INDONESIAN JOURNAL OF PHARMACY
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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FORMULATION AND OPTIMIZATION OF PIOGLITAZONE SOLID DISPERSIONS PREPARED BY HOT MELT EXTRUSION TECHNIQUE
Vidyadhara Suryadevara;
Ashis Kumar Mehatha;
Sasidhar R Lankapalli;
Abhijit M Deshmukh;
Laxmana P Sambath
Indonesian Journal of Pharmacy Vol 24 No 3, 2013
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia
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DOI: 10.14499/indonesianjpharm0iss0pp206-214
The main objective of the present study was to develop a novel and stable pioglitazone loaded solid dispersions with enhanced solubility and dissolution rate. Different drug-to-carrier ratios were prepared by employing hot melt extrusion technique. These formulations were characterized for solid state properties by differential scanning calorimetry, X-ray powder diffraction and FT-IR spectral studies. Formulations were further evaluated for dissolution and stability studies. The aqueous solubility of pioglitazone, in present formulation was improved by the presence of both the polymers. Solid-state characterization indicated pioglitazone was present as amorphous material in formulation with Soluplus and polyethylene glycol, due to efficient entrapment in polymer matrix. The diffraction patterns of solid dispersion indicated the amorphous nature of pioglitazone in solid dispersions. The dissolution rate of all the solid dispersions was found to be rapid when compared to pure pioglitazone. Pioglitazone in pure form has very slow dissolution rate, when compared with the solid dispersions. Thus the solid dispersion prepared with Soluplus and polyethylene glycol would be useful for delivering poorly soluble pioglitazone with enhanced solubility and dissolution rate.Key words: pioglitazone, soluplus, solid dispersions, melt extrusion technique.
FORMULATION AND IN VITRO EVALUATION OF METOPROLOL SUCCINATE FLOATING TABLETS
Sunil Thakral;
Gagan Deep Singh;
Neetu Kansal;
Amarjit Singh
Indonesian Journal of Pharmacy Vol 24 No 3, 2013
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia
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DOI: 10.14499/indonesianjpharm0iss0pp170-176
Gastroretentive dosage forms extend significantly the period of time over which the drug may be released. This prolonged gastric retention improves bioavailability, decrease drug waste and improve solubility of drugs that are less soluble in a high pH environment due to their availability in gastric pH for longer duration of time.Floating drug delivery systems have a bulk density less than gastric fluids and hence remain buoyant in the stomach. The main objective of the present study was to develop Gastroretentive (GR) controlled release ormulations of Metoprolol to prolong the gastric retention time so that its bioavailability can be improved. The formulations were prepared by using swellable polymers like HPMC K4M, HPMC K15M, HPMC K100M, Guar Gum, Xanthan Gum, Sodium carboxymethyl cellulose and various effervescent compounds, e.g. sodium bicarbonate, and citric acid by the direct compression method. All the formulations were evaluated for different parameters like floating lag time, total floating time, hardness, weight variation, density measurements, drug content and water uptake/swelling index. Dissolution studies were done for all formulations in 0.1N HCl (pH 1.2). Formulations F3, F4 and F10 were found to provide maximum sustained release of metoprolol s uccinate up to 24 h with optimum floating properties.Key words : Controlled release; Gastro retentive; HPMC; Guargum; Xantham gum
EFFECT OF HPMC/CARBOPOL ON THE RELEASE OF CHLORPHENIRAMINE MALEATE FROM MATRIX TABLETS
Bipin P. Patel;
Dasharath M. Patel;
Jayvadan K. Patel
Indonesian Journal of Pharmacy Vol 24 No 3, 2013
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia
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DOI: 10.14499/indonesianjpharm0iss0pp157-162
Chlorpheniramine maleate is widely used in treatment for allergic disorder and cold. The controlled release matrix tablets of chlorpheniramine maleate were prepared using HPMC K15M, HPMC K100M and carbopol and studied their effect on drug release. Prepared tablets were evaluated for various physical parameters. In vitro drug release study shows that slow release in HPMC K100M than other two polymers. If concentration of polymer increases than the drug release is decreases due to formation of polymeric matrix. Zero order, first order, Higuchi’s and Korsmeyer’s equations applied to know the mechanism of drug release from prepared tablets. The similarity and dissimilarity factor found to be 77.88 and 4.14, respectively for drug release in stability study which shows there was no significant difference in drug release.Key words: Chlorpheniramine maleate, matrix tablet, HPMC K15M, HPMC K100M, carbopol and swelling index
HEPATOPROTECTIVE ACTIVITY OF SAPONIN FRACTION OF OYONG SEED FLESH AND ITS COMBINATION AGAINST CCl4-INDUCED CHRONIC LIVER DAMAGE IN MALE WISTAR RAT
Rachmawati, Heni;
Y. Hartiadi, R. Leonny;
Fidrianny, Irda;
Adnyana, I Ketut
Indonesian Journal of Pharmacy Vol 24 No 3, 2013
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia
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DOI: 10.14499/indonesianjpharm0iss0pp177-185
Saponin 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, Phyllanthusniruri
A REVIEW ON SUPRAMOLECULAR CHEMISTRY IN DRUG DESIGN AND FORMULATION RESEARCH
Vepuri, Suresh B;
Anbazhagan, S.;
Divya, D.;
Padmini, D.
