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The impact of hot melt granulation method on propranolol hydrochloride physicochemical properties
Hot melt granulation is based on agglomeration by use of thermoplastic binder material that is solid at room temperature and softens and melts at higher temperature. By selecting a binder that is insoluble in water, melt granulation is a way of producing modified release granules, i.e. lipids/waxes to exhange the release of soluble drugs. The critical problem of this method is drugs instability because of heating. It has been studied the impact of hot melt granulation method on propranolol hydrochloride physicochemical properties. Physicochemical properties were evaluated including : water content titration – Karl Fischer, chemical structure analysis by Fourier Transforms Infrared Spectrophotometry (FTIR), and thermodynamic analysis by Differential Scanning Calorimetry (DSC). The results showed that hot melt granulation did not change the propranolol hydrochloride physicochemical structure but it changed anhydrate ß lactose to anhydrate a lactose. Key words : carnauba wax ; hot melt granulation; propranolol hydrochloride; physicochemical properties
Bioaccumulation of polycyclic aromatic hydrocarbons in Panaceus merquensis and Calappa flammea in south sea water Jogjakarta
Polycyclic aromatic hydrocarbons (PAHs) are a class of organic chemicals, composed of fused benzene rings, occurred in the environment due to incomplete combustion of fossil fuels. Health concerns are focused on the metabolite transformation of PAHs, which is carcinogenic, mutagenic and terratogenic. Due to their hydrophobicity in aquatic environment, PAHs are accumulated to the more lipophilic ecocompartments such as biolipid tissues and sediments, so PAHs can be distributed through food chain system. In this research, five kinds of PAHs (i.e. pyrene, benz(a)anthracene, benz(k)fluoranthene, benz(a)pyrene and perylene) in shrimps (Panaceus merquensis) and crabs (Calappa flammea) collected from the south sea beach water system at Jogjakarta were investigated. PAHs analysis were worked out by gas chromatography with flame ionization detector. It can be shown from this research that PAHs accumulate into each biota.The results showed that bioacumulation factor value of total PAHs in shrimp and crab are 2388.33-23486.54 and 13870.92-96078 respectively. The logarithmic value of bioacumulation factor of total PAHs in shrimp and crab are 3.378-4.371 and 4.142-4.983 respectively. According to the World Health Organization (WHO) recommendation, the level of PAHs concentration in water sample is safe.Key words : polycyclic aromatic hydrocarbons, bioacumulation, shrimp (Panaceus merquensis) and crab (Calappa flammea
The micromeritics parameter changing of three inhalation dosage forms
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 deviatio
FATTY ACID CONTENT IN DURIAN (Durio zibethinus, Murr) SEED
Fatty acids are part of fatty oils found in plants, animals and other organisms. Fatty oils are useful for human being, and they are also used as drug solvents, soaps, cosmetics and paint. Plant seeds usually contain fatty oil, protein and carbohydrate, useful for plants growth Durian seeds were just as common rubbish, therefore an investigation of fatty acids found in durian seeds were might be beneficial. Durian seeds were collected, dried, powdered, and was extracted with petroleum ether using Soxhlet apparatus. Physical and chemical parameters of Fatty oil i.e colour, acid value, saponification value, iodine value, and peroxide value were determined. Methyl ester of fatty acid composition produced by fatty oil transesterification was analyzed using a gas chromatography. The chemical parametrs of fatty oil are found to be: acid value (19,4 ± 0,17 ), saponification value (190,65 ± 0,84) , iodinevalue (81,7 ± 0,53) , and peroxide value (3,93 ± 0,12). Physical properties of fatty oil were : concentration of fatty oil was 6,12 ± 0,16 (%), w/w of dried seeds; transparenty yellow and durian odoured, the water content of durian seeds was 12,17 %. The composition of fatty acid containing in fatty oil was unsaturated fatty acid: oleic acid (14,95%) and linoleic acid (12,46%), and saturated fatty acid which is consist of stearic acid (45,84%) and palmitic acid, ( 26,75 %), relatively to pure stearic acid (E.Merck, pro analysis).Key Word: Durio zibethinus Murr, durian seed, fatty acids, identificatio
