scholarly journals Formulation Development and in vitro Evaluation of Drug Release Kinetics from Sustained Release Aceclofenac Matrix Tablets using Hydroxypropyl Methyl Cellulose

2012 ◽  
Vol 11 (1) ◽  
pp. 37-43 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Shimul Halder ◽  
Madhabi Lata Shuma ◽  
Abu Shara Shamsur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Drug Content ◽  
Compressibility Index ◽  
Originator Brand

The objective of the present study was to develop a once-daily sustained release matrix tablet of Aceclofenac using hydroxypropyl methyl cellulose (Methocel K 100M CR) as release controlling factor and to  evaluate drug release parameters as per various release kinetic models. The tablets were prepared by direct  compression method. The powder blends were evaluated for angle of repose, loose bulk density, tapped bulk density,  compressibility index, total porosity and drug content etc. The tablets were subjected to thickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolution study was carried out for 24  hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus in phosphate buffer (pH 7.4). The powder blends showed satisfactory flow properties, compressibility index and drug content etc. All the tablet formulations showed acceptable pharmacotechnical properties and complied with pharmacopoeial specifications. The results of dissolution studies indicated that the formulation F-3 (40% Methocel K100M CR of total weight of tablet) could extend the drug release up to 24 hours and the total release pattern was very close to the theoretical release profile. By comparing the dissolution profiles with the originator brand of Arrestin SR, the formulation F-3 exhibited drug release profile like originator brand. From this study, a decrease in release kinetics of the drug was observed by  increasing the polymer concentration. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport, which  was only dependent on the type and amount of polymer used. The drug release followed both diffusion and erosion  mechanism in all cases. The drug release from the formulation (F-3) was satisfactory after 3 months storage in 400C  and 75% RH. Besides, this study explored both of the optimum concentration and effect of polymer(s) on  Aceclofenac release pattern from the tablet matrix for 24 hour period. The matrix tablet of Aceclofenac using HPMC  with molecular weight of K100M controlled the drug release effectively for 24 hours; hence the formulation can be  considered as a once daily sustained release tablet of Aceclofenac in order to improve patient compliance. DOI: http://dx.doi.org/10.3329/dujps.v11i1.12485 Dhaka Univ. J. Pharm. Sci. 11(1): 37-43, 2012 (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 FORMULATION AND EVALUATION OF SUSTAINED RELEASE MATRIX TABLET OF LORNOXICAM BY DIRECT COMPRESSION METHOD

2021 ◽  
Vol 10 (5) ◽  
pp. 131-136
Author(s):  
Asim pasha ◽  
C N Somashekhar
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Prolonged Release ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Drug Content

The aim of the present work was to develop sustained release Lornoxicam matrix tablets with polymers like HPMC K15M, Ethyl cellulose, and Crospovidone as carriers in varying quantities. Direct compression was used to make matrix tablets. Various assessment parameters, such as hardness, friability, thickness, percent drug content, weight variation, and so on, were applied to the prepared formulations. In vitro dissolution studies were carried out for 24 hrs. The tablets were subjected to in-vitro drug release in (pH 1.2) for first 2 hrs. Then followed by (pH 6.8) phosphate buffer for next 22 hrs. And the results showed that among the six formulations FL3 showed good dissolution profile to control the drug release respectively. The drug and polymer compatibility were tested using FT-IR spectroscopy, which revealed that the drug was compatible with all polymers. It is also required to design an appropriate prolonged release formulation for Lornoxicam in order to maintain the drug's release. Hence by using the compatible polymers sustained release tablets were formulated and subjected for various types of evaluation parameters like friability, hardness, drug content and dissolution behaviour. Finally, the findings reveal that the prepared sustained release matrix tablets of lornoxicam have improved efficacy and patient compliance.

scholarly journals Formulation Development and In Vitro Evaluation of Metformin Hydrochloride Matrix Tablets Based on Hydroxypropyl Methyl Cellulose

1970 ◽  
Vol 1 (1) ◽  
pp. 51-56 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Tasbira Jeseem ◽  
Rumana Jahangir ◽  
DM Mizanur Rahman ◽  
Abu Shara Shamsur Rouf
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Bulk Density ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Metformin Hydrochloride ◽  
Direct Compression ◽  
Drug Content

