DESIGN AND CHARACTERIZATION OF ALFUZOSIN HCL GASTRORETENTIVE FLOATING MATRIX TABLETS EMPLOYING HPMC K 100M

INDIAN DRUGS ◽  
2018 ◽  
Vol 55 (11) ◽  
pp. 71-73
Author(s):  
Ch. Taraka Ramarao ◽  
◽  
J Vijaya Ratna ◽  
R. B. Srinivasa
Keyword(s):  
Drug Release ◽  
Dosage Forms ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Gastric Residence Time ◽  
Drug Release Mechanism ◽  
The Matrix ◽  
Gastro Retentive

The present investigation involves developing gastro retentive drug delivery systems (GFDDS) of alfuzosin HCl using HPMCK100M a is the matrixing agent and floating enhancer. Sodium bicarbonate in the acidic environment reacts with the acid and produces carbon dioxide. The gastro retentive tablets can be formulated to increase the gastric residence time and thereby increase the oral bioavailability. From the drug release study, it was concluded that the AFTB4 formula of HPMC K 100 M matrix tablets gives the controlled release up to 12 hours by showing increased release with floating lag time 24 seconds. Non – Fickian diffusion was the drug release mechanism from the matrix tablets formulated employing HPMC K 100 M. The matrix tablets (AFTB4) formulated employing 40 % HPMC K 100 M are best suited to be used for gastro retentive dosage form of alfuzosin HCl. Finally, it can be concluded that good candidates for the preparation of gastro retentive dosage forms due its gastric stability, gastric absorption and better bioavailability.

scholarly journals 5-Fluorouracil Release from Chitosan-Based Matrix.Experimental and Theoretical Aspects

2020 ◽  
Vol 57 (3) ◽  
pp. 180-188
Author(s):  
Roxana Iancu ◽  
Stefan Andrei Irimiciuc ◽  
Maricel Agop ◽  
Mihail Frasila ◽  
Maria-Alexandra Paun ◽  
...  
Keyword(s):  
Drug Release ◽  
Polarized Light ◽  
Crosslinking Density ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Morphological Aspects ◽  
Drug Release Mechanism ◽  
The Matrix

A series of four drug release formulations based on 5-fluorouracil encapsulated into a chitosan-based matrix were prepared by in situ hydrogelation with 3,7-dimethyl-2,6-octadienal. The formulations were investigated from structural and morphological aspects by FTIR spectroscopy, polarized light microscopy and scanning electron microscopy. It was established that 5-fluorouracil was anchored into the matrix as crystals, whose dimension varied as a function of the crosslinking density. The in vitro drug release simulated into a media mimicking the physiological environment revealed a progressive release of the 5-fluorouracil, in close interdependence with the crosslinking density. In the context of Pharmacokinetics behavioral analysis, a new mathematical procedure for describing drug release dynamics in polymer-drug complex system is proposed. Assuming that the dynamics of polymer-drug system�s structural units take place on continuous and nondifferentiable curves (multifractal curves), we show that in a one-dimensional hydrodynamic formalism of multifractal variables the drug release mechanism (Fickian diffusion, non-Fickian diffusion, etc) are given through synchronous dynamics at a differentiable and non-differentiable scale resolutions. Finally, the model is confirmed by the empirical data.

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>

scholarly journals THE ROLE OF MATRIX TABLET IN DRUG DELIVERY SYSTEM

2018 ◽  
Vol 10 (1) ◽  
pp. 1 ◽  
Author(s):  
Nita Mondal
Keyword(s):  
Controlled Release ◽  
Safety Margin ◽  
Oral Route ◽  
Dosage Forms ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Matrix Tablet ◽  
The Matrix ◽  
Potent Drug ◽  
Materials Used

