Sistem Penghantaran Obat Melewati Barrier Darah Otak

Brain barrier is effective barrier in drug delivery to brain. For effectiveness drug deliveryneed be desaigned a delivery with nanoparticle technology. Nanoparticles are solid colloidalparticles ranging in size from 1 to 1000 nm that are utilized as drug delivery agents. The primaryadvantages of nanoparticle carrier technology is that nanoparticles mask the blood – brain barrierlimiting characteristics of the therapeutic drug molecule. Furthermore, this system may slow drugrelease in the brain, decreasing peripheral toxicity. The method which elaboration in manufacturenanoparticles are emulsion polimerization, interfacial polimerization, desolvation evaporation andsolvent deposition. Currently, report evaluating nanoparticles for brain delivery have studiedanesthetic and chemoterapeutic agent. These studies are reviewed for efficacy and mechanisms oftransport. Physiological factors such as phagocytic activity of the reticuloendothelial system andprotein opsonization may limit the amount of brain delivered drug. Nanoparticle technology appearsto have significant promise in delivering therapeutic molecules across the blood-brain barrier

Preformulasi Sediaan Furoseivhda Mudah Larut: A Preformulation of a Water Soluble Furosemide Dosage Form

Sistem dispersi padat furosemida yang sukar larut dalam air dan polivinilpirolidon disiapkan melalui metode pelarut dengan perbandingan 1 : 11 : 31 : 51 : 7 dan 1 : 9 dalam upaya meningkatkan kelarutan dan disolusi furosemida. Peningkatan kelarutan furosemida dilakukan dengan metode kelarutan menggunakan shaking waterbath. Uji kelarutan memperlihatkan bahwa PVP dengan berbagai kadar dan pada suhu yang berbeda meningkatkan kelarutan furosemida secara bermakna (P < 0,05). . Uji disolusi sistem dispersi padat furosemida dilakukan menggunakan alat disolusi dengan kecepatan putar 50 rpm. Kadar furosemida terlarut ditentukan secara spektrofotometri UV. Uji ini memperlihatkan peningkatan jumlah furosemida yang terlarut secara bennakna (P < 0,05), tetapi tedadi penundaan waktu pelepasan awal. !Cab\u27 Kunci : dispersi padat, kelarutan, disolusi, furosemida. ABSTRACT Solid dispersion system of water-insoluble furosemide in polyvinylpirolidon (PVP) was prepared by a solvent method in various ratios of 1 : 1, 1 : 3, I : 5, 1 : 7 and 1 : 9 of the drug and PVP, respectively in order to improve furosemide solubility and dissolution. The improvement of furosemide solubility was studied by a solubility method in a shaking waterbath. The solubility test showed that various concentrations of PVP and temperature gave statistically significant increased of furosemida solubility (P < 0,05). The dissolution study of furosemide solid dispersion system was done using a dissolution tester at the rotation rate of 50 rpm. Furosemide concentration released was determined spectrophotometrically using a UV spectrofometer. This test showed a significant increased of furosemida solubility (P < 0,05), but with a prolonged of releasing time. Key Word : solid dispersion, solubility, dissolution, bioavailability

A COMPARATIVE BIOAVAILABILITY OF FUROSEMIDE IN SOLID DISPERSIONS FORMS

Furosemide is a poorly soluble diuretic drug, the solubility of which can be enhanced by solid dispersion with polyvinylpirolidon (PVP). The solid dispersion system was prepared by a solvent method in various ratios of 1 : 5 and 1 : 7 of the drug and PVP, respectively, in order to improve furosemide bioavailability. The bioavailability of furosemide - PVP solid dispersion was compared with pure furosemide (control) and Lasix (reference). The study was done in a cross over design with a single-dose peroral that administered to the white male rabbits (n = 6). Furosemide blood levels were determined spectrofluorometrically by an extraction method. The area under the blood concentration-time curve AUC0 - , peak blood concentration Cmax and time to reach peak blood concentration Tmax were used to compare their bioavailabilities. The solid dispersion systems produced a higher extent of bioavailability than pure furosemide (P &lt; 0,05). On the contrary, no statistically significant difference about the extent of bioavailability between solid dispersion and Lasix (P &gt; 0,05). Finally, furosemide – PVP solid dispersion (1 : 7) was the best formulation with the highest extent of bioavailability and bioequivalence with the Lasix formula.Key Word : Solid dispersion, solubility, dissolution, bioavailability, furosemide

