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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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Synthesis and gastric ulcer protective activity of chlorinated quercetin Tutus Gusdinar
Indonesian Journal of Pharmacy Vol 20 No 4, 2009
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Gastrointestinal toxicity due to non-steroid anti-inflammatory rugs can be inhibited by the compounds that have antioxidant activity. Quercetin is a flavonoid that has antioxidant activity and protection effect against gastric ulcer. Chlorination of quercetin enhanced the antioxidant activity. This study aims to obtain the chlorinated derivative of quercetin and examine the protection effect against acetosal-induced gastric ulcer. Chlorination was done by the addition of chlorine at room temperature. Ulcer induction was carried out on rats by oral administration of acetosal. Incidences of gastric ulcer were determined by macroscopic and microscopic observation. Chlorination of quercetin with chlorine gas produced 6-chloroqueretin as major product. The protection effect against acetosal-induced gastric ulcer of this compound was higher than quercetin. Key words : quercetin, chlorination, gastric ulcer, NSAIDs

INFLUENCE OF POMEGRANATE JUICE ON THE CYP3A4-MEDIATED METABOLISM AND P-GLYCOPROTEIN MEDIATED TRANSPORT OF SAQUINAVIR IN VIVO AND EX VIVO MODELS Vemulapalli, Sridhar
INDONESIAN JOURNAL OF PHARMACY Vol 27 No 3, 2016
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Cytochrome P450 3A4 (CYP3A4) and P-glycoprotein (P-gp) play an important role in the first pass metabolism thereby limits the oral bioavailability of many clinically important and frequently prescribed drugs. The absolute oral bioavailability of saquinavir is very low (i. e. 4%) due to its extensive first pass metabolism by the major metabolizing isozyme CYP3A4 and it is also a substrate of P-gp. Pomegranate juice (PGJ) was known to be a modulator of CYP3A4 and P-gp. Therefore, the aim of this study was to evaluate the influence of PGJ on the pharmacokinetics (PK) of saquinavir in wistar rats and on the P-gp mediated intestinal transport of saquinavir in everted gut sacs ex vivo. Â Rats were treated orally with saquinavir (100 mg/kg) alone and in combination with PGJ (0.5, 1.0 and 2.0 mL/200g, body weight) for 15 consecutive days. Blood samples were collected on 1st day in single dose pharmacokinetic study (SDS) and on 15th day in multiple dose pharmacokinetic study (MDS). The peak plasma concentration (Cmax)and area under the plasma concentration-time curve (AUC0-24) of saquinavir was increased with PGJ in SDS (p<0.001) may be due to inhibition of CYP3A4 and P-gp. But interestingly, the Cmax and AUC0-24 of saquinavir was decreased significantly with PGJ in MDS. This is may be due to induction of CYP3A4. The transport of saquinavir was increased in presence of PGJ and known P-gp inhibitors (Verapamil, Ketoconazole and Quinindine) across the rat everted gut sacs ex vivo. The present study results suggested that PGJ has both effects (inhibition, in SDS and induction, in MDS) on CYP3A4-mediated saquinavir metabolism in vivo and inhibitory effect on the P-gp mediated intestinal transport of saquinavir ex vivo. Further studies are needed to confirm this interaction at cellular level using cell lines and in humans.

FORMULA OPTIMIZATION OF ORALLY DISINTEGRATING TABLET CONTAINING MELOXICAM NANOPARTICLES Winarti, Lina; Ameliana, Lidya; Nurahmanto, Dwi
Indonesian Journal of Pharmacy Vol 28 No 1, 2017
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Meloxicam is one of oxicams anti-inflamatory drugs that are effective to relieve toothaches, arthritis, dysmenorrhea, and fever. Meloxicam in this study was milled with High Energy Milling (HEM) method to obtain its nano size and then direct compression method was used to produce Orally Disintegrating Tablet (ODT). ODT is designed to be rapidly dissolved on the tongue within a minute. It can be administered without water or chewing and may improve the bioavailability and effectiveness of the drug, and increase the patientâ€™s adherence. The present study aimed to understand the effects of Ac-Di-Sol and Kollidon CL as superdisintegrants, that were used separately or in combination, on the characteristics of nanoparticles meloxicam ODT. It was also to obtain the best proportion of combination between Ac-Di-Sol and Kollidon CL that can produce the optimum formula of meloxicam ODT. The effects of single or combined superdisintegrants were evaluated using Simplex Lattice Design (SLD). Ac-Di-Sol (X1) and Kollidon CL (X2) were the independent variables, while the dependent variables were friability (Y1), disintegrating time (Y2), wetting time (Y3), and percent meloxicam release after 60 seconds (Y4). Optimization of five nanoparticle meloxicam ODT formulas was conducted using Design Expert 7.1.5. The combination of Ac-Di-Sol 4.05mg (X1) and Kollidon CL 10.95mg (X2) in 150mg nanoparticles meloxicam ODT can produce optimal ODT characteristics. After verification there was no difference between predicted value and observed value with p value > 0.05.