Matrix tablet is an important tool for controlled and sustained release dosage forms. The oral route remains the most common route for the administration of drugs. Tablets offer the lowest cost approach to sustained and controlled release dosage forms. The hydrophilic polymer matrix is widely used in this dosage form. The use of different polymers in controlling the release of drugs has become the most important tool in the formulation of matrix tablets. The drug releases by both dissolution-controlled as well as diffusion-controlled mechanisms from the matrix. The development of oral controlled release systems has been a challenge to formulation scientists due to their inability to restrain and localize the system at targeted areas of the gastrointestinal tract. There are several advantages of matrix devices including improved patient compliance due to less frequent drug administration, reduction of fluctuation in steady-state drug levels, maximum utilization of the drug, increased safety margin of a potent drug. This review aims on the discussion of different materials used to prepare matrix tablets, different types of matrix tablets and the drug release mechanism from the matrices.

Techniques of Mucilage and Gum Modification and their Effect on Hydrophilicity and Drug Release

2020 ◽  
Vol 14 ◽  
Author(s):  
Rishabha Malviya ◽  
Vandana Tyagi ◽  
Dharmendra Singh
Keyword(s):  
Drug Release ◽  
Dosage Form ◽  
Extended Release ◽  
Release Mechanism ◽  
Release Agent ◽  
Drug Release Mechanism ◽  
Polymer Relaxation ◽  
Hydrophilic Matrices ◽  
The Matrix ◽  
High Degree

Aim: The manuscript aims to describe the techniques of modification of gums and mucilages and their effect on hydrophilicity and drug release. Discussion: The interest is increased in the fields of polymers which is obtained from natural origin and used in the preparation of pharmaceuticals. Mucilage and gum are natural materials, widely used in the preparation of novel dosage form and conventional dosage form. They are used in the pharmaceutical industry for various purposes like suspending, emulsifying, bio-adhesive, binding, matrix-forming, extended release and controlled release agent. Gum and mucilage are biodegradable, less toxic, cheap and easily available. Moreover, mucilage and gum can be changed to acquire tailored materials for the delivery of drugs and allow them to compete with commercially available synthetic products. These polysaccharides have unique swellability in an aqueous medium that can exert a retardant effect on drug release or act as a super disintegrant, depending on the concentration utilized in the preparation. Drug release mechanism from hydrophilic matrices consisting of gums and mucilages is based on solvent penetration-induced polymer relaxation, diffusion of entrapped drug followed by degradation or erosion of the matrix. Conclusion: The present manuscript highlight the advantages, modifications of gum and mucilage, their effects on hydrophilicity and drug release as well as aspects of the natural gums which can be assumed to be bifunctional excipient because of their concentration-dependent effect on drug release and their high degree of swellability.

Synthesis and Evaluation of Starch – Urea – Borate as Rate Controlling Matrix for Controlled Release

1970 ◽  
Vol 1 (2) ◽  
pp. 167-170
Author(s):  
Chowdary KPR ◽  
Murali Krishna MN
Keyword(s):  
Controlled Release ◽  
Release Rate ◽  
Guar Gum ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Drug Release Mechanism ◽  
Zero Order Kinetics ◽  
Diffusion Controlled ◽  
Controlled Release Tablets

The objective of the present investigation is to synthesize starch – urea – borate, a new starch based polymer and to evaluate its application in the design of controlled release matrix tablets of diclofenac and gliclazide. The release rate controlling efficiency of starch – urea – borate was also compared with that of known polymers. Starch – urea – borate (SUB) polymer was synthesized by gelatinization of starch in the presence of urea and borax. Matrix tablets of diclofenac (100 mg) and gliclazide (60 mg) were formulated employing starch – urea – borate polymer in different proportions of drug and polymer and the tablets were evaluated. With both diclofenac and gliclazide, release from the formulated matrix tablets was slow and spread over 24 h and depended on percent polymer in the tablet. Release was diffusion controlled and followed zero order kinetics. Non – fickian diffusion was the drug release mechanism from the formulated tablets. Diclofenac release from matrix tablets formulated employing 33 % SUB (DF3) and Gliclazide release from matrix tablets formulated employing 50 % SUB (GF4) was similar to that from the corresponding commercial SR tablets. Starch – urea – borate polymer was found suitable for the design of oral controlled release tablets of diclofenac and gliclazide. The order of increasing release rate controlling efficiency with various polymers was ethyl cellulose = guar gum > SUB > sodium CMC > HPMC. Starch – urea – borate is a better release rate controlling polymer than HPMC and sodium CMC for obtaining controlled release over    24 hours.