Characterization and dissolution studies of Furosemide solid dispersions using polyethylene glycol (PEG), talc and PEG-talc as dispersion carriers

Solid dispersions of furosemide were prepared by melting and solvent methods using polyethylene glycol (PEG) 6000, talc and PEG – talc as dispersion carrier in order to improve furosemide dissolution. The increase of dissolution and physical properties of its powder was evaluated. Only furosemide solid dispersions with combination of PEG – talc 1 : 3 showed a good physical properties. The assay of the effect of PEG – talc ratio on furosemide dissolution showed that the increase of ratio of PEG – talc increased significantly dissolution rate.Key Word : furosemide, solid dispersion, dissolutio

A Preformulation of a Water Soluble Furosemide Dosage Form

Solid dispersion system of water-insoluble furosemide in polyvinylpirolidon (PVP) was prepared by a solvent method in various ratios of 1 : 1, 1 : 3, 1 : 5, 1 : 7 and 1 : 9 of the drug and PVP, respectively in order to improve furosemide solubility and dissolution. The improvement of furosemide solubility was studied by a solubility method in a shaking waterbath. The solubility test showed that various concentrations of PVP and temperature gave statistically significant increased of furosemida solubility (P &lt; 0,05). The dissolution study of furosemide solid dispersion system was done using a dissolution tester at the rotation rate of 50 rpm. Furosemide concentration released was determined spectrophotometrically using a UV spectrofometer. This test showed a significant increased of furosemida solubility (P &lt; 0,05), but with a prolonged of releasing time.Key Word : solid dispersion, solubility, dissolution, bioavailability

Gold Nanoparticles with Natural Ingredients as Anti-Aging: A Systematic Review

Aging is a natural process characterized by physiological skin changes. It starts to appear when individuals are in their thirties, making it necessary to use anti-aging products with natural ingredients which are safe even though the penetration is relatively low into the skin. Natural ingredients that can be used are antioxidants that can inhibit aging and can act as bioreductants on gold nanoparticles. Gold nanoparticles can increase penetration into the target cells because of their small size with large surface area. This review article aimed to collect data relating to the development of gold nanoparticles with natural ingredients as anti-aging agents. This review searched through the PubMed and ScienceDirect databases with such keywords as aging, anti-aging, plant extract, antioxidants, and gold nanoparticles. The inclusion criteria were articles in English, available in a full-text version, and published in the last 10 years. Research on the use of natural ingredients as anti-aging agents found that natural ingredients perform better than chemical comparators. Gold nanoparticles are also reported to have been widely used in anti-aging products. Their activity is even better given the low IC50 value and a higher percentage of inhibition compared to those of the extracts without nanoparticle modification. It is reported that gold nanoparticles with natural ingredients as anti-aging agents have a better effect as opposed to purely natural ingredients

Ketersediaan hayati relatif furosemida dalam bentuk dispersi padat =Comparative Bio availability Furosemide in Solid Dispersion Forms

ABSTRACT Solid dispersion system of water-insoluble furosemide in polyvinylpirolidon (PVP) was prepared by a solvent method in various ratios of 1 : 5 and 1 : 7 of the drug and PVP, respectively in order to improve furosemide bioavailability. The bioavailability of furosemide - PVP solid dispersion was compared with pure furosemide (control) and Lasix® (reference). The study was done in a cross over design with a single-dose peroral that administered to the white male rabbits (n = 6). Furosemide blood levels were determined spectrofluorometrically by an extraction method. The area under the blood concentration-time curve AUC0 y peak blood concentration Cmax and time to reach peak blood concentration Tmax were used to compare their bioavailabilities. The solid dispersion systems produced a higher extent of bioavailability than pure furosemide (P 0,05). Finally, furosemide - PVP solid dispersion (1: 7) was the best formulation with the highest extent of bioavailability and bioequivalence with the Lasix® formula\u27s. Keywords: solid dispersion - solubility - dissolution - bioavailability -furosemide

PENAPISAN SENYAWA BIOAKTIF ANTIOKSIDAN DAN ANTIKANKER DARI BUAH NAGA SERTA FORMULASI TABLET EKSTRAKNYA SEBAGAI OBAT HERBAL TERSTANDAR ANTIKANKER

