scholarly journals FORMULATION AND OPTIMIZATION OF FLOATING TABLETS OF CLOPIDOGREL BISULPHATE USING DESIGN OF EXPERIMENTS

2018 ◽  
Vol 10 (6) ◽  
pp. 126
Author(s):  
Sanjeevani S. Deshkar ◽  
Arvind S. Pawara ◽  
Satish V. Shirolkar
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Factorial Design ◽  
Water Uptake ◽  
Lag Time ◽  
Matrix Tablets ◽  
Lower Percentage ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Bicarbonate Concentration

Objective: The present study aimed at designing of floating matrix tablet of clopidogrel bisulphate by design of experiments.Methods: The tablets were prepared by direct compression technique using hydroxypropyl methylcellulose K15 (HPMC) as a matrix polymer and sodium bicarbonate as a gas generating agent. In order to optimize the concentration of HPMC (X1) and sodium bicarbonate (X2), a 32 full factorial design was employed. The tablet formulations were evaluated for floating lag time (Y1), floating or buoyancy time (Y2), percent water uptake, and differential scanning calorimetry (DSC) and in vitro drug release (Y3).Results: The formulation variables, HPMC concentration, and sodium bicarbonate concentration exerted a significant effect on floating behavior and drug release characteristics of the tablet. The optimized formulation, with 15% sodium bicarbonate concentration and 30 % HPMC concentration resulted in 5±2.6 sec of floating lag time, 22.0±0.6 h of floating time and 42.0±0.99% of clopidogrel bisulphate release in 8 h of dissolution study. The drug release mechanism was identified as nonfickian. The water uptake studies revealed that with an increase in HPMC concentration, there was an increase in swelling index of tablet whereas higher sodium bicarbonate concentration supported the faster erosion of matrix tablets. DSC study revealed no interaction of drug and polymers. The lower percentage error between predicted and observed responses of the optimized formulation validated the design.Conclusion: The study demonstrated successful designing of floating clopidogrel bisulphate tablet with factorial design.

scholarly journals Design, development and optimization of sustained release floating, bioadhesive and swellable matrix tablet of ranitidine hydrochloride

PLoS ONE ◽  
2021 ◽  
Vol 16 (6) ◽  
pp. e0253391
Author(s):  
Birhanu Nigusse ◽  
Tsige Gebre-Mariam ◽  
Anteneh Belete
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
Lag Time ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Design Development ◽  
Gastro Retentive

Ranitidine HCl, a selective, competitive histamine H2-receptor antagonist with a short biological half-life, low bioavailability and narrow absorption window, is an ideal candidate for gastro-retentive drug delivery system (GRDDS). Controlled release with an optimum retentive formulation in the upper stomach would be an ideal formulation for this drug. The aim of the present study was therefore to develop, formulate and optimize floating, bioadhesive, and swellable matrix tablets of ranitidine HCl. The matrix tablets were prepared using a combination of hydroxypropyl methylcellulose (HPMC) and sodium carboxymethyl cellulose (NaCMC) as release retarding polymers, sodium bicarbonate (NaHCO3) as gas generating agent and microcrystalline cellulose (MCC) as direct compression diluent. Central composite design (CCD) was used to optimize the formulation and a total of thirteen formulations were prepared. Concentration of HPMC/NaCMC (3:1) (X1) and NaHCO3 (X2) were selected as independent variables; and floating lag time (Y1), bioadhesive strength (Y2), swelling index at 12 h (Y3), cumulative drug release at 1 h (Y4), time to 50% drug release (t50%) (Y5) and cumulative drug release at 12 h (Y6) were taken as the response variables. The optimized batch showed floating lag time of 5.09 sec, bioadhesive strength of 29.69 g, swelling index of 315.04% at 12 h, t50% of 3.86 h and drug release of 24.21% and 93.65% at 1h and 12 h, respectively, with anomalous release mechanism. The results indicate that sustained release matrix tablet of ranitidine HCl with combined floating, bioadhesive and swelling gastro-retentive properties can be considered as a strategy to overcome the low bioavailability and in vivo variation associated with the conventional ranitidine HCl tablet.

