Formulation and Evaluation of Gastro-Retentive Floating Extended Release Metoprolol Tablets using Sodium Alginate and HPMC K-100M Combination

2015 ◽  
Vol 8 (3) ◽  
pp. 2947-2954
Author(s):  
Ashok Thulluru ◽  
M. Mohan Varma ◽  
C M Setty ◽  
Pavan Kumar Chintamaneni ◽  
S. Sriharsha Vardhan
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Fickian Diffusion ◽  
Wet Granulation ◽  
Average Weight ◽  
Metoprolol Succinate ◽  
Floating Tablets ◽  
Zero Order Kinetics ◽  
Gastro Retentive

The present study was aimed to convert Metoprolol Succinate convert into Gastro Retentive Floating Tablet (GRFT). The gas generating floating tablets of Metoprolol Succinate were prepared to increase the gastric retention and to extend the drug release up to 12 hr. and thereby enhancing its bioavailability. The floating tablets were formulated using HPMCK 100M alone and with the combination of sodium alginate to the polymer of varying concentrations. The tablets were prepared by non-aqueous wet granulation method. The formulated granules were evaluated for pre-compression studies, after the compression of tablets they were subjected to various post-compression studies: Average weight, thickness, density, hardness, % friability, % drug content, (In vitro buoyancy studies: floating time, total floating time and matrix integrity up to 12 hr) and the In vitro drug release studies. The optimized formulation (F4) was found to follow a near perfect zero order kinetics (regression coefficient,      r2 = 0.978). Higuchi plot for formulation, F4, showed r2 value of 0.978, suggesting that the diffusion and erosion plays an important role in the controlled release of the drug. The data was fitted to the Korsemeyer-Peppa’s equation; and the value of the diffusion component (n=0.654), for the formulation F4, indicated that the drug release follows non-Fickian diffusion.  

scholarly journals FORMULATION AND IN-VITRO EVALUATION OF THEOPHYLLINE HYDROCHLORIDE EFFERVESCENT FLOATING TABLETS: EFFECT OF POLYMER CONCENTRATION ON TABLET BUOYANCY

2019 ◽  
pp. 59-65
Author(s):  
AKPABIO E. I. ◽  
EFFIONG D. E. ◽  
UWAH T. O. ◽  
SUNDAY N. I.
Keyword(s):  
Drug Release ◽  
Release Kinetics ◽  
Polymer Concentration ◽  
Hydroxypropyl Methylcellulose ◽  
Controlled Drug Release ◽  
Fickian Diffusion ◽  
Wet Granulation ◽  
Floating Tablets ◽  
Swelling Characteristics

Objective: This study was undertaken to formulate a floating drug delivery system of theophylline hydrochloride using different concentrations of a chosen polymer and then investigate how polymer concentration affects buoyancy and drug release properties of the tablets. Methods: Hydroxypropyl methylcellulose (HPMC) at different concentration levels of 15% (F1), 20% (F2) and 30% (F3) was used to form the three formulation batches of floating tablets. Wet granulation method was used for the granule preparation while Sodium bicarbonate and citric acid were used as the gas generating agent. The physical properties of the granules and the floating tablets were evaluated. Also determined were the physicomechanical properties, buoyancy and swelling characteristics of the tablets. The in vitro drug release study was carried out according to the USP I (basket method) for 8h in 900 ml 0.1N HCl at 50 rpm. Samples withdrawn at the regular predetermined time were analyzed spectrophotometrically at a wavelength of 271 nm and data obtained statistically analyzed by one-way analysis of variance (ANOVA). The differences between means were considered significant at P<0.05. Results: The result showed that polymer (HPMC) concentration significantly (p>0.05) increased swelling index and improved floating lag time, it had no significant effect on the total floating time. Percentage drug release at the end of 8 h was 100%, 98.2% and 96.13% for formulation F1, F2 and F3, respectively. All three formulations followed the Higuchi drug release kinetics model and the mechanism of drug release was the non Fickian diffusion with exponents of 0.46, 0.51 and 0.56 for the respective batch. Conclusion: Batch F3 gave a better-controlled drug release and floating properties in comparison to batch F1 and F2 thus Polymer concentration influenced the onset of floating and controlled the release of Theophylline.

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.

