scholarly journals CONTROLLED-RELEASE EFFERVESCENT FLOATING MATRIX TABLETS OF METFORMIN USING COMBINATION OF POLYMERS

2016 ◽  
Vol 8 (11) ◽  
pp. 114
Author(s):  
Meenakshi Bhavesh Patel ◽  
Farhatjahan Shaikh ◽  
Vandana Patel ◽  
Naazneen Imtiaz Surti
Keyword(s):  
Controlled Release ◽  
Xanthan Gum ◽  
Statistical Design ◽  
Matrix Tablets ◽  
High Dose ◽  
Direct Compression ◽  
Compression Method ◽  
Sustained Drug Release ◽  
Kappa Carrageenan ◽  
Gastro Retentive

Objective: It is always challenging to prepare the floating gastro retentive formulation of the high dose drug. The present research was aimed to prepare gastro retentive controlled release, matrix tablets of metformin, using the combination of different ionic, anionic and polyanionic polymers with HPMC.Methods: Formulations were prepared using sodium alginate, pullulan, kappa carrageenan, xanthan gum, poloxamer 68 in combination with HPMC K15M. All matrix tablets were prepared by direct compression method and evaluated for swelling, floating adhesive period and drug release.Results: All the tablets showed acceptable physicochemical properties. Statistical analyses of data revealed that tablets prepared using HPMC K15M and kappa carrageenan, formulation F2, is best in terms of showing excellent floating properties, extended adhesion periods and sustained drug release characteristics with similarity factor as 92 on comparison with the theoretical release of the drug.Conclusion: The combination of HPMC K15M and kappa carrageenan can be further optimized by applying the appropriate statistical design.

Development and Evaluation of Controlled Release Mucoadhesive Tablets of Captopril

1970 ◽  
Vol 9 (3) ◽  
pp. 3318-3329
Author(s):  
Kranthi Kumar Kotta ◽  
L. Srinivas
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Xanthan Gum ◽  
Diffusion Mechanism ◽  
Matrix Tablets ◽  
Fickian Diffusion ◽  
Content Uniformity ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets

The present investigation focuses on the development of mucoadhesive tablets of captopril which are designed to prolong the gastric residence time after oral administration. Matrix tablets of captopril were formulated using four mucoadhesive polymers namely guar gum, xanthan gum, HPMC K4M and HPMC K15M and studied for parameters such as weight variation, thickness, hardness, content uniformity, swelling index, mucoadhesive force and in vitro drug release. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M provide slow release of captopril over period of 12 hr and were found suitable for maintenance portion of oral controlled release tablets. The cumulative % of drug release of formulation F9 and F10 were 90 and 92, respectively. In vitro release from these tablets was diffusion controlled and followed zero order kinetics. The ‘n’ values obtained from the pappas-karsemeyer equation suggested that all the formulation showed drug release by non-fickian diffusion mechanism. Tablets formulated Xanthan gum or HPMC K4M with HPMC K15M (1:1) were established to be the optimum formulation with optimum bioadhesive force, swelling index & desired invitro drug release. This product was further subjected to stability study, the results of which indicated no significant change with respect to Adhesive strength and in vitro drug release study.

scholarly journals The Effect of Manufacturing Methods and Different Shapes on the Release Pattern of Diclofenac Sodium Matrix Tablet

1970 ◽  
Vol 2 (2) ◽  
pp. 76-80
Author(s):  
Tajnin Ahmed ◽  
Muhammad Shahidul Islam ◽  
Tasnuva Haque ◽  
Mohammad Abusyed
Keyword(s):  
Sustained Release ◽  
Release Rate ◽  
Diclofenac Sodium ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Compression Method ◽  
Release Pattern ◽  
Peg 600

In the present study sustained release diclofenac sodium matrix tablets were prepared using Kollidon SR polymer. Hydroxypropyl methylcellulose (HPMC 15 cps) and poly ethylene glycol (PEG-600) polymers respectively were used in formulating tablets prepared by direct compression and wet granulation methods. The polymers were used to explore the release pattern of the drug into the dissolution media. The tablets were also prepared in various shapes (caplet oval, round oval and flat oval). A comparatively higher release rate of drug was obtained from the polymer HPMC 15 cps at 10% concentration for directly compressed matrix tablet than those containing 20% of HPMC after a definite period of time. In wet granulation process, 10% PEG-600 containing tablets showed a better release than those containing 20% PEG. The drug release was also found to be sustained in case of wet granulation method than that of the direct compression method. Again the caplet shaped tablets in case of direct compression method showed better release rate of drug than those of the round oval and flat oval shaped tablets. Thus the result of this study shows that the proper selection of the percentage of polymer and the suitable shape of tablet and proper manufacturing method can provide a greater opportunity in designing sustained release dosage forms. Key words: Matrix tablet; release pattern; direct compression; wet granulation; PEG 600; Kollidon SR.DOI: 10.3329/sjps.v2i2.5828Stamford Journal of Pharmaceutical Sciences Vol.2(2) 2009: 76-80