Effects of release modifier on Carvedilol release from Kollidon SR based matrix

2012 ◽  
Vol 1 (8) ◽  
pp. 186 ◽  
Author(s):  
Urmi Das ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Microcrystalline Cellulose ◽  
Matrix Tablets ◽  
Dissolution Time ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Weight Variation ◽  
The Matrix ◽  
Tablet Formulations

<p>Sustained release Carvedilol matrix tablets constituting Kollidon SR were developed in this study in an attempt to investigate the effect of release modifiers on the release profile of Carvedilol from matrix. Three matrix tablet formulations were prepared by direct compression of Kollidon SR in combination with release modifier (HPMC and Microcrystalline Cellulose) and magnesium stearate. Tablets containing only Kollidon SR with the active ingredient demonstrated a rapid rate of drug release. Incorporation of HPMC in the matrix tablet prolonged the release of drug but incorporation of Microcrystalline Cellulose showed superimposable release pattern with an initial burst effect as confirmed by mean dissolution time and Higuchi release rate data. After 7 hours of dissolution, Carvedilol release from the matrix systems were 91.42%, 83.41%, from formulation F1 and F2 respectively. Formulation F3 exhibited 100 % release at 4 hours. All the tablet formulations showed acceptable pharmaco-technical properties and complied with the in-house specifications for tablet weight variation, friability, hardness, thickness, and diameter. Prepared tablets also showed sustained release property for carvedilol. The drug release mechanism from the matrix tablets of F1 and F2 was found to be followed by Fickian and F3 by Non-Fickian mechanism.</p><p>DOI: <a href="http://dx.doi.org/10.3329/icpj.v1i8.11095">http://dx.doi.org/10.3329/icpj.v1i8.11095</a></p> <p>International Current Pharmaceutical Journal 2012, 1(8): 186-192</p>

scholarly journals Development and evaluation of sustained release losartan potassium matrix tablet using kollidon SR as release retardant

2012 ◽  
Vol 48 (4) ◽  
pp. 621-628 ◽  
Author(s):  
Shahid Sarwar ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Polymer Concentration ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Losartan Potassium ◽  
Dissolution Time ◽  
Release Mechanism ◽  
Matrix Tablet

The present study was undertaken to develop sustained release (SR) matrix tablets of losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method, along with Kollidon SR as release retardant polymer. The amount of losartan potassium remains fixed (100 mg) for all the three formulations whereas the amounts of Kollidon SR were 250 mg, 225 mg, and 200 mg for F-1, F-2, and F-3 respectively. The evaluation involves three stages: the micromeritic properties evaluation of granules, physical property studies of tablets, and in-vitro release kinetics studies. The USP apparatus type II was selected to perform the dissolution test, and the dissolution medium was 900 mL phosphate buffer pH 6.8. The test was carried out at 75 rpm, and the temperature was maintained at 37 ºC ± 0.5 ºC. The release kinetics was analyzed using several kinetics models. Higher polymeric content in the matrix decreased the release rate of drug. At lower polymeric level, the rate and extent of drug release were enhanced. All the formulations followed Higuchi release kinetics where the Regression co-efficient (R²) values are 0.958, 0.944, and 0.920 for F-1, F-2, and F-3 respectively, and they exhibited diffusion dominated drug release. Statistically significant (P<0.05) differences were found among the drug release profile from different level of polymeric matrices. The release mechanism changed from non-fickian (n=0.489 for F-1) to fickian (n=0.439 and 0.429 for F-2, and F-3 respectively) as a function of decreasing the polymer concentration. The Mean Dissolution Time (MDT) values were increased with the increase in polymer concentration.

scholarly journals DESIGN AND IN VITRO CHARACTERIZATION OF FLOATING TABLETS OF METRONIDAZOLE

2019 ◽  
pp. 539-544
Author(s):  
CHINNA ESWARAIAH M ◽  
JAYA S
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Content Uniformity ◽  
Matrix Tablet ◽  
N Value