FORMULATION AND EVALUATION OF SUMATRIPTAN SUCCINATE AND NAPROXEN SODIUM GASTRORETENTIVE (FLOATING) BILAYERED TABLETS

INDIAN DRUGS ◽  
2021 ◽  
Vol 57 (10) ◽  
pp. 30-41
Author(s):  
K. Srinivasa Reddy ◽  
D. Vinay Kumar ◽  
CH. Lakshmi Bharath ◽  
P. Sri Ramya Madhuri
Keyword(s):  
Drug Release ◽  
Naproxen Sodium ◽  
Slow Release ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Direct Compression ◽  
Compression Method ◽  
Sumatriptan Succinate ◽  
Rapid Release ◽  
Gastro Retentive

The main aim of the present work was to formulate and evaluate sumatriptan succinate and naproxen sodium gastro retentive(floating) bilayered tablets. Floating bilayer tablets were formulated using direct compression method, it consist of two layers i.e IR layer containing Naproxen and floating CR layer containing sumatriptan. IR2 layer containing 2% concentration of Cross Povidone was found to be optimum and released 99.23% of naproxen in 45min. The optimized floating CR8 layer containing HPMC K 100M in 46% concentration showed 81.21% of drug release at the end of 12h. Among all formulations, IR2 & CR8 provided slow release of sumatriptan over 12h and rapid release of naproxen within 45 min, hence it is considered as an optimum bilayered formulation of sumatriptan and naproxen. The optimised formulation was fitted in the Kinetic models and it follows Korsmeyer-Peppas kinetics and the release mechanism was Case II non- fickian diffusion from these tablets.

scholarly journals Development and evaluation of gastroretentive norfloxacin floating tablets

2009 ◽  
Vol 59 (2) ◽  
pp. 211-221 ◽  
Author(s):  
Ramesh Bomma ◽  
Rongala Swamy Naidu ◽  
Madhusudan Yamsani ◽  
Kishan Veerabrahma
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Drug Bioavailability ◽  
Floating Tablets

Development and evaluation of gastroretentive norfloxacin floating tabletsFloating matrix tablets of norfloxacin were developed to prolong gastric residence time, leading to an increase in drug bioavailability. Tablets were prepared by the wet granulation technique, using polymers such as hydroxypropyl methylcellulose (HPMC K4M, HPMC K100M) and xanthan gum. Tablets were evaluated for their physical characteristics,viz., hardness, thickness, friability, and mass variation, drug content and floating properties. Further, tablets were studied forin vitrodrug release characteristics for 9 hours. The tablets exhibited controlled and prolonged drug release profiles while floating over the dissolution medium. Non-Fickian diffusion was confirmed as the drug release mechanism from these tablets, indicating that water diffusion and polymer rearrangement played an essential role in drug release. The best formulation (F4) was selected based onin vitrocharacteristics and was usedin vivoradiographic studies by incorporating BaSO4. These studies revealed that the tablets remained in the stomach for 180 ± 30 min in fasting human volunteers and indicated that gastric retention time was increased by the floating principle, which was considered desirable for the absorption window drugs.