scholarly journals FORMULATION AND EVALUATION OF EFFERVESCENT GASTRO-RETENTIVE FLOATING TABLETS FOR CONTROLLED RELEASE OF AN ANTI-ULCER COMPOUND

2013 ◽  
Vol 3 (1) ◽  
pp. 23-30
Author(s):  
Aleksandar Aleksovski ◽  
◽  
Emina Zahirović ◽  
Amra Demirović ◽  
Emilija Spaseska Aleksovska ◽  
...  
Keyword(s):  
Small Intestine ◽  
Controlled Release ◽  
Hydroxypropyl Methylcellulose ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Different Types ◽  
Model Drug ◽  
Absorption Window ◽  
Pharmacopoeial Requirements ◽  
Gastro Retentive

Effervescent floating gastro-retentive matrix tablets present novel and promising approach towards targeted and controlled drug delivery in the stomach and in the upper part of the small intestine. This kind of dosage form could be obtained by combining in a suitable ratio effervescent compounds and hydrophilic/hydrophobic polymer/s. The aim of our investigation was to develop controlled release effervescent matrix tablet which will float over the gastric media for longer than 8 hours and will release the active compound in a continuous manner over 8 hours period. We used ranitidine HCl as a model drug which has narrow absorption window in the upper small intestine, and is a good candidate for this type of dosage forms. We employed sodium bicarbonate and citric acid as effervescent compounds and two different types of hydroxypropyl methylcellulose (HPMC K4M and HPMC K15M) as a controlled release hydrophilic polymer. Three batches of tablets were produced (one containing HPMC K4M, other containing HPMC K15M, and the third containing 1:1 mixture of these two polymers) and every batch was compressed with two different forces 5.5 kN and 4.7 kN, so completely six probes of tablets were made. All six probes complied the pharmacopoeial requirements concerning mass uniformity, content, friability and hardness. All six probes tended to float fast to the surface of the medium and tend to hydrate and swell fast enough which actions provided controlled release of the compound over period of 8 hours. No significant differences in the dissolution profiles of all six probes were noticed during the investigation.

scholarly journals DoE-Based Design of a Simple but Efficient Preparation Method for a Non-Effervescent Gastro-Retentive Floating Tablet Containing Metformin HCl

Pharmaceutics ◽  
2021 ◽  
Vol 13 (8) ◽  
pp. 1225
Author(s):  
Byungsuk Kim ◽  
Youngjoo Byun ◽  
Eun Hee Lee
Keyword(s):  
Hydroxypropyl Methylcellulose ◽  
Cetyl Alcohol ◽  
Metformin Hydrochloride ◽  
High Dose ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Bootstrap Analysis ◽  
Similarity Factor ◽  
Gastro Retentive

A sustained-release non-effervescent floating matrix tablet was prepared using a simple and efficient direct compression of spray-dried granules containing metformin hydrochloride and cetyl alcohol with hydroxypropyl methylcellulose K15M (HPMC K15M). The design of experiments was employed to explore the optimal composition of the tablet. The similarity factor was employed to evaluate the equivalence in dissolution profiles between the test tablets and Glucophage XR as a reference. Bootstrap analysis was used to eliminate the formulations for which the dissolution profile was potentially inequivalent to that of the reference. The optimized tablet consisting of 150 mg of cetyl alcohol and 17% HPMC K15M showed a dissolution profile comparable with that of the reference with a similarity factor of 52.41, exhibited a floating lag time of less than 3 s in buffer media, remained floating for 24 h, and reduced the tablet weight by about 20% compared to that of the reference. The current study sheds light on the potential use of non-effervescent gastro-retentive extended-release tablets for high-dose drugs using a simple and efficient direct compression method, and as a potential alternative treatment for Glucophage XR. This study also highlights the importance of a systematic approach to formulation optimization and the evaluation of the dissolution profile.