Objective: The objective of the present study was to formulate the effervescent floating matrix tablet of metronidazole and to evaluate the effect of varying concentrations of hydrophilic polymers on drug release. Methods: Drug excipients interaction was studied by Fourier transform infrared spectrophotometer. The effervescent floating matrix tablets were prepared by direct compression technique using hydroxypropyl methylcellulose (HPMCK4) and xanthan gum alone and in combination as release retardants. Microcrystalline cellulose was used as diluent. Sodium bicarbonate was used as effervescent agent. The prepared matrix tablets were evaluated for their physicochemical parameters such as weight variation, hardness, friability, content uniformity, buoyancy time, and in vitro dissolution. Results: Micromeritic properties and post-compression parameters were evaluated and all the parameters were found within the acceptable limit. The drug release data were subjected to different models to evaluate release kinetics and mechanism of drug release. The matrix tablets prepared with xanthan gum and a mixture of xanthan gum and HPMCK4 were retarded the drug release up to 12 h. The release mechanism of metronidazole was evaluated on the basis of release exponent n value in Peppas model. The n value of the formulations ranged from 0.46 to 0.89 which indicated Case II transport and zero-order release. Conclusion: Floating matrix tablet is the simple, efficient, and economic method to sustain the release of metronidazole to eradicate Helicobacter pylori in peptic ulcer disease.

scholarly journals Assessment of Once Daily Sustained Release Hydrophilic Matrix Tablet of Carvedilol

2017 ◽  
Vol 16 (1) ◽  
pp. 43-53
Author(s):  
Uttom Kumar ◽  
Md Samiul Islam ◽  
Shimul Halder ◽  
Abu Shara Shamsur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Lower Percentage ◽  
Simulated Gastric Fluid ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Lauryl Sulfate ◽  
Once Daily ◽  
Release Profiles

The objective of the present study was to design and evaluate once daily sustained release tablet of carvedilol, using two molecular weight grades of hydrophilic polymers (methocel® K4M CR and methocel®K15M CR) as release retarding materials. Two sets of formulations were prepared, where first set of four formulations (F1- F4) contained variable ratios of methocel® K4M CR and methocel® K15M CR (15% : 15%, 15% : 13%, 15% : 11% and 15% : 9%) to optimize the composition of polymers in the tablet matrices such that the drug and polymer interaction was sufficient for sustaining release up to 24 hours and second set of five formulations (F5-F9) contained variable percentages of sodium lauryl sulfate (SLS) (1.0, 1.25, 1.5, 1.75 and 2.0%) to enhance the dissolution rate of the drug from the tablet matrices because of its poor aqueous solubility. The tablets were prepared by direct compression method and evaluated for hardness, thickness, friability, weight variation and in vitro drug release. The in vitro dissolution studies were carried out in simulated gastric fluid (900 ml, pH 1.2) for 24 hours using USP type II apparatus operated at 100 rpm and 37 ± 0.05°C. The release profiles were explored and explained by zero order, first order, Higuchi, Korsmeyer-Peppas and Hixson-Crowell models. From this study, the drug release profiles for formulations F6 to F9 were found to be satisfactory and the release mechanism followed both diffusion and erosion. Due to lower percentage of SLS used, F6 was considered as the best formulation.Dhaka Univ. J. Pharm. Sci. 16(1): 43-53, 2017 (June)

scholarly journals Design, Fabrication and Evaluation of Drug Release Kinetics from Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose

1970 ◽  
Vol 8 (1) ◽  
pp. 23-30 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Bishyajit Kumar Biswas ◽  
Abu Shara Shasur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Drug Content ◽  
Compressibility Index

The objective of this study was to develop a sustained release matrix tablet of aceclofenac usinghydroxypropyl methylcellulose (HPMC K15M and HPMC K100M CR) in various proportions as release controllingfactor by direct compression method. The powders for tableting were evaluated for angle of repose, loose bulkdensity, tapped bulk density, compressibility index, total porosity and drug content etc. The tablets were subjected tothickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolutionstudy was carried out for 24 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus inphosphate buffer (pH 7.4). The granules showed satisfactory flow properties, compressibility index and drug contentetc. All the tablets complied with pharmacopoeial specifications. The results of dissolution studies indicated that theformulations F-2 and F-3 could extend the drug release up to 24 hours. By comparing the dissolution profiles with themarketed product, it revealed that the formulations exhibited similar drug release profile. From this study, a decreasein release kinetics of the drug was observed when the polymer concentration was increased. Kinetic modeling of invitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport toanomalous type or non-Fickian transport, which was only dependent on the type and amount of polymer used. Thedrug release followed both diffusion and erosion mechanism in all cases. The drug release from these formulationswas satisfactory after 3 months storage in 40°C and 75% RH. Besides, this study explored the optimum concentrationand effect of polymer(s) on acelofenac release pattern from the tablet matrix for 24 hour period.Key words: Aceclofenac; sustained release; hydrophillic matrix; HPMC; direct compression.DOI: 10.3329/dujps.v8i1.5332Dhaka Univ. J. Pharm. Sci. 8(1): 23-30, 2009 (June)

