scholarly journals Studies on Formulation and Evaluation of Ethyl Cellulose Based Extended Release Metformin Hydrochloride Matrix Tablets

Author(s):  
Sundaramoorthy Kaliyan

Monolithic matrix tablets of metformin hydrochloride were formulated as extended release tablets by employing ethyl cellulose polymer and the extended release characterization of the formulated tablets was investigated.  Extended release matrix tablets containing 500 mg metformin hydrochloride were developed by changing concentration of drug :  polymer (EC) in the ratio of 5:1, 5:2, 5:3 and 5:4 by direct compression.  Formulations were optimized based on the acceptable tablet properties invitro and invivo drug release.  The resulting formulations produced robust tablets with optimum hardness, weight variation, drug content and low friability.  The result of invitro and invivo drug release studies indicated that formulation (drug:polymer =5:3), is the most successful of the study and exhibited constant and extended release of metformin hydrochloride 99-100.5% release at the end of 10 h compared with reference standard.  Further, the formulation F3 was subjected to exposure at room and accelerated condition to stability studies.  A decrease in release of the drug was observed on increasing polymer ratio at certain level.  Before tablet compression, the resulting formulation blends were evaluated for angle of repose, bulk density, % porosity, % compressibility index and drug polymer compatibility study of drug and excipients.  The t25, t50 and t90 drug release values was calculated from selected formulation F3 on every month of stability studies and comparision of both room and accelerated condition by statistical t-test, there is no difference between storage temperature. The formulation F3 was showed similar invitro and invivo drug release when compared to marketed sustained release tablet (F5M).

2020 ◽  
Vol 8 (02) ◽  
pp. 40-45
Author(s):  
Chhitij Thapa ◽  
Roma Chaudhary

INTRODUCTION Domperidone is a unique compound with gastro kinetic and antiemetic effects. It is used in the management of disorder by impaired motility like gastroesophageal reflux (in some instances), gastroparesis, dyspepsia, heartburn, epigastric pain, nausea, vomiting, and colonic inertia. The sustained release system is a widely accepted approach for slow drug release over an extended period to address the challenges of conventional oral delivery, including dosing frequency, drug safety, and efficacy. The study aims to formulate a domperidone sustained release tablet and compare the dissolution rate with the marketed formulations. MATERIAL AND METHODS Sustained release matrix tablets of domperidone were prepared by wet granulation method using different polymers such as HPMC K4M, ethyl cellulose, Gum acacia. Pre-compression studies like angle of repose, bulk density, tapped density, Carr's index, and Hausner’s ratio, and post-compression studies like weight variation, thickness, hardness, friability, drug content, and in-vitro drug release were evaluated.   RESULTS The release profile of domperidone sustained-release tablets was studied spectrophotometrically. The in-vitro dissolution study suggests the minimum %-cumulative drug release with 98.33% in F5. The %-cumulative drug release was maximum in F3 with 99.69%. The in-vitro drug release of all the formulations was non-significant compared to the marketed formulation (p<0.05), exhibiting the sustained-release property by all the formulations. CONCLUSION The pre-compression study concludes the better flow property of the granules of different formulations. The sustained release domperidone tablets were prepared successfully by the wet granulation method. The post-compression parameters of different formulations were within the acceptable range.


Author(s):  
Mahendar Rupavath ◽  
K. S. K Rao

The objective of the present investigation was to identify a suitable raft forming agent and to develop raft forming stavudine matrix tablets using different rate controlling natural, semi-synthetic and synthetic polymers to achieve prolonged gastric residence time, leading to an increase in drug bioavailability and patient compliance. Various raft forming agents were used in preliminary screening. Raft forming floating tablets were developed using pullulan gum as natural rate controlling polymer, and directly compressible grades of hydroxypropyl methylcellulose (Benecel K4M DC) as semi synthetic, and Carbopol 71G as synthetic rate controlling polymers respectively and optimum concentrations of sodium-bicarbonate as gas generating agent to generate optimum buoyancy by direct compression method. Raft forming tablets were evaluated for weight variation, thickness, hardness, friability, drug content, in vitro drug release, floating buoyancy and raft strength. Drug-excipients compatibility study showed no interaction between drug and excipients. Raft forming tablets showed satisfactory results when evaluated for weight variation, thickness, hardness, friability, drug content, and raft strength. The optimized formulation was selected based on physicochemical characteristics and in vitro drug dissolution characteristics. Further, the optimized formulation was evaluated for in vivo radiographic studies by incorporating BaSO4 as radio opaque substance. Optimized formulation showed controlled and prolonged drug release profiles while floating and raft formation over the dissolution medium. Diffusion followed by erosion with raft forming drug release mechanism was observed for the formulation, indicating that dissolution media diffusion and polymer erosion played an essential role in drug release. In vivo radiographic studies revealed that the raft forming formulations remained in the stomach for 240 30 min in rabbits and indicated that gastric retention time was increased by the floating and raft forming principle, which was considered and desirable for absorption window drugs.


