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INDONESIAN JOURNAL OF PHARMACY

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Published by Universitas Gadjah Mada

ISSN : 23389427 EISSN : 23389486 DOI : -

Core Subject : Health,

Medicine & Pharmacology

Indonesian Journal of Pharmacy (ISSN-e: 2338-9486, ISSN-p: 2338-9427), formerly Majalah Farmasi Indonesia (ISSN: 0126-1037). The journal had been established in 1972, and online publication was begun in 2008. Since 2012, the journal has been published in English by Faculty of Pharmacy Universitas Gadjah Mada (UGM) Yogyakarta Indonesia in collaboration with IAI (Ikatan Apoteker Indonesia or Indonesian Pharmacist Association) and only receives manuscripts in English. Indonesian Journal of Pharmacy is Accredited by Directorate General of Higher Education (DGHE) DIKTI No. 58/DIKTI/Kep/2013.

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Articles 706 Documents

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BIOTRANSFORMATION OF PENTAGAMAVUNON-0 (PGV-O) : IN VITRO AND IN VIVO STUDIES ., Sugiyanto; ., Oetari; Nugroho, Agung Endro
Indonesian Journal of Pharmacy Vol 14 No 2, 2003
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Pentagamavunon-0 (PGV-0) or 2,5-bis-(4-hydroxy-3-methoxy benzyilidin) cyclopentanon is a synthetic compound which has been proved to have an anti-inflamatory effect by animal experiments. The study was performed in order to investigate the possible route of biotransformation of PGV-0, which in turn can assist to elucidate the mechanism of its action.The in vivo biotransformation was predicted by identification of all metabolites of PGV-0 presence in urine and faeces after administration orally and intravenously. The in vitro studies were performed using microsomal or sitosolic fraction of the hepar. The metabolites were determined by thin layer chromatography and spectrophotometry.The results indicated that PGV-0 underwent oxydative biotransformation (phase I) and at least produced one metabolite. In vitro studies, PGV-0 also underwent glucuronidation and sulfatation. However, in vivo studies indicated that only metabolites of PGV-0 which have hydroxyl groups underwent conjugation process but PGV-0.Key words: Pentagamavunon-0, biotransformation, in vivo and in vitro.

SYNTHESIS AND PHARMACOLOGICAL EVALUATION: ANTIMICROBIAL, ANTI-INFLAMMATORY, ANALGESIC, ULCEROGENIC PROPERTIES OF SEVERAL BIS-HETEROCYCLIC DERIVATIVES Ravindra Kumar; Hament Panwar
Indonesian Journal of Pharmacy Vol 26 No 1, 2015
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

In Medicinal chemistry, heterocyclic derivatives contributed the largest classical division of organic chemistry. Thiadiazole compounds have been know many biological activities such as hypoglycemic, anticancer, anti-inflammatory, anti-asthmatic, antihypertensive and etc. On this research, several 1,1-Bis [2-{2-(5-(arylidene)imino-1,3,4-thiadiazol-2-yl) methyl amino}- 1,3,4-thiadiazo-5-yl] cyclopropane 5(a-h) have been synthesized from cyclopropane dicarboxylic acid comprising thiadiazole moieties. All the synthesized compounds have been characterized by elemental (C,H,N) and spectral (I.R., 1H- NMR, Mass) analysis. Furthermore, all synthesized compounds were screened for their antifungal, antimicrobial, anti-inflammatory, analgesic, ulcerogenic and toxic activities. The Compound 5f, 3-chlorophenyl substituted was found the most potent in antimicrobial spectrum against all the used microbes. On the other hand, compound 5g, 4-hydroxy-3-methoxy phenyl substituted was found the most potent in anti-inflammatory, analgesic, and ulcerogenic activities which further evaluated for lesser toxicity test.Key words: Bis-phenylarylidinylthiadiazolidinone cyclopropane, anti-microbial, anti-inflammatory, analgesic, ulcerogenic and toxicity studies

THE ABILITY OF CURCUMIN AND 4-ARYL CURCUMIN DERIVATIVES AS RADICAL SCAVENGER OF SUPEROKSID ., Satibi; AM, Supardjan
Indonesian Journal of Pharmacy Vol 12 No 3, 2001
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Superoxide radical scavenger property of curcumin and its derivatives was investigated using Nitro Blue Tetrazolium (NBT) method. Curcumin was modified at the active methyleen groups with aryl group (4-aryl curcumin), which supposed to be related to its anti-inflamatory activity. The experiment were carried out by mixing curcumin solution at five different concentrations and superoxide radical. After incubating for 60 minutes, NBT2+ (15,29 M) was added and measured at max of 687 nm, so as the curcumin derivatives. The result showed that superoxide radical made bathochromic shift of curcumin. Bathochromic shift was higher when aryl group was attached at active methyleen C-4 of curcumin. This shift made the max of curcumin and its derivatives moving close to max of diformasan (result of NBT2+ reduction by superoxide radical), producing an overlapping spectra. The increasing concentration of curcumin and its derivatives made the increasing max of diformasan absorbance. Thus, the method of NBT2+ reduction, in fact, unable to estimate the scavenger property of curcumin and its derivatives.Key words: curcumin derivatives, superoxide radical

