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    Optimization of chitosan and sodium carboxymethylcellulose as mucoadhesive system in theophylline tablet

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    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

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    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

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    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

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    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

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    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

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    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

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    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

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    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

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    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

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    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

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