate buffer pH of 6.8 within 360 minutes. The significant increasing of dissolution test was shown by the solid dispersion 58.71% ketoconazole was released. Dissolution test was also performed on tablets loaded solid dispersion and loaded physical mixture. Tablets were produced by direct compression method. Solid dispersion tablet showed improved dissolution rate. X-ray diffraction test revealed the change of crystalline ketoconazole and similar to Eudragit® E 100. This result was also supported by spectrum of infrared and endothermic peak of differential scanning calorimetry. Based on scanning electron microscopy morphology of pure Eudragit® E 100 and solid dispersion was similar. Tabletation process reduced dissolution rate of ketoconazole. Solid dispersion of ketoconazole with Eudragit® E 100 and glycerol improved solubilty and dissolution rate.Keywords: ketoconazole, solid dispersion, Eudragit® E 100.
Peningkatan Laju Disolusi Ketokonazol Dengan Teknik Dispersi Padat Sukmadjaja Asyarie; Rachmat Mauludin; Ratna A. Utami; Angga Cipta Narsa
Acta Pharmaceutica Indonesia Vol. 38 No. 4 (2013)
Publisher : School of Pharmacy Institut Teknologi Bandung

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

Abstract

Ketokonazol merupakan zat antijamur sintetik golongan azol yang merupakan turunan imidazol. Ketokonazol praktis tidak larut dalam air dan ketersediaan hayati melalui rute oral sangat beragam tergantung dari kondisi pH saluran pencernaan. Penelitian ini bertujuan untuk meningkatkan kelarutan dan laju disolusi ketokonazol dengan cara pembuatan dispersi padat mengunakan Eudragit® E 100, PEG 6000, serta gliserol. Dispersi padat di evaluasi dengan uji kelarutan, uji disolusi, kristalinitas, dan morfologinya. Uji disolusi juga dilakukan pada tablet yang mengandung dispersi padat. Formula terbaik yang diperoleh pada penelitian ini dengan peningkatan kelarutan tertinggi dihasilkan oleh dispersi padat dengan perbandingan ketokonazol - Eudragit® E 100 - gliserol (1:8:0,5). Hasil uji disolusi ketokonazol murni, dispersi padat ketokonazol - Eudragit® E 100 - gliserol 1:8:0,5 dan campuran fisiknya dalam media dapar fosfat pH 6,8 selama 360 menit secara berurutan yaitu 22,88, 28,41 dan 58,71%. Terjadi peningkatan persen terdisolusi pada campuran fisik dan dispersi padatnya dengan persen terdisolusi terbesar ditunjukkan oleh dispersi padatnya. Uji disolusi juga dilakukan pada sediaan tablet yang mengandung dispersi padat formula optimum dan campuran fisiknya yang dibuat dengan metode kempa langsung. Sediaan tablet yang mengandung dispersi padat juga menunjukkan peningkatan persen terdisolusi. Pengujian difraksi sinar-X menunjukkan adanya perubahan kristalinitas ketokonazol yaitu sama seperti Eudragit® E 100. Hasil ini juga didukung oleh hasil pengujian spetkrofotometer infra merah dan puncak endotermik differential scanning calorimetry. Berdasarkan hasil scanning electron microscopy terlihat morfologi dari Eudragit® E 100 murni dan dispersi padatnya yang hampir sama. Proses tabletasi mempengaruhi disolusi dispersi padat sehingga terjadi penurunan jumlah yang terdisolusinya. Pembentukan dispersi padat ketokonazol dengan Eudragit® E 100 dan gliserol dapat meningkatkan kelarutan dan disolusi ketokonazol. Pembuatan dispersi padat yang dilakukan tidak efektif untuk meningkatkan disolusi ketokonazol dari sediaan tablet.Kata Kunci: ketokonazol, dispersi padat, Eudragit® E 100.AbstractKetoconazole is an antifungal azole synthetic which derivatived from imidazole. Ketoconazole is practically insoluble in water and its bioavailability depend on pH condition of the gastrointestinal tract. The purpose of the research is to increase the solubility and dissolution rate of ketoconazole by solid dispersion method using Eudragit® E 100, PEG 6000, and glycerol. Solid dispersion was evaluated with respect to solubility, dissolution rate, cristalinity and morphology of solid dispersion. Dissolution test was also performed on tablets loaded solid dispersion. The optimum formulation with the highest solubility was resulted by solid dispersion with ratio ketoconazole - Eudragit® E 100 - glycerol of 1:8:0.5. Dissolution test was performed by pure ketoconazole, solid dispersion, and its physical mixture in medium of phosphate buffer pH of 6.8 within 360 minutes. The significant increasing of dissolution test was shown by the solid dispersion 58.71% ketoconazole was released. Dissolution test was also performed on tablets loaded solid dispersion and loaded physical mixture. Tablets were produced by direct compression method. Solid dispersion tablet showed improved dissolution rate. X-ray diffraction test revealed the change of crystalline ketoconazole and similar to Eudragit® E 100. This result was also supported by spectrum of infrared and endothermic peak of differential scanning calorimetry. Based on scanning electron microscopy morphology of pure Eudragit® E 100 and solid dispersion was similar. Tabletation process reduced dissolution rate of ketoconazole. Solid dispersion of ketoconazole with Eudragit® E 100 and glycerol improved solubilty and dissolution rate.Keywords: ketoconazole, solid dispersion, Eudragit® E 100.
Formulasi Sediaan Blush Cream dari Ekstrak Biji Kesumba Keling (Bixa orellana (L.)) sebagai Pewarna Alami Kosmetik Nova Mega Handayani; Lisna Meylina; Angga Cipta Narsa
Proceeding of Mulawarman Pharmaceuticals Conferences Vol. 10 (2019): Proceeding of Mulawarman Pharmaceuticals Conferences
Publisher : Fakultas Farmasi, Universitas Mulawarman, Samarinda, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (395.336 KB) | DOI: 10.25026/mpc.v10i1.376