The micromeritics parameter changing of three inhalation dosage forms Riswaka Sudjaswadi; Agatha Budi Susiana Lestari
Indonesian Journal of Pharmacy Vol 16 No 1, 2005
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Droplet and particle size measurements obtained after spraying of three inhalation aerosols dosage forms by microscopic methods, had been carried out, and their distributions had also been reported.The results showed that the geometric mean diameter ( dg ) is getting higher since the first spray to the last. Whilst the geometric standard deviation ( τg ) fluctuated preferably to the moderate polydispersity.Key words : inhalation aerosols, geometric diameter and standard deviation

Effects of pentagamavunon-0 on histaminemediated hyperresponsive airway in asthmatic models : in-vitro in-vivo Agung Endro Nugroho; Hemmy Prasetyo; Djoko Suhardjono; Mulyono Zhang Be; Shuang Liu; Supardjan A. Margono; Kazutaka Maeyama
Indonesian Journal of Pharmacy Vol 21 No 2, 2010
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Asthma is a chronic inflammatory airway disease involving reversible airway constriction and airway hyperresponsiveness (AHR) to allergens, airway edema, and increased mucus secretion tumor cells. To date, exploration of antiasthmatic drug is still being studied both from natural products or sinthetic processes. One of the sinthetic compound is pentagamavunon-0 (PGV-0) which possesses anti-inflammatory and inhibitory effects on histamine release from rat mast cells. The aim of the study is to look at the effects of PGV-0 on histaminemediated hyperresponsive airway in asthmatic models (in vitro and in vivo studies). In vitro study was conducted using isolated organ technique with isotonic transducer. The results have shown that PGV-0 could not inhibit the contraction of isolated guinea pig trachea induced by histamine. PGV-0 did not change the pD2 and Emax values of histamine on trachea smooth muscle. The finding indicates that PGV-0 does not have affinity and intrinsic activity on H-1 histaminergic receptor in trachea smooth muscle. In vivo study, we sensitized the rats with ovalbumin (OVA) to develop the airway hyperreactivity to histamine. Histamine level in bronchoalveolar lavage fluid (BALF) and airway tissue were determined using HPLC-fluorometry. Multiple exposures of ovalbumin significantly histamine level in BALF by 74.51±5.33 pmol/mL or 6-times higher than this of control saline group. Oral administration of PGV-0 (40 mg/kg BW) significantly decreased the histamine accumulation in BALF to 30 % of the value of control group in asthmatic rats. Besides, PGV-0 significantly prevented the histamine decrease in asthmatic rats to 37.8 % trachea, and 34.2 % in bronchus. However, PGV-0 did not succeed to prevent the histamine decrease in the lung of asthmatic rats. The result of the study may provide useful information for further discovering pharmacological synthetic compound for treatment of allergic inflammatory asthma.Key words: asthma, curcumin, pentamavunon-0, histamine, airway hyperresponsiveness

The Keto-Enol Tautomerism of Curcumin and Some 4-substituted Curcumin Derivatives : A Theoretical Study Based on Computational Chemistry Approach Enade Perdana Istyastono; Supardjan A. Margono; Harno Dwi Pranowo
Indonesian Journal of Pharmacy Vol 14 No 3, 2003
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Heat formation (DHf) for the enol and diketo tautomers of curcumin and some 4-substituted curcumin derivatives has been studied using semiempirical AM1 quantum-chemical calculations. The calculations on curcumin, 4-methylcurcumin, 4-ethylcurcumin, 4-npropylcurcumin, 4-isopropyl-curcumin, 4-n-butylcurcumin, and 4-benzylcurcumin showed that the more steric hindrance resulted from the subtituents, the more stable they were in the form of diketo tautomers than enol tautomers. Whereas, calculations on 4-phenylcurcumin, 4-(o-methoxyphenyl)-curcumin, and 4-(p-methoxyphenyl) curcumin showed that though steric hindrance influenced the keto-enol tautomerism, they were found more stable in the form of enol tautomers. This phenomenon was estimated to be related with conjugation effect of the aromatic groups with the enol moiety of the main bone structure.Keywords : 4-Substituted curcumin, the keto-enol tautomerism, AM1, semiempirical calculations.

