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Feasibility of transdermal transport of atenolol by combination of iontophoresis and oleic acid pretreatment
Get PDFAtenolol has a low oral bioavailability and a short elimination half-life. Therefore, alternative route and delivery system is important. Transdermal iontophoresis, i.e. a systemic drug delivery via the skin, implementing a low intensity of electrical current, is one attractive candidate. This study evalu ated feasibility of atenolol transdermal transport when iontophoresis is applied after enhancer pretreatment. There were 4 formulas prepared; 2 implemented iontophoresis for 3 hours (current density: 0.25 mA/cm2) while the others did not use iontophoresis. The enhancer was oleic acid (5 or 10% as a mixture in propylene glycol) with duration of pretreatment of one hour. Transport was evaluated in the diffusion studies across the fresh rat skin in a static-vertical diffusion system. Data were analyzed based on the numeric convolution method to obtain simulated Cp profiles as well as AUC of Cp profiles. Based on the simulated Cp, the best transport was achieved in Formula 3, where iontophoresis is performed across the skin, pretreated with 5% oleic acid for one hour. The value of simulated Cp indicated achievement of therapeutics level of atenolol, suggesting the feasibility of the atenolol delivery by iontophoresis.Key words : atenolol, transdermal, iontophoresis, enhance
Niosomes entrapment capacity of ketoprofen and prediction transdermal administration
Get PDFNiosomes are vesicles system that have applications in the delivery of lipophilic,hydrophilic and amphiphilic drugs. Ketoprofen, is very insoluble in water and cause gastric irritation when taken orally. It is very important to develop a transdermal delivery system for ketoprofen. This research was aimed to design niosomes which can deliver ketoprofen via transdermal route. Experiments were designed to incorporate ketoprofen into niosomes with lipid film hydration method. Lipid mixture consist of cholesterol and sorbitan ester (span 20, 60, 80). Niosomes which can deliver ketoprofen trough the skin barrier determined by calculating amount of ketoprofen in the blood of rabbit. The type of sorbitan ester was chosen based on the highest drugs entrapment and ketoprofen as drugs model. Preparation of niosomes was optimized for the highest percent drug entrapment by increasing molar concentration of lipidmixture with the stable comparison of 1:1. This research result are niosomes with lipid mixture span 60 and cholesterol have the highest drug entrapment efficiency of niosomes 66.16% with range size 1–6 µm. Niosomes can deliver ketoprofen to the systemic circulation via transdermal route with plasma level concentration achieved in 1.5 hour.Key words: niosomes, ketoprofen, transdermal
The determination of quercetin in Plectranthus scutellarioides(L.) R.Br. leaves extract and its In SilicoStudy on Histamine H4 Receptor
Get PDFPlectranthus scutellarioides (L.) R.Br., or jawer kotok, Family Lamiaceae, grows widely in Indonesia, and has a long history of therapeutic usage in Indonesian traditional jamuto cure various diseases. The brownish purple leaves of Plecranthus contain alkaloids, saponin, flavonoids, tannin, volatile oils, and quercetin which has been proven to exert antiinflammatory activity. In this research, a determination of quercetin in Plecranthus leaves extract was performed and followed by a study of its interaction with histamine H4 receptor to understand its anti-inflammatory activity. The dry leaves were macerated by using a mixture of methanol and water (1:1) for 48 hours and the solvent was evaporated at low temperature (40-50oC). Analysis of quercetin in the extract was performed by using reversed-phase HPLC method LC-10AT VP (Shimadzu), Atlantis Hilicsilica C18 (Waters®) 150 mm x 4.6 mm, 5 µm as stationary phase and a mixture of acetonitrile, phosphoric acid, and methanol (40:50:10), flow rate 0.8 mL/minute. In silicostudy of quercetin with histamine H4 receptor was performed by using AutoDock Tools 3.0.5. Histamine H4 receptor (H4R) belongs to G protein-coupled receptors which is involved in arthritis, asthma, and inflammations. The 3D structure model of H4R was built by using MODELLER 9v7. Quercetin contained in Plecranthus leaves extract was 0.05 %. This compound interacted with H4R viahydrogen bond formation with Lys158 (2.006 Å) and Glu182 (2.048 Å), and van der Waals interaction with Trp90, Leu91, Asp94, Tyr95, Phe168, Thr178, Ser179, Tyr319, Phe344, and Tyr340, therefore Plecranthus leaves extract might have a chance to be used as histamine H4 receptor inhibitor.Key words : histamine H4 receptor, in silico study, Plecranthus leaves, Plectranthus scutellarioides, querceti
Influence of learning and growth toward internal business processes: case studies on Departement of Hospital Pharmacy in DIY
