scholarly journals FORMULATION AND EVALUATION OF ONCE DAILY SUSTAINED RELEASE MATRIX TABLET OF VERAPAMIL HYDROCHLORIDE

2013 ◽  
Vol 3 (1) ◽  
Author(s):  
Brijesh Ray ◽  
M M Gupta
Keyword(s):  
Sustained Release ◽  
Matrix Tablet ◽  
Verapamil Hydrochloride ◽  
Once Daily

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 Once Daily Sustained-Release Matrix Tablet of Naproxen: Formulation and In Vitro Evaluation

1970 ◽  
Vol 9 (1) ◽  
pp. 47-52 ◽  
Author(s):  
Muhammad Rashedul Islam ◽  
Ishtiaq Ahmed ◽  
Mohiuddin Abdul Quadir ◽  
Md Habibur Rahman
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Once Daily ◽  
Weight Variation ◽  
Release Studies ◽  
The Matrix

The objective of the present study was to develop once-daily sustained-release matrix tablets of naproxen, one of the most potent non-steroidal anti-inflammatory agents used in the treatment of arthritic pain. The tablets were prepared by direct compression method using hydrophilic matrix materials like Methocel® K4M CR and Methocel® K15M CR. The tablets were subjected to measurement of thickness, diameter, weight variation, drug content, hardness and friability, the results of which were within compendial specification range. In vitro release studies were carried out by the USP basket method and were carried out at pH 7.4 buffer for ten hours. The results of dissolution studies indicated that higher polymer content in the matrix (40%) decreased the release rate of the drug as shown in formulation NMK4MF6 and NMK15MF6 (where lactose content is zero). The most successful formulations of the study, exhibited satisfactory drug release which was very close to the theoretical release profile. All the formulations exhibited diffusion-dominated drug release. Key words: Naproxen; Methocel® K4M CR; Methocel® K15M CR; Sustained release; Matrix tablets DOI: 10.3329/dujps.v9i1.7429 Dhaka Univ. J. Pharm. Sci. 9(1): 47-52 2010 (June)

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>

A Comparative Study of Matrix Tablets Designed by Different Methods

2017 ◽  
Vol 10 (2) ◽  
pp. 3645-3652
Author(s):  
Tulsi Bisht ◽  
Rishishwar Poonam
Keyword(s):  
Drug Release ◽  
Comparative Study ◽  
Guar Gum ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Once Daily ◽  
Gum Acacia ◽  
Weight Variation ◽  
Evaluation Parameters

The aim of present work was to develop once daily sustained release matrix tablet of aceclofenac by wet granulation technique using natural gums i.e.: gum acacia, guar gum and Xanthan gum. In this present study matrix tablets were prepared using three different methods and a comparative study was done. Aceclofenac sodium being the newer derivative of diclofenac having short biological half life (4hrs.), so it requires more than one dose per day to maintain therapeutic dose. The prepared tablets were evaluated for various parameters like weight variation, hardness, swelling index, friability, percent drug release and various release profile like zero order, first order, Higuchi's, and Koshemeyrs-peppa. All the evaluation parameters met pharmacopoeial specifications and through dissolution studies it was matrix tablets prepared with method 2 shows heighest percent drug release and matrix tablet prepared by method 3 showed lowest percent drug release at the end of 8 hrs. (Shown in fig. 8, comparative release study of all three formulations). Matrix tablet of aceclofenac were successfully prepared and evaluated and it can be concluded that matrix tablet prepared with natural gums showed release rate for a prolonged time and can be of great importance for “once daily” tablet to reduce side effects and toxicity related with NSAIDs.  

scholarly journals Development and Bio-Predictive Evaluation of Biopharmaceutical Properties of Sustained-Release Tablets with a Novel GPR40 Agonist for a First-in-Human Clinical Trial

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 804
Author(s):  
Ewelina Juszczyk ◽  
Kamil Kisło ◽  
Paweł Żero ◽  
Ewa Tratkiewicz ◽  
Maciej Wieczorek ◽  
...  
Keyword(s):  
Clinical Trial ◽  
Sustained Release ◽  
Development Strategy ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Mechanical Agitation ◽  
Development Cycle ◽  
Dissolution Tests ◽  
Sustained Release Tablets ◽  
Biopharmaceutical Properties

