scholarly journals In vitro Release Kinetic Study of Theophylline from Kollidon SR Polymer Based Matrix Tablet

2015 ◽  
Vol 14 (1) ◽  
pp. 43-48 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Shimul Halder ◽  
Abu Shara Shamsur Rouf

Controlled release tablet matrix of theophylline was prepared with kollidon SR, a spray dried powder grade polymer (polyvinyl acetate and povidone based matrix rate retarding hydrophobic materials) by utilizing direct compression technique. Different proportion of kollidon SR was used to develop the matrix builder in the five proposed formulations (F-1 to F-5) for the study of release rate retardant effect at 10, 12, 15, 18 and 21% of total weight of matrix tablet, respectively. The in vitro dissolution study of the matrices of those proposed tablet formulations were carried out in simulated gastric medium (pH 1.3) for first two hours and then in simulated intestinal medium (pH 6.8) for 6 hours using USP dissolution apparatus II (paddle method). The formulation F-3 (using 15% polymer) and F-4 (using 18 % polymer) met the optimum release profiles of active ingredient for 8 hr period of total study. The release kinetics for theophylline was plotted against zero order, first order and Higuchi release rate kinetics to evaluate the release mechanism of drug from the formulated tablet matrix. The release kinetics of formulation F-3 and F-4 was followed very closely by Higuchi release rate kinetic order than other kinetics such as zero order and first order kinetics which has been reflected the type of drug release from the tablet matrix by diffusion as well as erosion mechanism.Dhaka Univ. J. Pharm. Sci. 14(1): 43-48, 2015 (June)

1970 ◽  
Vol 7 (1) ◽  
pp. 39-45 ◽  
Author(s):  
Bishyajit Kumar Biswas ◽  
Md Safiqul Islam ◽  
Farida Begum ◽  
Abu Shara Shamsur Rouf

In the present study esomeprazole sustained release tablet matrix was prepared by utilizing different grades of hydroxypropyl methylcellulose (HPMC) polymers such as Methocel K15M & Methocel K100 LVCR by direct compression method. Different amount of Methocel K15M was used to develop matrix builder in the seven proposed formulations (F1-F7) for the study of release rate retardant effect at 20%, 25%, 30%, 35%, 40%, 45% and 50% of total weight of tablet matrix respectively. The dissolution study of Methocel K15M based tablet matrices of those proposed formulations were carried out in the simulated gastric medium (pH 1.3) for first two hours and then in the simulated intestinal medium (pH 6.8) for 8 hours using USP dissolution apparatus II. The formulation F-5 (40%) and F-6 (45%) met the optimum release rate of esomeprazole for 10h period of in vitro dissolution study. The release kinetics of formulation F-5 and F-6 very closely followed Higuchi kinetic order than first order and zero order kinetics. Similarly Methocel K100 LVCR was used to develop matrix builder in another seven proposed formulations (F8-F14). It was found that formulations F-11 (35%), F-12 (40%) and F-13 (45%) met the desired release rate of esomeprazole for 10h period. The release kinetics of formulation F-11, F-12 and F-13 followed Higuchi kinetic order. Between these two polymers, Methocel K100 LVCR showed better release retardant effect than Methocel K15M. Key words: Esomeprazole, Direct compression, Controlled release, Methocel K15M and Methocel K100 LVCRDOI = 10.3329/dujps.v7i1.1216 Dhaka Univ. J. Pharm. Sci. 7(1): 39-45, 2008 (June)  


2012 ◽  
Vol 10 (2) ◽  
pp. 87-92
Author(s):  
Utpal Das ◽  
Shimul Halder ◽  
Abul Kalam Lutful Kabir ◽  
Harun Or Rashid ◽  
Abu Shara Shamsur Rouf

Indapamide, a low-dose thiazide-type diuretic, is used for the treatment of essential hypertension. In this study, we developed an indapamide sustained release formulation using Methocel K15 MCR (a modified    hydroxypropyl methylcellulose), Methocel K100 LVCR (a modified hydroxypropyl methylcellulose), magnesium stearate, talc and starch 1500 by direct compression. The powders for tableting were evaluated for angle of repose, loose bulk density, tapped bulk density, compressibility index, total porosity etc. The tablets were subjected to thickness, weight variation test, hardness, friability and in vitro release studies. The in vitro dissolution study was carried out in the gastric medium (pH 1.3) for first two hours and then in the intestinal medium (pH 6.8) for 22 hours using United States Pharmacopoeia (USP) 22 paddle-type dissolution apparatus. The granules showed satisfactory flow properties, compressibility index etc. All the tablets complied with pharmacopoeial specifications. The results of    dissolution studies indicated that the formulation F-5 and F-7 (up to 75.36 % drug release in 12 hours) could extend the drug release up to 12 hours. The drug release patterns were simulated in different kinetic orders such as Zero Order release kinetics, First Order release kinetics, Higuchi release kinetics, Korsmeyer-Peppas release kinetics and Hixson-Crowell release kinetics to assess the release mechanism. From the study we observed that Higuchi release    kinetics was the predominant release mechanism than Zero Order and First Order kinetics. The drug release mechanism from the matrix tablets was found to be non Fickian mechanism.   DOI: http://dx.doi.org/10.3329/dujps.v10i2.11785   Dhaka Univ. J. Pharm. Sci. 10(2): 87-92, 2011 (December)  


