scholarly journals DEVELOPMENT AND CHARACTERIZATION OF FENOFIBRATE TABLET BY COMAPARING TWO DIFFERENT SOLUBILITY AND DISSOLUTION ENHANCEMENT METHODS

2018 ◽  
Vol 6 (5) ◽  
pp. 32-40
Author(s):  
J S Dua ◽  
Beerpal Kaur ◽  
D N Prasad
Keyword(s):  
Solid Dispersion ◽  
Excellent Result ◽  
Angle Of Repose ◽  
Dissolution Enhancement ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
System A ◽  
Tapped Density

 Fenofibrate is a drug included in BCS class II category, generally used to reduce cholesterol level in patient having a risk of cardiovascular disease. The main aim of this research was to ameliorate solubility and dissolution profile of Fenofibrate with comparison between two different methods i.e. Solid dispersion and liquisolid technique. In liquisolid system, a dry freely flowing and compressible powder mixture was obtained which absorb drug solution or suspension in non-volatile solvent. While in case of solid dispersion drug was dispersed with suitable hydrophillic carrier with or without volatile solvent to get powder material. Two formulation of Fenofibrate solid dispersion were prepared by solvent evaporation method using β-CD as a hydrophillic carrier with ratios 1:1 and 1:3. In case of liquisolid technique, two liquisolid compacts were prepared with ‘R’ value 20:1 and 40:1 using Avicel PH 102 as a carrier and Aerosil 200 as a coating material. All the formulations were characterized by FTIR, DSC and solubility studies. Precompression studies of all the batches were done by determining angle of repose (25.100- 35.020), bulk density (0.51- 0.56 g/ml), tapped density (0.60-0.66 g/ml), carr’s index (15.61-19.03%) and hausner’s ratio (1.13-1.25). Post compression evaluation was done by checking hardness (4-5 kg/cm2), thickness (3.56-4.01mm), friability (0.54-0.75%), disintegration time (3.50-5.56min), drug content (80.34-95.05%) and in-vitro drug release (81.55-92.93%). Out of all the four batches SD2 batch that was prepared by solid technology showed an excellent result by releasing drug at  96.91 %. Key words-  Fenofibrate, Solid dispersion, Liquisolid compact, Avicel PH 102, Aerosil 200.

scholarly journals FORMULATION AND EVALUATION OF FLURBIPROFEN FAST DISINTEGRATING TABLETS USING NATURAL SUPERDISINTEGRANTS

2016 ◽  
Vol 9 (6) ◽  
pp. 247 ◽  
Author(s):  
Mohammed Sarfaraz ◽  
Surendra Kumar Sharma
Keyword(s):  
Drug Release ◽  
Angle Of Repose ◽  
Lepidium Sativum ◽  
Disintegration Time ◽  
Natural Sources ◽  
Weight Variation ◽  
Wetting Time ◽  
Tapped Density ◽  
Fast Disintegrating Tablets

ABSTRACTObjective: The main objective of this research was to formulate Fast disintegrating tablets of Flurbiprofen incorporating superdisintegrants, isolated from natural sources like Plantago ovata (PO) seeds, Lepidium sativum (LS) seeds and agar-agar.Methods: Superdisintegrants were isolated from their natural sources using reported methods. Swelling index and hydration capacity was determined for the natural superdisintegrants to know their disintegration capacity. The tablet formulations were designed using isolated natural superdisintegrants. The powder blends were evaluated for pre-compressional parameters like angle of repose, bulk density, tapped density, carr’s index, and hausner’s ratio. Fast disintegrating tablets were prepared by direct compression method. The compressed tablets were characterized for post compression parameters.Results: All formulations had hardness, friability, weight variation and drug content within the pharmacopoeial limits. The wetting time was 84 to 254 sec, in vitro disintegration time was between 59.2 to 221 sec, and in-vitro drug release was as low as 11.80% (LS1) to a maximum of 98.99% (PO4) after 4 min of study. Among all, optimized formulation was PO4, as it showed good wetting time (84 sec), fastest disintegration time (59.2 sec), dispersion time (135 sec) and drug release of 98.99.% within 4 min.Conclusion: Flurbiprofen FDT’s were successfully developed using isolated natural disintegrants. The natural disintegrants isolated showed promising results and can prove as effective alternative for synthetic disintegrants.