Potency of use ferrous sulphate from iron waste workshop bubut for raw material pharmacy Sunardi Sunardi
Indonesian Journal of Pharmacy Vol 20 No 3, 2009
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Iron Deficieny Anemia (IDA) representing one of especial micronutrient deficiency that happened in Indonesia. IDA suffered by Indonesia resident about 100 million soul. One of effort of handling IDA is supplementation by ferro sulphate. To serve the purpose of raw material pharmacy have to be up to standard quality of set in Pharmacopoeia of Indonesia Edition IV.This Research aimed to make, to purify and characterization ferro sulphate from iron waste. The produce with reacted iron waste and acid sulphate 25% during 2 day. Crystal dissociated and purified by recrystalization, and then characterization with SEM-EDS.Result of research showed that ferro sulphate from iron waste of workshop bubut fulfill the standard quality of in Indonesia Pharmacopoeia Edition IV.Key words : iron waste, ferrous sulfate, recrystalization, characterization.

FORMULATION AND EVALUATION OF ORAL SUSTAINED IN SITU GELLING SYSTEM OF ROXATIDINE Mohammed Gulzar Ahmed; Chirag Kapoor; Sanjana A
Indonesian Journal of Pharmacy Vol 28 No 3, 2017
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Gel dosage forms are successfully used as drug delivery systems to control drug release and protect the medicaments from a hostile environment. The main objective of this present work is to formulate and evaluate in situ gels of roxatidine for the treatment of peptic ulcer. This system utilizes polymers that exhibit sol-to-gel phase transition due to change in specific physico-chemical parameters. In the present work in situ gels have been developed by using gellan gum and sodium alginate based on the concept of ion activated systems. Sol-to-gel transformation occurred in the presence of monovalent/divalent cations. Formulations were evaluated for clarity, drug content, in vitro gelling capacity, determination of pH, in situ release study, viscosity, gel strength, ex vivo gelation and stability study. All the results found to be satisfactory. Experimental part showed that viscosity of sols and gel strength was increased with increase in the concentration of polymers, also drug release gets sustaining. The formulations were therapeutically efficacious, sterile and provided sustained release of the drug over a period of time. These results demonstrated that the developed system is an alternative to conventional drug delivery systems and can improve patient compliance.Key words: In situ gels, Roxatidine, Peptic ulcer.

Estimation of total phenolic, total flavonoid content and evaluation of anti-inflammatory and antioxidant activity of Ixora coccinea Linn. stems R, Surana A; D, Wagh R
Indonesian Journal of Pharmacy Vol 28 No 2, 2017
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Ixora coccinea Linn. (Rubiaceae) has mentioned in Ayurveda as Paranti and traditionally stems used in inflammatory diseases like sprains, eczema, contusions and boils.Â Present study deals with evaluation of anti-inflammatory and antioxidant activity of extracts of I.coccinea stem. Anti-inflammatory activity was studied in vivo by carrageenan-induced paw edema in rat and in vitro by human red blood cell membrane stabilization method. Total tannin and flavonoid content of extracts was determined by using the Folin- Ciocalteu method and aluminum chloride method, respectively. Antioxidant activity was evaluated by in vitro assay involving nitric oxide scavenging, hydrogen peroxide scavenging, 2,2-Â diphenylpicrylhydrazyl (DPPH) radical scavenging, and ion chelating activity. Chloroform extract showed significant reduction in carrageenan induced rat paw edema (p<0.05) and protection of HRBC in hypotonic solution. Methanol extract contain more total tannin and flavonoid content as compared with petroleum ether and chloroform extract. All extracts showed concentration dependant free radical scavenging activity. Methanol extract and chloroform extract have shown better antioxidant activity and due to this antioxidant nature might be responsible for its anti-inflammatory activity. These activity supports to use of I.coccinea extract in traditional used in treatment of various inflammatory disaeses.

PHYTOCHEMICAL CONSTITUENTS AND HYPOGLYCEMIC EFFECT OF GYMNEMIC ACID EXTRACTS FROM BIG AND SMALL LEAF VARIETIES OF Gymnema Sylvestre R.Br Ramar Krishnamurthy; D. A. Animasaun; R. T. Patel; R. S. Ingalhalli
Indonesian Journal of Pharmacy Vol 27 No 2, 2016
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