1970 ◽  
Vol 4 (1) ◽  
pp. 79-83
Author(s):  
Shimul Halder ◽  
Madhabi Lata Shuma ◽  
Abul Kalam Lutful Kabir ◽  
Abu Shara Shamsur Rouf

The main aim of present investigation was to study the dissolution pattern of most commercially available formulations of Esomeprazole in Bangladesh. Commercially available ten national brands and originator brand of esomeprazole magnesium trihydrate tablets were studied in simulated gastric medium (pH 1.2) for first 15 minutes and simulated intestinal medium (pH 6.8) for next 30 minutes time period using USP reference dissolu-tion apparatus (Type II). No brands met the dissolution pattern like the originator brand (E1). But three brands (E3, E6 and E7) were found to be very close to it in terms of dissolution pattern. One brand E11 was found to be sub-standard compared to originator one. Drug release profiles were analyzed for zero order, first order and Higuchi equation to reveal the release kinetics perspective of Esomeprazole magnesium trihydrate enteric coated tablets. It was found that first order kinetics was predominant for E1 (Originator Brand). Zero order and Higuchi release kinetics was predominant release mechanism than first order release kinetics for E2, E4 and E11. First order release kinetics was predominant for rest of the brands (E3, E5, E6, E7, E8, E9 and E10). It was found that drug release of those brands followed moderately diffusion method and concentration dependant from the dosage form. Among all of these locally manufactured Esomeprazole brands E3, E6 and E7 showed compatible dissolution pattern and release kinetics compared with the originator brand. Key words: In vitro dissolution; Market preparations; Kinetics study; Esomeprazole; National brand; Originator brand. DOI: http://dx.doi.org/10.3329/sjps.v4i1.8875 SJPS 2011; 4(1): 79-83


2019 ◽  
Vol 9 (4-s) ◽  
pp. 398-403
Author(s):  
Nidhi Kumari Pandey ◽  
Sailesh Kumar Ghatuary ◽  
Amit Dubey ◽  
Prabhat Kumar Jain

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.  


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

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


Author(s):  
CHINNA ESWARAIAH M ◽  
JAYA S

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.


1970 ◽  
Vol 8 (1) ◽  
pp. 23-30 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Bishyajit Kumar Biswas ◽  
Abu Shara Shasur Rouf

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)


2002 ◽  
Vol 70 (2) ◽  
pp. 189-198
Author(s):  
Genç Lütfi ◽  
Hegazy Nahed ◽  
Arica Betül

Matrix tablets of ketorolac trometharnine (KT) were prepared by direct compression technique and Carbopol 934, 940 and 1342 have been used as polymers in different concentrations (5-15 % ). For the quality control of tablets; physical tests as crushing strength, diameter-height ratio and fkiability, KT amount assay and in vitro dissolution techniques were performed and dissolution profiles were plotted and evaluated kinetically. The in vitro release kinetics of ten different formulations of KT matrix tablet were studied at pH 1.2 and pH 7.0 using the USP dissolution technique and apparatus with basket assembly. Dissolution results were evaluated kinetically and statistically. According to our results, different types and concentrations of carbopol to tablet formulations may effect in controlled drug release.


2013 ◽  
Vol 11 (2) ◽  
pp. 129-136 ◽  
Author(s):  
Monnujan Nargis ◽  
Md Saiful Islam ◽  
Fatima Naushin ◽  
Syed Shabbir Haider

Sustained release formulations of metoclopramide HCl (4-amino-5-chloro-N-(2-diethylaminoethyl)-2- methoxybenzamide hydrochloride) (MH) were prepared using carnauba wax (CW) and stearic acid (SA) as matrix formers. Granules were prepared by melt granulation method while direct compression technique was used to prepare the tablets. The drug release profiles of these products were studied by in-vitro dissolution testing in simulated gastric, gastrointestinal and intestinal media of pH 1.2, 4.5 and 7.5, respectively. The increase in the proportion of SA in the granules produced a concomitant decrease of the initial drug release rate but later on the release rate was enhanced in the intestinal medium. Drug release was found to be affected by compression force and stirring rate but also showed a dependency on pH of the dissolution fluid. The fastest release rate was found at pH 4.5 and the slowest at pH 1.2 which was consistent with the drug’s solubility behavior. Matrix erosion and water uptake rates were highest in the intestinal medium and lowest in the gastric medium. The drug release kinetics followed the Higuchi’s model in all cases. DOI: http://dx.doi.org/10.3329/dujps.v11i2.14563 Dhaka Univ. J. Pharm. Sci. 11(2): 129-136, 2012 (December)


2012 ◽  
Vol 11 (1) ◽  
pp. 37-43 ◽  
Author(s):  
Abul Kalam Lutful Kabir ◽  
Shimul Halder ◽  
Madhabi Lata Shuma ◽  
Abu Shara Shamsur Rouf

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)


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