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TASTE MASKING OF DONEPEZIL HYDROCHLORIDE USING DIFFERENT ION EXCHANGE RESINS- A COMPARATIVE STUDY
Get PDFTaste mainly depends on the physiology, sensitivity and structure of taste buds. It is an important parameter in administering drugs orally. Bitter taste is a major limitation to patient compliance. Donepezil hydrochloride (DH) is a bitter drug used in Alzheimer's disease. Amongst the many techniques for taste masking, using ion exchange resins has been extensively reported. The technique of forming tasteless complexes with bitter drugs involves selection of most appropriate exchanger and optimization of complexing ratio. The aim of the present work was to select the best cationic exchanger amongst Indion 414, Indion 234 and Indion 214. All parameters were optimized to produce drug-loaded tasteless complexes. Complexation was carried out using batch process prior to which, acid-alkali activation was performed to remove adsorbed impurities from the resin bed surface and hence improve loading efficiency. UV-spectrophotometric method was used to determine percent drug loading. The molecular properties of drug resin complexes were studied using Fourier Transform Infra-red Spectroscopy, Differential Scanning Calorimetry and Xray Powder Diffraction which confirmed complexation. Indion 414 was found to give highest drug loading and minimal drug was released from the complex at salivary pH.
Key words: Donepezil HCl, Ion exchange resins, Molecular properties, Taste maskin
EFFECTS OF AVURVEDIC SHODHANA (PROCESSING) ON DRIED TUBEROUS ACONITE (Aconitum napellus Linn.) ROOT
Get PDFAconite (Aconitum napellus Linn.) commonly known as atis is a poisonous plant used extensively as antihypertensive, antipyretic, analgesic and antirheumatic. Ayurveda recommended the administration of aconite roots only after purification, i.e., boiling roots in cow’s urine (Gomutra). In the present study an attempt was made to compare the pro-arrhythmic and antihypertensive effects of powdered aconite root purified by shodhana process with that of unpurified form of aconite roots in order to provide scientific support of the claim in ayurvedic texts that purification of aconite root by shodhana process retains its antihypertensive activity and is devoid of pro-arrhythmic activity. Aconite root treatment in both forms purified and unpurified) caused significant reduction in BP when compared with diseased control group (P<0.05). The unpurified aconite root group showed significant increase in heart rate, increase in QRS complex time and increase in QT interval, however these parameters were statistically insignificant in purified aconite root treated group. The PRA, SC and BUN levels was significantly decreased in aconite root treatment groups. The probable mechanism of antihypertensive activity of aconite root can be attributed to decrease in plasma renin activity, decrease in oxidative stress and increase in NO levels. Key words: Aconite, shodhana process, antihypertensive, proarrhythmi
ANTIANGIOGENESIS AND ANTIBACTERIAL ACTIVITIES FROM AN INDONESIAN MARINE-DERIVED FUNGUS Dactylaria sp
Get PDFMarine-derived fungi have been proven to be rich sources of chemically diverse natural products with a broad range of biological activities. The aim of this study was to determine the antibacterial and antiangiogenesis activities of marine derived fungi Dactylaria sp. Cultivation of the fungus Dactylaria sp (strain TID 24041021-1) was isolated from the marine invertebrate sponge. Culture of marine fungus was macerated with acetone and partitioned with ethyl acetate. The ethyl acetate extracts with 50, 100, and 200µg/mL concentrations, were assayed for their antiangiogenic activity by using chorioallantoic membrane in vivo. At the same time, ethyl acetate extracts at levels of 5, 10, 15, and 20mg/mL were assayed to pathogenic bacteria Bacillus subtilis, Escherichia coli, and Staphylococcus aureus using well diffusion method. The result of this study showed that ethyl acetate extract at concentration 50µg/mL could inhibit angiogenesis. The best antiangiogenic activity was showed at concentration of 200µg/mL ethyl acetate extract. Antibacterial activity from ethyl acetate extract inhibited the growth of B. subtilis (2.25-5mm), E. coli (0.63-3.50mm) and S. aureus (01.75mm) bacteria.