scholarly journals Enhancement of dissolution rate of Olmesartan medoxomil using urea as carrier by different solid dispersion techniques

2018 ◽  
Vol 1 (1) ◽  
pp. 36-42
Author(s):  
B Sangameswaran ◽  
M Gomathi
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Olmesartan Medoxomil ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Poor Solubility ◽  
Co Precipitation

The poor solubility of drug substances in water and their low dissolution rate in aqueous G.I.T fluid often leads to insufficient bioavailability. As per Biopharmaceutical Classification System (BCS), Olmesartan belongs to the class-II category having poor solubility and high permeability. Since only dissolved drug can pass the gastrointestinal membrane, the proper solubility of the drug is ultimately desired. Its oral bioavailability is 26%. Hence, an attempt was made to enhance its solubility by formulating solid dispersions using different techniques viz., Melting, Kneading, Co-precipitation, Solvent evaporation and Physical mixing etc., Drug and carrier (Urea) in different ratios like 1: 1, 1: 2, 1: 3 and 1:4 were used for formulating solid dispersions. The compatibility of the drug with the carrier was checked by FTIR studies, these results revealed that there was no interaction between them. The angle of repose, bulk density, tapped density; Carr’s index and Hausner ratio were calculated for the micrometric characterization of all the solid dispersions. The drug content was found to be high and uniform in all formulations. The prepared Solid dispersion SEM4 (1:4) showed minimal wetting time of 13 seconds compared with the other formulations. In vitro dissolution, release studies in Phosphate buffer pH of 6.8 revealed that the prepared solid dispersions showed faster drug release compared with the pure drug.  The in vitro dissolution profile showed ascendency on increasing the carrier concentration

scholarly journals FORMULATION AND EVALUATION OF METRONIDAZOLE TABLETS USING NATURAL GUM

2019 ◽  
pp. 304-306
Author(s):  
SUDIPTA DAS ◽  
SOUMITRA DAS
Keyword(s):  
Aloe Vera ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Binding Agent ◽  
Binding Properties ◽  
Disintegration Time ◽  
Hausner Ratio ◽  
Percentage Release ◽  
Tapped Density

Objectives: The objective of the present study was to formulate the metronidazole tablets using natural Aloe vera gum as binding agent. Materials and Methods: To determine the binding properties of the extracted A. vera gum were used for the preparation of metronidazole tablets and compared with other binding agents such as acacia and sodium carboxymethyl cellulose (CMC). Physical properties such as hardness, friability, disintegration time, and in vitro dissolution rate are the important parameter which determines for each formulation. Three batches of metronidazole tablets are prepared using acacia (F1), sodium CMC (F2), and A. vera gum (F3) as binding agent. Results: The granules were evaluated by determining the angle of repose (26.01 ± 0.110–27.18 ± 0.166°), bulk density, tapped density, Hausner ratio, and Carr’s index. It shows satisfactory results. At time 90 min, the percentage release of drug for F1, F2, and F3 was 44.947%, 31.467%, and 53.424%, respectively. The tablets prepared with A. vera gum showed faster release profile than other binders. Conclusion: From the results, it was shown that tablets prepared with A. vera gum have good binding properties and also helped tablets for faster release.

scholarly journals CINNARIZINE LIQUID SOLID COMPACTS: PREPARATION EVALUATION

2019 ◽  
Vol 11 (1) ◽  
pp. 150
Author(s):  
Sreenivas Patro Sisinthy ◽  
Shubbaneswarei Selladurai
Keyword(s):  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Scanning Calorimetry ◽  
Disintegration Time ◽  
Dsc Studies ◽  
Weight Variation ◽  
Drug Concentrations ◽  
R Value

