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Ibuprofen salt production and its application in tablet dosage form
Get PDFIbuprofen is an anti-inflammatory drug and is practically insoluble in water. The low melting point and the poor flowability of ibuprofen can lead to process difficulty in tablets production. The purpose of this research was to make the sodium salt form of ibuprofen which has better solubility in water.Sodium ibuprofen salt was prepared by reacting the ibuprofen and sodium hydroxide, then characterized using TG/DTA, DSC, spectrophotometer UV-VIS, spectrophotometer IR, X-ray diffraction, and SEM. Tablets were prepared by wet granulation method.The characterization result showed that sodium ibuprofen result of the synthesis was dehydrate form with melting point of 199.9 °C. Granules of sodium ibuprofen result of the synthesis had better flowability and bigger density than ibuprofen granules. The physical characterization of the tablet showed that the formula of sodium ibuprofen resulted from the. Sodium ibuprofen showed the higher release rate than ibuprofen so can give quicker onset of action.Key words: sodium ibuprofen, ibuprofen, dissolution
Chemical investigation on Indonesian marine sponge Mycale phyllophila
Get PDFChemical investigation on marine sponge Mycale phyllophila collected from Bali, Indonesia has been performed. This study was aimed to isolate and to identify structures of the sponge secondary metabolites as well as to test their cytotoxic activity on mouse lymphoma cell line L5178Y.The sponge extract was fractionated by liquid-liquid partition followed with a vacuum liquid chromatography method. Structure elucidation was performed on the basis of extensive spectroscopic analysis involving one and two dimensional NMR spectroscopy as well as mass spectrometry. Cytotoxicity was tested on mouse lymphoma cell line L5178Y by using the microculture tetrazolium (MTT) assay. This study found a mixture of 5-pentadecyl-1H-pyrrole-2-carbaldehyde and (6’E)-5-(6’pentadecenyl)-1H-pyrrole-2-carbaldehyde as major constituents of the sponge extract. Those compounds were expected to be the active constituent to show growth inhibition of mouse lymphoma cell line (L5178Y) in vitro.Key words : Mycale phyllophila, cytotoxic agent, NMR spectroscopy
Isolation and identification of eurycomanone from akar pasak bumi (Eurycoma longifolia, Jack) and its antiangiogenic activity
Get PDFPasak bumi is one of the Indonesian original plants having anti cancer activity. One compound of akar pasak bumi, i.e eurycomanone was proven to have cytotoxic effect on cancer cell culture by apoptosis induction on HeLa cells. Therefore, this study was aimed to isolate and identify euycomanone from akar pasak bumi and to look at the anti angiogenic activity of the compounds on corio alantois membrane (CAM) of chicken embryo induced by bFGF.The akar pasak bumi was ground and was macerated with methanol. The macerate was fractioned by mean of VLC. Six fractions was obtained. The second fraction exhibited two spots on a TLC system, one spot was cochromatographed with eurycomanone as the reference standart and another spot exhibited blue fluorecence at 254 nm. This second fraction, then, was chromatographed on a preparative scale TLC to separate isolate A. Anti angiogenic test was performed for Isolate A at concentration series of 5, 10, 15, 20, 40 μg/mL respectively. Egg embrio (8-9 days) were divided into 8 groups. The first group was implanted paper disc only, the second group were given bFGF on Tris HCl buffer and the third group were given bFGF (on Tris HCl buffer) + 0,8 % DMSO. The fourth to eighth group were induced by 10 ng bFGF and the test preparation at the respective concentration. After incubation at 39 °C for 3 days, each egg was opened, the content of each was aspired and discarded, the CAM sticked to its shell was examined macroscopically and microscopically for the formation of new blood vessels.Based on spectral data of UV, IR, 1H NMR, 13C NMR and MS of isolate A and comparison with the spectral data of the standart, the isolate A was eurycomanone. Eurycomanone inhibited angiogenesis at concentration of 10 μg/mL.Key words: antiangiogenic, angiogenesis, E.longifolia, eurycomanone,CAM
Teratogenicity study of combination of ginger rhizome extract and noni fruit extract in Wistar rat