Phytochemical and hypoglycemic effects of two varieties of Gymnema sylvestre were studied. The leaves of Big-leaf (MCL) and the small-leaf (ZMGL) varieties were grown in Uka Tarsadia University, Bardoli, India. Water, ethanol, methanol, petroleum ether, haxane and chloroform were used for phytochemical extraction from the dried leaves. Gymnemic acid was extracted and purified from the two varieties by Thin Layer Chromatography (TLC). Four groups of matured whisker rats (six per group) were induced with high-glucose level. Three groups were treated with standard drug Glibenclamide (5mg/kg), gymnemic acid extracts from MCL and ZMDL respectively while the fourth group served as experimental control. Hypoglycemic activities of extracts were evaluated using animals’ blood sample. Result showed water and methanol are best solvents for phytochemical extraction from the plant and the yield is higher in ZMGL than MCL. Also, gymnemic acid yield varied. From the results, hypoglycemic activities from the animals’ blood revealed that treatments from both MCL and ZMGL are not significantly different from standard drug Glibenclamide. The study concluded that water or methanol is appropriate solvent for phytochemical extraction from G. sylvestre leaves and extract from both lines of the plant could be utilized to reduce blood glucose levelKeywords: phytochemical extraction, extraction solvents, gymnemic acid, hypoglycemic effects

AN LC- MS/MS METHOD FOR THE DETERMINATION OF OMEPRAZOLE ON PROTON PUMP INHIBITOR IN HUMAN PLASMA T. Sudha; Kalan Kumar Reddy; P. V. Hemalatha; V. R. Ravikumar
Indonesian Journal of Pharmacy Vol 27 No 2, 2016
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

A sensitive and selective liquid chromatographic method coupled with tandem mass spectroscopy (LC-MS/MS) was developed for the quantification of omeprazole in human plasma. Lansoprazole was used as internal standard with plasma samples, extracted using 10mM ammonium acetate. A centrifuged upper layer was then evaporated and reconstituted with Acetonitrile: mobile phase buffer 70:30%v/v. The reconstructed samples were injected into a C18 column purospher star 5µ. The mobile phase was composed of ACN: mobile phase buffer (5mm ammonium bicarbonate buffer) in the ratio of 70:30%v/v with flow rate 1.0mL/min. The mass spectrometer was operated using positive ion mode and turbo electro spray ionisation. Nitrogen was used as the nebulizer, curtain, collision and auxiliary gases. Using MS/MS with multiple reactions monitoring (MRM) mode, omeprazole was detected without severe interferences from plasma matrix. Detection of omeprazole in human plasma was accurate and precision. This method has been successfully applied to the study of omeprazole in human specimensKeywords: Proton pump inhibitor, omeprazole, lansoprazole, LC-MS/MS, liquid liquid extraction

OPTIMIZING STRUCTURE-BASED VIRTUAL SCREENING PROTOCOL TO IDENTIFY PHYTOCHEMICALS AS CYCLOOXYGENASE-2 INHIBITORS Istyastono, Enade Perdana
Indonesian Journal of Pharmacy Vol 27 No 3, 2016
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

By employing Databases of Useful Decoys (DUD) and its enhanced version (DUD-E), several attempts to construct validated Structure-based Virtual Screening (SBVS) protocols to identify cyclooxygenase-2 (COX-2) inhibitors have been performed. Both databases tagged active COX-2 inhibitors for compounds with IC50 values < 1mM. In the search for phytochemicals as natural COX-2 inhibitors, however, most of their IC50 values are in the micromolar range, which will likely be identified as non-inhibitors for COX-2 by the available SBVS protocols. In this article, validation of an SBVS protocol by adding marginal active COX-2 inhibitors from DUD-E as active compounds is presented. Binary quantitative-structure activity relationship analysis by using recursive partition and regression tree method was performed subsequently to optimize the predictive ability of the protocol. The enrichment factor and the F-measure values of the optimized protocol could reach 44.78 and 0.47, respectively. The optimized protocol could identify 1 out of 9 phytochemicals as COX-2 inhibitors.

Modulatory effect of Drosera peltata J.E.Sm on development of metabolic syndrome in tumor bearing mice Raju A; Seeja S Raj; Christina AJM
Indonesian Journal of Pharmacy Vol 27 No 4, 2016
Publisher : Faculty of Pharmacy Universitas Gadjah Mada, Yogyakarta, Skip Utara, 55281, Indonesia

The purpose of the study conducted was to know the extent of protection over the cancer associated metabolic syndrome development after administration of ethanol and aqueous extracts of Drocera peltata against Dalton’s ascites lymphoma (DAL) and Ehrlich's Ascites Carcinoma (EAC) bearing mice. Animals were divided into thirteen groups with a normal control, EAC control, DAL control, two groups with standard drug 5-Flurouracil 20mg/kg+ DAL & EAC and eight groups with 250 and 500 mg/kg of ethanol and aqueous extracts of D.peltata + EAC & DAL, for respective cell lines. After 24 hours of both tumor cell inoculation, animals were treated with extracts,once in a day for 14 days continuously. The indicators for the development of metabolic syndrome such as changes in blood glucose, serum hormone and lipid profile were found with both cell line bearing mice. Both ethanol and aqueous extracts of D.peltata at doses of 250 and 500mg/kg significantly reduced the elevated blood glucose, hormonal and lipid profile changes. These results confirmed that ethanol and aqueous extracts can stabilize the tumor induced hormonal, blood glucose and lipid profile changes in tumor bearing mice. This effect might be due to the presence of pharmacologically active phytoconstituents in extracts.

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