Abstract

Blush is a type of decorative cosmetics used in the cheek area there used with the aim of adding aesthetic value to the face so that the face looks prettier, fresher and has more dimension. Currently there are many blush preparations on the market that contain hazardous chemicals, then a blush preparation made from kesumba keling seed extract containing bixin as natural coloring is made. The purpose of this study was to formulation and evaluate blush cream preparations by utilizing the acetone and maceration is concentrated with a rotary vacuum evaporator. Blush cream formula made using dyes from kesumba keling seed extract with a concentration of 0.5%, 1%, 2%, and 3% into the chosen base formula that produced color in successive orange-yellowish, soft-orange, dark-orange and orange-brownish color. Evaluations undertaken include organoleptic, homogeneity test, dispersion test, pH test, viscosity test and preferences test. The results obtained are based on parameters test, namely the four formulas enter the required value range. Aseptability test results showed that the preparation of blush cream with a concentration of 2% of the most preferred color of kesumba rivet seed extract and at a concentration of 0.5% was the easiest to spread.
Seleksi Parameter yang Mempengaruhi Sintesis Kalkon dengan Metode Plackett-Burman Indah Silvia Sugiyamin; Harra Ismi Farah; Agung Rahmadani; Angga Cipta Narsa
Proceeding of Mulawarman Pharmaceuticals Conferences Vol. 11 (2020): Proceeding of Mulawarman Pharmaceuticals Conferences
Publisher : Fakultas Farmasi, Universitas Mulawarman, Samarinda, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (347.386 KB) | DOI: 10.25026/mpc.v11i1.385

Abstract

Chalcone is a compound that has various biological activities. The organic synthesis approach has been widely used to obtain chalcone compouds. The aim of this research is to select the main parameters which influence chalcone synthesis. This study was conducted using Plackett-Burman experimental design. Of eleven parameters used, eight of them showed a significant effect on the yield of chalcones namely temperature, reaction time, mole number of benzaldehyde, volume of acetophenone solvent, incubation time, volume of distilled water, volume of benzaldehyde solvent, catalyst volume and dummy. In addition, the highest yield is 32.43%.
Uji Aktivitas Antibakteri Ekstrak Etanol Daun Andong Merah terhadap Eschericia coli dan Staphylococcus aureus Reca Indiyen; Fika Aryati; Angga Cipta Narsa
Proceeding of Mulawarman Pharmaceuticals Conferences Vol. 11 (2020): Proceeding of Mulawarman Pharmaceuticals Conferences
Publisher : Fakultas Farmasi, Universitas Mulawarman, Samarinda, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (442.396 KB) | DOI: 10.25026/mpc.v11i1.388

