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Optimization of chitosan and sodium carboxymethylcellulose as mucoadhesive system in theophylline tablet
Mucoadhesive tablet for asthma treatment were prepared by mixing theophylline with two variations of polymers. The purpose of this research was to controlled drug release from the dosage form. Theophylline mucoadhesive tablets were prepared by direct compression using chitosan and sodium carboxymethylcellulose as mucoadhesive polymers. Mucoadhesive strength measured using rabbit gastric mucosa and in vitro drug dissolution was subjected in a hydroclorid acid buffer pH 1.2 for 10 hours. The optimized formula was obtained by analyzing both evaluation using factorial design. Formula with 5.4 % of chitosan and 14.5 % of sodium carboxymethylcellulose followed zero order kinetics. The optimized formulation showed by 8.38-10.91% of chitosan and 28.84-29.09% of sodium carboxymethylcellulose with mucoadhesive strength between 25-40 gram and 43.5%-55% drug was released in 10 hours.Key words: Mucoadhesive, chitosan, CMC Na, E, factorial design.
Potency of cinnamaldehyde of cinnamon oil as an antidiabetic compound
Cafeic and cinnamic compounds have been reported to give an excellent performance as α-glucosidase inhibitor. Inhibition of α-glucosidase in the intestine of mammals are able to lower blood sugar levels of the carbohydrates metabolism so it can reduce postprandial hyperglycemia which can prevent chronic complications of Diabetes Mellitus (DM). Based on cafeic and cinnamic structures in terms of organic chemistry and economic considerations, it can be offered a very promising alternative to provide their derivative compounds of cafeic from cinnamon oil, which is cinnamaldehyde. Cinnamaldehyde can be isolated from cinnamon oil by addition of sodium bisulphite to provide salt compounds which are separated easily from the mixed system. The aldehyde compound can be obtained by acid addition. Structure elucidation of cinnamaldehyde was done by mean of an infra red spectrophotometer and a gas chromatography-mass spectroscopy. Activity test of anti-diabetic compounds was carried through the measurement of the concentration of minimum resistance against α-glucosidase activity. Cinnamaldehyde which is isolated from cinnamon oil was yellowish oil and cinnamaldehyde’s yield was up to 42.67%, and its purity was 99.8723%. Structure elucidation of cinnamaldehyde by mean of infra red spectrophotometer (FTIR) showed carbonyl vibration at 1676 cm-1, -C-H aldehyde at 2813.9 cm-1 and 2742.6 cm-1. From mass spectra, it can be known that cinnamaldehyde had M+ 132 with m/z of main fragmentation were 131, 103, 77, and 51. Inhibition activity of α-glucosidase test showed that inhibitory concentration at 50 ppm of cinnamaldehyde was 93.29%, and IC50 to the α-glucosidase was 27.97 ppm.Key words :cinnamon oil, cinnamaldehyde, anti-diabetic
Medicine advertisements: evaluation and implementation of cema-community method
Non-prescription medicines are advertised widely to general public. These advertisements attempt to influence consumers’ choices about medicines. Since the advertisements rare to give objective information, therefore it may affect people’s perception and have potential harmful effect for public health. In order to improve the use of medicines by general public, the CEMA-community (Critical Evaluation Medicine Advertisement by the community)) was proven effective empower community in evaluating medicine advertisements. The objectives of the study, therefore, were to investigate medicine advertisements, and improve knowledge and skills of participants in critically evaluating medicine advertisements. Medicine advertisements running within the period of study were evaluated and analyzed according to the Indonesian legal requirements. Community empowerment to improve participants’ knowledge and skills was conducted using CEMA-community method. The method consisted of two activites, the first was a brief lecture and the second was small group discussions in a problem-oriented approach. Data on knowledge was obtained by questionnaire. Data on skills was assessed by the number of inappropriate claims they could identify the advertisements. All data was collected at baseline, immediately, and one month after intervention. Medicine advertisements in television media accounted for 15% off all commercials, with 21.53%; 17.98%; 