FORMULATION AND EVALUATION OF LEVOFLOXACIN HEMIHYDRATE SUSTAINED RELEASE TABLET FROM HYDROPHILIC MATRICES

INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (01) ◽  
pp. 43-49
Author(s):  
S. K Sahoo ◽  
◽  
A Behera ◽  
S. Patil
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Drug Diffusion ◽  
Weight Variation ◽  
Lower Viscosity ◽  
Sustained Release Tablets ◽  
Through Diffusion ◽  
Higuchi Model

Stable sustained release tablets of levofloxacin hemihydrate were successfully prepared by wet granulation technique. Compatible excipients were selected and different formulations were prepared with varying proportion and grades of hydroxy propyl methyl cellulose. Tablets were prepared by compressing free flowing granules and evaluated for hardness, thickness, friability, weight variation, percentage drug content and drug release. As concentration of HPMC increased the drug release decreased might be due to increased amount of polymer around tablets provided gelation which inhibits the release. For formulation F5 only 55 % drug was released in 8 h whereas up to 90 % drug was release for formulation F2 and F3 within the same time. Thus, higher viscosity HPMC retards the drug release directly than lower viscosity HPMC. All the formulations follow Higuchi model which has indicated that drug release from homogenous matrix was through diffusion. Thus, increase in concentration of polymer decreases the drug diffusion from tablet.

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 Development and Characterization of Bilayer Sustained Release Tablets of Tramadol HCl and Acetaminophen

2016 ◽  
Vol I (I) ◽  
pp. 6-16
Author(s):  
Rashid Javed ◽  
Sana Ijaz ◽  
Kainat Waqar ◽  
Muhammad Imran Khan
Keyword(s):  
Sustained Release ◽  
Promising Result ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Tramadol Hydrochloride ◽  
Weight Variation ◽  
Sustained Release Tablets ◽  
S 100 ◽  
Eudragit S 100

The aim of the present study was to develop bilayer sustained release tablets of to improve patient compliance of two drugs, tramadol and paracetamol. Immediate release layer contained both drugs tramadol hydrochloride and acetaminophen while the sustained release layer was designed only for the tramadol hydrochloride. Hydrophobic polymers Eudragit L-100, Eudragit S-100 and hydrophilic polymer hydroxy propyl methyl cellulose (HPMC K15), and wet granulation technique to produce bilayer matrix tablets. FTIR studies revealed no incompatibility among the ingredients. Out of 16 trials developed and characterized for weight variation, thickness, diameter, hardness, and friability, F16 showed promising result with immediate layer releasing drug 29% in 2 hours followed by sustained release 77% drug over 12 hours and followed zero order release. Therefore, bilayer sustained release tablets of tramadol with simultaneous loading of Paracetamol can be developed using Eudragit S-100 and hydroxyl propyl methylcellulose (HPMC K15) at equimolar content levels.

scholarly journals Chitosan and Hydroxy Propyl Methyl Cellulose as a Carrier for Aceclofenac for Prolonged Release

2021 ◽  
pp. 173-182
Author(s):  
R. G. Katedeshmukh ◽  
A. V. Yadav ◽  
J. S. Dhumal ◽  
A. B. Kumbhar ◽  
P. V. Rane ◽  
...  
Keyword(s):  
Drug Release ◽  
Mechanical Strength ◽  
Methyl Cellulose ◽  
Storage Conditions ◽  
Wet Granulation ◽  
Prolonged Release ◽  
Natural Polymers ◽  
Design Expert ◽  
Weight Variation ◽  
Accelerated Stability

Numerous natural polymers either alone or in combination with other polymers were found effective in controlling the drug release. In this study the attempts were made to combine chitosan (degree of deacetylation 84.14 %) and as hydroxylpropyl methylcellulose (HPMC K 15M) to retard the release of aceclofenac in tablet formulation. The tablets were prepared by wet granulation and evaluated for pre and post- compression parameters. All the pre-compression parameters were found within the limit.  Hardness and friability values were found in the range of 4.30-4.89 kg/cm2 and 0.1-0.6% respectively. These results proved the good mechanical strength of the formulations.  The drug content was found in the range of 97.56 – 99.10 %.  Weight variation was found within the official limit. The percent drug release and swelling index was found to be dependent on the concentration of polymer. With increasing the concentration of both the polymers the swelling index was increased and drug release decrease. Highest concentration of both the polymers was found to retard the drug release up to 8 h.  The effect of Chitosan and HPMC on drug release was evaluated by design expert software to achieve the optimized formulation. The response of the drug release after 4h was considered to check the drug release. It was found that the enhanced concentration of both the polymers had negative effective on the drug release. The formulation containing highest concentration of the chitosan and HPMC was found be fit in the limits of optimized formulations. The optimized formulation was found to be stable at accelerated stability storage conditions.