Objective: The objective of this research was to formulate cinnarizine tablets using the liquid-solid compact technique to enhance its solubility and dissolution rate.Methods: Cinnarizine liquid-solid compacts were formulated using propylene glycol as the non-volatile solvent, Neusilin US2 as the carrier material, Aerosil 200 as the coating material and croscarmellose sodium as the disintegrant. The interaction between drug and excipients were characterized by Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) studies. Different batches of liquid, solid compacts were prepared by using varying carrier-coating excipient ratio and different concentration of liquid medication. Flow parameters such as bulk density, tapped density, Carr’s Index, Hausner’s Ratio as well as an angle of repose were used to test the flowability of the powder blend. The liquid-solid compacts were produced by direct compression method and were evaluated for tests such as weight variation, drug content, hardness, thickness, friability, wetting time, disintegration time as well as the in vitro dissolution studies.Results: The results of the preformulation studies of liquisolid compacts showed acceptable flow properties. The results of FTIR and DSC studies showed that there is no drug-excipient interactions. The different R values and concentrations were found to have a marked effect on the dissolution profile. Formulations with higher carrier: coating ratio (R-value) and lower drug concentrations displayed a better dissolution profile. The percentage of drug release of F3 with an R-value of 20 and a drug concentration of 10% was found to be 88.11% when compared to the conventional marketed tablet which released only 44.07% at the end of 2 h.Conclusion: From this research, it is inferred that liquid-solid technique is a promising and effective approach that can be used to enhance the dissolution rate of cinnarizine.

scholarly journals Effect of Hydrophilic Carriers for Solubility and Dissolution Enhancement of Sulfamerazine by Solid Dispersions Technique

2021 ◽  
pp. 313-326
Author(s):  
Jitendra Gupta ◽  
Reena Gupta
Keyword(s):  
Solid Dispersion ◽  
Solid Dispersions ◽  
Poloxamer 407 ◽  
Dissolution Enhancement ◽  
Infrared Spectrometry ◽  
Antibacterial Drug ◽  
Dissolution Profile ◽  
Fusion Technique ◽  
Pure Drug

Aims: The present research was carried out to investigate the effect of hydrophilic carriers in enhancing the solubility and dissolution rate of Sulfamerazine (SMZ) employing the fusion technique of solid dispersions (SD). Methodology: SMZ is an oral antibacterial drug exhibiting a poor dissolution profile and water solubility. SD of SMZ was prepared using poloxamer 407 (PX407) and Polyethylene glycol 6000 (PEG6000) as a hydrophilic carrier by employing the fusion technique. Results: The powder SDs were subjected for solubility, Fourier transform infrared spectrometry (FTIR), Differential scanning calorimetry (DSC), in-vitro dissolution profile, Scanning electron microscopy (SEM), and X-ray diffraction (XRD) study. The FTIR spectral analysis showed no significant incompatibility between drug and carriers and confirmed the presence of SMZ. From XRD and DSC, SMZ indicated the amorphous form in solid dispersion with larger specific surface area, resulting in a better in-vitro rate of dissolution of the drug from solid dispersions than pure drug. However, SD of PX407 (SDSMFF8) indicated higher aqueous solubility than pure SMZ. Further, SDSMFF7 showed higher in-vitro drug release 96.45±0.3% within 60 minutes, and pure drug (18.54±0.8%). Conclusion: In conclusion, enhancing thesolubility and dissolution of SMZ using hydrophilic carriers by solid dispersion technique provides new strategies for broadening its potential clinical application.

Formulation and Evaluation of Taste Masked Oral Disintegrating Tablets of Aripiprazole

2015 ◽  
Vol 8 (1) ◽  
pp. 2723-2734
Author(s):  
Y. Shravan Kumar ◽  
Prashanthi Patel ◽  
Sravanthi Ch ◽  
Rashmi B
Keyword(s):  
Depressive Disorders ◽  
Partial Agonist ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Sodium Starch Glycolate ◽  
Weight Variation ◽  
Croscarmellose Sodium

Aripiprazole is an atypical antipsychotic agent used for treatment of schizophrenia, bipolar disorder and major depressive disorders. In the present work, oral  disintegrating tablets of aripiprazole were developed to  enhance the patient compliance and provide rapid onset of  action. The efficacy of aripiprazole is mediated through a combination of partial agonist activity at dopamine D2 and serotonin 5HT-1A receptors and antagonist activity at 5HT-2A receptors. It has a bitter taste and poor-solubility in water. Thus, the main objective of the study is to formulate taste masked oral disintegrating tablets of aripiprazole by using inclusion complex beta-cyclodextrin to achieve a better dissolution rate and further improving the bioavailability of the drug. Oral disintegrating tablets were   prepared by direct compression method using  super disintegrant like crospovidone, croscarmellose sodium,  sodium starch glycolate and combinations of  cros-povidone with croscarmellose sodium, and crospovidone with sodium  starch glycolate in different concentrations. They were evaluated for the pre-compression parameters such as bulk density, compressibility, Hausner ratio and angle of repose. The prepared batches of tablets were evaluated for hardness, weight variation, thickness, friability, drug content, disintegration time, wetting time,    in vitro dispersion time, and in vitro dissolution profile. All these parameters were found to be satisfactory. Among all, the formulation F15 containing crospovidone 5% + cros-povidone with croscarmellose sodium 5% was considered to be the optimum formulation, which released nearly 99% of the drug in 20 minutes with a disintegration time of 10. 20 seconds. These studies indicate the viability and benefits of oral disintegrating tablets of aripiprazole. 