14.17%; and 10.08% being medicine products for influenza, analgesic/antipyretic, supplement, and cough, respectively. Incomplete and misleading information mostly appeared in the advertisements. Intervention study showed that the average of participants’ knowledge in subtopic of medicine misleading was low and could be increased from 34.2 (pretest) with maximum score 100, to 65.3 (post I) and 58.3 (post II). Participants’ skills also improved immediately after intervention and this was maintained at the one month follow up (score means: 3.33; 26.67; 26.67 of maximum score 100, at pre test, post I, and post II, respectively).Key words: medicine advertisements, community empowerment, CEMA-community method, knowledge; skills
Effect of the combination of curcuminoid and essential oil on the serum ureum and creatinine level of patientswith osteoarthritis
The curcuminoid of Curcuma domesticaVal. rhizome and the essential oil of Curcuma xanthorrhizaRoxb. rhizome can be used for rheumatic treatment,but no enough data regarding those side effects. This study aimed to determine the efect of curcuminoid of Curcuma domestica Val. combined with essential oil from Curcuma xanthorriza Roxb. to the serum ureum and creatinine level of patients with osteoarthritis. This treatment was compared tothat of piroxicam. This was a Prospective Randomized Open end Blinded Evaluation (PROBE), involving 38 patients with knee osteoarthritis.The treatment group were given the combination of 15 mg curcuminoid of Curcuma domestica Val. and 100 mg essential oil of Curcuma xanthorrhizatwice daily for two weeks. The control group were given 10 mg piroxicam twice daily for two weeks. In the treatment group the serum ureum level decreased 4.58±6.20% mg, while in the control group the ureum level increased 1.68±8.24% mg. In the treatment group the serum creatinine level decreased 0.12±0.36% mg, while in the control group the creatinine level increased 0.18±0.29% mg. Decreasing of serum ureum level in the treatment group was significantly different compared to increasing of that level in the control group (p<0.01). Decreasing of the creatinine level in the teatment group was significantly different compared to increasing of that level in the control group (p<0.01).Key words: Curcuminoid, Essential Oil, Ureum, Creatinine, Osteoarthriti
Optimization formula gastroretentive tablet of ranitidine HCl with floating system
Ranitidine HCl is an H-2 receptor antagonists for the treatment of peptic gastric secretion with a small bioavailability, so that should be developed in a sustained release dosage form are retained in the stomach. Ranitidine HCl floating tablet was formulation by effervescent system. Simplex lattice design was applied to optimize the formula of ranitidine HCl floating tablet by varying levels of Methocel K15M 100-185 mg, sodium bicarbonate 15-100 mg, and citric acid0-85 mg. The Optimum formula determined by superimposed contour plot from various parameters: flowability of granules, physical properties of tablet and drug release using Design-Expert®program. Based on superimposed contour plot obtained optimum formula for the area in the range of Methocel K15M 100-145 mg, sodium bicarbonate 20-80 mg and citric acid 25-80 mg.Key words: Ranitidine HCl, Gastroretentive, Simplex lattice design
Influence of filler-binders on ibuprofen iablets with direct compression method
Ibuprofen is a active ingredient that have low melting point, but it has poor flowability, and poor compactibility, this causes ibuprofen tablets are not suitable to be made by direct compression method. The use of appropiate filler-binders can improved the flow properties and compactibility powder that can be made by direct compression. Filler binders commonly use are Avicel PH 102, Emcompress, SDl, and Starch 1500. Formula tablet ibruprofen using Avicel PH 102 as filler-binder will produce tablet with good hardness, low friability, fast disintegrating, and high dissolution. This is because the hydrophilic properties and plastic deformation which is owned by Avicel PH 102.Key words:Ibuprofen, Avicel PH 102, direct compressio
Determination of total phenol, condensed tannin and flavonoid contents and antioxidant activity of Uncaria gambirextracts