Formulation and In vitro Release Characterization of Metoprolol Succinate Extended Release Tablets

2012 ◽  
Vol 4 (4) ◽  
pp. 1537-1543
Author(s):  
Sakthikumar T ◽  
Rajendran N N ◽  
Natarajan R
Keyword(s):  
Drug Release ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Direct Compression ◽  
Metoprolol Succinate ◽  
Extended Release Formulations ◽  
Vitro Release

The present study was aimed to develop an extended release tablet of metoprolol Succinate for the treatment of hypertension.  Four extended release formulations F1-F4 were developed using varying proportions of hydroxylpropyl-methylcellulose K100M, sodium carboxy methyl cellulose and Eudragit L30 D55 by wet granulation. Five extended release formulations F5-F9 containing HPMC K100M and HPMC 5 cps in varying concentration were developed by direct compression. The physicochemical and in vitro release characteristics of all the formulations were investigated and compared. Two formulations, F7 and F8 have shown not more 25% drug release  in 1st h, 20%-40% drug release at 4th hour, 40%-60% drug release at 8th hour and not less than 80% at 20th hour and the release pattern conform with USP specification for 24 hours extended release formulation. It can be conclusively stated that optimum concentration of HPMC K100M (58%-65%) by direct compression method can yield an extended release of metoprolol succinate for 24 hours.

3 (2) Factorial Design Assisted Crushed Puffed Rice-HPMC-Chitosan based Hydrodynamically Balanced System of Metoprolol Succinate

2020 ◽  
Vol 10 (3) ◽  
pp. 237-249
Author(s):  
Shashank Soni ◽  
Veerma Ram ◽  
Anurag Verma
Keyword(s):  
Drug Release ◽  
Factorial Design ◽  
Hydroxypropyl Methylcellulose ◽  
Batch Size ◽  
Metoprolol Succinate ◽  
Zero Order Kinetics ◽  
Two Factors ◽  
Puffed Rice ◽  
Model Drug

Introduction: Hydrodynamically balanced system (HBS) possesses prolonged and continuous delivery of the drug to the gastrointestinal tract which improves the rate and extent of medications that have a narrow absorption window. The objective of this work was to develop a Hydrodynamically Balanced System (HBS) of Metoprolol Succinate (MS) as a model drug for sustained stomach specific delivery. Materials and Methods: Experimental batches were designed according to 3(2) Taguchi factorial design. A total of 9 batches were prepared for batch size 100 capsules each. Formulations were prepared by physically blending MS with polymers followed by encapsulation into hard gelatin capsule shell of size 0. Polymers used were Low Molecular Weight Chitosan (LMWCH), Crushed Puffed Rice (CPR), and Hydroxypropyl Methylcellulose K15 M (HPMC K15M). Two factors used were buoyancy time (Y1) and time taken for 60% drug release (T60%; Y2). Results: The drug excipient interaction studies were performed by the thermal analysis method which depicts that no drug excipient interaction occurs. In vitro buoyancy studies and drug release studies revealed the efficacy of HBS to remain gastro retentive for a prolonged period and concurrently sustained the release of MS in highly acidic medium. All formulations followed zero-order kinetics. Conclusion: Developed HBS of MS with hydrogel-forming polymers could be an ideal delivery system for sustained stomach specific delivery and would be useful for the cardiac patients where the prolonged therapeutic action is required.

scholarly journals Development and Optimization of Gastro-Retentive Formulation of Hydralazine HCl

2016 ◽  
Vol 8 (05) ◽  
Author(s):  
Himanshu Acharya ◽  
Rakesh Patel
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Methyl Cellulose ◽  
Optimization Procedure ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Floating Tablets ◽  
Hydralazine Hydrochloride ◽  
Predicted Values

Hydralazine hydrochloride has a half-life of 2 to 4 hours with an oral bioavailability of 26-50%. Since hydralazine has a demethylating effect on various suppressor genes, it can be used in various types of cancer to support chemotherapy. The purpose of this study was to optimize and evaluate floating tablets of hydralazine hydrochloride designed to prolong the gastric residence time and to provide controlled release of the drug for 24 h. The floating tablets of hydralazine hydrochloride were prepared by the wet granulation method. Polymers of hydroxy propyl methyl cellulose (HPMC K100M), HPMC K15M, carbopol 940 and sodium bicarbonate were used as the release retarding agents. This study investigated utility of a 3-factor, 3-level Box-Behnken design and optimization process for floating tablet of Hydralazine with 5 replicates of center points. Amount of HPMC K4 (Hydroxy Propyl Methyl cellulose), amount of sodium bicarbonate were selected as the independent variables whereas total floating time (TFT), T90, % cumulative drug release at 24 hours, and T20, Q1 were selected as dependent variables. Non-Fickian diffusion release transport was confirmed as the release mechanism for the optimized formulation and the predicted values agreed well with the experimental values. Drug excipient compatibility studies were investigated by FTIR, DSC and XRD. The produced tablets exhibited good floating time and controlled drug release over a period of 24 h. The resultant data were critically analyzed to locate the composition of optimum formulations. All predicted values of response variables of optimized formulation demonstrated close agreement with the experimental data during optimization procedure.