PREFORMULATION OF DICLOFENAC SODIUM SUSTAINED RELEASE BY ION EXCHANGER RESINE
The aim of the study was to find out a formula of granules giving a constant release of drug and also to search for the influence of pH on the drug release from the formula. One type of drug-resin complexes was used in this study ion exchanger the complex of diclofenac sodium and dowex. After 12 hours mixing the drug-resin complex was dried at 40 oC in an oven for 3 days. Afterwards, they were granulated and shieved. The particle size used were 20-40 mesh. The granules were tested for the dissolution of diclofenac sodium from the granules. The dissolution experiments were performed in a modified model of USP XX and the dissolution media used were phosphate buffer with the pHs of 5,8; 6,8 and 7.6 and the temperature was maintained at 37 oC. The amount of diug released in to the medium was assayed spectrophotometrically. The extent of dissolution was expressed as dissolution efficiency in 8 hours (DE8, % ). The results showed that the extent of dissolution of dtclofenac sodium from the granules complexed with the resin were low. The correlation between the amount of drug release from the complex and time was linier with the highest coefficient correlation having the ratio of l:5. The higher the pH values of the media, the higher the drug release from granules was. The drug release from drug-resin complex was well controlled which may be used for making a sustained release dosage form.Key Word : sustained release, diclofenac sodium, ion exchanger resin, granule
Cost-minimization analysis of intravenous sulbenicillin versus coamoxiclav for cesarean section
The cost of antibiotic prophylaxis sulbenicillin versus coamoxiclav (in term of medication use and treatment of complications) to treat cesarean section was compared.The medical records of patient receiving intravenous sulbenicillin orcoamoxiclav for the treatment of cesarean section in PKU Muhammadiyah Hospital were retrospectively reviewed. Data were collected for patients treated from January 1, 2000 to December 31, 2000. Patient data collected included patient data based, indication of cesarean section, abdominal incision and oral antibiotics. Cost data collected included drug acquisition cost, cost of drug supplies, nursing time to administer the agents and cost of managing complication.The medical records of 98 patients were identified and reviewed. The average length of stay was 4.85 days for the sulbenicillin group and 4.90days for the coamoxiclav group. The average total including the cost of complication was Rp. 140.509 in sulbenicillin group and Rp. 376.310 in coamoxiclav group.In conclusion, the study demonstrates that intravenous coamoxiclav has a higher cost than that of intravenous sulbenicillin. This result can be used to assist institution, clinicians and pharmacists in determining the most appropriate and efficient use of drugs. These data can be a powerful tool to support various clinical and policy drug use decisions, for example included formulary management and drug use policy or guidelines.Key words: antibiotics, cesarean section, cost
Evaluation of using Antihipertensi of Angiotensin Renin system to kidney protection on Diabetic patient in X hospital of Yogyakarta
The renin-angiotensin-system antihypertensive drugs (RAS), i.e. Angiotensin Converting Enzyme Inhibitors (ACEIs) and Angiotensin II Receptor Antagonists (AIIRAs) are prescribed for diabetes patients to slow the nephropathy progression. There are only limited clinical evidence of the RAS for Indonesian patients. This study aimed at assessing the antihypertensive drug selection and the renoprotective effect on Indonesian patients.The study was done with retrospective survey and descriptiveevaluative design. A total of 116 diabetic patients were participated in the drug selection assessment and the renoprotective effect among 52 patients was analyzed by Kruskal-Wallis non-parametric statistics. The results showed that the antihypertensive drug selection consisted of RAS (ACEIs 48% and AIIRAs 11%), non-RAS 22%, and without antihypertensive drugs 19%. The RAS antihypertensive drugs were administered at 53%; 56%; 92%; and 71% by normal; mild; moderate; and severe kidney dysfuntion patients respectively.The annual clearance creatinine (Clcr) reduction were 3.93; 9.95; 0.85ml/min and the Clcr reduction in 23 months were 9.27; 8.66; 7.76% for non-RAS; without; and RAS antihypertension respectively, but the effects were not significantly different (p>0.05). In conclusion, renoprotection on diabetic patients by RAS was not more superior than that by non-RASantihypertensive drugs. Key words: Diabetic Nephropathy, Renoprotection, ACE-Inhibitors (ACEI), Angiotensin II Receptor Antagonists (AIIRA)