Preparation and Evaluation of Ternary Polymeric Blends for Controlled Release Matrices Containing Weakly Basic Model Drug

2020 ◽  
Vol 17 ◽  
Author(s):  
Wasfy M. Obeidat ◽  
Shadi F. Gharaibeh ◽  
Abdolelah A. Jaradat ◽  
Osama Abualsuod
Keyword(s):  
Controlled Release ◽  
Drug Release ◽  
Sodium Alginate ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Sustained Drug Release ◽  
Basic Drug ◽  
Basic Model ◽  
Polymeric Compositions ◽  
Model Drug

Objective: The objective of this study was to evaluate the suitability of ternary mixture of smart polymers comprised of Eudragit®E100, Eudragit®L100, and sodium alginate to serve as a carrier for sustained drug release for weakly basic drugs. The model drug chosen in this part of the study is Metronidazole. Methods: Matrix tablets formulations were prepared by either direct compression or by wet granulation. Dissolution studies were conducted using USP XXΠ rotating paddle apparatus in three different consecutive stages (pH 1.2, 4.8 and 6.8). Tablets made of low to intermediate proportions of sodium alginate and an approximately equal proportions of Eudragit®E100 and Eudragit®L100 were found to have significant modification of drug release rates. Result: Thus, indicating a potential for controlling the drug release for 12 hours depending on polymers ratios in the formulation. The ratio of sodium alginate to total Eudragit® polymers and the ratio of Eudragit®E100 to Eudragit®L100 within the ternary polymeric composition were found critical in determining the controlled release performance. Conclusion: Results of swelling studies were in agreement with the dissolution behaviors of the tablets. The findings suggest the significance of the ternary polymeric compositions in controlling the release of weakly basic drug.

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 Formulation and evaluation of gastro-retentive floating tablets of terbinafine

2020 ◽  
Vol 13 (1) ◽  
pp. 257-266
Author(s):  
Kapil Jalodiya ◽  
Sourabh Jain ◽  
Karunakar Shukla
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Extended Period ◽  
Direct Compression ◽  
Compression Method ◽  
In Vitro Drug Release ◽  
Floating Tablets ◽  
Gastro Retentive

Gastro-retentive dosage forms enable prolonged and continuous input of the drug to the upper parts of the gastrointestinal tract and improve the bioavailability of medications those are characterized by a narrow absorption window. The purpose of this research was to develop a novel gastro retentive drug delivery system based on direct compression method for sustained delivery of active agent to improve the bioavailability, reduce the number of doses and to increase patient compliance. Gastro retentive floating tablets of terbinafine were prepared by direct compression method using altered concentrations of HPMC K4, HPMC K15 and PVP K30 as polymers. The prepared tablets of terbinafine were evaluated tablet hardness, uniformity of weight, friability, uniformity of content, in vitro buoyancy test, swelling index, in vitro dissolution study and stability study. All the compositions were resulted in adequate Pharmacopoeial limits. Compatibility studies was execution during FTIR shown that there was absence of probable chemical interaction between pure drug and excipients. The varying concentration of gas generating agent and polymers was found to affect on in-vitro drug release and floating lag time. In vitro drug release of floating gastro retentive tablet of terbinafine shown that the formulation F5 was found to be the best formulation as it releases 96.22% terbinafine in a controlled manner for an extended period of time (up to 480 min). The release data was fitted to various mathematical models such as Higuchi, Korsmeyer-Peppas, First order and Zero order to evaluate the kinetics and mechanism of the drug release. Prepared floating tablets of terbinafine may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system.

scholarly journals Formulations of sustained release matrix tablets of Furosemide using natural and synthetic polymers

2021 ◽  
Vol 11 (5) ◽  
pp. 105-109
Author(s):  
Shivani Soni ◽  
Vivek Jain ◽  
Sunil Kumar Jain ◽  
Pushpendra Kumar Khangar
Keyword(s):  
Sustained Release ◽  
Xanthan Gum ◽  
Dosage Form ◽  
Spectroscopic Method ◽  
Synthetic Polymers ◽  
Matrix Tablets ◽  
Matrix Tablet ◽  
Direct Compression ◽  
The Matrix ◽  
Pharmaceutical Industries