Uncaria gambir, a well known Southeast Asia plant have been previously used as an alternative medicine for treatment such as diarrheal, sore throat and spongy gums. Due to its useful properties, in this study we have analysed the total phenol, condensed tannin, flavonoid content and antioxidant activity of Uncaria gambir in three different solvent extracts. Characterization and quantification analysis using Fourier Transform Infrared (FTIR) spectroscopy and reverse phase-high performance liquid chromatography (RP-HPLC) has confirmed that the major chemical constituents of Uncaria gambir are mainly catechins. It was revealed that the ethyl acetate gambir extract gives the highest catechin content and antioxidant activity compared with other solvent extracts.Key words: Uncaria gambir, antioxidant activity, condensed tannin, flavonoid
Development of fast disintegrating tablet formula of ketoprofen-β-cyclodextrin inclusion complexes
Ketoprofen is one of non steroidal anti inflammatory drugs (NSAID) used for rheumatoid arthritis. However, unpleasant taste of ketoprofen leads to difficulty in the formulation, in particular for oral route. Therefore, in present study, a technique to mask the unacceptable taste of ketoprofen was developed. Then, a fast disintegrating tablet on this inclusion complex was established for rapid release and faster analgesic effect of ketoprofen. Taste masking was prepared by complex inclusion with β-cyclodextrin. The ratio of ketoprofen and β-cyclodextrin was varied. The fast disintegrating tablet was formulated with direct compression using various ratios of mannitoland lactose as tablet diluent, the main factor influencing the successful of fast disintegrating tablet. Evaluation of final product was performed according to compendial standard and specific requirements for fast disintegrating tablet. The best ratio from ketoprofen and β-cyclodextrin was 2:3 with concentration of ketoprofen in inclusion complex was 40.32%. The tablet met standard requirement was resulted with the composition of ketoprofen-cyclodextrin equivalent to 50 mg of pure ketoprofen and mannitol and lactose (ratio 1:1) as tablet diluent. Fast disintegrating tablet of modified ketoprofen in inclusion complex was fulfilled standard specification for ketoprofen tablet with better acceptance.Key words:ketoprofen, inclusion complex, fast disintegratingtablet, beta cyclodextrin
The effect of the extract of pasak bumi roots (Eurycoma longifoliaJack.) on liver function
The aim of this research is to study the effects of the methanol extract and its derived fraction (n-hexane, chloroform, ethyl acetate, and methanolwater) on liver function of male rats. The treatment groups were administered 500 mg/kg body weight of metanol extract and its derived fractions (n-hexane, chloroform, ethyl acetate, n-butanol, methanol-water) of E. longifolia for 7 consecutive days. Positive control group received 25 mg silymarin/kg body weight and negative control group received 2 mL aquadest/kg body weight daily for 7 consecutive days. Liver function was monitored by measuring alanine transaminase (ALT), aspartate transaminase (AST), total protein, alkaline phosphatase (ALP), total bilirubin, direct bilirubin, and indirect bilirubin consentrations in the serum. Compared with control, oral administration of methanol extract and derived fractions of methanol extract of E. longifolia root had no significant effects on liver function (p>0.05). Methanol-water fraction gave similar results to silymarin.Key words: Eurycoma longfolia Jack.,liver function, biochemical blood Histopatholog
Synthesis and cytotoxicity test of LR-2 on breast cancer cell line T47D
LR-2 is a compound analog of monastrol, an anticancer agent, which has been succesfully synthesised through the application of Biginelli reaction and one of LR compound series that synthesised in Faculty of Farmacy, Universitas Gadjah Mada. This reserach was aimed to synthesized the LR-2 compound and to investigate the cytotoxicity of LR-2 on breast cancer cell line. The reaction was carried out by using the one pot reaction method. In this reaction benzaldehyde, 2-indanone and thiourea were reacted together for 6hours in acid catalyst. The cytotoxicity test was carried by using breast cancer cell line the MTT assay method and the LC50 was ditermined by using the probit analysis with Miller and Tainter method. The product was isolated by using preparative TLC in 54 % yield. The structure was elucidated by spectroscopymethods (UV-Vis, H-NMR, IR and GC-MS).The LC50 is 159 µM.Keywords : LR-2, benzaldehyde, 2-indanone, thiourea, T47D