scholarly journals Comparison of drug release and mechanical properties of tramadol-hydrochloride matrix tablets prepared with selected hydrophilic polymers

2015 ◽  
Vol 21 (3) ◽  
pp. 369-378
Author(s):  
Nenad Nikolic ◽  
Djordje Medarevic ◽  
Jelena Djuris ◽  
Dragana Vasiljevic
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Large Scale ◽  
Mechanical Characteristics ◽  
Matrix Tablets ◽  
Hydrophilic Polymers ◽  
High Dose ◽  
Compression Pressure ◽  
Tramadol Hydrochloride ◽  
Compaction Simulator

This study investigates using of high molecular weight hydrophilic polymers, hypromellose and hydroxypropylcellulose, for the preparation of sustained release matrix tablets containing high dose, highly soluble drug, tramadol HCl. Proportion of polymer, type of insoluble filler, proportion of tramadol HCl, amount of drug in the tablet and compression pressure were recognized as critical formulation and process parameters and their influence on drug release and tablet mechanical properties was evaluated. Tensile strength was used as indicator of mechanical properties of the tablets. Experiments were performed with utilization of compaction simulator as a device which simulates compaction profiles of large scale rotary tablet presses. In formulations with both polymers proportion of tramadol HCl was the most critical formulation parameter wherein increasing of the tramadol HCl proportion increased its release rate in early stages of drug release. Regarding the tablet mechanical characteristics, the influence of the filler type has the most pronounced effect in formulations with both polymers. Higher tensile strengths were obtained with Avicel PH 102 as filler in formulations with both HPMC and HPC.

scholarly journals Evaluation of formulation and effects of process parameters on drug release and mechanical properties of tramadol hydrocloride sustained release matrix tablets

2015 ◽  
Vol 69 (5) ◽  
pp. 503-510 ◽  
Author(s):  
Nenad Nikolic ◽  
Djordje Medarevic ◽  
Svetlana Ibric ◽  
Zorica Djuric
Keyword(s):  
Mechanical Properties ◽  
Tensile Strength ◽  
Drug Release ◽  
Sustained Release ◽  
Process Parameters ◽  
Water Soluble ◽  
Matrix Tablets ◽  
High Dose ◽  
Compression Pressure ◽  
Water Soluble Drug

This study investigates using of high molecular weight polyethylene oxide (PEO WSR Coagulant) for the preparation of sustained release matrix tablets containing high dose, highly water soluble drug, tramadol HCl. Proportion of PEO polymer, type of insoluble filler, proportion of tramadol HCl, amount of drug in tablet, tablet diameter and compression pressure were recognized as critical formulation and process parameters and their influence on drug release and tablet mechanical properties was evaluated. Percentages of tramadol HCl released after 30 and 240 minutes were selected for evaluation of drug release, while tensile strength was used as indicator of tablet mechanical properties. Only proportion of tramadol HCl exhibits statistically significant effect on percentages of tramadol HCl released after 30 and 240 minutes, with higher, wherein increasing of the tramadol HCl proportion increased its release rate among the evaluated variables in selected ranges. All of the investigated factors exhibit statistically significant effect on tablets tensile strength, with the largest influence of filler type. Tablets prepared with highly compressible filler (microcrystalline celullose) exhibit higher tensile strength and therefore better mechanical properties to those prepared with partially pregelatinised starch (Strach 1500).

scholarly journals Formulation and Evaluation of Sustained Release Matrix Tablets of Aceclofenac

2021 ◽  
Vol 4 (2) ◽  
pp. 99-109
Author(s):  
Priyanka Singh ◽  
Amit Kumar Shrivastava ◽  
Sachin Kumar ◽  
Manish Dhar Dwivedi
Keyword(s):  
Drug Release ◽  
Guar Gum ◽  
Polymer Concentration ◽  
Matrix Tablets ◽  
Hydrophilic Polymers ◽  
Wet Granulation ◽  
Drug Release Profile ◽  
In Vitro Drug Release ◽  
Study Results

