scholarly journals DEVELOPMENT AND EVALUATION OF BILAYER TABLETS FOR IMMEDIATE AND CONTROLLED RELEASE OF METFORMIN HYDROCHLORIDE

Author(s):  
Rablee Saikia ◽  
Bhanu Pratap Sahu

Objective: The purpose of this study was to develop and evaluate bi-layer tablets for the immediate and controlled release of Metformin Hydrochloride for effective treatment of type 2 Diabetes mellitus.Methods: The immediate release layer was prepared by using super disintegrants like cross carmellose sodium, sodium starch glycolate and sustained release layer was prepared by using hydrophilic polymer like HPMC K 100 and PVP. Various proportions of super disintegrants and polymer were used to select the best formulation composition. Bilayer tablet of metformin was prepared by wet granulation method and was evaluated for physical characteristics like hardness, weight variation, and friability. In vitro release of drug was performed in USP type II dissolution test apparatus using phosphate buffer (pH 6.8) as dissolution media and dissolution was continued for 9 h for the sustained release layer. For immediate release layer, readings were recorded in each 10 min time interval for the first 1h.Results: From the obtained result it was found that all the formulations were within the limit of the standard. The hardness was found to be in the ranges from 5.1 to 5.5 kg/cm2, weight variation was in the range 0.53% to 0.83%, friability of all the formulations was within the range (<1%)and percentage of drug content was more than 97%. The drug release of the tablet was in the range of 85%-91% in 9 h.Conclusion: From the result obtained, it is found that the formulation F6 satisfies all the criteria as sustained release tablet for the effective treatment of type 2Diabetes mellitus.  

Author(s):  
Manoj Kr. Das ◽  
Bhanu P. Sahu ◽  
Jahan Nur Rahman Hazarika

Objective: The purpose of this study was to develop and evaluate bilayer tablet for the immediate and controlled release of Allicin (Garlic Extract) for effective treatment of Hypertension.Methods: The immediate release layer was prepared by using super disintegrants-sodium starch glycolate and binder used xantham gum and the sustained release layer was prepared by using hydrophilic polymer like HPMC K 100 and PVP. Before preparation of the tablets, all the pre-formulation parameters were checked and the tablet of Allicin were prepared by direct compression method and was evaluated for physical characteristics like hardness, weight variation, drug content and friability. In vitro release of drug was performed USP type II dissolution test apparatus using phosphate buffer (pH 7.4) as dissolution media and dissolution was continued for 8 hrs for the sustained release layer.Results: It was found that all the formulations were within the limit of the standard. The drug release of the tablet was in the range of 66%-83% in 8 h.Conclusion: It was concluded that the F4 formulation showed the optimum result as a bilayer tablet for the effective treatment of hypertension. 


Author(s):  
Mayuri B. Patil ◽  
Avish D. Maru ◽  
Jayshree S. Bhadane

The aim of the present study was to design and evaluate bilayer tablets of metformin hydrochloride as sustained release form for the treatment of Type-II diabetes mellitus. The basic aim of any Bi-layer tablet formulation is to separate physically or chemically incompatible ingredients and to produce repeat action or prolonged action of tablet. They are many drugs for treating type-II diabetes. Sulphonyl urea and biguanides are used commonly by a wide section of patients. Melt granulation process was used for the formulation of sustained comprising metformin layer and wet granulation of immediate comprising layer of glimepiride. The precompression studies like bulk density, tapped density, angle of repose, compressible index and post formulation studies includes weight variation, hardness, thickness, friability and dissolution study. The in-vitro release profile of Glimepiride was dissolved within 45 min, and Metformin Hydrochloride was able to release more than 12 hrs. They all the formulation was optimized formula due to its higher rate of dissolution and collate all other parameters with the official specifications.


Author(s):  
Hemalatha S. ◽  
Srikanth P. ◽  
Mounica Sai G.

In present investigation an attempt has been made to design and develop the Bilayered tablet of Glimepiride and Metformin using Mangifera Indica Gum (MIG) and HPMC as Immediate Release and Sustained Release Layer polymers. Glimepiride and Metformin are oral-hypoglycaemic drugs which lower blood glucose level and have been selected to prepare Bilayered tablets. Glimepiride immediate release layer was prepared using MIG by wet granulation technique and Metformin sustained release layer was prepared using HPMC by dry granulation technique. Prepared Bilayered tablets were evaluated for parameters like thickness, diameter, weight variation, hardness, friability, disintegration and in-vitro release studies. All the prepared tablets were of smooth surface and elegant texture. The weights of the tablets were in the range of 540±0.551 mg. The thicknesses of the tablet were in the range of 4±0.05mm. The drug content uniformity study showed uniform dispersion of drug throughout the formulation in the range of 97.16±0.50%. The hardness was in the range of 4.0±0.5 kg/cm2 and friability is in the range of 0.67±0.06%. The bilayered tablets were also subjected to model fitting analysis to know the order and mechanism of drug release from the formulation by treating the data according to zeroorder, first-order, Higuchi and peppas equations.The bioequivalence studies conducted between prepared and marketed (Glycomate) bilayered tablet showed the similarity factor value of 70.120 for IR layer and 57.689 for SR layer.


