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ENHANCEMENT OF DISSOLUTION RATE OF MODAFINIL USING SOLID DISPERSIONS WITH POLYETHYLENEGLYCOLS
Get PDFSolid dispersions (SDs) of modafinil (MDF) were prepared using polyethyleneglycols (PEGs), in 1;1, 1;2 and 1;4 proportions by fusion, solvent evaporation and physical mixing method. Differential scanning calorimetry (DSC) and X-ray powder diffractometry (XRD) were used to examine the physical state of the drug. The data from the XRD showed that the drug was converted to amorphous form as the number and intensity of peaks were decreased in solid dispersion as compared to pure drug and physical mixture of drug and carrier. DSC thermograms also confirmed the change in physical state of the drug as the peaks were altered or disappeared. With the highest ratio of the carriers (1:4), the drug solubility was enhanced by 38.68, 34.78 and 9.29 folds in solvent evaporation, fusion and physical mixing methods respectively. Solid dispersion batch S6 containing drug:PEG6000 in 1:4, was selected to be formulated as tablet (batch TS6) and evaluated for in vitro drug dissolution & six month stability. An increased dissolution rate of modafinil was observed from SDs and PMs, as compared to pure crystalline drug. The dissolution rate of modafinil from its PMs or SDs increased with an increasing amount of polymer.Key words: Fusion, solvent evaporation, physical mixture, in vitro dissolution, characterization.
A BIOAVAILABILITY STUDY OF INDONESIAN GENERIC TABLET OF CAPTOPRIL IN HEALTHY VOLUNTEERS
Get PDFCaptopril is a selective inhibitor of angiotensin-converting enzyme (ACE) and is formulated by several pharmaceutical companies in Indonesia. This study was conducted to compare the bioavailability of a captopril tablet with reference products in healthy volunteers. The relative bioavailability of captopril was determined in single dose, randomized, crossover, and two-phase studies. The relative bioavailability of the test product (a generic captopril 50 mg tablet) with respect to the reference product was determined. Twelve healthy volunteers in two groups took part in these studies and took either the test or reference tablets in the first phase and received the other tablet in the second phase of each study. The bioavailability parameters include the peak concentration of captopril in serum (Cmax); the time to achieve the peak concentration (Tmax); and the area under the curve of captopril in serum versus time. Non-compartmental analysis on observed concentration versus time data has resulted in the mean value of Cmax of 545.26 ± 22.90 ng/mL (test product) and 548.91 ± 25.07 ng/mL (reference product) and mean Tmax of 1.13 ± 0.08 hours (test product) and 1.08 ± 0.08 hours (reference product), mean of AUC0-7 value of 1820.51 ± 75.31 ng. hour/mL (test product) and 1822.09 ± 99.29 ng. hour/mL (reference product), and mean of AUC0-inf value of 1967.83 ± 95.65 ng. hour/mL (test product) and 1996.94 ± 124.52 ng. hour/mL (reference product). Based on the data, it can be concluded that there is no significant difference (p>0.05) in bioavailability between both captopril Tablet (test and reference product).Key words: Bioequivalence, Captopril, HPLC, Human serum, Generic
PHYSICAL PROPERTIES OF WOUND HEALING GEL OF ETHANOLIC EXTRACT OF BINAHONG (Anredera cordifolia (Ten) Steenis) DURING STORAGE.
