Pectin/anhydrous dibasic calcium phosphate matrix tablets for in vitro controlled release of water-soluble drug

Background: Venlafaxine HCl is a selective serotonin reuptake inhibitor which is given in the treatment of depression. The delivery of the drug at a controlled rate can be of great importance for prolonged effect. Objective: The objective was to prepare and optimize the controlled release core in cup matrix tablet of venlafaxine HCl using the combination of hydrophilic and hydrophobic polymers to prolong the effect with rate controlled drug release. Methods: The controlled release core in cup matrix tablets of venlafaxine HCl were prepared using HPMC K5, K4, K15, HCO, IPA, aerosol, magnesium sterate, hydrogenated castor oil and micro crystalline cellulose PVOK-900 using wet granulation technique. Total ten formulations with varying concentrations of polymers were prepared and evaluated for different physicochemical parameters such FTIR analysis for drug identification, In-vitro drug dissolution study was performed to evaluate the amount of drug release in 24 hrs, drug release kinetics study was performed to fit the data in zero order, first order, Hixson–crowell and Higuchi equation to determine the mechanism of drug release and stability studies for 3 months as observed. Results: The results of hardness, thickness, weight variation, friability and drug content study were in acceptable range for all formulations. Based on the In vitro dissolution profile, formulation F-9 was considered to be the optimized extending the release of 98.32% of drug up to 24 hrs. The data fitting study showed that the optimized formulation followed the zero order release rate kinetics and also compared with innovator product (flavix XR) showed better drug release profile. Conclusion: The core-in-cup technology has a potential to control the release rate of freely water soluble drugs for single administration per day by optimization with combined use of hydrophilic and hydrophobic polymers.

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In vitro and in vivo evaluation of guar gum matrix tablets for oral controlled release of water-soluble diltiazem hydrochloride

AAPS PharmSciTech ◽

10.1208/pt060105 ◽

2005 ◽

Vol 6 (1) ◽

pp. E14-E21 ◽

Cited By ~ 26

Author(s):

Saleh M. Al-Saidan ◽

Yellela S. R. Krishnaiah ◽

S. Patro ◽

Vemulapalli Satyanaryana

Keyword(s):

Controlled Release ◽

Guar Gum ◽

Water Soluble ◽

Matrix Tablets ◽

Diltiazem Hydrochloride ◽

In Vivo Evaluation

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FORMULATION DEVELOPMENT AND EVALUATION OF HIGHLY WATER-SOLUBLE DRUG-LOADED CONTROLLED RELEASE MATRIX TABLETS

Bulletin of Pharmaceutical Sciences. Assiut ◽

10.21608/bfsa.2021.174122 ◽

2021 ◽

Vol 44 (1) ◽

pp. 15-29

Author(s):

Aqsa Siraj ◽

Muhammad Nasiri ◽

Syed Naqvi ◽

Tariq Ali ◽

Rabia Yousaf ◽

...

Keyword(s):

Controlled Release ◽

Water Soluble ◽

Matrix Tablets ◽

Formulation Development ◽

Water Soluble Drug

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Formulation Development of Metoprolol Succinate Controlled Release Tablets using Ethyl-cellulose-polyvinyl-pyrrolidone Coating

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2015.8.2.8 ◽

2015 ◽

Vol 8 (2) ◽

pp. 2851-2857

Author(s):

Kiran Kumar Vangara ◽

Kishore K. Konda ◽

Shiva K. Ravula ◽

Pradeep K Vuppala ◽

Vijay K. Sripuram ◽

...

Keyword(s):

Weight Gain ◽

Controlled Release ◽

Drug Release ◽

Ethyl Cellulose ◽

Film Coating ◽

Release Profile ◽

Water Soluble ◽

Metoprolol Succinate ◽

Water Soluble Drug

It is challenging to develop a controlled release (CR) formulation for a freely water soluble drug molecule without using rate controlling polymers in the core matrix. This study is aimed to develop and evaluate cost-effective ethyl cellulose (EC)-polyvinyl pyrrolidone (PVP) film coating that can effectively control the release of freely water soluble drug, metoprolol succinate (MS) and to match that of release profile with its marketed tablet. Simple core tables of MS were compressed and coated with a solution composed of hydrophobic rate controlling polymer, EC and water soluble pore forming polymer, PVP. The effect of formulation parameters such as the ratio of EC to PVP and tablet coating weight gain on the in-vitro drug release were evaluated. Release profile of the optimized formulation at different pH conditions was determined and the similarity factor (f2) with marketed release profile was calculated.It was observed that drug release rate increased with a decrease in the ratio of ethyl cellulose to PVP and decreased with increased weight gain of the coating membrane. Among all the formulations, the formulation with EC and PVP at a ratio of 60:40 %w/w and 9% weight gain showed matching release profile to marketed tablet with f2 value of 72.25. The optimized formulation showed pH independent in-vitro release. This study successfully demonstrated that EC-PVP film coating can effectively control the release rate of freely soluble drugs. Once a day CR formulation of metoprolol succinate pharmaceutically equivalent to marketed tablet was developed.