Get PDFGinger (Zingiber officinale Roscoe var. sunti Val.) extract in combination with noni (Morinda citrifolia Linn.) extract has been proven to be effective in tuberculosis patients. To examine its safety in pregnancy condition, the influence of combination of ethanol extract of ginger and ethanol extract of noni fruit had been studied in pregnant Wistar rat. The ginger and noni extract were administered orally at dose level combination of 50 and 50 mg/kg BW , 500 and 500 mg/kg BW , 1000 and 1000 mg/kg BW on day sixth to fifteenth of gestation. The mother was sacrified on day nineteenth of gestation to observe life fetus, resorption, and growfail fetus. One third of the fetuses eviscerated for skeletal staining with alizarin red and two third of the fetuses were hardened with Bouin’s fixation solution. No malformation were found in the eviscerated group. The combination at all doses did not cause any fetus resorption, growth failure and did not cause malformation in organ and skeleton. The combination dose of 500 and 500 as well as 1000 and 1000 mg/kg BW caused dark red to black color in the liver of rat fetuses of 7.3 and 8.3 % respectively.Key words: teratogenicity study, Zingiber officinale Roscoe var. sunti Val, Morinda citrifolia Linn
Assay method validation of triamcinolone acetonide (TA) to support the investigation of TA-loaded nanoparticles
Get PDFThe aim of this study was to develop the valid analytical method which used for the assay of triamcinolone acetonide (TA) in the investigation of TA-loaded nanoparticle formulations. High Performance Liquid Chromatography (HPLC) method was applied in this study by using an Econosil column, C18 10 'm, 250 x 4.6 mm (Alltech Associates Inc, PA, USA) as the stationary phase. The mobile phase consisted of a composition of acetonitrile (ACN) and 20mM phosphate buffer solution (pH 4.2) in the proportion of 50:50 v/v. The HPLC assay of TA was validated for selectivity, linearity, precision, recovery (accuracy), sensitivity and stability of TA during the assay. Results showed that the concentration of TA in the samples can be determined against the standard in the concentration range of calibration curve. The system precision and level of recovery were considered to be acceptable, and the method was selective and sensitive.Key words: triamcinolone acetonide, assay, validatio
The cytotoxic and antiproliferative effects of gamavuton-0 in rat basophilic Leukemia cells
Get PDFGamavuton-0 (GVT-0), also named as 1,5-bis(4’-hydroxy-3’- methoxyphenyl)-1,4-pentadiene-3 one is a 1,5-diphenyl-1,4-pentadiene-3-one analog of curcumin by modifying the center site of curcumin leading to 1,4-pentadiene-3-ones to maintain the hydroxy moiety at aromatic rings which are responsible for its biological activities. Curcumin has been reported to have potent anticarcinogenic effects. Besides, curcumin was found to induce apoptosis in human Leukemia cells. In our study, we investigated the cytotoxic and antiproliferative effects of gamavuton-0 in rat basophilic leukemia cells. Cell viability was determined by WST-1 assay. In brief, tetrazolium salts were cleaved to formazan by cellular enzymes of viable cells, determined by colorimetric methods with a microplate (ELISA) reader at 450 nm.In the present study, we evaluated cytotoxic and proliferative effects of GVT-0 in rat basophilic leukemia cells. In the study, GVT-0 induced rat basophilic leukemia cells death in a dose dependent manner after overnight incubation. GVT-0 also impaired the content of histamine and b-hexoaminidase enzyme in cells. However, the cytotoxic effect of GVT-0 (IC50 : 43,67 mM) was less potent than this of curcumin (IC50 : 29,14 mM). GVT-0 (1 mM) also showed a significant inhibition of cell growth after 48 and 72 hr. Its fact indicates that GVT-0 could prolong the cells doubling time. These results provide useful information to guide the development of new synthetic compounds for the treatment of cancer diseases.Key words : gamavuton-0, curcumin, cancer, cytotoxic, antiproliferative
The effect of mengkudu fruit methanolic extract and methanolic residual fraction on GLUT-4 protein elevation