Get PDFBinahong (Anredera cordifolia (Ten) Steenis) has been used as wound healing in traditional Indonesian medicine. The developing of the dosage forms using the formulation technology approach has been done. The aim of this study was to examine the physical properties of the wound healing gel of ethanolic extract of binahong during storage. The factorial design method 3 factors and 2 levels was employed to achieve this study. The three factors used in this study were Carbopol, CMC-Na and Caalginate with low and high level for each factor. The physical properties of the wound healing gel of ethanolic extract of binahong was evaluated on day 1, 30, 60 and 90 for viscosity and bioadhesion study. The result showed that CMC-Na and Caalginate increased the alteration of physical properties of wound healing gel of ethanolic extract of binahong during storage. The carbopol maintained the physical properties of the gel during storage.Key words: bioadhesion, binahong, viscosity, wound healing gel
ISOLATION AND IDENTIFICATION OF FLAVONOIDS FROM Sesamum indicum
Get PDFNatural substances have long served as sources of therapeutic drugs. Many substances have been derived from traditional medicines. The plants are rich in secondary metabolites. The medicinal properties of these plants have been attributed to the biochemicals present in the plant materials. In addition to their role in human and animal nutrition, knowledge of micronutrients and phytochemical composition is fundamental to the understanding of modes and mechanisms of action of medicinal plants in general. In the present investigation, quercetin and kaempferol have been isolated and identified from stem, leaves and unorganized cultures of Sesamum indicum and maintained by frequent subculturings on Murashige and Skoog’s medium (1962) supplemented with NAA+BAP(5.0+0.5mg/L). The study showed that maximum content of quercetin and kaempferol was observed in 6 weeks old calli and minimum in stem of S. indicum. The structure of the isolated compound was established on the basis of physical, chemical test and spectroscopic evidences.Key words: Flavonoids, quercetin, kaempferol, Sesamum indicu
EFFECT OF BENZALDEHYDE EXCESS IN THE SYNTHESIS OF LR-2 AND CYTOTOXIC ACTIVITY OF LR-2 AGAINTS HeLa CELL
Get PDFLR-2(4-phenyl-3,4-dihydro-indeno[2’,1’]pyramidine-2(1H)- thione; Leni Ritmaleni 2), which designed and assumed to have biologically activity as anticancer, has been successfully synthesized by using the Biginelli reaction. This research was aimed to investigate the effect of benzaldehyde excess in the synthesis of LR-2 and to evaluate the cytotoxic activity of LR-2against HeLa cancer cell lines. The synthesis was done by reacting benzaldehyde, 2-indanone and together with thiourea at one time as said as one pot reaction synthetic methodology and the reaction was acid catalysed. The mole equivalent of benzaldehyde was in excess compare to others. The effect of benzaldehyde in excess is the higher the mole of benzaldehyde, the lower the yield of LR-2. The cytotoxicity of LR-2 was done by using MTT method and the LC50 was 268.15 μM.Key words : LR-2, benzaldehyde, cytotoxic, HeLa
SELAGINELLA ACTIVE FRACTIONS INDUCE APOPTOSIS ON T47D BREAST CANCER CELL
Get PDFApoptosis is an important target on anticancer mechanism. The purpose of this research is to investigate apoptosis induction of Selaginella plana Hieron active fractions on T47D cells. Absolute ethanol was used to extract Selaginella plana powders. Ethanolic extract was dilluted by methanol:water (4:1) and then fractionated by hexane (S_Hex), methylene chloride (S_MTC), ethyl acetate (S_EA), and buthanol (S_BuOH). The proliferation of T47D cell line was detected by SRB (Sulforhodamine B) assay which was measured at a wavelength of 515nm. Flowcytometry analysis to determine apoptosis was examined by Propidium Iodide (PI) and Annexin V assay using T47D breast cancer cell line. The result showed that the IC50 value of S_Hex, S_MTC, S_EA, and S_BuOH on T47D cells were 107 µg/mL, 4 µg/mL, 6 µg/mL, and 17 µg/mL respectively. The active fractions (S_MTC and S_EA) at its IC50 concentration significantly (P<0.05) increased the total number of early apoptotic cells in the T47D cells 3.39% and 4.1% respectively compared to that of control (1.95%). Based on the result, methylene chloride and ethyl acetate fraction of Selaginella plana induced apoptosis on T47D cell.Keywords: apoptosis, breast cancer, Selaginell
Econazole depleted calcium release-activated calcium (CRAC) current through blockade of voltage-dependent Ca 2+ channels
Get PDFEconazole is an azole antifungal agent which can block the calcium release-activated calcium (CRAC) current in human leukaemic T cell line. The phenomenon is also possible to occur in mast cell such as RBL-2H3 (rat basophilic leukemia) cells, a tumor analog of mast cells. In the study, we investigated effect of econazole on 45Ca2+ uptake into the cells in response to thapsigargin, an ATP-dependent Ca2+ (SERCA) inhibitor, by direct measurement of radiolabelled Ca2+ uptake in cells. The mechanism underlying this effect of econazole was studied using molecular modelling. In present study, econazole inhibited 45Ca2+ influx into mast cells in absence of mast cells inducer, thapsigargin. Moreover, econazole potently suppressed the 45Ca2+ influx induced by thapsigargin. It was supported that econazole also inhibited Ca2+-induced tracheal contraction. The increase of Ca2+ was stimulated by the opening of voltage-dependent Ca2+ channels activated by KCl-induced membrane depolarization. Based on molecular docking study, score of interaction (equal to energy of interaction) of 3FGO, a main protein target on Ca2+ -ATPase, with native ligan, thapsigargin and econazole were -76.941, -117.205, and -92.277, respectively. The interaction of thapsigargin and Ca2+ -ATPase was more stable than this of econazole and Ca2+ -ATPase. It suggests that it would be difficult for econazole to block the interaction of thapsigargin with Ca2+ -ATPase to increase intracellular Ca2+.In conclusion, econazole inhibited the increase of intracellular Ca2+involving the blokade of voltage-dependent Ca2+ channels, but not involving the Ca2+ -ATPase pathway.Key words :econazole, Ca2+ -ATPase, CRAC current, thapsigargin
Liquisolid ibuprofen tablets
Get PDFIbuprofen is an antiinflamatory drugs with poor solubility in water but good permeability in the gastrointestinal tract. Liquisolid tablet is the one method of increasing solubility and dissolution rate of ibuprofen. The aims of this study was to determine the effect of glycerine and propylene glicol as non volatile solvent and PVP K-30 as hydrophilic polymer on the dissolution rate of liquisolid ibuprofen tablets. In this research, there are 7 formulas of liquisolid ibuprofen tablets were made. The ratio of ibuprofenin glycerine is 1 : 3 and of propilene glicol is 5:1 with various concentration of PVP K-30 (5, 10, and 15%). Formula I was made as a control so there was no addition of non volatile solvent and hydrophilic polymer. Based on the results, liquisolid ibuprofen tablets using glycerine or propylene glycol as a non volatile solvent and PVP K-30 as a hydrophilic polymer can increase the dissolution rate constant of liquisolidibuprofen tablets comparedthat of ibuprofen conventional tablets (non liquisolid). The addition of PVP K-30 as a hydrophilic polymer can increase the dissolution rate constants liquisolid ibuprofen tablets until a concentration of more than 10% because the polymer will swell and form a viscous layer that inhibits the disintegration so that the percent release decrease.Key words:Ibuprofen, liquisolid, non volatile solvent, hydrophilic polymer
Effect of Indonesian medicinal plants essential oils on Streptococcus mutansbiofilm
Get PDFEssential oil’s component such as menthol and eucalyptol were already used as dental plaque inhibitors. In searching of potential dental plaque inhibitor from natural products, a study to explore the potency of essential oils extracted from several Indonesian medicinal plants against planktonic growth and biofilm adherence of S. mutans was performed. A total of 14 essential oils from some selected Indonesian medicinal plants were extractedby steam-hydro distillation. Antibacterial assay was performed against S. mutansby micro dilution technique on nutrient broth media. Biofilm formation inhibition assay was conducted on a flexible U-bottom 96-wells PVC micro plate by using BHI enriched with sucrose 2% at 36.6 °C for 18-24 h. After staining with 1% crystal violet, the optical density was read at 595 nm. A mouthwash commercial product containing essential oil component was used as a positive control. Result showed that the essential oils of C. sintoc exhibited the highest biofilm formation inhibition (IC50 = 0.005%), and Z. officinale showed the highest biofilm degradation with EC50 value of 0.013%. Both were active against bacterial planktonic growth but C. sintocshowed lower MIC90 value (0.6%) in comparison to Z. officinale(0.06%). Meantime, C. citratus was showed promising antibacterial and antibiofilmactivities with MIC90 value of 0.06%, MBC 0.6%, IC50 0.008% and EC50 0.026%. It is concluded that the essential oils of C. citratus, Z. officinaleand C. sintocare potential to be developed as dental plaque inhibitors.Key words: essential oils, antibacterial, biofilm, Streptococcus mutan
Optimization of Theophylline Tablet Formula Using CoProcessed Excipients of Lactose and Avicel
Get PDFTablet excipients in direct compression should have good flowability and compactibility. Improvement of excipients properties may be obtained by coprocessing. Co-processing is defined as combining two or more excipients by an appropriate process. Co-processed excipients of lactose and avicel, which were fabricated by spray drying technique, would be used as filler-binder in theophylline tablet formulation. The co-processed excipients were evaluated for their physical properties, i.e; particle size distribution, average diameter, density, flowability, compactibility and water absorption. Simplex lattice design was used for optimizing flowability, compactibility and water absorption of coprocessed excipients. The results showed that proportion of lactose and avicel with optimum physical properties was determined by the ratio 1:1 with a response of flowability was 8.79 ± 0.02 seconds, compactibility was 5.61 ± 0.08 kg and water absorption was 61.30 ± 0.40 mg/min. Superimposed contour plot of theophylline tablet formulation using co-processed excipients as filler-binder by factorial design was determined by the optimum proportion of magnesium stearate and eksplotab (1:3.74) with the response of hardness was 5.54 ± 0.042 kg, friability was 0.303 ± 0.015%, disintegration time was 1.83 ± 0.115 minutes and DE20was 85.66 ± 0.35%.Key words: theophylline tablets; co-processed excipients; lactose; avicel