Author(s):  
Ankit Acharya ◽  
Mohammed Gulzar Ahmed ◽  
Ravi Chaudhari ◽  
Renukaradhya Chitti

Divalproex sodium is considered as the most important antiepileptic drug and widely used for treatment of epilepsy and bi-polar disorders and prophylaxis of migraine. The present work has been done to formulate bi-layered tablet of Divalproex sodium containing immediate release layer and sustained release layer. The FTIR study revealed that there was no interaction between drug and polymer and combination. Both layers were prepared by wet granulation technique as poor flow property exhibited by pure drug. The immediate release layer was formulated by using superdisintegrants and evaluated for physical parameters, disintegration time and in vitro drug release. The optimized immediate release layer (IF6) with highest in vitro release of 98.11 was selected for bi-layered tablet formulation. HPMC K4M and HPMC K100M polymer were used to retard the drug release from sustained release layer in different proportion and combination and evaluated for physical parameter along with in vitro drug release studies. The optimized sustained release layer (SF8) which extends the Divalproex sodium release more than 18 hrs was selected. Finally, bi-layered tablets were prepared by double compression of selected sustained release layer and immediate release layer of Divalproex sodium. The tablets were evaluated for hardness, thickness, weight variation, friability, drug content uniformity and in vitro drug release. All the physical parameters were in acceptable limit of pharmacopeial specification. The stability studies, shown the bi-layer tablet was stable at 40oC / 75% RH for a period of 3 months.  


2018 ◽  
Vol 2 (1) ◽  
pp. 01-03
Author(s):  
Swathi chilukala

Drugs that are easily absorbed from the GI tract and have a short half-life are eliminated quickly from the blood circulation, require frequent dosing. To avoid this problem, the oral controlled release formulations are being developed. Gastro-retentive dosage forms have the potential from use as controlled release systems. The purpose of this research is to develop the gastro retentive drug delivery system of centrally acting alpha adrenergic agonist cyclobenzaprine Hydrochloride (cyclobenzaprine HCl). It is well absorbed from the upper part of the GIT, due to short gastric residence time the bioavailability is low and hence it is need to develop a dosage form that releases the drug in stomach using gastro retentive system. Different formulations of cyclobenzaprine HCl gastro-retentive floating tablets were prepared by wet granulation method using various concentrations of HPMC K4M / HPMC K100M and combination of Psyllium husk and HPMC K100M as matrix forming agent. Sodium bicarbonate and citric acid were used as a gas generating agent that helps in maintaining the buoyancy. The prepared cyclobenzaprine HCl gastro-retentive floating granules were subjected to pre-compression properties to comply with pharmacopoeial limits and the prepared gastro-retentive floating tablets were characterized for weight variation, hardness, thickness and friability drug content, swelling studies. The floating lag time of all formulation is good and the Total floating time of all the formulations was >12 hours. The tablets were evaluated for in vitro release characteristics for 12hrs in 0.1N HCl at 37 oC and from this in vitro release studies the formulations F-5, F-9 and F-15 exhibited good controlled release profile of about 96.0%, 94.5% and 95.0% when compared with other formulations while floating on the dissolution medium.


2018 ◽  
Vol 21 (2) ◽  
pp. 101-108
Author(s):  
Sreebash Chandra Bhowmik ◽  
Marzia Alam ◽  
Md Saiful Islam Pathan

Metformin hydrochloride is a first line BCS class III oral anti-diabetic drug used for the treatment of type 2 diabetes. The main goal of this study was to formulate, prepare and evaluate natural gum-based immediate release metformin hydrochloride tablet. Seven different formulations of compressed tablets were prepared following wet granulation process using different concentrations (10, 20, 30, 50, 60, 70, 80 and 90 mg) of Aegle marmelos gum as a binder. Aegle marmelos gum is a biodegradable natural gum which is economic, easily available and found useful as tablet binder for both conventional and novel dosage forms. Other excipients used in the formulation were microcrystalline cellulose (MCC), croscarmellose sodium (CCS), maize starch, colloidal silicon dioxide (CSD), sodium starch glycolate (SSG), magnesium stearate etc. In the present study, the compressed tablets were evaluated for weight variation, thickness, hardness, friability, disintegration time and dissolution. In vitro drug release study was carried out in phosphate buffer (pH 6.8) at 37 ± 0.5oC with 50 rpm using USP Dissolution Apparatus 2-Paddle method. The flowability of granules for all the batches was optimum which reflected in the bulk density and angle of repose. It can be concluded from this study that combination of Aegle marmelos as a binder with other excipients can be prospectively used in the preparation of metformin hydrochloride immediate release (IR) tablet.Bangladesh Pharmaceutical Journal 21(2): 101-108, 2018


INDIAN DRUGS ◽  
2012 ◽  
Vol 49 (02) ◽  
pp. 26-32
Author(s):  
N. S Ranpise ◽  
◽  
S. S. Somavanshi ◽  
R. K Bhujbal . ◽  
Y. M. Jagtap