Isolation of bioactive compound from dragon fruit have been investigated. The dragon fruit was extracted with methanol and the extract was concentrated using rotary vacuum evaporator. The extract exhibited strong antioxidant activity in DPPH method with IC50 of 192.667 µg/ml, and total phenol in Folin-Ciocalteu method with 246 ppm/1 Kg dry extract. Organoleptic characterization of methanolextract exhibited pasta form, brown, bitter, and aromatics smell. Thin Layer Chromatography (TLC) with silicagel F254 as stationary phase and mix of n-butanol:acetic acid:water (4:1:5) as mobil phase show that there are 4 spot and the first spot contains flavonoid. Dragon fruit extract was formulated into tablets and efferfescent tablets, with the composition of dragon fruit extract, Citric Acid, Tartat acid, sodium bicarbonate, lubricant, Aspartame and fillers. Tablet evaluated the quality of its physical properties, including uniformity bobit, hardness, brittleness and time dissolve, and found that the effervescent tablets of dragon fruit extract to fulfill the requirements qualifies as a good tablet. Isolasi senyawa bioaktif dari buah naga telah diselidiki. Buah naga diekstraksi dengan metanol dan ekstrak dipekatkan dengan rotary evaporator. Ekstrak metanol menunjukkan aktivitas antioksidan yang kuat dalam metode DPPH dengan IC50 sebesar 192,667 mg/ml, dan total fenol dalam metode Folin-Ciocalteu sebesar 246 ppm/1 Kg ekstrak kering. Karakterisasi organoleptik ekstrak metanol menunjukkan bentuk pasta, coklat, pahit, dan bau aromatik. Kromatografi Lapis Tipis (KLT) dengan silicagel F254 sebagai fase diam dan campuran n-butanol: asam asetat: air (4:01:05) sebagai fase mobil menunjukkan bahwa ada 4 spot dan spot pertama positif mengandung flavonoid. Ekstrak buah naga diformulasikan dalam bentuk tablet biasa dan tablet efferfescent, dengan komposisi buah naga ekstrak, Asam sitrat, asam Tartat, natrium bikarbonat, pelumas, Aspartam dan pengisi. Tablet dievaluasi kualitas sifat fisik, meliputi keseragaman bobot, kekerasan, kerapuhan dan waktu larut, dan diketahui bahwa tablet biasa dan tablet effervescent ekstrak buah naga untuk memenuhi persyaratan memenuhi syarat sebagai tablet yang baik

PHYTOCHEMICAL SCREENING AND ANALYSIS POLYPHENOLIC ANTIOXIDANT ACTIVITY OF METHANOLIC EXTRACT OF WHITE DRAGON FRUIT (Hylocereus undatus)

White dragon fruit is a well known and widely used herbal medicine, especially in Asia, which contains several interesting bioactive constituents and possesses health promoting properties. The aim of this study was to analyze for the bioactive compounds, evaluate total phenolic contents and antioxidant capacities of methanolic extract of white dragon fruit. The antioxidant activity was determined by the 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity assay. Total phenolic content were determined by Folin-Ciocalteu method. Phytochemical screening of the white dragon fruit showed the presence of triterpenoid, alkaloid, flavonoid and saponin. The extract exhibited strong antioxidant activity with IC50 of 193 μg/mL, and total phenolic content of 246 μg/mL in 1 Kg dry extract

Effect of Tragacanth as Binding Agents to Ginger (Zingiber Officinale Roxb.) Lozenges

Ginger (Zingiber Officinale Roxb.) is a traditional plants usually used to relieve pain, rheumatism, and neutralize poison. The aim of this study was to get the optimum concentration of tragacanth as a binding agent in ginger lozenges formulation. The components from ginger were extracted using percolation with ethanol 70% and then evaporated using rotary evaporator. Lozenges were made in three formulas ; formula 1 (5%), 2 (7,5%), 3 (10%) of tragacanth using wet granulation method. Granules and tablets were tested for its physical properties, and analyzed using Pearson correlation. The result showed that, all of three formulas were good, comply with a regulation of physical properties and soluble time in the mouth. Variation of tragacanth concentration affected physical properties of tablets. It showed that the greater concentration of tragacanth, the larger the hardness and the longer the soluble time of tablets. The formula (tragacanth 10% b/v) gave an optimum physical properties and soluble time of tablets, with weight variety deviation 0,98%, hardness 10,18 kg, friability 0.11% and soluble time 11.50 minutes. The three formulas were received by respondens with prerequirement of improving sweetness, repairing form and the color of tablets