PERILAKU DISOLUSI KETOPROFEN DAN INDOMETASIN FARNESIL TERSALUT GEL KITOSAN-GOM GUAR

2012 ◽  
Vol 12 (1) ◽  
Author(s):  
Purwantiningsih Sugita ◽  
Bambang Srijanto ◽  
Budi Arifin ◽  
Fithri Amelia ◽  
Mahdi Mubarok
Keyword(s):  
Room Temperature ◽  
Guar Gum ◽  
Tween 80 ◽  
Chitosan Solution ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Magnetic Stirrer ◽  
Dissolution Behaviour ◽  
Shrimp Shell Waste

Chitosan, a modification of shrimp-shell waste, has been utilized as microcapsule. However, it’s fragile gel property needs to be strengthened by adding glutaraldehyde (glu) and natural hydrocolloid guar gum (gg). This research’s purposes were to study dissolution behaviour of ketoprofen and infar through optimum chitosan-guar gum microcapsule. Into 228.6 mL of 1.75% (w/v) chitosan solution in 1% (v/v) acetic acid,38.1 mL of gg solution was added with concentration variation of 0.35, 0.55, and 0.75% (w/v) for ketoprofen microcapsules and 0.05, 0.19, and 0.33% (w/v) for infar microcapsules, and stirred with magnetic stirrer until homogenous. Afterwards, 7.62mL of glu was added slowly under stirring, with concentrations varied: 3, 3.5, and 4% (v/v) for ketoprofen microcapsules, and 4, 4.5, and 5% (v/v) for infar microcapsules. All mixtures were shaked for 20 minutes for homogenization. All mixtures wereshaked for 20 minutes for homogenization. Into each  microcapsule mixture for ketoprofen, a solution of 2 g of ketoprofen in 250 mL of 96% ethanol was added, whereas solution of 100 mg of in 250 mL of 96% ethanol was added into each microcapsule mixture for infar. Every mixture was then added with 5 mL of 2% Tween-80 and stirred with magnetic stirrer for an hour at room temperature. Everymixture was then added with 5 mL of 2% Tween-80 and stirred with magnetic stirrer for an hour at room temperature. Conversion of suspension into fine powders/granules (microcapsules) was done by using spray dryer. The data of [gg], [glu], and medicine’s content from each microcapsule were treated with Minitab 14 software to obtain optimum [gg] and [glu] for microencapsulation. The dissolution behaviour of optimum ketoprofen and infar microcapsules were investigated. The result of optimization by using Minitab Release 14 software showed that among the microcapsule compositions of [gg] and [glu] were 0.35% (w/v) and 3.75% (v/v), respectively, optimum to coat ketoprofen, whereas [gg] and [glu] of 0.05% (w/v) and4.00% (v/v), respectively, optimum to coat infar, at constant chitosan concentration (1.75% [w/v]). In vitro dissolution profile showed that chitosan-guar gum gel microcapsule was more resistant in intestinal pH condition (rather basic) compared with that in gastric pH (very acidic).

scholarly journals Perilaku Disolusi Ketoprofen Tersalut Gel Kitosan-Karboksimetilselulosa (CMC)

2012 ◽  
Vol 13 (1) ◽  
pp. 21
Author(s):  
Purwantiningsih Sugita ◽  
Suminar Setiati Achmadi ◽  
Yuyu Yundhana
Keyword(s):  
Guar Gum ◽  
Tween 80 ◽  
Chitosan Solution ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Drying Process ◽  
Dissolution Behaviour ◽  
Before And After ◽  
Sem Morphology

Study dissolution behaviour of ketoprofen through optimum chitosan-CMC microcapsule has been carried out. Into228.6 ml of 1.0% (w/v) chitosan solution in 1% (v/v) acetic acid, 38.1 ml of CMC solution was added with concentrationvariation of 0.075; 0.0875; and 0.10% (w/v). Afterwards, 7.62 mL of glu was added slowly under stirring, withconcentrations varied: 3; 4.5; and 6% (v/v). All mixtures were shaked for 20 minutes for homogenization. Into eachmicrocapsule mixture for ketoprofen, a solution of 2 g of ketoprofen in 250 mL of 96% ethanol was added. Everymixture was then added with 5 ml of 2% Tween-80 and stirred with magnetic stirrer for an hour at room temperature.Conversion of suspension into fine powders/granules (microcapsules) was done by using spray dryer. Thedissolution behaviour of optimum ketoprofen microcapsules were investigated in gastric and intestinal medium.Microcapsule morphology before and after dissolution as well as empty microcapsule (blank) were observed withSEM. Spray drying process had successfully coated ketoprofen in chitosan-CMC microcapsule. Optimization byusing Minitab Release 14 software showed that among the microcapsule compositions studied, CMC and glu of0.0925% (w/v) and 3.01% (v/v), respectively, optimum to coat ketoprofen at constant chitosan concentration 1.0%(w/v). Result of SEM morphology and In vitro dissolution profile showed that ketoprofen in chitosan-CMCmicrocapsule was relatively well than chitosan-guar gum microcapsule. Kinetically, dissolution of ketoprofen frommicrocapsule in intestinal pH condition was first order with release rate constant, k, of 7.285  10-4 % min-1 andrelease half-time, t1/2, of approximately 15 hours.