scholarly journals FORMULATION AND EVALUATION OF FAST DISSOLVING TABLETS OF AMOXYCILLIN TRIHYDRATE AND POTASSIUM CLAVULANATE

2017 ◽  
Vol 9 (2) ◽  
pp. 48
Author(s):  
Ashish Masih ◽  
Ajay Kumar Tiwari
Keyword(s):  
Drug Release ◽  
Angle Of Repose ◽  
Mechanical Resistance ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Weight Variation ◽  
Compressibility Index ◽  
Potassium Clavulanate ◽  
Tapped Density

Objective: The present work is aimed to formulate fast dissolving stable tablet formulation a preferred combination of Amoxycillin trihydrate (Beta-lactum antibiotic) and Potassium clavulanate (Beta-lactum inhibitor) by using various super disintegrants.Methods: Fast dissolving tablets are prepared by direct compression method using super disintegrants i.e. sodium starch glycolate, crospovidone, croscarmellose sodium. Aspartame as a sweetener and trusil mango flavor were used to increase palatability. Reduction in the dose of Amoxycillin trihydrate and Potassium clavulanate tablet was possible by developing fast dissolving tablet. Results: The powder blends were subjected to various pre-formulation evaluations such as, tapped density, bulk density, hausner’s ratio, the angle of repose and compressibility index. The prepared Amoxycillin trihydrate and Potassium clavulanate fast dissolving tablets were evaluated for thickness, weight variation, friability, disintegration time, hardness, wetting time and in vitro drug release. All fast dissolving tablet formulations shown uniform weight, hardness and friability data indicates the good mechanical resistance of the fast dissolving tablet. Fast dissolving tablets were disintegrated between 25-50 second and in vitro disintegration time of the best fast disintegrating tablets was found to be 25 second. Conclusion: Amoxycillin trihydrate and Potassium clavulanate fast dissolving tablets were found to be of good quality fulfilling all the needs for fast dissolving tablets. The optimised (F-4) formulation had shown best disintegration time and released profile with a maximum in vitro drug release as compare to marketed preparation at all time intervals of in vitro drug release.

scholarly journals Formulation and evaluation of orodispersible Enalapril maleate tablets: a comparative study on natural super disintegrents and synthetic super disintegrents

2015 ◽  
Vol 1 (7) ◽  
pp. 313
Author(s):  
Kameswara Rao.S ◽  
Yusuf MD. ◽  
Saraswathi P. ◽  
Ch.R.Raghavendra Rao ◽  
Murali P. ◽  
...  
Keyword(s):  
Research Work ◽  
Hepatic Metabolism ◽  
Angle Of Repose ◽  
Dissolution Profile ◽  
Compression Technique ◽  
Disintegration Time ◽  
Enalapril Maleate ◽  
Drug Content ◽  
The Individual

The aim of the present investigation is to formulate Enalapril maleate oral disintegrating tablet by using natural and synthetic superdisintegrents..ODTs may also be used to deliver drugs to the oral cavity, for local action or, in some cases, absorption across the oral mucosa, thereby avoiding first-pass hepatic metabolism and potentially increasing the rate and extent of uptake, and reducing undesirable metabolites. The objectives of the research work is to formulate oral disintegrating tablets of Enalapril maleate by using different super disintegrates(Natural, Synthetic) in different ratio by direct compression technique and tablets were evaluated for precompressional and postcompressional Parameters such as angle of repose, bulk density, tapped density, compressibility index, drug content and in-vitro drug release study, hardness, friability, wetting time and invitro dispersion time. To study the physical characteristics of the individual drug and optimized formulations by FTIR spectroscopy. To evaluate various characteristics of the resulting tablets. Formulation CCS3, IH2 were subjected to stability Studies as per ICHguidelines at temperatures and humidity of 255C/605%RH; and 405C/755%RH.Tablets didnt reveal any appreciable changes in respect to hardness, disintegration time, drug content and dissolution profile.