INDONESIAN JOURNAL OF PHARMACY Vol 24 No 3, 2013
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia
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DOI: 10.14499/indonesianjpharm0iss0pp131-150
Supramolecular chemistry, other way called as intermolecular chemistry disclose the relationship of molecules with environment. It exploits while exposing the physicochemical phenomina that happens when two like or unlike molecules/ions/systems contact each other. Drug action involve the target recognition process and response triggered by the intermolecular complex of drug and target. Drug design therefore require in depth study of intermolecular forces that exist between drug and target. Formulation of the drug or Active Pharmaceutical Ingredient (API) is also regulated by these forces. Compatibility and incompatibility in formulations are nothing but of the effect of the intermolecular forces on physical behavior of systems. Therefore review of intermolecular chemistry in general and its role particularly in pharmaceutical research is presented here for the benefit of the students and research scholars who aspire to work on interdisciplinary projects in the field of pharmacy. Key words: intermolecular forces, hydrogen bond, drug design, active pharmaceutical ingredient (API), crystal.
COMPRESSIONAL CHARACTERISTICS OF Piper Guineense FRUIT
Bakre Lateef Gbenga;
Ayodele Damilola
Indonesian Journal of Pharmacy Vol 24 No 3, 2013
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia
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DOI: 10.14499/indonesianjpharm0iss0pp186-192
The dried fruit of Piper guineense is widely used for its antibacterial and antifungal properties. The objective of this present study was to examine the compressibility of dried powdered fruits of Piper guineense with a view to determining the suitability of its formulation into tablet dosage form. The compressional properties was studied in comparison with that of microcrystalline cellulose, dicalcium phosphate dihydrate and corn starch BP using density measurements and the Heckel and Kawakita equations for the analysis of the compression data at dwell times 5, 15 and 30s. The Heckel plots showed that the P. guineense powder is a Type A material and the degree of onset of plastic deformation increases as the dwell time is increased. Piper guineense exhibited the fastest onset of plastic deformation at 30s dwell time and the overall amount of plastic deformation was higher for Piper guineense than cornstarch and dicalcium phosphate dihydrate at all dwell times. The overall amount of plastic deformation for Piper guineense was highest at 15s dwell time. Results suggest that it should be of significant benefit to use a dwell time of 15s for the compression of Piper guineense powder.Key words: Piper guineense, cornstarch, microcrystalline cellulose, dwell time, compressional characteristics
SYNTHESIS AND ANTIMICROBIAL ACTIVITY EVALUATION OF SOME SCHIFF BASES DERIVED FROM 2-AMINOTHIAZOLE DERIVATIVES
Gupta, Rajul;
Fuloria, Neeraj Kumar;
Fuloria, Shivkanya
Indonesian Journal of Pharmacy Vol 24 No 3, 2013
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia
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DOI: 10.14499/indonesianjpharm0iss0pp193-197
Various substituted acetophenones (1-5) on treatment with iodine and thiourea yielded 2-amino-4-(substituted-phenyl)-thiazole (1a-5a), which on further treatment with various substituted aldehydes to get N-(substitutedbenzylidene)-4-(substitutedphenyl) thiazol-2-amine (1b-5b). All the synthesized compounds were characterized by their respective FTIR, 1H NMR and mass data. Synthesized compounds (1b-5b) were subjected to investigation for their antibacterial and antifungal studies against Staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Candida albicans, Asperigillus flavus and Asperigillus fumigatus by disk diffusion method. Compound 5b was found to be most effective with largest zone of inhibition.Key words: thiazole, acetophenones, antibacterial, antifungal, substituted aldehydes.
IN–VITRO PHARMACEUTICAL EVALUATION OF TWO BRANDS OF DISPERSIBLE ACETYL SALICYLIC ACID TABLETS AVAILABLE IN OMAN
Khan, Shah Alam;
Al Shabibi, Maryam Nasser;
Nazmi, Abdul Salam
Indonesian Journal of Pharmacy Vol 24 No 3, 2013
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia
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DOI: 10.14499/indonesianjpharm0iss0pp151-156
Acetyl salicylic acid (ASA), a non-steroidal anti-inflammatory drug (NSAID) is widely used for its analgesic, antipyretic, antiinflammatory and anti-thrombotic action. The aim of the present study was to investigate the pharmaceutical equivalence of two brands of dispersible ASA tablets marketed in Oman. Two different brands of dispersible ASA tablets (300mg) were purchased from the retail pharmacy outlets and their pharmaceutical quality were assessed by using in-vitro tests as per the British Pharmacopoeia (BP) and unofficial standards as recommended by the manufacturers. The assessment of tablets included the evaluation of uniformity of weight and diameter, friability, crushing strength, disintegration and chemical assay by volumetric titration and colorimetric methods to determine the content of active pharmaceutical ingredient (API). Both brands of the ASA tablets passed the BP standards for uniformity of weight and diameter, disintegration, friability and crushing strength. However one of the two brands did not comply with the standard assay of content of active ingredient. Thus based on these results it can be concluded that these two brands of ASA are not pharmaceutically equivalent.Key words: ASA tablets, pharmaceutical equivalence, disintegration, volumetric method.
SYNTHESIS AND EVALUATION OF ANTIOXIDANT AND ANTIINFLAMMATORY ACTIVITIES OF 2-(4’-DIMETHYLAMINO BENZYLIDENE)-6-BENZYLIDENE CYCLOHEXANONE
Sardjiman .;
Ni Nyoman Yuliarti;
Sasmito .;
Agung Endro Nugroho
Indonesian Journal of Pharmacy Vol 24 No 3, 2013
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia
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DOI: 10.14499/indonesianjpharm0iss0pp198-205
The 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-inflammatory
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
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DOI: 10.14499/indonesianjpharm0iss0pp163-169
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