scholarly journals Formulation of Metformin Sustained Release Tablet Using Natural Polymer

2021 ◽  
Vol 11 (2) ◽  
pp. 31-37
Author(s):  
Mehak Siddiqui ◽  
L. K. Omray ◽  
Pushpendra Soni
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Guar Gum ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Absolute Bioavailability ◽  
Dissolution Time ◽  
Content Uniformity ◽  
Weight Variation

The overall objective of the present work was to develop an oral sustained-release (SR) Metformin tablet that is prepared by the direct compression method by using hydrophilic hydroxyl propyl methyl cellulose (HPMC) and Guar gum polymer alone as well as in combination at different concentrations. Metformin is a biguanide that has a relatively short plasma half-life. It has low absolute bioavailability. All the properties were evaluated for thickness, weight variation, hardness and drug content uniformity and in vitro drug release. The mean dissolution time is used to characterize the drug release rate from a dosage form that indicates the drug release-retarding efficiency of the polymer. The hydrophilic matrix of HPMC alone could not control the Metformin release effectively for 12 h but when combined with Guar gum, it could slow down the release of drug and, thus, can be successfully employed for formulating Sustain Release matrix tablets. Keywords: Guar gum, hydroxylpropylmethylcellulose, matrix tablets, release kinetics,

scholarly journals Formulation development and evaluation of voriconazole sustained release tablets

2013 ◽  
Vol 2 (10) ◽  
pp. 165-169 ◽  
Author(s):  
Manivannan Rangasamy ◽  
Venkata Krishna Reddy Palnati ◽  
Lakshmi Narayana Rao Bandaru
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Angle Of Repose ◽  
Type I ◽  
Dissolution Test ◽  
Formulation Development ◽  
Drug Release Profile ◽  
Weight Variation ◽  
Sustained Release Tablets

The present study involves in the formulation and evaluation of sustained release tablets of Voriconazole (250mg). The objective of the present study was to formulate Voriconazole sustained release tablets by wet granulation method by using natural (Xanthan gum, Karaya gum) and semi synthetic polymers (HPMC K100M). Lactose was used as diluting agent, Magnesium stearate was used as a lubricant and Talc was used as a glident. These sustained release tablets can release the drug up to 12 hours in predetermined rate. The formulated powder blend was evaluated for bulk density, tapped density, compressibility index and angle of repose. The formulated tablets were evaluated for physical characteristics of sustained release tablets such as thickness, hardness, friability, weight variation and drug content. The results of the formulations found to be within the limits specified in official books. The tablets were evaluated for In-vitro drug release studies by using USP type I dissolution test apparatus. The dissolution test was performed in 0.1 N HCL for 2 hr and phosphate buffer pH 6.8 for 10hrs. The in-vitro cumulative drug release profile of all formulations F1-F10 at 12 hours showed 84.25% to 99.82% drug release, respectively. From the data it was clear that by increasing the amount of polymer in the formulation the amount of drug release was decreased. Hence, Formulation F9 was the most promising formulation as it gives satisfactory release (99.82%) for 12 hours and F9 found to be the best formulation.DOI: http://dx.doi.org/10.3329/icpj.v2i10.16410 International Current Pharmaceutical Journal, September 2013, 2(10): 165-169

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.

scholarly journals Formulation and In-Vitro Evaluation of Sustained Release Matrix Tablets of Domperidone

2020 ◽  
Vol 8 (02) ◽  
pp. 40-45
Author(s):  
Chhitij Thapa ◽  
Roma Chaudhary
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Epigastric Pain ◽  
Matrix Tablets ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
In Vitro Drug Release ◽  
Weight Variation