The primary benefit of a sustained release dosage form compared to a conventional dosage form, is the consistent drug plasma concentration and consequently uniform therapeutic effect. Matrix system are preferential because of their ease, patient compliance etc, than  traditional drug delivery which have several drawbacks like reiterated administration, variation in blood concentration level etc. The aim of the present research study was to develop and evaluate sustained release matrix tablets of furosemide using direct compression method using  natural  gummy  and  waxy  materials (Xanthan  gum, bees  wax)  and synthetic  polymers  (HPMC K4M). The matrix tablet formulations were prepared by using different drug: polymer ratios (1:1, 1:2 and 1:3). All formulations were assessed using micromeritics studies of powder blend and diverse physicochemical tests. All the physicochemical characters of the formulated tablets were within acceptable limits. The release pattern of the drug was viewed over a period of 12 hours and determined the amount of drug by the UV-Visible spectroscopic method. Dissolution data demonstrated that the formulated tablets with Xanthan gum and hydroxyl propyl methylcellulose (HPMC) provided sustained release of the drug up to 12 hrs. Therefore inexpensively it may be appropriate for the pharmaceutical industries to employ this kind of simple technologies for the expansion of advanced formulations. Hence, we conclude that the purpose of this study was to formulate a sustained release matrix tablet of furosemide using diverse polymers and their dissimilar proportions have been attained. Keywords: Furosemide, Direct compression, Natural, Synthetic polymers, Sustained release tablets.

scholarly journals Formulation development and evaluation of gastroretentive mucoadhesive tablets of glimepiride using natural polymers

2020 ◽  
Vol 10 (4-s) ◽  
pp. 153-159
Author(s):  
Rahul Malasiya ◽  
Tarkeshwar P. Shukla
Keyword(s):  
Drug Delivery ◽  
Drug Release ◽  
Drug Delivery System ◽  
Extended Period ◽  
Direct Compression ◽  
Compression Method ◽  
In Vitro Drug Release ◽  
Mucoadhesive Tablets ◽  
Gastro Retentive

Glimepiride, a third-generation sulfonylurea is poorly soluble anti-diabetic drug. Currently, the use of natural gums and mucilage is of increasing importance in pharmaceutical formulations as valuable drug excipients. Natural plant-based materials are economic, free of side effects, biocompatible and biodegradable. The development of mucoadhesive sustained release drug delivery system is recommended in order to enhance the bioavailability. A mucoadhesive tablets were developed using the natural polymer sodium alginate and gum tragacanth. Mucoadhesion is a complex phenomenon which involves wetting, adsorption and interpenetration of polymer chains. The tablets of glimepiride were prepared by direct compression method. Pre-compression parameters were evaluated. The tablets were evaluated for post-compression parameters such as thickness, hardness, average weight, friability and In vitro release studies. All the compositions were resulted in adequate pharmacopoeial limits. The varying concentration of polymers was found to affect on in-vitro drug release and mucoadhesive strength. In vitro drug release of gastro retentive tablet of glimepiride shown that the formulation F5 was found to be the best formulation as it releases 98.78%.  Glimepiride in a sustain release manner for an extended period of time (up to 12 hrs). The release data was fitted to various mathematical models such as higuchi, korsmeyer-peppas, first order and zero order to evaluate the kinetics and mechanism of the drug release. Prepared tablets of glimepiride may prove to be a potential candidate for safe and effective controlled drug delivery over an extended period of time for gastro retentive drug delivery system. Keywords: Glimepiride, Gastro retentive, Anti-diabetic drug, Direct compression method

scholarly journals Formulation and In-vitro evaluation of sustained release matrix tablet of Metformin hydrochloride

2019 ◽  
Vol 9 (3) ◽  
pp. 95-98
Author(s):  
Ravi U Gaware ◽  
Gayatri R Waykar ◽  
Madhuri K Yewale ◽  
Rutuja B Mhaske ◽  
Poonam S Mhaske
Keyword(s):  
Sustained Release ◽  
Ethyl Cellulose ◽  
Metformin Hydrochloride ◽  
High Dose ◽  
Matrix Tablet ◽  
Direct Compression ◽  
Compression Method ◽  
Hydrophilic Matrix ◽  
Compaction Behavior

The low bioavailability and short half-life of Metformin hydrochloride (MH) make the development of sustained-release forms desirable. Present work involves preparation and optimization of sustained release matrix tablet of MH by direct compression method using HPMC K 100 and ethyl cellulose as a matrix forming polymer. Avicel was added as a direct compaction vehicle to improve the compaction behavior of Metformin which otherwise exhibits poor compaction behavior which again is further increased by its relatively high dose. Hydrophilic matrix of HPMC alone resulted in initial burst of Metformin release, however when combined with ethyl cellulose drug release was slowed down and thereafter it became optimal at particular concentration of polymers. Keywords:  Metformin, HPMC, Ethyl cellulose, sustained release, matrix, tablet.

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