Sustained-release (SR) formulations may appear advantageous in first-in-human (FIH) study of innovative medicines. The newly developed SR matrix tablets require prolonged maintenance of API concentration in plasma and should be reliably assessed for the risk of uncontrolled release of the drug. In the present study, we describe the development of a robust SR matrix tablet with a novel G-protein-coupled receptor 40 (GPR40) agonist for first-in-human studies and introduce a general workflow for the successful development of SR formulations for innovative APIs. The hydrophilic matrix tablets containing the labeled API dose of 5, 30, or 120 mg were evaluated with several methods: standard USP II dissolution, bio-predictive dissolution tests, and the texture and matrix formation analysis. The standard dissolution tests allowed preselection of the prototypes with the targeted dissolution rate, while the subsequent studies in physiologically relevant conditions revealed unwanted and potentially harmful effects, such as dose dumping under an increased mechanical agitation. The developed formulations were exceptionally robust toward the mechanical and physicochemical conditions of the bio-predictive tests and assured a comparable drug delivery rate regardless of the prandial state and dose labeled. In conclusion, the introduced development strategy, when implemented into the development cycle of SR formulations with innovative APIs, may allow not only to reduce the risk of formulation-related failure of phase I clinical trial but also effectively and timely provide safe and reliable medicines for patients in the trial and their further therapy.

Treatment of Mild Hypertension with Low Once-Daily Doses of a Sustained-Release Capsule Formulation of Verapamil

1995 ◽  
Vol 35 (1) ◽  
pp. 52-58 ◽  
Author(s):  
Pamela J. Davis ◽  
Timothy C. Fagan ◽  
Mary J. Topmiller ◽  
Jon H. Levine ◽  
Keith C. Ferdinand
Keyword(s):  
Sustained Release ◽  
Mild Hypertension ◽  
Capsule Formulation ◽  
Once Daily

Formulation and Evaluation of Sustained Release Bilayer Matrix Tablet of Glimepiride and Metformin Hydrochloride

2021 ◽  
pp. 273-279
Author(s):  
Mayuri B. Patil ◽  
Avish D. Maru ◽  
Jayshree S. Bhadane
Keyword(s):  
Sustained Release ◽  
Type Ii Diabetes ◽  
In Vitro Release ◽  
Angle Of Repose ◽  
Metformin Hydrochloride ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Type Ii ◽  
Weight Variation

The aim of the present study was to design and evaluate bilayer tablets of metformin hydrochloride as sustained release form for the treatment of Type-II diabetes mellitus. The basic aim of any Bi-layer tablet formulation is to separate physically or chemically incompatible ingredients and to produce repeat action or prolonged action of tablet. They are many drugs for treating type-II diabetes. Sulphonyl urea and biguanides are used commonly by a wide section of patients. Melt granulation process was used for the formulation of sustained comprising metformin layer and wet granulation of immediate comprising layer of glimepiride. The precompression studies like bulk density, tapped density, angle of repose, compressible index and post formulation studies includes weight variation, hardness, thickness, friability and dissolution study. The in-vitro release profile of Glimepiride was dissolved within 45 min, and Metformin Hydrochloride was able to release more than 12 hrs. They all the formulation was optimized formula due to its higher rate of dissolution and collate all other parameters with the official specifications.

scholarly journals The Effect of Manufacturing Methods and Different Shapes on the Release Pattern of Diclofenac Sodium Matrix Tablet

1970 ◽  
Vol 2 (2) ◽  
pp. 76-80
Author(s):  
Tajnin Ahmed ◽  
Muhammad Shahidul Islam ◽  
Tasnuva Haque ◽  
Mohammad Abusyed
Keyword(s):  
Sustained Release ◽  
Release Rate ◽  
Diclofenac Sodium ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Compression Method ◽  
Release Pattern ◽  
Peg 600

In the present study sustained release diclofenac sodium matrix tablets were prepared using Kollidon SR polymer. Hydroxypropyl methylcellulose (HPMC 15 cps) and poly ethylene glycol (PEG-600) polymers respectively were used in formulating tablets prepared by direct compression and wet granulation methods. The polymers were used to explore the release pattern of the drug into the dissolution media. The tablets were also prepared in various shapes (caplet oval, round oval and flat oval). A comparatively higher release rate of drug was obtained from the polymer HPMC 15 cps at 10% concentration for directly compressed matrix tablet than those containing 20% of HPMC after a definite period of time. In wet granulation process, 10% PEG-600 containing tablets showed a better release than those containing 20% PEG. The drug release was also found to be sustained in case of wet granulation method than that of the direct compression method. Again the caplet shaped tablets in case of direct compression method showed better release rate of drug than those of the round oval and flat oval shaped tablets. Thus the result of this study shows that the proper selection of the percentage of polymer and the suitable shape of tablet and proper manufacturing method can provide a greater opportunity in designing sustained release dosage forms. Key words: Matrix tablet; release pattern; direct compression; wet granulation; PEG 600; Kollidon SR.DOI: 10.3329/sjps.v2i2.5828Stamford Journal of Pharmaceutical Sciences Vol.2(2) 2009: 76-80

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