INTRODUCTION Domperidone is a unique compound with gastro kinetic and antiemetic effects. It is used in the management of disorder by impaired motility like gastroesophageal reflux (in some instances), gastroparesis, dyspepsia, heartburn, epigastric pain, nausea, vomiting, and colonic inertia. The sustained release system is a widely accepted approach for slow drug release over an extended period to address the challenges of conventional oral delivery, including dosing frequency, drug safety, and efficacy. The study aims to formulate a domperidone sustained release tablet and compare the dissolution rate with the marketed formulations. MATERIAL AND METHODS Sustained release matrix tablets of domperidone were prepared by wet granulation method using different polymers such as HPMC K4M, ethyl cellulose, Gum acacia. Pre-compression studies like angle of repose, bulk density, tapped density, Carr's index, and Hausner’s ratio, and post-compression studies like weight variation, thickness, hardness, friability, drug content, and in-vitro drug release were evaluated.   RESULTS The release profile of domperidone sustained-release tablets was studied spectrophotometrically. The in-vitro dissolution study suggests the minimum %-cumulative drug release with 98.33% in F5. The %-cumulative drug release was maximum in F3 with 99.69%. The in-vitro drug release of all the formulations was non-significant compared to the marketed formulation (p<0.05), exhibiting the sustained-release property by all the formulations. CONCLUSION The pre-compression study concludes the better flow property of the granules of different formulations. The sustained release domperidone tablets were prepared successfully by the wet granulation method. The post-compression parameters of different formulations were within the acceptable range.

scholarly journals FORMULATION AND DESIGN OF EXTENDED RELEASE MATRIX TABLETS OF ZIDOVUDINE HYDROCHLORIDE: A STUDY ON EFFECT OF VARIOUS GRADES OF ETHOCEL AND HPMC

2018 ◽  
Vol 10 (3) ◽  
pp. 138
Author(s):  
Harekrishna Roy
Keyword(s):  
Drug Release ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Release Kinetic ◽  
Scanning Calorimetry ◽  
Differential Scanning Calorimetry Study ◽  
Scanning Electron Microscope Study ◽  
Weight Variation ◽  
Pure Drug

Objective: The current research was an attempt to formulate and design an extend release dosage form of zidovudine hydrochloride using various grades of ethyl cellulose (ethocel) such as ethocel 4CPS, ethocel 7 CPS and aqualon T10 Pharm EC with two grades of hydroxy propyl methyl cellulose (HPMC K4M and HPMC K15M).Methods: Pilot scale batches of nine formulations were prepared using kollidon and adopting wet granulation technique. Physiochemical properties of tablet and granules were examined prior compression to get tablet. Tablets were characterized as drug content, percentage weight variation, thickness, Hardness, percentage friability and in vitro drug release pattern and studied for 12 hour in USP Type-II apparatus using 900 ml Phosphate buffer at 37±0.5 °C. The dissolution release profile of drug in tablet was performed by various drug release kinetic modelling.Results: The result revealed formulation F8 containing ethocel 7CPS and aqualon T10 was able to delay the pure drug release for 12 h and followed Higuchi pattern. Whereas; formulations containing only ethocel 4CPS provided earlier drug release. Dissolution data of promising formulation were analysed with innovator formulation for similarity factor (f2), exhibited an acceptable value more than 50. FT-IR (fourier-transform infrared spectroscopy) and DSC (differential scanning calorimetry) study revealed no such incompatibility found between the pure drug and polymers but slight change in crystalinity were observed in XRD study (X-ray diffraction). SEM (scanning electron microscope) study revealed very rare intragranular pore and cavity.Conclusion: From that, it can be marked as viscosity and selection of ethocel have great importance in delay drug release. 

Formulation Development and In-vitro Evaluation of Sustained Release Tablets of Metoprolol Succinate

2021 ◽  
pp. 269-275
Author(s):  
Priyanka M. Salve ◽  
Rajendra K. Surawase
Keyword(s):  
Sustained Release ◽  
Half Life ◽  
Wet Granulation ◽  
Direct Compression ◽  
Formulation Development ◽  
Metoprolol Succinate ◽  
Dissolution Studies ◽  
Weight Variation ◽  
Sustained Release Tablets

Metoprolol succinate is a β1 selective antagonist used an anti-arrhythmic, antiagina, antihypertensive. sustained release tablet of metoprolol succinate were formulated using polymers. The half-life of drug is relatively 4-6 hours. The formulation of metoprolol succinate tablet were produced by direct compression or wet granulation method. The formulations were evaluated for thickness, hardness, weight variation, friability and dissolution, drug content all the physical characteristics of the formulated tablets were within acceptable limits. The dissolution studies of Metoprolol succinate sustained release tablets reflects USP specification NMT 25%by 1 hours, 20-40%by 4 hours,40-60%by 8 hours and more than 80% by 20 hrs.

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>

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