scholarly journals STABILITY OF KETOPROFEN COATED BY CHITOSAN-GUAR GUM GEL

2010 ◽  
Vol 9 (3) ◽  
pp. 391-397
Author(s):  
Purwantiningsih Sugita ◽  
Bambang Srijanto ◽  
Budi Arifin ◽  
Ellin Vina Setyowati
Keyword(s):  
Room Temperature ◽  
Degradation Rate ◽  
Guar Gum ◽  
Reaction Kinetic ◽  
Tween 80 ◽  
Chitosan Solution ◽  
Climatic Chamber ◽  
Fine Powders ◽  
Magnetic Stirrer ◽  
Degradation Rate Constant

The coating stability of ketoprofen by chitosan-guar gum gel has been studied. Into 228.6 mL of 1.75% (w/v) chitosan solution in 1% (v/v) acetic acid, 38.1 mL of guar gum (gg) solution was added with concentration variation of 0.35, 0.55, and 0.75% (w/v) for ketoprofen microcapsules, and stirred with magnetic stirrer until homogenous. Afterwards, 7.62 mL of glutaraldehyde (glu) was added slowly under stirring, with concentrations varied: 3, 3.5, and 4% (v/v). All mixtures were shaked for 20 min for homogenization. Into each microcapsule mixture for ketoprofen, a solution of 2 g of ketoprofen in 250 mL of 96% ethanol was added. Every mixture was then added with 5 mL of 2% Tween-80 and stirred with magnetic stirrer for an hour at room temperature. Conversion of suspension into fine powders/granules (microcapsules) was done by using spray dryer. Every microcapsule formula was packed into capsules, as much as 100 g per capsule. The capsules were contained in 100-mL dark bottles and the bottles were kept in climatic chamber at (40 ± 2) °C and RH (75 ± 5) % for 3 months. The microcapsule stabilities were tested chemically and physically. The result showed that formulation of ketoprofen preparation composed of 1.75% (w/v) chitosan, 0.35% (w/v) gg, and 3.50% (v/v) glu, was relatively the best, with ketoprofen percentage left in microcapsule after 3 months, degradation rate constant, and shelf life of 80.33%, 0.0351 % week-1, and 18.92 months, respectively. Reaction kinetic model for this formula followed Prout-Tompkins equation and the degradation of ketoprofen was seem to follow autocatalytic reaction mechanism controlled by the formation and growth of reaction core.   Keywords: Ketoprofen, chitosan-guar gum gel

scholarly journals Dissolution enhancement of glimepiride dispersion using glyceryl monostearate and ?-cyclodextrin as carrier

2015 ◽  
Vol 4 (10) ◽  
pp. 436-441 ◽  
Author(s):  
Md. Abu Shuaib Rafshanjani ◽  
Md. Mofizur Rahman ◽  
Shumaia Parvin ◽  
Md. Abdul Kader
Keyword(s):  
Tween 80 ◽  
Homogenization Method ◽  
In Vitro Dissolution ◽  
Precipitation Method ◽  
Dissolution Enhancement ◽  
Dissolution Profile ◽  
Nano Particle ◽  
Glyceryl Monostearate ◽  
Solid Lipid