Key words: Marine sponge-derived fungi, antiangiogenesis activity, antibacterial activit
SELECTION OF pEGFP-c1-TRANSFECTED-CHO-K1 CELLS BY G418 DECREASED THE EXPRESSION OF GREEN FLUORESCENT PROTEIN
Get PDFThe most common proteins used for reporter protein is the green fluorescent protein (GFP). It is very convenient to detect the GFP fluorescent by fluorescent microscopy or flowcytometry to monitor the successful transfection. The gfp gene can be introduced into the cells by transfecting of two different plasmid vectors or one vector containing both gfp and the gene of our interest. In this current experiment, we used pEGFP-c1 plasmid to express gfp in CHO-K1 cells. We transfected the CHO-K1 cells by using cationic lipid Lipofectamin 2000. We used this study as a way for predicting our human erythropoietin gene expression study in the CHO-K1 cells. In this study, we showed that expression of GFP decreased after incubation of the cells in selection medium containing G418. Expression of GFP seemed to be stable after about three weeks incubation in selection medium. Recombinant erythropoietin was also detected in the day 20.
Key words: Ctionic lipid, CHO-K1 cells, erythropoietin, G418, green fluorescent protei
OXIDATION AND POLYMORPHISM OF FATTY ACIDS AND NUTRITIONAL ASPECTS CONJUGATED OF LINOLEIC ACIDS
Get PDFFats and oils are triglycerides containing one unit of glycerol with three units of fatty acids. It also contained mono- and diglycerides, phosphatides, cerebrosides, sterols, terpenes, fatty alcohols, free fatty acids, fat-soluble vitamins, and other substances. Fats and oils are recognized as essential nutrients in both human and animal diets. They provide the most concentrated source of energyand also provide essential fatty acids which are precursors for important hormones. Conjugated linoleic acid (CLA) is a group of geometrical and positional isomers of linoleic acid. In contrast to linoleic acid, double bonds in CLA are usually located at positions 9 and 11 or 10 and 12 and each double bond can be either in the cis or trans configuration. Meat and dairy products from ruminant animals are the principal natural sources of CLA in the human diet. Dietary CLA has been shown to have potent anti-carcinogenic, antiatherogenic, immune modulating and also have other biological activities. The CLA was also reported to reduce body fat content.Key words: anti-atherogenic, anticarcinogenic, conjugated linoleic acid, Fats and oils, immune modulato
PHARMACEUTICAL EXCIPIENTS: GLOBAL REGULATORYISSUES
Get PDFAn excipient may be defined as an ingredient that is intentionally added to a drug for purposes other than the therapeutic or diagnostic effect at the intended dosage. Excipients have functional roles in pharmaceutical dosage forms which include the suitable form of consistency, modulating solubility and bioavailability of active ingredients, enhancing stability of the active ingredients in finished dosage form and many others. In most of the developed countries, the excipients are regulated as an active pharmaceutical ingredient. In Europe, it is assumed that novel excipients need to be evaluated as new chemical entities. In United State, the Food and Drug Administration assesses and permits use excipients as part of new drug application. The lack of harmonized international regulatory guidelines leads to the formation of the International Pharmaceutical Excipients Council (IPEC) in 1991. The IPEC was found to calibrate with different countries like Japan, Europe and China to address prevalent industry concerns related to the international harmonization of excipients standards, the introduction of useful new excipients to market place, and development of safety evaluation guidelines for the excipients. In the present study, an attempt has been made to investigate global issues governing regulations of pharmaceutical excipients.Key words: pharmaceutical excipient, regulatory guidelines, IPE
HEPATOPROTECTIVE ACTIVITY OF SAPONIN FRACTION OF OYONG SEED FLESH AND ITS COMBINATION AGAINST CCl4-INDUCED CHRONIC LIVER DAMAGE IN MALE WISTAR RAT
Get PDFSaponin fraction of seed flesh of Oyong (Luffaacutangula [L.]Roxb) has been investigated to have a hepatoprotective activity in rats with fibrotic chronic liver damage. This research was conducted to evaluate whether saponin fraction of Oyongseed flesh has a hepatoprotective activity in CCl4-induced acute liver damage. Hepatoprotective activity was determined by measuring the activity of liver enzymes (SGOT, SGPT, LDH), total nitrite/nitrate level, liver index and liver histology. Saponin fraction of Oyong flesh seeds 10mg/kg BW and meniran extract 400mg/kg BW alone showed hepatoprotective activity. Administration of saponin fraction 10mg/kb BB decreased SGPT and LDH significantly over untreated group. Group given meniran extract at dose