Get PDFInvestigating in the Diabetes Mellitus drug which one having good activity and tolerance to patients are still in researchers’ concern. One of the main topics now days is the use of mengkudu plants as a traditional medicine of Diabetes Mellitus. This research was aimed to determine the increase of GLUT-4 protein in type 2 Diabetes Mellitus rats after given methanolic extract and methanolic residual of mengkudu fruit. The male rats were diabetic induced with exogenous i.p. insulin for 10 days. After showing hyperglycemic effect, the rats were given orally methanolic extract and methanolic residual fraction of mengkudu fruit for 4 days. On the fifth day, fasting blood glucose was measured and the rats were sacrificed to take the thigh muscle tissue for immunohistochemical calculation. The result showed that methanolic extract and methanolic residual of mengkudu fruit increase the amount of GLUT-4 protein, but can not reduce fasting blood glucose levels of male white rats.Key words : mengkudu fruit (Morinda citrifolia L.), methanolic extract and methanolic residual, type 2 Diabetes Mellitus, GLUT-4 protei
The effect of combination therapy of sulfonylurea, metformin, and acarbose in type 2 diabetes mellitus patients
Get PDFDiabetes mellitus is a complex disorder that involves multiple pathophysiological defects. As the disease progresses, further functional decline in β-cell is apparent. In most cases, patients on oral antidiabetic therapy will require not only an increase in dose, but also the addition of a second or third oral agent. The aim of this study was to evaluate the effectiveness and safety of triple therapy with sulfonylurea, metformin, and acarbose in patients with poorly controlled glycemia. The study design was a prospective observational study in 49 type 2 diabetic patients followed in Department of Endocrinology RSUP Dr Sardjito Indonesia from May 2007 to September 2008. Patients with hypertension were included if their blood pressure was well controlled with antihypertensive medication. All patients with documented gastrointestinal disease were excluded. At baseline and at 3-month intervals, levels of HbA1C, fasting and postprandial plasma glucose, hypoglycemic episodes, and edverse event were evaluated. Fourty nine patients, 22 men and 27 women, aged 62.84 +7.85 years, diabetes duration of 11.92 +6.09 years were studied. The initial HbA1C level was 8.08 +1.89 % which significantly increased to 8.73 +2.37 % (p<0.05). Only 32.98 % of subjects achieved target value of HbA1C (≤ 7 %). Fasting and post-prandrial plasma glucose values were increased from 160.39 +60.25 mg/dL to 170.71+56.60 mg/dL and 210.31+ 75.88 mg/dL to 218.67 +75.03 mg/dL respectively, but not significantly different. Acarbose was more frequently associated with flatulence (46 %) and abdominal bloating (12 %), metformin with flatulence (12 %), nausea (14 %), diarrhea (2 %) and abdominal discomfort (6 %). In conclusion, combination therapy of sulfonylurea, metformin, and acarbose in type 2 diabetic patients with poorly controlled glycemia can cause the additive risk of adverse events.Key words : triple therapy, glycemic control, type 2 diabetes mellitu
Antibacterial activity and GC-MS analysis of the Citrus amblycarpa (Hassk) Ochse essential oil
Get PDFA research about anti-bacterial activity and components of essential oil from leaves and peels of Citrus amblycarpa have been done.The components of essential oil had been identified by using GC-MS and anti-bacterial activity against S. aureus ATCC 25923 and E. coli ATCC 25922 had been determined with liquid dilution method. The component of essential oil from leaves that can be identified are β-pinene, linalool, citronellal, citronellol and geraniol, while from peels are β-pinena, cymene, limonene and citronellal.Oil from the leaves has stronger anti-bacterial activity against S. aureus than from peels. On the other hand oil from peels is stronger anti-bacterial activity against E coli.Key words : Citrus amblycarpa, essential oil, anti-bacterial activity
Methyleugenol, a major metabolite on culture of endophytic fungi isolated from pandan wangi plant
Get PDFTwo kinds of endophytic fungi i.e. Colletotricum sp. PWD2 and Coelomycetes PWA1 isolated from pandan wangi (Pandanus amarylifolius) have been cultivated in a liquid medium, GYP for 3 weeks at room temperature without agitation. The ethyl acetate extracts derived from liquid cultures showed antifungal activity against Saccharomyces cerevisiae. The GC-MS analysis results showed methyleugenol as main metabolite in the ethyl acetate extract of both fungi cultures.Key words: pandan wangi, Pandanus amarylifolius, endophytic fungi, antifungal, methyleugeno