Get PDFHospital Pharmacy have revenue contribution to the Hospital reached 40-60%, thus becoming one of the hospital revenue center. However hospital pharmacy services in Indonesia are still many shortcomings, is considering several constraints such as the ability of pharmaceutical workers, the limited ability of hospital management, hospital management policies, and limited knowledge of the relevant parties of hospital pharmacy services. Such conditions must be efforts to change with the development of learning and growth factors, because these factors (human capital, organizational capital and information capital) and that effective management is a source of sustainable competitive advantage. The research objective is to determine the relationship and influence of learning and growth to the internal business processes in Hospital Pharmacy. Kind of research is non-experimental research is associative. Research tool includes a questionnaire indicators of learning andgrowth, and internal business processes. The subjects was the head of hospital pharmacy in the hospital region of Daerah Istimewa Yogyakarta (DIY). Sample size was 35 hospital. In addition to sending questionnaires, random interviews will be conducted on several hospital pharmacies to enrich the results of the survey questionnaire. The data was analyzed by correlation and linear regression to determine the relationship and influence the learning and growth factors to the internal business processes in hospital pharmacy. Results obtained from statistical calculations with 95% confidence show that there is a strong relationship between the organizational culture against internal business processes with r value of 0.981 with a contribution of 96.20% of theorganizational capital of the sustainability of the internal business processes in Hospital pharmacy in Yogyakarta Special Region. There is not significant relationship between the human capital against internal business processes. There is not significant relationship between the information capital against internal business processesKey words:learning and growth, internal business processes, the hospital pharmacy
Antibacterial activity of ethanolic extract and fraction of leaves of singawalang (Petiveria alliaceae) against resistant bacteria
Get PDFOne of the plants that grow in Indonesia, and still does not use widely is singawalang (Petiveria alliaceae) from Phytolaceae family. Traditional herbal medicine preparations contained of Petiveria alliacea in the Caribbean, Latin America, West Africa and other regions for hundreds years has been used to treat pain, colds, inflammation, tumor, bacterial and fungal infection,hyperlipidemia, diabetes and other diseases. This study aims to determine the antibacterial activity of singawalang growth in Indonesia against resistant bacteria to antibiotics. The minimum inhibitory concentration (MIC) and minimum bactericidal concentration(MBC) were determined by microdilution broth method and type of antibacterial action were determined by observing the profile of bacterial growth curve. Ethanol extract of dried leaves showed activity against bacteria i.e. MRSA (Methicillin-Resistant Staphylococcus aureus), MRCNS (Methicillin-Resistant Coagulase-Negative Staphylococci), VRE (VancomycinResistant Enterococcus). Further studies conducted by reviewing the type of work by looking at the growth curve and the observed changes in cell walls by scanning electron microscopy (SEM) at MRCNS (Methicillin-Resistant Staphylococcus coagulase-Negative). The results showed that ethanol extracts and all fractions showed good antibacterial activity against resistant bacteria, are bacteriostatic hexane fraction until the concentration of 8 MIC and change the morphology of the cell wall of MRCNS.Key words:Singawalang, Antibacteria, Broth Microdilution, bacterial growth curve, SEM
Evaluation of side effect of risperidon on schizophrenic patient in Amino Gondohutomo hospital Semarang
Get PDFSchizophrenia is a psychiatrical chronical disease of human being’s mind which can influence someone so that it bothered the interpersonal relation and ability to have a social relationship. Antipsychotic drug can be used to overcome the symptom of schizophrenia, for example risperidone. This study was aims to evaluate the side effects of the use of risperidoneon the inpatient of Dr. Amino Gondohutomo Mental Hospital Semarang for a month in the period of February 2008. This evaluation covers the side effects of medicine that occur due to the use of risperidone, concomitant administration of risperidone and other antipsychotic, drug interaction,and also executed therapy of the side effects of the risperidone. This study followed the descriptive analysis, while the data collecting was conducted prospectively. The subjects of research were represented by the entire patients of the inpatient ward of Dr. Amino Gondohutomo Mental Hospital Semarang during the period of February 2008 and fulfilled the inclusive criteria. The inclusive criteria covered the patients who were diagnosed as paranoid schizophrenia, hebephrenic schizophrenia, catatonic schizophrenia, undetailed schizophrenia and received anti-psychotic risperidone medication. Based on these criteria 31 samples were found. The result of the study indicated that the most possibility of side effects of the use of risperidone was agitation (19.51 %), with the most anti-psychotic combination of risperidone and haloperidol (45.83 %) and there were 15 interactions which could potentially cause a drug side effect.Key words: schizophrenia, drug side effects, anti-psychoticrisperidon
Scientific Aspects of Water Extract Katola (Arcangelisia flava L. Merr) as Antidiarrhea Agent in Mina South Sulawesi