An attempt was to formulate the oral sustained release Metformin hydrochloride matrix tablets by using hydroxyl methyl cellulose polymer (HPMC) as rate controlling factor and to evaluate drug release parameters as per various release kinetic models. The tablets were prepared by direct compression method. The granules were evaluated for angle of repose, loose bulk density, tapped bulk density, compressibility index, total porosity, drug content etc. and showed satisfactory results. The tablets were subjected to thickness, weight variation test, drug content, hardness, friability and in vitro release studies. The in vitro dissolution study was carried out for 8 hours using United States Pharmacopoeia USP 2 (paddle-type dissolution apparatus) in phosphate buffer (pH 7.4) as dissolution media. All the tablet formulations showed acceptable pharmacotechnical properties and complied with pharmacopoeial specifications. The release mechanisms were explored and explained with zero order, first order, Higuchi, Korsmeyer and Hixson-Crowell equations. The results indicated that a decrease in release kinetics of the drug was observed by increasing the polymer concentration. Kinetic modeling of in vitro dissolution profiles revealed the drug release mechanism ranges from diffusion controlled or Fickian transport to anomalous type or non-Fickian transport, which was only dependent on the type and amount of polymer used. The drug release followed both diffusion and erosion mechanism in all cases. Besides, this study explored both of the optimum concentration and the effect of polymer on drug release pattern from the tablet matrix for 8 hours period. Key Words: Metformin HCl, Sustained release, Hydrophilic matrix, HPMC, Direct compression   doi:10.3329/sjps.v1i1.1808 S. J. Pharm. Sci. 1(1&2): 51-56

Design and Development of Prochlorperazine Maleate Sustained Release Tablets: Influence of Hydrophilic Polymers on the Release rate and In vitro Evaluation

2010 ◽  
Vol 3 (2) ◽  
pp. 965-977
Author(s):  
Nagasamy Venkatesh D ◽  
Sankar S ◽  
S N Meyyanathan ◽  
K Elango ◽  
B Suresh ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Sustained Release Tablets ◽  
Compression Characteristics

 The objective of the present investigation was to develop and evaluate sustained release matrix tablets of prochlorperazine maleate employing different types and levels of hydrophilic matrix agents namely hydroxyl propyl methyl cellulose (HPMC), carbopol and combination of these polymers by wet granulation technique. Prior to compression process, the prepared granules were evaluated for its flow and compression characteristics. The in vitro dissolution of the newly formulated sustained release tablets were compared with standard formulation. The excipients used in this study did not alter the physicochemical properties of the drug, as indicated by the thermal analysis using differential scanning calorimetry technique. The flow and compression characteristics of the prepared granules significantly improved by virtue of granulation process. Also, the prepared matrix tablets showed good mechanical properties in terms of hardness and friability. HPMC based tablet formulations alone showed high release retarding efficiency as compared to carbopol, carbopol and HPMC combinations. The studies indicated that the drug release can be modulated by varying concentrations of polymers. Mathematical analysis of the release kinetics indicated the nature of the drug release from the matrix tablets followed quasi-fickian obeying first order kinetics. 

scholarly journals Release Profile of Losartan Potassium from Formulated Sustained Release Matrix Tablet

2015 ◽  
Vol 16 (2) ◽  
pp. 177-183
Author(s):  
Md Ziaur Rahman ◽  
Sayed Koushik Ahamed ◽  
Sujan Banik ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Losartan Potassium ◽  
Matrix Tablet ◽  
Vitro Release

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 and Methyl Cellulose as release retardant polymers. The evaluation involves two stages- the physical properties studies of tablets and in vitro release kinetics assessment. The USP paddle method was selected to perform the dissolution test and 900 ml phosphate buffer of pH 6.8 was used as dissolution medium at 50 rpm at 370C. The release kinetics were analyzed. All the formulations followed Higuchi release kinetics. When the release data was plotted into Korsmeyer-Peppas equation, then it was confirmed that F-1, F-2, F-3, F-4 and F-5 exhibited non-fickian type drug release whereas F-6 exhibited fickian type drug release from the tablet matrix. The in-vitro release studies revealed that the formulation F-2 can be taken as an ideal or optimized formulation of sustained release tablets for 24 hours release as it fulfills all the requirements for sustained release tablet. Furthermore, when the tablets were preheated at different temperature (300C, 450C, 600C) before dissolution they showed decrease in drug release compared with ambient temperature DOI: http://dx.doi.org/10.3329/bpj.v16i2.22301 Bangladesh Pharmaceutical Journal 16(2): 177-183, 2013

scholarly journals Formulation and In Vitro Evaluation of Sustained Release Floating Matrix Tablet of Levofloxacin by Direct Compression Method