scholarly journals Preparation and In vitro Evaluation of Theophylline Loaded Gastroretentive Floating Tablets of METHOCEL K4M

1970 ◽  
Vol 7 (1) ◽  
pp. 65-70 ◽  
Author(s):  
Ferdous Khan ◽  
Md Shaikhul Millat Ibn Razzak ◽  
Md Ziaur Rahman Khan ◽  
Kazi Rashidul Azam ◽  
Sams Mohammad Anowar Sadat ◽  
...  
Keyword(s):  
Citric Acid ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Release Rate ◽  
Lag Time ◽  
Release Mechanism ◽  
Drug Release Profile ◽  
Floating Tablets ◽  
Time Required

This investigation describes the preparation and in vitro evaluation of gastroretentive floating tablets of theophylline. Hydrophilic polymer METHOCEL K4M was used for its gel forming and release controlling properties. Sodium bicarbonate and citric acid were incorporated as gas generating agents. The effects of soluble components (sodium bicarbonate and citric acid), gel forming agent (METHOCEL K4M) and dose variation on drug release profile and floating properties were investigated. It has been observed that in all cases increase of the amount of floating agent caused a decrease of the floating lag time. Increase of theophylline load showed an increase of the floating lag time, which was independent of floating agent content. The release mechanisms were explored and explained with zero order, first order, Higuchi, Korsmeyer and Hixon-Crowell equations. The release rate, extent and mechanisms were found to be governed by the content of polymer and floating agent. The content of active ingredient was also a vital factor in controlling drug release pattern. It was found that polymer content and amount of floating agent significantly affected the time required for 50% of drug release (T50%), percentage drug release after 8 hours, release rate constant, and diffusion exponent (n). Kinetic modeling of dissolution profiles revealed that the drug release mechanism could range from diffusion controlled to case II transport, which was mainly dependent on presence of relative amount of theophylline, polymer and floating agent. Key words: Gastroretention, Floating tablet, Theophylline  DOI = 10.3329/dujps.v7i1.1220 Dhaka Univ. J. Pharm. Sci. 7(1): 65-70, 2008 (June)

scholarly journals Formulation and characterization of gastroretentive drug delivery system of losartan potassium

2012 ◽  
Vol 2 (1) ◽  
pp. 11-17
Author(s):  
Manish Jaimini ◽  
Yuveraj Singh Tanwar ◽  
Birendra Srivastava
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Drug Delivery System ◽  
Delivery System ◽  
Gastrointestinal Transit ◽  
Matrix Tablets ◽  
Losartan Potassium ◽  
Release Mechanism ◽  
Drug Release Profile

Floating matrix tablets of losartan potassium were developed with an aim to prolong its gastric residence time and increase the bioavailability of drug. Rapid gastrointestinal transit could result in incomplete drug release from the drug delivery system above the absorption zone leading to diminished efficacy of the administered dose. The tablets were prepared by wet granulation technique, using polymers Methocel K15 and Methocel K100 in combination with other standard excipients. Sodium bicarbonate was incorporated as gas generating agent. The effects of sodium bicarbonate and polymers on drug release profile and floating properties were investigated. It was found that viscosity of Methocel K15 and Methocel K100 along with sodium bicarbonate had significant impact on the release and floating properties of the delivery system. The decrease in the release rate was observed with an increase in the viscosity of the polymeric system. Polymer with high viscosity Methocel K100 was shown to be beneficial than low viscosity polymer Methocel K15 in improving the floating properties of gastric floating drug delivery system (GFDDS). The observed difference in the drug release and floating properties of GFDDS could be attributed to the difference in the basic properties of two polymers, Methocel K15 and Methocel K100 due to their water uptake potential and functional group substitution. The release mechanism were explored and described with zero-order, first-order and Korsmeyer-Peppas equations. The drug release profiles and buoyancy of the floating tablets were stable when stored at 40°C/75% RH for 6 months.DOI: http://dx.doi.org/10.3329/icpj.v2i1.12872 International Current Pharmaceutical Journal 2012, 2(1): 11-17 