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In vitro evaluation of sustained released matrix tablets containing ibuprofen: a model poorly water-soluble drug

Brazilian Journal of Pharmaceutical Sciences ◽

10.1590/s1984-82502016000400020 ◽

2016 ◽

Vol 52 (4) ◽

pp. 751-759 ◽

Cited By ~ 13

Author(s):

Wendy Leticia Guerra-Ponce ◽

Sandra Leticia Gracia-Vásquez ◽

Patricia González-Barranco ◽

Ivonne Antonieta Camacho-Mora ◽

Yolanda Araceli Gracia-Vásquez ◽

...

Keyword(s):

Water Soluble ◽

Matrix Tablets ◽

In Vitro Evaluation ◽

Water Soluble Drug ◽

Poorly Water Soluble ◽

Poorly Water Soluble Drug

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Swelling and Erosion Modulation of Sterculia Foetida Gum Through Real Time Texture Probing

Dhaka University Journal of Pharmaceutical Sciences ◽

10.3329/dujps.v7i2.2167 ◽

1970 ◽

Vol 7 (2) ◽

pp. 127-132 ◽

Cited By ~ 1

Author(s):

Bendgude Namdeo ◽

Iyer Vidya ◽

Poddar Sushilkumar

Keyword(s):

Controlled Release ◽

Drug Release ◽

Real Time ◽

Microcrystalline Cellulose ◽

Release Profile ◽

Water Soluble ◽

Matrix Tablets ◽

Diltiazem Hydrochloride ◽

Drug Release Profile ◽

Water Soluble Drug

In the present investigation an attempt has been made to increase therapeutic efficacy, reduce frequency of administration and improve patient compliance by developing controlled release matrix tablets of diltiazem hydrochloride. Diltiazem hydrochloride was formulated as oral controlled release matrix tablets by using sterculia foetida gum. SFG fines were characterized with scanning electron microscopy. The purpose of this study was to optimize release profile of the highly water soluble drug from SFG matrix by using water soluble and swellable excipients like lactose and microcrystalline cellulose respectively. Tablets were prepared by direct compression, and their swelling behavior in presence of these excipients was assessed with the help of a Texture Analyzer. Dissolution assessment was performed using USP 26 apparatus 2 modified by insertion of a mesh to prevent sticking of the tablets to the bottom of vessel and allow them to swell three dimensionally. The interdependence of swelling front movement in relation to excipients type and progression of drug release are explained. It was concluded that unlike in conventional dosage forms insertion of excipients in hydrophilic controlled release tablets containing a water soluble drug gave the finger print information of drug release profile. In vitro drug release from these matrices was characterized and confirmed with the help of real time texture probing. Results indicated that it is possible to achieve desired modulation in the drug release profile by inclusion of lactose and microcrystalline cellulose. Key words: Diltiazem HCl, Sterculia Foetida Gum, Swelling and erosion, Lactose, Texture analysis. doi: 10.3329/dujps.v7i2.2167 Dhaka Univ. J. Pharm. Sci. 7(2): 127-132, 2008 (December)

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Controlled Release of Resveratrol and Lignan by Matrix Tableting

Advanced Materials Research ◽

10.4028/www.scientific.net/amr.746.330 ◽

2013 ◽

Vol 746 ◽

pp. 330-336

Author(s):

Mont Kumpugdee-Vollrath ◽

Mario Helmis

Keyword(s):

Controlled Release ◽

Release Kinetics ◽

Research Work ◽

Magnesium Stearate ◽

Water Soluble ◽

Matrix Tablets ◽

Water Soluble Drug ◽

The Matrix ◽

Best Fitting ◽

Model Drug

The aim of this research work was to develop the controlled release of two model drugs i.e. water insoluble drug - resveratrol and water soluble drug - lignan by matrix tableting with an eccentric tablet machine. For this purpose different kinds of polymers i.e. Metolose 90 SH-4000® (HMPC), Fetocel RT-N-100® (EC) and Eudragit RLPO® (polymethacrylate) were used. The matrix tablets containing 2 %wt of a model drug which were mixed with 5, 10, 20, 30 and 50 %wt of the polymers mentioned above. In addition, a glidant composed of 1 %wt talc and 1 %wt magnesium stearate as well as a filler Ludipress® were processed. Different physical properties of the powder mixtures (e.g. flowability) and of the tablets (e.g. hardness, uniformity of mass or drug content, drug release, etc.) were determined. Most of the tablets met the physical requirements. If the polymer content got higher the release was slower, which can be confirmed by the lower values of k. The release kinetics were described by three typical mathematic models i.e. biphasic, Noyes-Whitney and KorsmeyerPeppas. The best fitting results were ordered as follows: biphasic > Noyes-Witney > KorsmeyerPeppas.

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