Abstract

Infection disease is one of the most common diseases in the world. Infection can be caused by bacteria Escherichia coli and Staphylococcus aureus which are now resistant to some antibiotics, so new agents are needed to overcome antibiotic resistance. Red andong leaves are empirically efficacious for treating wounds, hemorrhoids, inflammation, diarrhea and stopping bleeding (hemostasis). This study aims to determine the yield of ethanol extracts red andong leaves and determine the antibacterial activity of ethanol extracts of red andong leaves against Escherichia coli and Staphylococcus aureus. The research began with the process of extracting red andong leaves by maceration method, then carried out antibacterial testing by the well diffusion method. The results showed the extract concentrations of 10%, 30%, and 50% were able to inhibit the growth of Escherichia coli and Staphylococcus aureus. The biggest antibacterial activity of red andong extract was obtained at a concentration of 50% with a inhibition zone of 17,836 mm (Staphylococcus aureus) and 9,012 mm (Escherichia coli).
Kajian Literatur: Aktivitas Antibakteri Ekstrak Herba Suruhan (Peperomia pellucida L.) Ayu Rahmawatiani; Dewi Mayasari; Angga Cipta Narsa
Proceeding of Mulawarman Pharmaceuticals Conferences Vol. 12 (2020): Proceeding of Mulawarman Pharmaceuticals Conferences
Publisher : Fakultas Farmasi, Universitas Mulawarman, Samarinda, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (197.057 KB) | DOI: 10.25026/mpc.v12i1.401

Abstract

Suruhan (Peperomia Pellucida L.) is one of the weed plants that grow wild in humid environments. This plant is commonly found in Indonesia and has been used by the community as a medicinal plant. The secondary metabolites contained oh suruhan are saponins, phenols, flavonoids, and tannins. These compounds are thought to provide antibacterial activity. The purpose of writing this literature review is to determine the compound of secondary metabolites, the antibacterial activity of the extract, and the effective concentration as an antibacterial agent. The method used is literature review by searching journals database with the Google Scholar, PubMed, and Scient Direct. Based on the literature review, the secondary metabolites contained are flavonoids, tannins, steroids, phenols, saponins, glycosides, anterquinone, pellucidin A, stigmasterol, and fucosterol. The antibacterial activity test showed that the extract was able to inhibit gram-positive bacteria such as Bacillus subtilis, Propionibacterium acne, and Staphylococcus aureus, as well as gram-negative bacteria, such as Klebsiella pneumoniae, Shigella dysentriae, Pseudomonas aeruginosa, Pseudomonas fluoescens, Escherichia coli, and Salmonella typhi. The activity produced by gram-negative bacteria is more sensitive than gram-positive bacteria. While the effective concentrations of n-hexane extract against gram-positive and gram-negative bacteria were 10 mg/mL and 200 mg/L, the resulting inhibition zone diameters were 17.9 mm and 18 mm.
Literature Review: Aktivitas Kulit Jeruk dalam Bidang Farmasi Ayu Wulan Dari; Angga Cipta Narsa; Nur Masyithah Zamruddin
Proceeding of Mulawarman Pharmaceuticals Conferences Vol. 12 (2020): Proceeding of Mulawarman Pharmaceuticals Conferences
Publisher : Fakultas Farmasi, Universitas Mulawarman, Samarinda, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (369.333 KB) | DOI: 10.25026/mpc.v12i1.417