Optimization and Evaluation of Solubility-Modulated Gastroretentive Floating Matrix Tablet of Furosemide

2014 ◽  
Vol 7 (3) ◽  
pp. 2581-2589
Author(s):  
Anita Lalwani ◽  
D Bhalodiya ◽  
C Patel ◽  
L Panchal ◽  
P Shelat
Keyword(s):  
Experimental Design ◽  
Drug Release ◽  
Sodium Bicarbonate ◽  
Delivery System ◽  
Solid Dispersion ◽  
Lag Time ◽  
Storage Conditions ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Scanning Calorimetry

The objective of the present study was to prepare delivery system for furosemide which has poor solubility and has specific absorption in stomach. Solid dispersion of furosemide (SD) was prepared in polyethylene glycol 6000 and characterized using differential scanning calorimetry. Floating gastroretentive tablets of the prepared solid dispersion were then prepared by wet granulation technique, using polymer Methocel K100M CR (HPMC) and sodium bicarbonate. A 32 factorial design was applied systematically to study the effect of the amount of HPMC (X1) and sodium bicarbonate (X2) on the floating lag time (YFLT) and amount of drug release at the end of 1st hr (Y60), 6th hr (Y360) and 12th hr (Y720). The solubility of SD was higher than that of drug alone and the physical mixture. The results of multiple regression analysis, when applied to responses obtained for experimental design batches, indicated that low level of HPMC and high level of sodium bicarbonate decreased the floating lag time, while the amount of drug released at all time points decreased with increase in level of HPMC. Swelling behavior of experimental design batches was studied and its relationship with mechanism of drug release was interpreted.  Batch D3 came close to satisfying the drug release and floating criteria. Drug compatibility with the excipients used was ascertained using FTIR. Stability studies were carried out at recommended storage conditions and the tablets were found to be stable. Delivery system could be developed for furosemide which addressed the solubility and site specificity issues of drug.  

scholarly journals Formulation and Evaluation of Gastroretentive Floating Tablets of Quetiapine Fumarate

2021 ◽  
Vol 11 (3-S) ◽  
pp. 65-73
Author(s):  
Keyur S. Patel ◽  
Akshar N. Rao ◽  
Deepa R. Patel ◽  
Dhaval M. Patel ◽  
Advaita B. Patel
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Factorial Design ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Lag Time ◽  
Quetiapine Fumarate ◽  
Floating Tablets ◽  
Vitro Release

The objective of the present study was to develop gastroretentive floating tablets of quetiapine fumarate. The gastroretentive floating tablets of quetiapine fumarate were formulated using natrosol 250 HHX as a sustained release polymer and sodium bicarbonate as a gas forming agents.  A 32 factorial design was employed to study the influence of concentration of natrosol HHX 250 (X1) and concentration of sodium bicarbonate (X2) on the dependent variables % drug release at 1h (Y1), % drug release at 8 h (Y2) and floating lag time (Y3). The optimized formulation (O1) showed floating lag time 49 ± 3 sec and % drug release 99.54± 0.81 at 12 h. The in vitro release of F1-F9 batches were found in between 99.95 ± 1.18 %  to  86.32 ±1.71 % at 12 h. Floating lag time of F1-F9 batches were found to be 25± 2 sec to 178 ± 3 sec. FTIR studies shown that there was no  interaction between quetiapine fumarate and excipients. From the factorial design batches it was found that floating lag time was decreased with increasing the amount of sodium bicarbonate and decreasing the amount of natrosol 250 HHX. Here % release of drug was decreased with increase the extent of natrosol 250 HHX. The in-vitro release kinetics revealed Korsmeyer-Peppas model is followed and drug release is by anomalous diffusion. Keywords: Quetiapine fumarate, Natrosol 250 HHX, Sodium bicarbonate, Gastroretentive floating tablets

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