scholarly journals Polyethylene oxide matrix tablet swelling evolution: The impact of molecular mass and tablet composition

2021 ◽  
Vol 71 (2) ◽  
pp. 215-243
Author(s):  
Petra Draksler ◽  
Urša Mikac ◽  
Peter Laggner ◽  
Amrit Paudel ◽  
Biljana Janković
Keyword(s):  
Percolation Threshold ◽  
Molecular Mass ◽  
Matrix Tablets ◽  
Heat Of Fusion ◽  
Matrix Tablet ◽  
Polyethylene Oxides ◽  
Erosion Coefficient ◽  
Gel Layer ◽  
Mass Dependent ◽  
The Impact

AbstractThis article describes the designing of matrix tablets composed of polyethylene oxides (PEOs) with relative molecular masses of 1 × 106, 2 × 106, and 4 × 106. Percolation thresholds were determined for all of the selected PEO formulations (18, 16, and 12 %, m/m), taking into consideration excipients and tablet surface area which significantly increased the percolation threshold. Moreover, the robustness of the gel layer in PEO matrix tablets was evaluated by magnetic resonance imaging under various mechanical stresses (no flow, 12 mL min−1, and 64 mL−1 of medium flow). Correlations between the percolation threshold and gel thickness (R2 = 0.86), gel thickness and the erosion coefficient (R2 = 0.96) was detected. Furthermore, small-angle X-ray scattering of the selected PEOs detected differences in polymer molecular complexity at the nanoscale. Finally, the ratio of the heat of coalescence to the heat of fusion has confirmed the PEO molecular mass-dependent percolation threshold.

scholarly journals Effect of solubility enhancers on the release of Carbamazepine from Hydrophilic Polymer based matrix tablet

2015 ◽  
Vol 13 (2) ◽  
pp. 167-173 ◽  
Author(s):  
Sharifa Sultana ◽  
Shimul Halder ◽  
AK Lutful Kabir ◽  
Abu Shara Shamsur Rouf
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Release Rate ◽  
Release Profile ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Solubility Enhancers ◽  
The Impact

In the present study, an attempt has been taken to evaluate the effect of sodium lauryl sulphate (SLS) and glyceryl mono stearate (GMS) as solubility enhancers on the release profile of a poorly soluble drug, carbamazepine. Matrix tablets of carbamazepine were prepared by wet granulation technique using hydrophilic polymers (10% of Methocel K15 MCR and 10% of Methocel K100LV CR) as release controlling agents. Varying amounts of SLS and GMS were used in six different formulations to observe the impact on the release rate and mechanism of drug release. The dissolution study of carbamazepine from these extended release matrix tablets was conducted for 24 hours using basket method in 900 ml distilled water as dissolution medium. The data obtained from the dissolution studies were explored and explained with the help of zero order, Higuchi, first order, Korsmeyer- Peppas and Hixson-Crowell equations. It was found that the dissolution rate of carbamazepine with the formulation containing SLS was higher than GMS containing formulation and increased concentration of SLS increasing the release rate. Where there was no SLS or smaller amount of SLS or GMS release rate was decreased. Formulation having equal ratio of SLS and GMS did not show the desire release profile. The drug release mechanism followed mainly super case II transport. These results clearly demonstrated that the dissolution rate, extent and mechanism of carbamazepine release could be changed by optimizing the amount of SLS and GMS in the tablet formulation. DOI: http://dx.doi.org/10.3329/dujps.v13i2.21894 Dhaka Univ. J. Pharm. Sci. 13(2): 167-173, 2014 (December)

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>

Formulation and Evaluation of Galantamine Hydrobromide Floating Matrix Tablet

2018 ◽  
Vol 8 (2) ◽  
Author(s):  
Poreddy Srikanth Reddy ◽  
Penjuri Subhash Chandra Bose ◽  
Vuppula Sruthi ◽  
Damineni Saritha
Keyword(s):  
Sodium Alginate ◽  
Xanthan Gum ◽  
Lag Time ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Matrix Tablet ◽  
Compression Technique ◽  
Weight Variation ◽  
The Matrix

The aim of the present work was to prepare floating tablets of galantamine HBr using sodium alginate and xanthan gum as matrix forming carriers. Galantamine HBr is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments, in particular those of vascular origin. The matrix tablet formulations were prepared by varying the concentrations of sodium alginate and xanthan gum. The tablets were prepared by direct compression technique using PVP K-30 as a binder and sodium bicarbonate for development of CO2. The prepared matrix tablets were evaluated for properties such as hardness, thickness, friability, weight variation, floating lag time, compatibility using DSC and FTIR. In vitro dissolution was carried out for 12 hrs in 0.1N HCl at 37±0.5 ºC using USP paddle type dissolution apparatus. It was noted that, all the prepared formulations had desired floating lag time and constantly floated on dissolution medium by maintaining the matrix integrity. The drug release from prepared tablets was found to vary with varying concentration of the polymers, sodium alginate and xanthan gum. From the study it was concluded that floating drug delivery system for galantamine HBr can be prepared by using sodium alginate and xanthan gum as a carrier.