Abstract

Jeruk manis (Citrus sinensis (L.) Osbeck) adalah buah yang ditanam diiklim tropis ataupun subtropis dan termasuk komoditas buah penting dipasaran baik didalam negeri maupun dunia. Banyaknya permintaan jeruk ini mengakibatkan tingginya jumlah limbah kulit jeruk di Indonesia yang mencapai 309.678 ton pertahun. Kulit buah jeruk biasanya hanya dibuang dan tidak dimanfaatkan dan menjadi sampah yang tidak ada manfaatnya. Tujuan penulisan artikel ini yaitu untuk mengetahui kandungan senyawa metabolit sekunder, aktivitas farmakologis, dan bentuk sediaan yang telah dibuat dari kulit jeruk manis. Metode yang digunakan yaitu studi literaturdengan penelusuran jurnal dan karya tulis ilmiah dengan database Google Scholar, Sematic Scholar, Science Direct, dan Wiley Online Library. Berdasarkan kajian literatur diketahui bahwa kandungan senyawa metabolit sekunder kulit jeruk manis yaitu flavonoid, alkaloid, tanin, glikosida, steroid, karbohidrat, pektin, senyawa fenolik, kumarin, glikosida, saponin, dan terpenoid. Diketahui aktivitas farmakologis pada kulit jeruk manis yaitu sebagai antibakteri (senyawa 1,8-cineole, d-limonene, 5-C-glycosyl flavones: lucenin-2, vicenin-2, stellarin-2, lucenin-2-41- methyl ether and scoparin; one 3-hydroxy-3-methylglutaryl glycolsyl, flavonol: 3-hydroxy-3-methyl-glutaryl glycosyl quercetin), antijamur (senyawa limonene, ?-pinene, ?-pinene, dan ?-myrcere), antioksidan (senyawa neohesperidin, hesperidin, 5-C-glycosyl flavornes: lucenin-2,vicenin-2, stellarin-2, lucenin-2-41- methyl ether and scoparin; one 3-hydroxy-3 methylglutaryl glycosylflavonol: 3-hydroxy-3-methylglutaryl glycosyl quercetin; and one flavone O-glycosides: chrysoeriol7-O-neoesperidoside dan komponen fenolik yaitu polymethoxylated flavones, O-glycosylated flavones, C-glycosylated flavones, O-glycosylated flavonols, O-glycosylated flavanones (glycosylated flavonones), insektisda (senyawa flavonoid, d-limonene, limonoid, saponin, dan tanin), tabir surya (senyawa antranilat dan hesperidin), peluruh steroform (senyawa limonene), antidiabetes (senyawa flavonoid), antikolesterol (senyawa flavonoid dan pektin) dan penyembuh luka (senyawa hesperidine, PMF, limonene, vitamin A, vitamin C , dan vitamin E). Serta bentuk sediaan yang telah dibuat dari kulit jeruk manis yaitu berupa masker peel-off sebagai antibakteri, masker gel sebagai antioksidan, tablet hisap sebagai vitamin C, sabun mandi cair sebagai antioksidan, serta gel untuk penyembuhan luka.
Aktivitas Antibakteri Ektrak Batang Bagore (Caesalpinia bonduc (L.) ROXB): Antibacterial Activity of Bagore Stem Extract (Caesalpinia bonduc (L.) ROXB) Muhammad Fauzi Zainal Abidin; Risna Agustina; Angga Cipta Narsa
Proceeding of Mulawarman Pharmaceuticals Conferences Vol. 13 (2021): Proc. Mul. Pharm. Conf.
Publisher : Fakultas Farmasi, Universitas Mulawarman, Samarinda, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (284.953 KB) | DOI: 10.25026/mpc.v13i1.454

Abstract

Bagore (Caesalpiniabonduc (L.) Roxb) from the Febaceae / caesalpiniaceae family is a thorny shrub. This plant is reported to have some activity and also has metabolites of alkaloids, flavonoids, saponins, tannins and triterpenoids. The purpose of this study was to determine the antibacterial activity of bagore stem extract. The extraction method used is the maceration method using ethanol solvent and the yield of 5.5% bagore stem extract followed by the determination of secondary metabolites. The stem extract was found to have positive results of flavanoid and saponin compounds which have antibacterial activity. Testing for the inhibition of Streptococcus aureus and Propionibacterium acnes as gram-positive bacteria and Escherichia coli as gram-negative bacteria using the well diffusion method. The extract concentrations used were 10%, 20%, and 30%, and the negative control used water and ethanol. the results of antibacterial tests against Streptococcus aureus bacteria obtained the respective inhibition zone diameters; 11,836 mm; 13,671 mm and for Propionibacterium acnes bacteria obtained the diameter of the inhibition zone for each success; 10,781 mm; 13,169 mm; 14,190 mm, while the Escherichia coli bacteria obtained the respective inhibition zone diameter; 10,552 mm; 13,436 mm; 14,036 mm
Penambatan Molekuler Senyawa Metabolit Sekunder Bawang Dayak (Eleutherine bulbosa) Sebagai Penghambat Dipeptidil Peptidase IV (DPP-4): Molecular Binding of Secondary Metabolite Compounds of Dayak Onion (Eleutherine bulbosa) As Dipeptidyl Peptidase IV (DPP-4) Inhibitors Nur Ainah; Mukti Priastomo; Angga Cipta Narsa
Proceeding of Mulawarman Pharmaceuticals Conferences Vol. 13 (2021): Proc. Mul. Pharm. Conf.
Publisher : Fakultas Farmasi, Universitas Mulawarman, Samarinda, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (354.191 KB) | DOI: 10.25026/mpc.v13i1.458