Glimepiride is an antidiabetic drug of sulfonylurea group and indicated for the treatment of type 2 diabetes mellitus. The present study was conducted to enhance the dissolution rate of glimepiride solid lipid nano particle dispersions using hot homogenization method and glimepiride solid dispersion by precipitation method. Solid lipid nanoparticles have been used as suitable carriers for delivery of drug with poor solubility. In this investigation glyceryl monostearate and stearic acid were used as solid lipid, Lutrol F-68 as surfactant, Tween 80 as stabilizer and the used polymer were urea crystal and ?-cyclodextrin. Three formulations were prepared in different ratios for two methods and were designated as GMLN1 to GMLN3 in case of hot homogenization method and GMP1 to GMP3 for precipitation method. The evaluation of all the dispersions were done by in vitro dissolution studies using US Pharmacopeia type II apparatus (paddle method) in 900ml distilled water at 50 rpm to a temperature of 37°C ± 0.5°C for 45 minutes. In situ and externally sink method revealed the release pattern of drug was found to follow zero order, first order and Korsmeyer-Peppas equations. Improved dissolution profile was observed in all the solid lipid nano particle dispersions as compared to pure drug as well as market preparation. Thus, glyceryl monostearate and ?-cyclodextrin can be successfully used as carrier for improvement of dissolution and bioavailability of glimepiride.Rafshanjani et al., International Current Pharmaceutical Journal, September 2015, 4(10): 436-441

scholarly journals Enhancement of Dissolution Rate and Bioavailability of Nifedipine by Chitosan Based Cocrystallization Technique

2021 ◽  
pp. 206-219
Author(s):  
. Reetu ◽  
Ashutosh Yadav ◽  
Anita Singh ◽  
Arun Garg
Keyword(s):  
Dissolution Rate ◽  
Sodium Citrate ◽  
Chitosan Solution ◽  
In Vitro Dissolution ◽  
Salting Out ◽  
Design Expert ◽  
Dissolution Behaviour ◽  
Main Effects

The objective of present study was to enhance solubility and dissolution behaviour of nifedipine by using cocrystallization method. A significant increase in solubility and dissolution rate of nifedipine has been demonstrated by solvent change method using chitosan. In this method, chitosan was precipitated on nifedipine crystals using sodium citrate as a salting out agent. An accurately weighed chitosan was dissolved in 1% acetic acid and drug was added in the chitosan solution. This resulting solution was added drop wise into 1% sodium citrate solution with continuous stirring. Sodium citrate precipitate polymer on drug crystals. FTIR, DSC, XRD, SEM, In-vitro dissolution studies, were studied for characterization of prepared cocrystals. Stability studies showed a good stability character of prepared cocrystals. Design Expert® software version 10.0 was used to develop polynomial models which were analysed to delineate the main effects for each CQA (critical quality attributes) through Box-Bhenken design expert. Pharmacokinetic study clearly showed the enhancement of dissolution rate of cocrystals. The above investigation concluded that the significant dose reduction is possible for nifedipine with cocrystal formulation which leads to improve patient compliance.

Preparation and in-vitro evaluation of cilostazol self-emulsifying drug delivery system

2020 ◽  
pp. 13-30
Keyword(s):  
Drug Delivery ◽  
Oleic Acid ◽  
Drug Delivery System ◽  
Delivery System ◽  
Tween 80 ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Phosphodiesterase Iii Inhibitor

This work reported a first liquid self-nanoemulsifying drug delivery system (SEDD) of cilostazol using oleic acid as oil phase, tween 80 as surfactant, and transcutol as co-surfactant. Cilostazol is a poor water-soluble phosphodiesterase III inhibitor, which has antiplatelet and vasodilator effect used to relief intermittent claudication symptoms. Cilostazol solubility was determined in various oils, surfactants and co-surfactants and phase diagram was constructed at different oil: surfactant: co-surfactant ratios to determine the existence of nano-emulsion region. The in-vitro dissolution profile showed an optimized cilostazol SEDD formula (LT1) containing oleic acid (10%) as oil, tween 80 (45%) as surfactant, and transcutol (45%) as co-surfactant in comparison with the commercial conventionally Tablets. The LT1 formula was thermodynamically sTable, with a zeta potential of -30.48 mV and droplet size 154 nm. The LT1 capsule showed a superior dissolution profile (100%) when compared to the commercial Tablet (64%) of cilostazol. The objective of the present study is to formulate cilostazol as an oral liquid SEDD with better solubility and drug release to overcome a variable bioavailability of the commercial Tablet in which a high-fat meal increases absorption to approximately 90%.