ANTIMICROBIAL METABOLITES FROM A MARINE-DERIVED FUNGUS Wilmar Maarisit; Katsuhiro Ueda
Indonesian Journal of Pharmacy Vol 24 No 3, 2013
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

A marine fungus was separated from the surface of a marine red algae. Ethyl acetate extract of the cultivated marine fungus inhibited the growth of the pathogenic bacteria E.coli and S.aureus, and the phytopathogenic fungus C. cucurbitarum. Separation of the EtOAc extract gave four compounds, which were identified as new anthraquinonederivatives 3 and 4, and the known chrysophanol (1) and rubelin A (2) by the extensive analysis of NMR data. Compounds 1-4 inhibited the growth of the gram negative bacteria E. coli and gram positive bacteria S. aureus. Compound 3 also inhibited the fungus C. cucurbitarum.Key words: marine-derived fungus, structure elucidation, anthraquinone, antimicrobial activity

A BIOEQUIVALENCE STUDY OF AMPICILLIN (GENERIC PRODUCTS) IN RABBITS Wahyono, Djoko; ., Nurlaila
INDONESIAN JOURNAL OF PHARMACY Vol 12 No 4, 2001
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

The use of generic medicine in health services has strongly been suggested by government. Production of those type of medicine by government appointed pharmaceutical manufacturers has shown a good progress. However, monitoring to those products in the market, based on the bioequivalence quality, still need to be improved. An example of medicine produced in generic form is Ampicillin, one of the broad spectrum antibiotic effective to treat upper respiratory tract infections. The aim of this research was to evaluate the bioavailability of generic ampicillin capsules (500 mg) compared to the patented product. The research was carried out as follow: six male rabbits weighing 2.0 - 2.5 kg were assigned to a cross - over design to receive both products orally after 24 hour fasting. The generic and patented products were given to the rabbits with a week wash-out period. Following drug administration, the blood samples (11 samples) were drawn from the marginal ear vein at designated time (5-330 minutes) to analyse unmetabolized ampicillin fluorometrically. Detection of the ampicillin was recorded at maximum excitation (350 nm) and maximum emission (420 nm) wavelengths. The result showed that the AUC value of the generic product (3,211.25 Â± 635.23 ïg hour/ml) was significantly higher than that of patented product (2,425.68 Â± 895.26 ïg hour/ml) (p<0.05). The peak level of ampicillin (Cmax) was significantly higher for the generic (17.00 Â± 5.10 ïg/ml) than patented product (11.25 Â± 2.75 ïg/ml), while time to reach Cmax was not significantly different between the two products, ie. 77.34 Â± 16.70 minutes (generic) and 82.48 Â± 13.57 minutes (patented). The study concluded that the ampicillin capsules in generic form had a better biovailability than patented product. Key words: ampicillin, generic product, bioequivalence

Isolation of cytotoxic substance from Kaliapsis sponge Erna Prawita Setyowati; Umar Anggara Jenie; Sudarsono .; Broto Kardono; Rachmaniar Rahmat; Edy Meiyanto
Indonesian Journal of Pharmacy Vol 18 No 4, 2007
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

An isolation of cytotoxic substance of Kaliapsis sponge has been conducted. The substance was isolated using maceration, partition, vacuum liquid chromatography and preparative thin layer chromatograpy methods.The result of research showed that peak 1 has the most cytotoxic activity. Cytotoxicity test with MTT [3 (4,5-dimetiltiazol-2-il)-2,5-difeniltetrazolium bromide] reagen on myeloma cell showed that the peak 1 had a high activity against myeloma cell. It has IC50 equal to 0,18 μg/mL.Key word: Kaliapsis sponge, cytotoxic, myeloma cell

PHYTOCHEMICAL SCREENING AND ANALYSIS POLYPHENOLIC ANTIOXIDANT ACTIVITY OF METHANOLIC EXTRACT OF WHITE DRAGON FRUIT (Hylocereus undatus) VH, Elfi Susanti; Utomo, Suryadi Budi; Syukri, Yandi; Redjeki, Tri
Indonesian Journal of Pharmacy Vol 23 No 1, 2012
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

White dragon fruitÂ isÂ a wellÂ knownÂ andÂ widelyÂ usedÂ herbal medicine,Â especiallyÂ inÂ Asia,Â whichÂ containsÂ severalÂ interesting bioactive constituents and possesses health promoting properties. TheÂ aimÂ ofÂ thisÂ studyÂ wasÂ toÂ analyzeÂ forÂ theÂ bioactive compounds,Â evaluateÂ totalÂ phenolicÂ contentsÂ andÂ antioxidant capacitiesÂ ofÂ methanolicÂ extractÂ ofÂ whiteÂ dragonÂ fruit.Â The antioxidantÂ activityÂ wasÂ determinedÂ byÂ theÂ 1,1-diphenyl-2-picrylhydrazyl (DPPH) free radical scavenging activity assay. Total phenolicÂ contentÂ wereÂ determinedÂ byÂ Folin-CiocalteuÂ method. PhytochemicalÂ screeningÂ ofÂ theÂ whiteÂ dragonÂ fruitÂ showed theÂ presenceÂ ofÂ triterpenoid,Â alkaloid,Â flavonoidÂ andÂ saponin. TheÂ extractÂ exhibitedÂ strongÂ antioxidantÂ activityÂ withÂ IC50 of 193 Î¼g/mL, and total phenolic content of 246 Î¼g/mL in 1 Kg dry extract.Key words: antioxidant activity, total phenolic, DPPH, white dragon fruit

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