This study aimed to improve the dissolution rate of aceclofenac and release the drug in a controlled manner over a period of 24 hours. Matrix tablets were prepared by direct compression method, using hydrophilic polymers (HPMC/guar gum). Matrix tablets were prepared by wet granulation method using different hydrophilic polymers (HPMC/guar gum). Tablets were evaluated for in vitro drug release profile in phosphate buffer with pH 6.8 (without enzymes). The thickness and hardness of prepared tablets were 3.23 ± 0.035 to 3.28 ± 0.008 mm and 3.26 ± 0.115 to 3.60 ± 0.200 kg/cm2, respectively. The friability was within the acceptable limits of pharmacopoeial specifications (0.31 to 0.71%), which indicates the good mechanical strength of the tablets. Drug release was retarded with an increase in polymer concentration due to the gelling property of polymers. The in vitro drug release from the proposed system was best explained by Higuchi’s model, indicating that drug release from tablets displayed a diffusion-controlled mechanism. The results clearly indicate that guar gum could be a potential hydrophilic carrier in developing oral controlled drug delivery systems. Based on the study results, formulations F8 was selected as the best formulation.

scholarly journals Determining the Polymer Threshold Amount for Achieving Robust Drug Release from HPMC and HPC Matrix Tablets Containing a High-Dose BCS Class I Model Drug: In Vitro and In Vivo Studies

2014 ◽  
Vol 16 (2) ◽  
pp. 398-406 ◽  
Author(s):  
Uroš Klančar ◽  
Saša Baumgartner ◽  
Igor Legen ◽  
Polona Smrdel ◽  
Nataša Jeraj Kampuš ◽  
...  
Keyword(s):  
Drug Release ◽  
Matrix Tablets ◽  
Class I ◽  
In Vivo Studies ◽  
High Dose ◽  
Model Drug ◽  
Threshold Amount

scholarly journals Effect of compression pressure on mechanical and release properties of tramadol matrix tablets

2015 ◽  
Vol 28 (2) ◽  
pp. 120-125 ◽  
Author(s):  
Olutayo A. Adeleye ◽  
Mbang N. Femi-Oyewo ◽  
Michael A. Odeniyi
Keyword(s):  
Drug Release ◽  
Xanthan Gum ◽  
The Body ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Sodium Carboxymethylcellulose ◽  
Compression Pressure ◽  
Significant Difference ◽  
Tablet Manufacturing ◽  
Tablet Hardness

Abstract Drug delivery to the proper site of action in the body is greatly influenced by the excipients used and some processing variables such as changes in compression force. The aim of this investigation was to study the influence of changes in compression forces during tablet manufacturing on the mechanical and release properties of Tramadol matrix tablet. Hardness and friability were used as assessment parameters for mechanical properties while release properties were analysed using dissolution test. Data were analysed using One-way ANOVA at p < 0.05. Tablet hardness and friability were typically compression pressure-dependent with a significant difference in tablet hardness and friability with increase in compression pressure (p < 0.001). Drug release was best expressed by Korsmeyer-Peppas equation as the plots showed high linearity (r2) of 0.998 and 0.988 for formulations containing Xanthan gum and Sodium carboxymethylcellulose, respectively. Drug release from formulations containing Xanthan gum was mainly by diffusion while a combination of diffusion and chain relaxation was the mechanism of drug release from formulation containing Sodium Carboxymethylcellulose. The release properties of tramadol matrix tablet were not significantly influenced by compression pressure but rather by the polymer and the material properties of the drug.

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>

Influence of Formulation Variables and Processing Techniques on Drug Release from Carbopol-971 based Matrix Tablets of Cinnarizine and Nimodipine.

2010 ◽  
Vol 2 (1) ◽  
Author(s):  
Singh K. ◽  
Pandit K. ◽  
Mishra N.
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Polymer Concentration ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Weight Variation ◽  
Diffusion Controlled ◽  
The Matrix ◽  
Processing Techniques ◽  
Formulation Variables

The matrix tablets of cinnarizine and nimodipine were prepared with varying ratio of Carbopol- 971P and co-excipients of varying hydrophilicity (i.e. dicalcium phosphate and spray dried lactose) by direct compression and wet granulation using alcoholic mucilage. The prepared tablets were evaluated for weight variation, hardness and friability. The influence of concentration of the matrix forming material and co-excipients on the release rate of the drug was studied. The release rate of Cinnarizine (more soluble drug) from tablets followed diffusion controlled mechanism whereas for nimodipine (less soluble drug), the drug release followed case-II or super case- II transport mechanism based on Korsmeyer- Peppas equation. The results indicated that the drug release from matrix tablets was increases with increase in hydrophilicity of drug and co-excipients. The release of drug also increased with thermal treatment and decreasing polymer concentration.

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.  

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