Formulation and Evaluation of Isabgol and Liquorice Based Nutraceuticals Floating Tablets for Management of Gastric Ulcer

2020 ◽  
Vol 01 ◽  
Author(s):  
Ritesh Kumar Tiwari ◽  
Lalit Singh ◽  
Shashi Verma ◽  
Vijay Sharma
Keyword(s):  
Drug Release ◽  
Sodium Bicarbonate ◽  
Magnesium Stearate ◽  
Gastric Ulcers ◽  
Physical Parameters ◽  
Floating Tablets ◽  
Zero Order Kinetics ◽  
Liquorice Extract ◽  
Tablet Formulations

Background: Floating tablets extend drug residence time, enhance bioavailability and promote the delivery of local drugs to the stomach. With this objective, floating tablets were prepared for the treatment of gastric ulcers containing aqueous extract of liquorice and Isabgol. Methods: Tablets containing HPMC K100M (hydrophilic polymer), liquorice extract, sodium bicarbonate (gas generating agent), talc, and magnesium stearate were prepared using direct compression method. Physical parameters of formulations such as diameter, thickness, hardness, friability, weight uniformity, drug content, buoyancy time, dissolution, and mechanism for drug release, were assessed. The formulations have been optimized based on buoyancy time and in- vitro drug release. Results: The diameter of all formulations was in the range 11.310-11.833 mm; thickness was in the range 4.02-4.071 mm. The hardness ranged from 3.1 to 3.4 kg/cm. All formulations passed the USP requirements for friability and uniformity of weight. All tablet formulations had a buoyancy period of less than 5 min and throughout the research, the tablet stayed in floating condition. All tablet formulations were accompanied in drug discharge by zero-order kinetics and model Korsemeyer-Peppas. Conclusion: It was discovered that the optimized formulation was F7, which released 98.5 percent of the drug in 8 hr. invitro, while the buoyancy time was 3.5 min. For gastroretentive drug delivery systems, formulations containing Isabgol, sodium bicarbonate and HPMC K100 M in combination may be promising.

Formulation and Evaluation of Sustained Release Floating Tablets of an Antihypertensive Diltiazem

2017 ◽  
Vol 10 (5) ◽  
pp. 3844-3852
Author(s):  
Gururaj S Kulkarni ◽  
Prabhansh P Chaudhary ◽  
Shivakumar Swamy
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Angle Of Repose ◽  
Polymeric Chain ◽  
Release Mechanism ◽  
Natural Polymers ◽  
Floating Tablets ◽  
Higuchi Model

The aim of the present study was to develop and evaluate sustained release floating tablets of Diltiazem hydro-chloride, an antihypertensive agent. The sustained release floating tablets were prepared by direct compression method and formulated using different polymer combinations, formulations such as F1 to F9. Natural polymer Sodium alginate and synthetic polymer HPMC K4M were used. Developed formulations were evaluated for the pre compression parameters i.e., drug- excipients compatibility by FTIR, bulk density, compressibility, and angle of repose etc. Post compression parameters i.e. weight variation; full factorial design was applied to optimize the developed formulation. SA and HPMC K4M were selected as independent variable at three different concentrations. The in-vitro drug release study revealed that formulation F8 combination of both synthetic (HPMC) and natural polymers (sodium alginate) was the most successful formulation of the study, all tablets but one exhibited gradual and near complete sustained release for diltiazem HCl (90-100%) that extended the drug release up to 8 hours, with satisfactory drug release in the initial hours, and the total release pattern was close to the theoretical release profile.  Model equations of zero and first order, Higuchi, Hixson-Crowell and Peppas, intended to elucidate the drug release mechanism, and were fitted to the release data. Mathematical modelling of in-vitro dissolution data indicated the best-fit release kinetics was achieved with Higuchi model with r2 vales of 0.994 in its semi log plot. The ‘n’ value in Higuchi model was >0.89 which indicated, Super Case-II transport of drug from polymer sustained, i.e., diffusion with relaxation of polymeric chain. In conclusion, the results indicated that the prepared sustained-release tablets of Diltiazem hydrochloride could perform therapeutically better than conventional tablets with improved efficacy and better patient compliance.     