Colon targeting oral matrix tablets of mesalamine: Design, development and invitro evaluation

2020 ◽  
Vol 10 (1) ◽  
pp. 18-27
Author(s):  
Audinarayana N ◽  
Anala Srinivasulu ◽  
Vellore Sruthikumari ◽  
Likitha ◽  
Ananda Deepak V
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Stability Study ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Matrix Tablet ◽  
Cellulose Acetate Phthalate ◽  
Design Development ◽  
Release Pattern ◽  
The Matrix

The principle in this present research is to formulate Mesalamine containing colon targeted tablets by using different polymers and evaluate the effect of different polymers in drug release pattern. The matrix tablets of Mesalamine are formulated by polysaccharides based polymers like Cellulose acetate phthalate (CAP), Ethyl cellulose (EC), Guar gum (GG) and Xanthan gum (XG) which protects the drug to release in Stomach and Small Intestine. The invitro drug dissolution investigation of F2 (GG and XG) Matrix tablet was controlled by swelling into a viscous gel in colonic pH, which have been accomplished as the best tablet. The optimized tablet F2 was found to be stable in stability study (short term) with reproducible evaluation data, which also shows the highest swelling index, increased viscosity in colonic pH. The drug release pattern from the F2 formulation follows swelling and erosion behavior. From the data it show that F2 tablets suitable for providing colon targeted drug delivery.

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.  

Formulation and Evaluation of Atenolol and Indapamide SR Matrix Tablets for Treatment of Hypertension

2014 ◽  
Vol 7 (2) ◽  
pp. 2450-2458
Author(s):  
Sarika Pundir ◽  
Ashutosh Badola
Keyword(s):  
Kinetic Studies ◽  
Film Coating ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Simultaneous Estimation ◽  
Matrix Tablet ◽  
Release Agent ◽  
Disintegration Time ◽  
Weight Variation

In the present study we have formulated (F1 to F6) matrix tablets of atenolol and indapamide for the management of hypertension. As in simultaneous estimation of these drugs it was found that a confined release can be formulated. In the formulation of SR matrix tablet by using different concentration of delayed release agent DCP and pregelatinized starch as disintegrant we prepared tablets by wet granulation method. For sustained release action HPMC polymers were used for film coating. Preformulation studies were performed prior to compression. The compressed SR matrix tablets were evaluated for weight variation, hardness, friability, drug content, disintegration time and in vitro drug release using USP dissolution apparatus type 2 (paddle). It was found that the optimized formulation showed 49.33%, 48.90%, 48.52%, 47.65%, 46.84% and 46.51% release for atenolol in 12 hours respectively. However, indapamide released 49.62%, 49.39%, 48.72%, 48.27%, 47.59% and 47.36% at the end of 12 hr. The IR spectrum study revealed that there is no disturbance in the principal peaks of pure drugs atenolol and indapamide. This confirms the integrity of pure drugs and no incompatibility of them with excipients. The stability studies were carried out for the optimized batch for one months and it showed satisfactory results. The kinetic studies of the formulations revealed that diffusion is the predominant mechanism of drug and release follows Zero-order, Super case II transport.

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.

Influence of exopolysaccharides on viscosity of sugar juices with low sucrose contents

2021 ◽  
pp. 523-528
Author(s):  
Radosław Gruska ◽  
Aneta Antczak-Chrobot ◽  
Agnieszka Sobala ◽  
Maciej Wojtczak
Keyword(s):  
Molecular Mass ◽  
Dynamic Viscosity ◽  
High Molecular Mass ◽  
Sucrose Content ◽  
Beet Sugar ◽  
The Impact ◽  
Dry Substance

The presence of dextran originating from frost-damaged or degraded beet is highly detrimental during beet sugar manufacture, because they cause difficulties in filtering the carbonatation juice. In this paper the impact of exopolysaccharides on the viscosity of low sucrose content juices including: raw juice, juice after the 1st filtration and thin juice were analyzed. Studies have shown that high molecular mass exopolysaccharides have a stronger effect on the juice viscosity than low molecular mass exopolysaccharides. However, the dynamic viscosity of technical sugar solutions (raw juice or thin juice) with exopolysaccharides at a content of up to 0.5 g/kg, is lower than the viscosity of pure sugar solutions having the same refractometric dry substance content (RDS).

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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