Tablet Formulation of a Synthesized Celecoxib Potassium Salt and Development of a Validated Method for Its Analysis

2020 ◽  
Vol 26 ◽  
Author(s):  
Murad Abualhasan ◽  
Nidal Zatar ◽  
Kefah Abu Shehab ◽  
Nasr Shraim
Keyword(s):  
Potassium Salt ◽  
Room Temperature ◽  
Water Solubility ◽  
Limit Of Detection ◽  
Reversed Phase ◽  
Hplc Method ◽  
Tablet Formulation ◽  
In Vitro Dissolution ◽  
Dissolution Profile

Background: Celecoxib is a non-steroidal anti-inflammatory drug (NSAID) and cyclooxygenase-2 (COX-2) inhibitor. It is used for the treatment of rheumatoid arthritis, osteoarthritis, juvenile arthritis, and acute pain. Celecoxib has low systemic bioavailability due to its low water solubility. This study aimed to improve water solubility and dissolution profile by synthesizing a suitable celecoxib potassium salt (celecoxib–K salt). Methods: Four celecoxib salts were synthesized, and the solubility of these four salts was determined. Celecoxib–K monohydrate salt was chosen for tablet formulation. A simple and feasible reversed-phase high-performance liquid chromatography (HPLC) method was developed for the analysis of the formulated tablet and then validated according to international guidelines. The dissolution profile, shelf life, and accelerated stability studies on the formulated tablet were conducted. Results: Celecoxib–K monohydrate salt exhibited increased water solubility by more than 140-folds (0.464 mg/ml) compared with celecoxib. The in vitro dissolution profile of the formulated celecoxib–K salt tablet was totally dissolved after 10 min. The developed analytical HPLC method was a reliable and valid method with good linearity, accuracy, and precision. Moreover, it was sensitive, and the limit of detection and and quantification (LOD and LOQ) were 0.001 and 0.1 mg/L, respectively. The formulated celecoxib–K monohydrate salt tablet was stable under room temperature and accelerated condition for 60 days. Conclusion: The potassium salt of celecoxib was highly increased, and the formulated tablet of celecoxib–K salt exhibited a good dissolution profile in water. In addition, the developed HPLC method was valid and reliable for analysis and quantification of the formulated tablet. The formulated tablet was stable both at room temperature and under stress conditions.

scholarly journals Formulation and In-Vitro Evaluation of Darifenacin Hydrobromide as Buccal Films

2019 ◽  
Vol 28 (2) ◽  
pp. 83-94
Author(s):  
Ishraq K. Abbas ◽  
Nawal A. Rajab ◽  
Ahmed A. Hussein
Keyword(s):  
Tween 80 ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Film Forming ◽  
M3 Receptor ◽  
Croscarmellose Sodium ◽  
In Vitro Disintegration ◽  
Buccal Films

         Darifenacin hydrobromide (DH) is the more recent uroselective M3 receptor antagonist for treating uncomplicated overactive bladder (OAB). This study was aimed to formulate DH as fast dissolving buccal films (FDBFs) using a solvent casting method to enhance patient’s compliance.          Films were prepared by using polyvinyl alcohol (PVA) as a film forming polymer. Different types and concentrations of superdisintegrants (croscarmellose sodium, sodium starch glycolate, indion 414) were used to select the best formula by studying the physicochemical properties of the films, disintegration time (DT) and percent drug release.          The results revealed that formula (F9) that containing 7.5mg DH, 2%w/v PVA, 30%w/w glycerol, 0.5%w/v tween 80, 4%w/w indion 414 was the preferred formula.  F9 showed the shortest in-vitro disintegration time (31.28sec).  In-vitro dissolution profile showed the lowest T80% of the drug in 3.05 min and the highest release of the drug (94%) within 5 min (D5min %).           It was concluded that the FDBFs of DH could be considered as a promising drug delivery system with an enhanced disintegration and dissolution rate and better patient compliance.

Formulation and Evaluation of Microbially- triggered tablets of Valdecoxib

2010 ◽  
Vol 2 (1) ◽  
Author(s):  
Surender Verma ◽  
S. Singh ◽  
D. Mishra ◽  
Atul Gupta ◽  
Rakesh Sharma
Keyword(s):  
Phosphate Buffer ◽  
Guar Gum ◽  
Oral Route ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Dissolution Study ◽  
Caecal Content ◽  
Model Drug

The objective of present study was to develop colon targeted drug delivery using bacterially triggered approach through oral route. Valdecoxib (COX-2 inhibitor) was chosen as a model drug in order to target it to colon which may prove useful in inflammatory bowel disease and related disorders. Matrix tablets of Valdecoxib were prepared by wet granulation technique utilizing different ratio of Guar gum and Sodium starch glycholate. The prepared matrix tablets were evaluated for uniformity of weight, uniformity of content, hardness and in vitro dissolution study in simulated gastric and intestinal fluid (Phosphate Buffer pH-1.2, pH-6.8 and pH-7.4), followed by Dissolution study in bio-relevant dissolution media Phosphate Buffer (pH-6.8) containing rat caecal content. The results revealed that the formulated batch had released lesser quantity of drug at pH 1.2 and pH 7.4 in 2 hors whereas in biorelevent dissolution media containing rat caecal content it released significantly higher amount of drug which was also significantly higher than the dissolution media of same pH without caecal content (microflora) and it was concluded that guar gum can be used as a potential carrier for targeting drugs to colon.