FORMULATION, OPTIMIZATION AND EVALUATION OF MOXIFLOXACIN HYDROCHLORIDE GASTRO RETENTIVE TABLETS

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (01) ◽  
pp. 79-84
Author(s):  
Raghavendra K. Gunda ◽  
◽  
A. Vijayalakshmi ◽  
K. Masilamani ◽  
◽  
...  
Keyword(s):  
Fickian Diffusion ◽  
In Vivo Studies ◽  
Pharmacokinetic Parameters ◽  
Wet Granulation ◽  
Statistical Parameters ◽  
Compression Technique ◽  
Ich Guidelines ◽  
Gastro Retentive

The objective of the current study was to develop gastro retentive formulation of moxifloxacin. HCl using various drug release modifiers and performing in vitro and in in vivo evaluations. Moxifloxacin is a novel synthetic fluoro quinolone antibacterial agent. Floating, muco adhesive tablets of moxifloxacin. HCl were prepared using variable amounts of HPMCK100M, Lannea coromandelica gum by direct compression technique and wet granulation technique, respectively. Formulations were developed, optimized and checked for pharmacopoeial tests. Results show that all the batches lie within the standard limits. Dissolution parameters of all formulations were sy=ubjected to kinetic fitting and various statistical parameters were determined. Formulation (FS5 ) containing 50 mg of HPMCK100M and 50 mg of LCG, is the best formulation showing similarity f2 =71.734, f1 = 4.271 with the marketed product (Avelox). It follows Higuchi's kinetics, non-fickian diffusion first order kinetics(n=0.717). In vivo studies were performed for the FS5 with 6 healthy rabbits and pharmacokinetic parameters were determined, compared with Avelox and it was found that FS5 produced similar results. Stability studies were performed for FS5 as per ICH guidelines. Results were found to be satisfactory. FS5 is expected to improve patient compliance by means of providing good clinical outcome

scholarly journals Formulation and Evaluation of Floating Tablets of Sitagliptin with Extract of Triphala

2019 ◽  
Vol 9 (4-A) ◽  
pp. 38-47
Author(s):  
Revathi Sundaramoorthy ◽  
V Gopal ◽  
G Jeyabalan
Keyword(s):  
Drug Release ◽  
Chemical Interaction ◽  
Lag Time ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
In Vitro Drug Release ◽  
Floating Tablets ◽  
Drug Content ◽  
Soxhlet Apparatus

The aim of the present work is to formulate, optimize and evaluate hydrodynamically balanced antidiabetic system incorporated with sitagliptin and phytochemical constituents of Triphala extract for the treatment of constipation associated with diabetes.  The Triphala churna of two different ratios, 1:1:1 (TC1) and 1:2:4 (TC2) were subjected to hot percolation using Soxhlet apparatus using methanol as solvent. The floating matrix tablets of Sitagliptin with methanolic Triphala extract was prepared by wet granulation technique using HPMC K4M as polymer, starch/honey as binder and sodium bicarbonate & citric acid as effervescent agents by 24 factorial design.  The compatibility studies showed that there is no chemical interaction between the drug, polymer and the excipients used in the tablets.  The independent variables are drug & Triphala extract ratio (X1), Triphala proportion (X2), binder used for granulation (X3), and amount of effervescent excipients used (X4).  The dependent variables are hardness (Y1), buoyancy lag time (Y2), total floating time (Y3), in-vitro drug release (Y4), and T50% (Y5).  The prepared floating tablets were subjected to all post compression parameters such as hardness, friability, swelling capacity, buoyancy, total floating time, drug content & in-vitro drug release and were found to be within normal limits.  Based on drug content, buoyancy lag time and in-vitro drug release the formulations F14 and F16 were selected for in-vivo study of the formulation.  Keywords:  Triphala, Sitagliptin, honey, floating tablet. 

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.

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