No full textWater extract of katola (Arcangelisia flava L. Merr) stem is traditionally used in communities Muna Distric for the treatment of many diseases, including anti diarrhea. According to the information of Muna Distric Health Office, diarrhea is one of the 10 groups diseases in this district. The objective of this study was conducted to determine the potential antimicrobial, acute toxicity and identified of the water extract of bioactive compounds and alkaloid relative concentration content. Infection of microbial was induced by oral administration of Shigella flexneri ATCC 12022 1 x 108 CFU/mL. Boiling water of katola dose 12 mg/kg, 24 mg/kg and 48 mg/kg body weight and the antibiotic ampicillin 24 mg/kg administered 2 times daily for 5 days. The number of S. flexneri in feces were determined every day. The toxicity of water extract of katola stem is determined based on the value of LD50 acute oral toxicity testing followed by guidelines OECD 423. The bioactive compounds was determined by bioautografi method and the concentration alkaloid relative content was calculated as berberine hydrochloride. The results showed that boling water extract of katola stem did not cause toxic symtoms, with LD50 > 31.5 g/kg body weight (unclassified) or 104 times the dose therapy of human. In vitro, the Minimum Inhibition Concentration (MIC) and Minimum Bactericidal Concentration (MBC)value of the boiling water were 1.2 and 2.4%, respectively. In vivo, the boiling water dose 48 mg/kg body weight given twice a day have an effect on eradication the S. flexneri 100% by day 5. Bioactive compounds of antimicrobial in the water extract is alkaloid berberine HCl. A cocentration of berberine hydrochloride in water exract stem and leaves dosage use of the public were 16.7% and 0.75% respectively.Key words: Katola, toxicity, anti diarrhea, antimicroba, Arcangelisia flava L. Merr
Development of ciprofloxacin radiopharmaceutical formulation in single vial
Get PDFBacterial infection diseases is the greatest death causes in Indonesia. Detection of the deep-seated infection location caused by the gram positive and gram negative bacteries could be done with nuclear technique using 99mTc-ciprofloxacin radiopharmaceutical. In order to fulfill the necessity of this radiopharmaceutical, the development of formulation in single vial based on Sn(II) chloride and tartaric acid instead of Sn(II) tartrat has been carried out. The aim of this investigation is to obtained the optimum condition of 99mTc-ciprofloxacin preparation with maximum labelling efficiency. Several parameters influencing the labelling process of 99mTc-ciprofloxacin such as the amount of tartaric acid, pH of the reaction, the amount of Sn(II) ion as a reducing agent and the incubation time has been studied. The labelling efficiency and the radiochemical purity of 99mTc-ciprofloxacin were determined by double chromatography system using Whatman I/methyl ethyl keton to determine the free 99mTc-pertechnetate and ITLCSG/(ethanol:water:ammonia = 2:5:1) to separate the free 99mTc-reduced. The optimum preparation condition was obtained at pH = 2.95-3.20, 2 mg of ciprofloxacin, 0.06 µg of tartaric acid, 50 µg of SnCl22H2O and 15 minutes incubation time at room temperature, gave 90-93 % of labelling efficiency, in wchich was stable for 20 minutes at room temperature. Beside that, studies on the effect of Na99mTcO4 solution volume to the 99mTc-ciprofloxacin labelling efficiency was carried out. Labelling with up to 0.3 mL of Na99mTcO4 solution volume gave less than 90 % labelling efficiency.Key words: radiopharmaceutical, ciprofloxacin, 99mTc, single via
Testing of antiplasmodium activity substance from endophytic fungus of Artemisia annua L.
Get PDFMalaria is a life-threatening disease caused by Plasmodium parasites. The rapid spread of malaria-quinoline resistance enforce to find of new antimalaria drug. Artemisia annua L having artemisinin as secondary metabolites, has been used as antimalaria agent for long time. One of source of bioactive compound is endophytic fungus. This fungus can produce similar bioactive compound to host plant. The thin layer chromatography result showed that endophytic fungusfrom A.annua had similar chromatogram profile with artemisinin. This metabolite was not secreted in the fermentation medium, but was kept in the fungus mycelium. The result of the haem polymerization inhibitory activity assay showed that this secondary metabolites inhibited the haem polymerization. Ethyl acetate extract of fungus A had IC50 value 0.824 ± 2.89 μM to inhibit the haem polymerization; fungus E was 0.861± 2.43 μM; and fungus F was 1.394 ± 3.73 μM.Key words : endophytic fungus, antiplasmodium, the haem polymerization, IC50
Identification of physical interaction between trimethoprim and sulfamethoxazole by contact method koflerand crystallization reaction
Get PDFIdentification of solid state interaction between TMP and SMZ by hot contact method Kofler and crystallization reaction had been carried out. The results of hot contact method Koflershown formation a new crystalline habit as long and thin needle shaped on contact zone (mixing zone) between Solid TMP and SMZ. It had a different melting point in compared to its single component. Crystallization reaction between two of supersaturated solution of component TMP and SMZ in methanol solvent also indicated the growth of crystal habit as similar as hot contact method Kofler. Solid state interaction between TMP and SMZ was confirmed by microscopic SEM, powder X-ray diffraction, and thermal DSC. Microscopic analysis by SEM showed significantly the change of habit and morphology of crystal as long and thin needle shaped. New powder X-ray diffraction (PXRD) interferences peaks were observed in addition to PXRD interference peaks of each component that proved formation of cocrystalline phase. Thermogram DSC indicated a new endothermic peak corresponding to melting point of a new cocrystalline phase at temperature 178,82 °C.Key words : trimethoprim, sulfamethoxazole, physical interaction, cocrystalline phas