SYNTHESIS AND CHARACTERIZATION OF THIOLATED GUM KONDAGOGU AND EVALUATION AS MUCOADHESIVE POLYMER

INDIAN DRUGS ◽  
2020 ◽  
Vol 57 (01) ◽  
pp. 37-43
Author(s):  
Ashwin A. Patil ◽  
Ketan B. Patil ◽  
Laxmikant R. Zawar
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Matrix Tablet ◽  
Disintegration Time ◽  
Weight Variation ◽  
Zero Order Release ◽  
Gum Kondagogu ◽  
Ellman’S Method

Present work focused on thiolation for enhancing the mucoadhesive potential of Gum kondagogu (GK). Thiolation of GK was done by esterification process with 80 % thioglycolic acid in presence of 7N HCl. Thiolated Gum kondagogu (ThioGK) was determined to possess 1.59 ±0.04 mmol of thiol groups/g of the polymer by Ellman’s method. ThioGK was characterized by FTIR, NMR, DSC, XRD, and FE-SEM. The tablets were prepared by direct compression using 75 mg of ThioGK and GK. Tablets containing ThioGK (F1) and GK (F2) were subjected to evaluation of weight variation, hardness and friability and show enhanced disintegration time, swelling behavior, drug release and mucoadhesion. In vitro drug release of batch F1 exhibits complete release of drug in 24 hr with zero order release kinetics. Comparative mucoadhesive strength was studied using chicken ileum by texture analyzer and revealed higher mucoadhesion of tablet containing ThioGK. From the above study, ThioGK was suitability exploited as mucoadhesive sustained release matrix tablet.

scholarly journals Enhancement of Solubility and Improvement of Dissolution Rate of Atorvastatin Calcium Prepared as Nanosuspension

2019 ◽  
Vol 28 (2) ◽  
pp. 46-57
Author(s):  
Ahmed H. Ali ◽  
Shaimaa N. Abd-Alhammid
Keyword(s):  
Particle Size ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Precipitation Method ◽  
Size Analysis ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
Atorvastatin Calcium ◽  
Freeze Dried

       Atorvastatin have problem of very slightly aqueous solubility (0.1-1 mg/ml). Nano-suspension is used to enhance it’s of solubility and dissolution profile. The aim of this study is to formulate Atorvastatin as a nano-suspension to enhance its solubility due to increased surface area of exposed for dissolution medium, according to Noyes-Whitney equation.         Thirty one formulae were prepared to evaluate the effect of ; Type of polymer, polymer: drug ratio, speed of homogenization, temperature of preparation and inclusion of co-stabilizer in addition to the primary one; using solvent-anti-solvent precipitation method under high power of ultra-sonication. In this study five types of stabilizers (TPGS, PVP K30, HPMC E5, HPMC E15, and Tween80) were used in three different concentrations 1:1, 1:0.75 and 1:0.5 for preparing of formulations. At the same time, tween80 and sodium lauryl sulphate have been added as a co-stabilizer.          Atorvastatin nano-suspensions were evaluated for particle size, PDI, zeta potential, crystal form and surface morphology. Finally, results of particle size analysis revealed reduced nano-particulate size to 81nm for optimized formula F18 with the enhancement of in-vitro dissolution profile up to 90% compared to 44% percentage cumulative release for the reference Atorvastatin calcium powder in 6.8 phosphate buffer media. Furthermore, saturation solubility of freeze dried Nano suspension showed 3.3, 3.8, and 3.7 folds increments in distilled water, 0.1N Hcl and 6.8 phosphate buffers, respectively. Later, freeze dried powder formulated as hard gelatin capsules and evaluated according to the USP specifications of the drug content and the disintegration time.        As a conclusion; formulation of poorly water soluble Atorvastatin calcium as nano suspension significantly improved the dissolution of the drug and enhances its solubility.

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