2019 ◽  
Vol 9 (4-s) ◽  
pp. 398-403
Author(s):  
Nidhi Kumari Pandey ◽  
Sailesh Kumar Ghatuary ◽  
Amit Dubey ◽  
Prabhat Kumar Jain
Keyword(s):  
Drug Release ◽  
Acute Infection ◽  
Methyl Cellulose ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Compression Method ◽  
Weight Variation

The objective of the present work was to develop Gastro retentive dosage forms which would remain in the stomach and upper part or GIT for a prolonged period of time thereby maximizing the drug release at desired site within the time before GRDFs left the stomach and upper part of the GIT, has provoked a great deal of increased interest in the formulation of such drug as floating drug delivery systems. Levofloxacin, (BCS class I) is a fluoroquinolone anti-bacterial agent. The rationale for the formulation of floating matrix tablet are acidic solubility of levofloxacin, residence of Halicobactor pylori mainly in sub region of stomach and the overdosing associated adverse effect due to continuous intake of drug in acute infection. A simple visible spectrophotometric method was employed for the estimation of levofloxacin at 294 nm and Beer’s law is obeyed in the concentration range of 2-10 μg /ml. Floating matrix tablet of levofloxacin was prepared by direct compression method using different polymers like hydroxyl propyl methyl cellulose (HPMC K4) and carbopol 934 as matrix formation polymers, sodium bicarbonate and citric acid was used as gas generating agents. The FTIR spectra of the levofloxacin and other excipients alone and in combination show the compatibility of the drug and excipients. Six formulations of different polymer percentages were formulated (F1-F6). Pre-compression parameters were evaluated. The influence of matrix forming agents and binary mixtures of them on levofloxacin release was investigated. The formulated tablets were characterized by hardness, friability, thickness, weight variation and in vitro drug release. The formulated tablets had acceptable physicochemical characters. The data obtained from the in-vitro dissolution studies of optimized batch F4were fitted in different models. The optimized formulation F4 showed 99.25% drug content and swelling index of 79.85 %. Drug release mechanism was found to be first order kinetics. Levofloxacin floating tablets exhibited increased gastric residence time, there by improved bioavailability and therapeutic effect of the drug.  

scholarly journals In Vitro Release Kinetics Study of Different Brands of Esomeprazole Sustained Release Tablets Available in Bangladesh

1970 ◽  
Vol 2 (1) ◽  
pp. 27-31 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Tasbira Jesmeen ◽  
Md Mesbah Uddin Talukder ◽  
Abu Taher Md Rajib ◽  
DM Mizanur Rahman
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
National Brand ◽  
First Order ◽  
Time Period ◽  
Esomeprazole Magnesium

Commercially available four national and four international brands of esomeprazole magnesium sustained release matrix tablets were studied in simulated gastric medium (pH 1.2) for 2 hours and simulated intestinal medium (pH 6.8) for 8 hours time period using USP reference dissolution apparatus. All the national and international brands complied with the USP in-vitro dissolution specifications for drug release in simulated gastric medium. However, one of the national brands (Code: MP-1) and one of the international brands (MP-7) failed to fulfill the official requirement of 80% drug release within 8th hour in simulated intestinal medium. Drug release of that national and international brand were 70.49% and 67.05% respectively within the specified time period, however one national brand (Code: MP-4) released 103.46 % drug within 8th hour in intestinal medium. Drug release profiles were analyzed for zero order, first order and Higuchi equation to reveal the release kinetics perspective of esomeprazole magnesium sustained release matrix tablets. It was found that zero order release kinetics was the predominant release mechanism than first order and Higuchi release kinetics for those brands (Code: MP-2, MP-3, MP-4, MP-5, MP-6 and MP-8) which complied with the USP in vitro dissolution specification for drug releases. On the other hand, first order release kinetics was predominant for one national and also one international non compliant brands (Code: MP-1 and MP-6). Key Words: In vitro dissolution; Sustained release; Market preparations; Kinetic analysis; Esomeprazole; National brand; International brand. DOI: 10.3329/sjps.v2i1.5812Stamford Journal of Pharmaceutical Sciences Vol.2(1) 2009: 27-31

scholarly journals FORMULATION AND CHARACTERIZATION OF SUSTAINED RELEASE COATED MATRIX GRANULES OF METFORMIN HYDROCHLORIDE

2018 ◽  
Vol 11 (7) ◽  
pp. 387
Author(s):  
Radha Rani Earle ◽  
Kiran Kumar Bandaru ◽  
Lakshmi Usha A
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Metformin Hydrochloride ◽  
Scanning Calorimetry ◽  
Diabetes Mellitus Type Ii ◽  
Drug Content ◽  
Percentage Yield

