Formulation and Evaluation of Levetiracetam Matrix Tablet Using Polyethylene Oxides

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.

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Effects of release modifier on Carvedilol release from Kollidon SR based matrix

International Current Pharmaceutical Journal ◽

10.3329/icpj.v1i8.11095 ◽

2012 ◽

Vol 1 (8) ◽

pp. 186 ◽

Cited By ~ 1

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

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.DOI: <a href="http://dx.doi.org/10.3329/icpj.v1i8.11095">http://dx.doi.org/10.3329/icpj.v1i8.11095</a> International Current Pharmaceutical Journal 2012, 1(8): 186-192

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Formulation and Evaluation of Galantamine Hydrobromide Floating Matrix Tablet

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v8i2.13868 ◽

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.

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

International Journal of Novel Trends in Pharmaceutical Sciences ◽

10.26452/ijntps.v10i1.1144 ◽

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.

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A Comparative Study of Matrix Tablets Designed by Different Methods

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2017.10.2.2 ◽

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.

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

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2014.7.2.7 ◽

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.

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Development of Prolonged Delivery of Tramadol and Dissolution Translation by Statistical Data Treatment

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2011.4.1.5 ◽

2011 ◽

Vol 4 (1) ◽

pp. 1331-1337

Author(s):

P B Parejiya ◽

B S Barot ◽

P K Shelat

Keyword(s):

Drug Release ◽

Study Data ◽

Stability Study ◽

Dissolution Time ◽

Matrix Tablet ◽

Burst Effect ◽

The Matrix ◽

The Mean ◽

The Difference ◽

Dissolution Efficiency

The present study was carried out to fabricate a prolonged design for tramadol using Kollidon SR (Polyvinyl acetate and povidone based matrix retarding polymer). Matrix tablet formulations were prepared by direct compression of Kollidon SR of a varying proportion with a fixed percentage of tramadol. Tablets containing a 1:0.5 (Drug: Kollidon SR) ratio exhibited a rapid rate of drug release with an initial burst effect. Incorporation of more Kollidon SR in the matrix tablet extended the release of drug with subsequent minimization of the burst effect as confirmed by the mean dissolution time, dissolution efficiency and f2 value. Among the formulation batches, a direct relationship was obtained between release rate and the percentage of Kollidon SR used. The formulation showed close resemblance to the commercial product Contramal and compliance with USP specification. The results were explored and explained by the difference of micromeritic characteristics of the polymers and blend of drug with excipients. Insignificant effects of various factors, e.g. pH of dissolution media, ionic strength, speed of paddle were found on the drug release from Kollidon-SR matrix. The formulation followed the Higuchi kinetic model of drug release. Stability study data indicated stable character of Batch T6 after short-term stability study.

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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 ◽

10.3390/pharmaceutics13060804 ◽

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.

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