of 200mg/kg BW showed decreased on LDH, while at dose of 400mg/kg BW decreased SGPT, SGOT, and LDH significantly. Hystological observation revealed any improvement in liver morphology especially after treated with saponin fraction 10mg/kg BWand meniran extract at dose of 400mg/kg BW. However, all groups treated with combination of saponin and meniran did not show improvement both at biochemical parameter and liver histology. In conclusion, saponin extract with dose of 10mg/kg BW and meniran extract at dose of 400mg/kg BW showed hepatoprotector activity. In contrast, combination of both did not show any hepatoprotective effect and it was suspected that they have antagonist effects.Key words:hepatoprotective, CCl4-induced liver fibrosis, Luffaacutangula, Phyllanthusnirur
CONSTRUCTION OF IN SILICO STRUCTURE-BASED SCREENING TOOLS TO STUDY THE OXIDATIVE METABOLITES FORMATION OF CURCUMIN BY HUMAN CYTOCHROME 450 3A4
Get PDFCytochrome P450 3A4 (CYP3A4) is a phase 1 metabolism enzyme which is responsible for the metabolism of about 3040% drug in the market. This CYP3A4 is the most abundant CYP450 expressed in human body and also the one who is responsible for the biotransformation of most drugs. The competitive inhibition of curcumin (a yellow bioactive pigment discovered in Curcuma sp.) towards human CYP3A4 indicates that curcumin can be a substrate for the enzyme. In this study, in silico approaches employing molecular docking and interaction fingerprinting were used to predict the binding mode and the site of metabolism (SOM) of curcumin. Together with the SOMs retrieved previously and the list of possible reactions catalyzed by CYP3A4, the docking and fingerprinting results indicate that the most probable metabolite of curcumin metabolism by human CYP3A4 is an oxidative metabolite 1-(3,4-dihydroxyphenyl)-5hydroxy-7-(4-hydroxy-3-methoxy-phenyl)hepta-1,4,6-trien-3one.Key words: site of metabolism (SOM), curcumin, biotransformation, in silico, molecular docking, protein-ligand interaction fingerprintin
IDENTIFICATION OF BAWANG SABRANG (Eleutherine americana Merr. ex K. Heyne) IN INDONESIA BASED ON CHROMOSOME CHARACTERS
Get PDFBawang Sabrang (Eleutherine americana Merr. ex K. Heyne) is a plant belongs to Iris family (Iridaceae). Genetic study of the Eleutherine species should be investigated to yield valuable information for breeding program. The aim of this research was to determine chromosome characters as a preliminary research on the genetic characterization of Bawang Sabrang. Squash method on the root tips was used for chromosome preparation of this plant. The results showed that the time of cell division and prometaphase stages of Bawang Sabrang were occurred at about 08.00-08.30 a.m. and 08.20 a.m., respectively. Chromosome number of Bawang Sabrang was 2n=12 and the karyotype consisted of 8 (4 pairs) of metacentric chromosomes, 2 (1 pair) submetacentric chromosomes and 2 (1 pair) subtelocentric chromosomes which have the longest of total length chromosomes. Therefore, the karyotype formula of Bawang Sabrang was 2n=12=8m+2sm+2stSAT. Besides that, on the pair of subtelocentric chromosomes there was a satellite at each of the chromosome. Analysis of chromosome characters exhibited that the long of total length chromosomes was about 1.687 ± 0.111 µm to 5.320 ± 0.716 µm. Based on the R value ( 3,65 ± 0,41), it revealed that there was variation of chromosome size on this Eleutherine species in Indonesia. Moreover, data of the chromosome characters is important to complete the database of Bawang Sabrang as a potential medicinal herb in Indonesia Keywords: Bawang Sabrang, Eleutherine americana, chromosome, karyotyp
SYNTHESIS AND EVALUATION OF ANTIOXIDANT AND ANTIINFLAMMATORY ACTIVITIES OF 2-(4’-DIMETHYLAMINO BENZYLIDENE)-6-BENZYLIDENE CYCLOHEXANONE
Get PDFThe study was designed to investigate whether 2-(4’-dimethylamino benzylidene)-6-benzylidene cyclohexanone (named code “B”) can be synthesized by reaction of Claissen–Schmidt condensation with 4'-dimethylamino benzal-dehyde, benzaldehyde, and cyclohexanone as starting materials and to evaluate its antioxidant and anti-inflammatory activities. The study showed that compound B at the concentration of 5, 10, 20, 40, and 80ppm did not exhibit antioxidant activity. In order to access the antiinflammatory activity, this compound was administered orally an hour before intra-plantar injection of carraagenan 1% on rat paw. Anti-inflammatory effect was evaluated by measuring the volume of edema every hour for 5h. Statistical analysis was performed by one way anova at 95% confidence level and followed by LSD test. “B” was potential as an anti-inflammatory agent at the dose of 132.40mg/200g BW by decreasing the volume of paw edema.Key words: synthesis; 2-(4’-dimethylaminobenzylidene)-6-benzylidene cyclohexanone; antioxidant; anti-inflammator