THE INFLUENCE OF DISTILATION TIME, POWDER SIZE, ON THE CINAMYLALDEHYDE CONTENT AND VOLATILE OIL Cinnamomum burmanii Nees ex. Bl. BARK
The content of volatile oil in samples depends on the harvest time, distilation method, sample powder size, and location of sample cultured. The aim of this study was to investigate the influences of interval time of distillation and mesh size of bark powder, upon the concentration of major component (cinamylaldehyde). The distillate was collected with various interval times 1, 2, 3 and 4 hours and it was counted after the first drop of distillate. The mesh size of bark powder (4, 8 and 20 mesh) was set after the interval time of distillation had been studied. The major component was analysed using Gas Chromatography (GC). The results showed that the interval time of distillation at the second hour gave the highest volatile oil and cinamylaldehyde contents in the relative prosentage 0.19 % and 29.36 % respectively, compared with the first hour distilate, (0.16 %, 24.88 %), third hours distilate (0.14 %, 23.29 %) and fourth distilate (0.08 %, 17.65 %). The powder size of bark (8 mesh) gave the highest volatile oil and cinamylaldehyde contents (0.22 %, 32.81 %), compared to powder size of 4 mesh( 0.17 %, 20.45 %) and 20 mesh (0.19 %, 21.32 %). The results is still lower than standard of cinnamon oil, (cinamylaldehyde content 60 %). The lowering cinamylaldehyde content could be caused by low quality of material, collected from marketing method, early harvesting time, and storing for long.time.Key words: C. burmanii, bark, distilation time, cinamylaldehid
In Vitro CYTOTOXIC ASSAY OF CHLOROFORM EXTRACT OF Brucea javanica L .(Meer), Ipomoea batatas Poir., Mussaenda pubescens Ait.F., AND Portulaca oleracea L. TO HeLa CELLS
Some plants, such as Ipomoea batatas Poir., Mussaenda pubescens Ait. F., Portulaca oleracea L., Brucea javanica L. (Meer), have been used traditionally to treat cancer, even though the scientific base of this activity has yet been completely investigated. The study was conducted to evaluate the cytotoxic activity of these plants on HeLa cell lines.The cytotoxicity of chloroform extract from these plants were determined using micro radioactive method by measuring an incorporation (3H)-hipoxanthine on the cells after 24 and 48 hours incubation with each extract, using doxorubicine as a positive control. Extract free cell culture was refered to as 100% growth. IC50 value, showing 50% inhibition of the cell growth, was determined based on the concentration versus percentage inhibition curves.The result showed the extract B. javanica was the most active to hela cells with the IC50 value of 13.69 1.07 and 55.78.4 g/ml after 24 and 48 hours incubation respectively.Key words: Ipomoea batatas Poir., Mussaenda pubescens Ait. F., Portulaca oleracea L., Brucea javanica L. (Meer), Cytotoxic, HeLa cell lines
EFFECT OF PENTAGAMAVUNON-0 TO THE THEOPHYLLINE PHARMACOKINETICS IN RATS
The research was aimed to observe pentagamavunon-0 activities to theophylline pharmacokinetics in rats. The study of interaction pentagamavunon-0 and theophylline was conducted employing a completely randomized design using male Wistar rats which were divided into 5 groups (6 rats for each group). The groups were given a single oral theophylline 25 mg/kg BW as a control group and were administered single oral pentagamavunon-0 2, 5, 10 and 40 mg/kg BW each dose 4 hours before treatment with theophylline. Serial blood samples (0,2 ml) were withdrawn at various interval via the tail vein for HPLC analysis of unchanged theophylline in blood. The concentration of theophylline was determined based on a standard curve. The concentration-time data determines theophylline pharmacokinetics i.e. Ka, Cmaks, tmaks, AUC0-, Vdss, t1/2 elimination, Clt and MRT. The results indicated that pentagamavunon-0 was found to be able to decrease theophylline clearance 40-51% (P<0.05). The decrease in clearance causes the prolonged life of theophylline in the body.Key words : Pentagamavunon-0, Theophylline, Pharmacokinetic