Abstract

Diabetes is a frightening disease that threatens people's lives, because almost every 10 seconds in the world, people die from complications of this disease. A new DM treatment approach in the creatinase system that inhibits dipeptidyl peptidase IV (Dpp-4) has been developed, and has been shown to effectively increase insulin secretion, maintain pancreatic -integration, and slow gastric emptying. antidiabetic, namely inhibition of the -glucosidase enzyme in one of its compounds and has not been found to inhibit the Dpp-4 enzyme. This study aims to determine the potential of the compounds in Dayak onions as inhibitors of the Dpp-4 enzyme. The method used is molecular anchoring or in silico because the research time is short and the cost is cheaper than in vitro or in vivo. The software used is autodock which is a device that can attach ligand molecules to receptor macromolecules. Then visualized using discovery studio 2020 and other devices to support tethering such as chemdraw and chimera 1.4. vidagliptin as an antidiabetic which has activity against inhibiting Dpp-4 inhibitors was used as a standard. The grid is placed on natural ligands with a box size of 52? x 28? x 26? and a center of 40,926? x 50,522? x 35,031? with a spacing of 0.375?. Based on the docking that has been done, the secondary metabolite compounds in Dayak onions have a low bond energy value, with the lowest value being -8.46 kcal/mol and the highest -5.54 with different values of inhibition constant and bond form. Eleuthoside C has the lowest bond energy of -8.46 and has the most similar interaction with natural ligands. The bond that occurs is the type of hydrogen bonding at the residues of Phe357, Arg125, Arg358, Tyr666, Tyr662, and Glu205. With this, Dayak onions have antidiabetic activity but further docking still needs to be done to see other compounds in Dayak onions as Dpp-4 inhibitors.
Optimasi Basis Sabun Padat Transparan Menggunakan Minyak Zaitun dan Pengaruh Konsentrasi Sukrosa Terhadap Transparansi Sabun: Optimization of Transparent Solid Soap Base Using Olive Oil and the Effect of Sucrose Concentration on Soap Transparency Risma Dwi Novianti; Wisnu Cahyo Prabowo; Angga Cipta Narsa
Proceeding of Mulawarman Pharmaceuticals Conferences Vol. 13 (2021): Proc. Mul. Pharm. Conf.
Publisher : Fakultas Farmasi, Universitas Mulawarman, Samarinda, Indonesia

Show Abstract | Download Original | Original Source | Check in Google Scholar | Full PDF (326.312 KB) | DOI: 10.25026/mpc.v13i1.461

Abstract

Transparent solid soap has a luxurious, classy, and attractive appearance so it is often sold as a souvenir which is relatively expensive but still has a unique and exclusive appearance. In the process of making transparent soap, sugar (sucrose) functions to form transparency on the soap. Olive oil is one of the potential raw materials for soap making because it has a high content of oleic acid which is good for skin health. This study aims to formulate a transparent solid soap based on raw materials of olive oil and lintut leaf essential oil that meets the characteristics of transparent solid soap and soap quality requirements in accordance with SNI (1994). Sucrose as a transparent agent for soap is concentrated into 14%, 18%, and 22%. Then the base optimization was carried out by varying olive oil and 30% NaOH in three formulations. The results showed that the sucrose concentration was 22% which resulted in the most transparent preparation. Then the evaluation of base optimization shows that all formulas have good characteristics and only formula 2 (18% olive oil and 12% NaOH) fulfills all the soap quality requirements according to SNI (1994).