The aim of present work was to develop a metformin hydrochloride sustained release tablet by aqueous coating. Eudragit RL and Eudragit RS were used for coating of tablets. Eudragit RL having 10% and Eudragit RS having 5% of functional quaternary ammonium groups, which give rise to pH independent permeability of the polymer. Metformin hydrochloride uncoated tablets were prepared by wet granulation technique. Tablets were coated with blends of Eudragit RS30D and Eudragit RL30D in 5:1 and in 3:1 ratios at different coating level viz. 7%, 5%, 3%, 1.5%, 1%. Two dissolution media: pH 1.2 and pH 6.8 phosphate buffer were employed for in vitro release behaviors of metformin hydrochloride tablets. Coating with blends of Eudragit RS 30D and Eudragit RL 30D in 5:1 and in 3:1 ratio at 1% and at 3% showed sustained release effect for 12 h. The two Eudragit polymers with different features as coating materials produced the desired results.


Author(s):  
Rai V. K. ◽  
Pathak N. ◽  
Bhaskar R. ◽  
Nandi B. C. ◽  
Dey S. ◽  
...  

The purpose of this research is to prepare Raloxifene Hydrochloride immediate release tablet by wet granulation technique. In order to obtain the best, optimized product six different formulations were developed. Different filler, binder, disintegrant and lubricant were taken as variables. Weight variation, thickness, hardness, friability, disintegration time, in-vitro release and pharmaceutical assay were studied as response variables. Sticking was observed when the formulation containing stearic acid and sodium stearyl fumarate. However, in the remaining four formulation containing magnesium stearate, no sticking was observed. The formulation NP061 was selected as an optimized product. The different physical properties and in-vitro release profile showed best comparable with reference product. Optimization has proven as an effective tool in product development.


Author(s):  
Y Madhusudan Rao ◽  
Sunil Reddy ◽  
Panakanti Pavan Kumar ◽  
Rajanarayana Kandagatla

 The aim of present study was to design the concept of bilayered tablets containing Glimepride for immediate release using sodium starch glycolate as super disintegrant and Metformin hydrochloride (HCl) for sustained release by using  Hydroxyl propyl methyl cellulose (HPMC K 4M) and Sodium Carboxy Methyl cellulose (SCMC) as the matrix forming polymer, and PVPK-30 as binder. The tablets were evaluated for physicochemical properties. All the values were found to be satisfactory. In vitro release studies were carried out as per USP in pH 1.2 with (0.1% sodium lauryl sulphate w/v) and phosphate buffer pH 6.8 using the apparatus I. The release kinetics of Metformin HCl was evaluated using the regression coefficient analysis. The formulated tablets (F5) shows zero order release and diffusion was the dominant mechanism of drug release. The polymer (HPMC K4M, SCMC) and binder PVPK-30 had significant effect on the release of Metformin HCl matrix tablets (F5). Thus formulated bilayer tablets provided immediate release of Glimepride and Metformin HCl as sustained release over a period of 8 hours.  Stability studies and FT-IR studies clearly indicated that there is no drug –polymer interaction.


Author(s):  
Mashkura Ashrafi ◽  
Jakir Ahmed Chowdhury ◽  
Md Selim Reza

Capsules of different formulations were prepared by using a hydrophilic polymer, xanthan gum and a filler Ludipress. Metformin hydrochloride, which is an anti-diabetic agent, was used as a model drug here with the aim to formulate sustained release capsules. In the first 6 formulations, metformin hydrochloride and xanthan gum were used in different ratio. Later, Ludipress was added to the formulations in a percentage of 8% to 41%. The total procedure was carried out by physical mixing of the ingredients and filling in capsule shells of size ‘1’. As metformin hydrochloride is a highly water soluble drug, the dissolution test was done in 250 ml distilled water in a thermal shaker (Memmert) with a shaking speed of 50 rpm at 370C &plusmn 0.50C for 6 hours. After the dissolution, the data were treated with different kinetic models. The results found from the graphs and data show that the formulations follow the Higuchian release pattern as they showed correlation coefficients greater than 0.99 and the sustaining effect of the formulations was very high when the xanthan gum was used in a very high ratio with the drug. It was also investigated that the Ludipress extended the sustaining effect of the formulation to some extent. But after a certain period, Ludipress did not show any significant effect as the pores made by the xanthan gum network were already blocked. It is found here that when the metformin hydrochloride and the xanthan gum ratio was 1:1, showed a high percentage of drug release, i.e. 91.80% of drug was released after 6 hours. But With a xanthan gum and metformin hydrochloride ratio of 6:1, a very slow release of the drug was obtained. Only 66.68% of the drug was released after 6 hours. The percent loading in this case was 14%. Again, when Ludipress was used in high ratio, it was found to retard the release rate more prominently. Key words: Metformin Hydrochloride, Xanthan Gum, Controlled release capsule Dhaka Univ. J. Pharm. Sci. Vol.4(1) 2005 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website


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