Objective: Metformin hydrochloride is a biguanide antihyperglycemic agent which is a generally recommended first-line drug for the treatment of diabetes mellitus (Type II). The purpose of this investigation is to prepare sustained release matrix granules of metformin hydrochloride which are coated to extend the drug release over a longer time period.Methods: Metformin hydrochloride granules were prepared by mixing all the dry powders in a V-cone blender and wetting the powder mix with aqueous solution of hydroxypropyl methyl cellulose K100. The prepared granules (MG1-MG5) were investigated for drug release. The batch of granules which exhibited extended release for up to 4 h was coated in a standard coating pan with blends of Eudragit RS and RL to further enhance release period. These were marked as coated metformin granules (CMG3) and CMG4 which were later filled into empty capsules. The granules were characterized for micromeritic properties, percentage yield, particle size distribution, percentage of drug content, and in vitro release of the drug.Results: All the formulations showed percentage yield in the range of 77.66–82.86% and drug content in the range of 78.23–96.62%. CMG3 showed drug release of 97.02% for 12 h. Fourier-transform infrared spectroscopy and differential scanning calorimetry studies indicated that no possible interaction existed between the drug and the polymers used. Scanning electron microscopy images revealed that the granules were spherical in shape with smooth surface and completely covered with a coating of polymer. Kinetic analysis of drug release confirmed that drug release followed zero-order kinetics where it is independent of the concentration.Conclusion: From the results, it was analyzed that design of coated granules employing the polymers used in the present work can produce a sustained release of the drug over a period of 12 h.

scholarly journals Formulation and Evaluation of Gabapentin Sustained Release Matrix Tablet Using Hibiscus rosa sinensis Leaves Mucilage as Release Retardant

2021 ◽  
pp. 564-572
Author(s):  
P. Amsa ◽  
G. K. Mathan ◽  
S. Magibalan ◽  
E. K. Velliyangiri ◽  
T. Kalaivani ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Hibiscus Rosa Sinensis

The major goal of this study was to develop and evaluate Sustained release matrix tablets of Gabapentin with Hibiscus rosa - sinensis leaves mucilage prepared by using wet granulation technique with microcrystalline cellulose as a diluents and magnesium stearate as a lubricant. Pre-compression and post-compression evaluation of physicochemical parameters were carried out and to be within acceptable limits. Drug and polymer compatibility were validated by FTIR measurements. Further, tablets were evaluated for in vitro release study. To get the sustained release of Gabapentin, the concentration of Hibiscus rosa- sinensis mucilage was tuned with a gas-generating agent. The % drug release of all formulation from F1 to F5 showed 91.24%, 80.24%, 70.53%, 62.12% and 49.83% respectively. All the dosage form release kinetics was computed using zero order, first order, Higuchi, and Korsmeyer–Peppas methods. From the above results, it is concluded that the n value of formulation F5 showed 0.78 suggesting anomalous (non-fickian) behavior of the drug. Mucilage from the leaves of Hibiscus rosa-sinensis has a great retarding effect in drug release from sustained release tablets.

Formulation and in vitro Evaluation of Matrix tablets containing Repaglinide

2021 ◽  
pp. 4429-4434
Author(s):  
C.C. Patil ◽  
J. Vekatesh ◽  
S. R Karajgi ◽  
Vijapure Vitthal ◽  
Ashwini G. ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Fourier Transforms ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Differential Scanning Calorimetric ◽  
Content Uniformity ◽  
Drug Content ◽  
Weight Variation

The aim of this project was to develop sustained release matrix tablets of Repaglinide. Sustained release matrix tablets of Repaglinide were prepared by the wet granulation method using polymers like Hydroxy propyl methyl cellulose, Microcrystalline cellulose, Eudragit RS-100 in different ratios. The matrix tablets of Repaglinide were evaluated for hardness, weight variation, friability, drug content uniformity, and in-vitro drug release. In order to determine the drug release mechanisms and kinetics, the data was subjected to zero order, first order, and higuchi and peppas diffusion model. Twelve batches of sustained release matrix tablets of Repaglinide were developed. Among these formulations F4, F8 and F12 formulation showed satisfactory physicochemical properties and drug content uniformity and sustained release of drug for 12 hours with maximum release of 86.95%, 84.91% and 84.91%. The optimized formulations were characterized for Differential scanning calorimetric analysis; Fourier transforms infrared spectroscopy and scanning electron microscopic studies. IR spectroscopic studies indicated that there were no drug-excipient interactions. The prepared sustained release matrix tablets of Repaglinide were successfully developed and evaluated.

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