Preparation and evaluation of sustained release carbamazepine matrix tablets using Eudragit RS 100 and Tragacanth

The aim of this study was to formulate and evaluate sustained release microsphere of Venlafaxine HCl (VF-HCl). It has many side effects with a half life around 5 hr. To reduce the adverse actions due to burst effect a sustained release (SR) Eudragit RS-100 microspheres embedded VF-HCl was formulated. The VF-HCl microspheres were prepared by oil in oil (O/O) solvent evaporation method. Drug and Polymer interaction for formulated SR Eudragit RS-100 microsphere embedded on VF-HCl was characterized by FT-IR and X-RD studie. The result showed that there is no interaction between the drug and polymer. Surface morphology of formulation carried out by FE-SEM showed good spherical geometry and uniformity in size and shape. It can be concluded that the formulated VF-HCl microspheres using widely accepted O/O method and polymer were capable for exhibiting sustained release formulation with decreasing dosing frequency thereby minimizing the occurrence of side effects with improved bioavailability. DOI: http://dx.doi.org/10.3329/dujps.v13i1.21867 Dhaka Univ. J. Pharm. Sci. 13(1): 83-91, 2014 (June)

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Preparation and Evaluation of Sustained Release Calcium Alginate Beads and Matrix Tablets of Acetazolamide

Drug Research ◽

10.1055/s-0032-1331755 ◽

2013 ◽

Vol 63 (02) ◽

pp. 60-64 ◽

Cited By ~ 5

Author(s):

M. Barzegar-Jalali ◽

J. Hanaee ◽

Y. Omidi ◽

S. Ghanbarzadeh ◽

S. Ziaee ◽

...

Keyword(s):

Sustained Release ◽

Calcium Alginate ◽

Alginate Beads ◽

Matrix Tablets ◽

Calcium Alginate Beads ◽

Preparation And Evaluation

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Preparation and Evaluation of Sustained-Release Matrix Tablets Based on Metoprolol and an Acrylic Carrier Using Injection Moulding

AAPS PharmSciTech ◽

10.1208/s12249-012-9848-6 ◽

2012 ◽

Vol 13 (4) ◽

pp. 1197-1211 ◽

Cited By ~ 17

Author(s):

T. Quinten ◽

G. P. Andrews ◽

T. De Beer ◽

L. Saerens ◽

W. Bouquet ◽

...

Keyword(s):

Sustained Release ◽

Injection Moulding ◽

Matrix Tablets ◽

Preparation And Evaluation

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Studies in Preparation and Evaluation of pH‐Independent Sustained‐Release Matrix Tablets of Verapamil HCl Using Directly Compressible Eudragits

Pharmaceutical Development and Technology ◽

10.1081/pdt-120024686 ◽

2003 ◽

Vol 8 (4) ◽

pp. 323-333 ◽

Cited By ~ 15

Author(s):

Mukesh C. Gohel ◽

Tejas P. Patel ◽

Shital H. Bariya

Keyword(s):

Sustained Release ◽

Matrix Tablets ◽

Verapamil Hcl ◽

Preparation And Evaluation

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Preparation and evaluation of dual modified Ethiopian yam (Dioscorea abyssinica) starch for sustained release tablet formulations

Ethiopian Pharmaceutical Journal ◽

10.4314/epj.v34i1.4 ◽

2019 ◽

Vol 34 (1) ◽

pp. 37-50

Author(s):

Yohaness Mulualem ◽

Anteneh Belete ◽

Tsige Gebre-Mariam

Keyword(s):

Sustained Release ◽

Moisture Sorption ◽

Flow Property ◽

Matrix Tablets ◽

Cross Linking ◽

Disintegration Time ◽

Swelling Properties ◽

Hausner Ratio ◽

Modified Starches ◽

Preparation And Evaluation

Starch has been intensively studied over decades due to the fact that native starches are diverse, biodegradable, amenable to modifications and have enormous applications. In this study, Dioscorea abyssinica starch has been chemically dual modified by cross-linking using sodium hexametaphosphate (SHMP) followed by acetylation with acetic anhydride (AA). The physicochemical and tablet forming properties of the modified starches were investigated to determine potential usages in sustained release (SR) applications. Moisture sorption and swelling properties of the native starch (NS) were improved by the dual modification. The reduction observed in viscosity values indicated the effectiveness of cross-linking in reducing swelling of the NS. On the basis of powder properties analysis, it was evident that acetylation improved the poor flow property of NS. The starch acetylated at starch:AA ratio of 1:2 was found to be free flowing with angles of repose of 23.02o and flow rate 10.54 g/sec. The Hausner ratio and Carr’s index also confirmed the same, 1.25 and 20.24, respectively. Tablets were prepared and evaluated for hardness, tensile strength, friability, and disintegration time. Results indicated that both cross-linking and acetylation processes improved tablet forming properties of the NS with more significant effect in the dual modified starches. Matrix tablets containing Ac-CLS-F, where cross-linked starch (CLS – at 15% SHMP) reacted in a 1:2 ratio with AA, loaded with 20, 30 and 40% theophylline released 80% of theophylline in about 10.62, 9.35, and 8.18 h, respectively. From the foregoing, it can be concluded that Ac-CLS-F could have a potential for use as a sustained release excipient.Keywords: Dioscorea abyssinica, cross-linking, acetylation, dual modification, sustained release

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Directly Compressed Mini Matrix Tablets Containing Ibuprofen: Preparation and Evaluation of Sustained Release

Drug Development and Industrial Pharmacy ◽

10.1080/03639040500388482 ◽

2006 ◽

Vol 32 (1) ◽

pp. 95-106 ◽

Cited By ~ 21

Author(s):

Carla M. Lopes ◽

José Manuel Sousa Lobo ◽

Paulo Costa ◽

João F. Pinto

Keyword(s):

Sustained Release ◽

Matrix Tablets ◽

Preparation And Evaluation

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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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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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