Formulation of Oral Mucoadhesive Tablets using Mucilage Isolated from Buchanania lanzan spreng Seeds

2014 ◽  
Vol 7 (2) ◽  
pp. 2494-2503
Author(s):  
Sudarshan Singh ◽  
Ayaz Ahmad ◽  
Sunil Bothara B
Keyword(s):  
Drug Delivery ◽  
Guar Gum ◽  
Physical Property ◽  
Flow Property ◽  
Relative Effect ◽  
Losartan Potassium ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Microbial Count

The present study was taken to formulate and evaluate mucilage obtained from Buchanania lanzan spreng seeds (BL) belonging to family anacardiacea for oral mucoadhesive drug delivery system containing losartan potassium. Physiochemical characteristics of mucilage, such as swelling index, microbial count, viscosity, hydration capacity, flow property, and pH were studied. The mucilage was evaluated for its mucoadhesive properties in compressed tablet, containing losartan potassium. Granules were prepared by wet granulation process using polyvinylpyrrolidone as binding agent. Mucilage was used in four different concentrations i.e., 21, 42 and 55% w/w. The tablet were prepared and evaluated for its physical property. Further, in vitro dissolution and swelling index was determined. The property of bioadhesive strength of isolated mucilage was compared with Guar gum and HPMC E5LV, which was used as standard mucoadhesive agent concentration. Bioadhesive strength of the tablet was measured on the modified physical balance. Result revealed that tablets had good physiochemical properties, and drug release was retarded as concentration of mucilage was increased. The force of adhesion was obtained 0.1238N, 0.2822N, 0.5175N, 0.8679N and 0.3983N respectively for F1, F2, F3, F4 and F5. Formulations were subjected for study the effect of agitation at different rpm. Formulation showed relative effect on release of drug from formulation. All the formulations were subjected to stability studies for three months, all formulations showed stability with respect to release pattern. In conclusions, these results indicate that the seed mucilage of BL can be a suitable excipient for oral mucoadhesive drug delivery systems.  

scholarly journals In vitro and in vivo Evaluation of Ibuprofen Nanosuspensions for Enhanced Oral Bioavailability

2021 ◽  
Author(s):  
Mohsen Hedaya ◽  
Farzana Bandarkar ◽  
Aly Nada
Keyword(s):  
Particle Size ◽  
Tween 80 ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
In Vivo Evaluation ◽  
Poorly Soluble ◽  
Extent Of Absorption ◽  
Better Than

Introduction: The objectives were to prepare, characterize and in vivo evaluate different ibuprofen (IBU) nanosuspensions prepared by ultra-homogenization, after oral administration to rabbits. Methods: The nanosuspensions produced by ultra-homogenization were tested and compared with a marketed IBU suspension for particle size, in vitro dissolution and in vivo absorption. Five groups of rabbits received orally 25 mg/kg of IBU nanosuspension, nanoparticles, unhomogenized suspension, marketed product and untreated suspension. A sixth group received 5 mg/kg IBU intravenously. Serial blood samples were obtained after IBU administration. Results: The formulated nanosuspensions showed significant decrease in particle size. Polyvinyl Pyrrolidone K30 (PP) was found to improve IBU aqueous solubility much better than the other tested polymers. Addition of Tween 80 (TW), in equal amount as PP (IBU: PP:TW, 1:2:2 w/w) resulted in much smaller particle size and better dissolution rate. The Cmax achieved were 14.8±1.64, 11.1±1.37, 9.01±0.761, 7.03±1.38 and 3.23±1.03 μg/ml and the tmax were 36±8.2, 39±8.2, 100±17.3, 112±15 and 105±17 min for the nanosuspension, nanoparticle, unhomogenized suspension, marketed IBU suspension and untreated IBU suspension in water, respectively. Bioavailability of the different formulations relative to the marketed suspension were the highest for nanosuspension> unhomogenized suspension> nanoparticles> untreated IBU suspension. Conclusion: IBU/PP/TW nanosuspensions showed enhanced in vitro dissolution as well as faster rate and higher extent of absorption as indicated from the higher Cmax, shorter tmax and larger AUC. The in vivo data supported the in vitro results. Nanosuspensions prepared by ultra-high-pressure-homogenization technique can be used as a good formulation strategy to enhance the rate and extent of absorption of poorly soluble drugs.

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