Development and Evaluation of Gastrobioadhesive Glimepiride Sustained Release Matrix Tablet Using Aegle Marmelos Polysaccharide

2020 ◽  
Vol 14 (1) ◽  
pp. 5297-5306
Author(s):  
M. A. Shende ◽  
Yogesh P Khedkar
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Residence Time ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Matrix Tablet ◽  
Aegle Marmelos ◽  
Gastric Residence Time ◽  
Weight Variation

The purpose of present study was to formulate and evaluate glimepiride gastrobioadhesive drug delivery using Aegle Marmelos polysaccharide and synthetic polymer for prolongation of gastric residence time and reduce the dosing frequency. Glimepiride matrices were prepared by direct compression method and evaluated with an aim of presenting glimepiride as sustained release for improving the patient’s compliance. A central composite design (CCD) was employed as Aegle Marmelos polysaccharide (X1) and HPMC K4M (X2) independent variables to optimize the glimepiride in terms of sustained release and gastrobioadhesive. The response (Y1) as bioadhesive strength, (Y2) percentage drug releases at 8 h and (Y3) time (t50) required to 50% drug release were measured for each trial and statistical equations with significant interaction terms were derived to predict relation. The physical properties of all formulations hardness, friability, drug content and weight variation were found within limits indicating that the prepared matrix tablets met the USP specifications. Among all the formulations, F1 formulation found to be optimized based on the criteria of attaining the maximum value of drug released Q8 of 98.58±1.12%, 18.43 g bioadhesive strength and time to 50% drug release (t50) of 6 h. An in-vitro drug release studies reveals that as concentrations of polymers increases the drug release decreases, producing sustained release of glimepiride. The release co-efficient values ‘n’ (˂0.3645) indicated that the drug release (F1) followed fickian diffusion mechanism kinetics. A glimepiride gastroadhesive matrix was developed to enhance its bioavailability by prolonging the gastric residence time with desirable release modulation for a once daily administration.

scholarly journals STUDIES ON CROSS-LINKED CHITOSAN HYDROGEL FOR MATRIX TABLETS OF MONTELUKAST SODIUM

2017 ◽  
Vol 9 (4) ◽  
pp. 22
Author(s):  
Srinivas Hebbar ◽  
Akhilesh Dubey ◽  
Ravi G. S. ◽  
Shanon Ben Mascarenhas
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Cross Linking ◽  
Release Mechanism ◽  
Release Kinetic ◽  
Montelukast Sodium ◽  
Hydrogel Matrix ◽  
Crosslinking Agents

Objective: The aim of the present study was to prepare hydrogel matrix tablets for controlled release of an anti-asthma drug (Montelukast sodium) by modifying the applications of chitosan by crosslinking it with the different cross linking agent.Methods: The hydrogels were prepared by crosslinking chitosan using three different crosslinking agents namely, anhydrous dextrose (DXT), sodium tripolyphosphate (TPP) and glutaraldehyde (GL). Formulations were prepared by direct compression method and pre and post compression parameters were evaluated.Results: FTIR (Fourier transform infrared spectroscopy) studies of tablet formulation indicated that there is no drug-excipient interaction in the prepared formulations. The matrix tablets were capable of releasing the drug for 11 h depending upon the formulation variables. The tablets prepared by plain chitosan discharged the drug quickly, while those prepared by using GL crosslinked-hydrogel released the drug more slowly in a controlled manner. In general, the order of drug release from the crosslinked hydrogel matrix tablets on the basis of crosslinking agents, was found to be DXT>TPP>GL. The type of cross-linking agents affected the drug release rate and in the case of the tablets prepared with CHTPP (95 % to 83 %) it was slower than for the tablets prepared with CHDX (96 % to 88 %) at the end of 11th h. CHGL tablets showed more prolonged drug release profiles (86 % to 74 %) as compared to CHDX and CHTPP at the end of 11th h. In vitro release data was fitted into various release kinetic models to study the release mechanism and showed zero order kinetics and “n” value were found to be less than 0.5 indicated the release mechanism followed fickian diffusion due to swelling of gel matrix and high solubility of montelukast sodium.Conclusion: From the experimental results it can be concluded that hydrogels of chitosan were successfully prepared by using DXT, TPP and GL with different concentration.

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