2020 ◽  
Vol 10 (2) ◽  
pp. 59-68
Author(s):  
D. Hema Naga Durga ◽  
T. Lakshmi Sowjanya ◽  
T. Pavani ◽  
Lohithasu Duppala

Colon targeted tablets were prepared in two steps. Initially core tablets were prepared and then the tablets were coated by using different pH dependent polymers. Ethyl cellulose, Eudragit L100 and S100 were used as coating polymers. FT-IR studies were carried out to find out the possible interaction between the selected drugs and polymer. FT-IR studies revealed that there  was  no  interaction between the selected drug and excipients. The pre-compression blend of all formulations was subjected to various flow property tests and all the formulations passed the tests. The tablets were coated by using polymers and the coated tablets were subjected to various evaluation techniques. The tablets passed all the tests. Among all the formulations F3 formulation was found to be optimized as it was retarded the drug release up to 12 hours and showed maximum of 97.57% drug release. It followed zero order kinetics mechanism. The ideal formulation was subjected to stability studies at 40°C/75%RH. The stability studies indicated that the formulation was stable and retained its pharmaceutical properties at 40°C/75%RH over a period of 1 month. Keywords: Colon target, Ethyl cellulose, Eudragit L100 and S100, pH dependent polymers.


2015 ◽  
Vol 14 (9) ◽  
pp. 1557-1563
Author(s):  
M Zaman ◽  
RM Sarfraz ◽  
S Adnan ◽  
A Mahmood ◽  
M Hanif ◽  
...  

Purpose: To formulate and characterize once daily controlled release tablet of loxoprofen sodium.Methods: Eudragit RS-100, hydroxylpropyl methylcellulose (HPMC) and pectin were used as release retarding polymers. All the formulations were prepared by direct compression method. Various precompression studies were carried out to determine Hausner’s ratio, Carr’s index, angle of repose, bulk density and tapped density Differential scanning calorimetry (DSC) studies and also post-compression studies to evaluate hardness, friability, weight variation, drug content, in-vitro drug release were conducted on the tablets. The drug release data were subjected to kinetic models, including zero order, first order, Hixon Crowell, Higuchi and Korsmeyer-Peppas.Results: Compressibility index (7.6 ± 1.32 - 12.5 ± 1.43%), Hausner’s ratio (1.08 ± 0.04 - 1.14 ± 0.03), angle of repose (27.78 ± 0.47 - 30.49 ± 0.46°), hardness (6.25 ± 0.27 - 7.21±0.21 kg/cm2), friability (0.14 ± 0.06 - 0.28 ± 0.0 %), weight variation (249.5 ± 2.09 - 251.35 ± 2.41 mg) and drug content  (97.30 ± 0.28 - 103.70 ± 0.31 %) were within generally accepted limits for the pre-and post-compression formulations, respectively. The tablets having the maximum amount of among the three polymers tested as matrix materials, HPMC, represented by F3 tablets, exerted better sustained release properties after 12 h. Release pattern was more of Fickian diffusion followed by Higuchi mechanism.Conclusion: The release of the loxoprofen sodium was optimized up to 12 h.Keywords: Loxoprofen, Sustained release, hydroxypropyl methylcelluose, Pectin, Eudragit, Matrix tablets


2012 ◽  
Vol 1 (8) ◽  
pp. 186 ◽  
Author(s):  
Urmi Das ◽  
Mohammad Salim Hossain

<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>


Author(s):  
Singh K. ◽  
Pandit K. ◽  
Mishra N.

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.


Author(s):  
Tulsi Bisht ◽  
Rishishwar Poonam

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.  


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):  
Mohammed Sarfaraz ◽  
Surendra Kumar Sharma

ABSTRACTObjective: The main objective of this research was to formulate Fast disintegrating tablets of Flurbiprofen incorporating superdisintegrants, isolated from natural sources like Plantago ovata (PO) seeds, Lepidium sativum (LS) seeds and agar-agar.Methods: Superdisintegrants were isolated from their natural sources using reported methods. Swelling index and hydration capacity was determined for the natural superdisintegrants to know their disintegration capacity. The tablet formulations were designed using isolated natural superdisintegrants. The powder blends were evaluated for pre-compressional parameters like angle of repose, bulk density, tapped density, carr’s index, and hausner’s ratio. Fast disintegrating tablets were prepared by direct compression method. The compressed tablets were characterized for post compression parameters.Results: All formulations had hardness, friability, weight variation and drug content within the pharmacopoeial limits. The wetting time was 84 to 254 sec, in vitro disintegration time was between 59.2 to 221 sec, and in-vitro drug release was as low as 11.80% (LS1) to a maximum of 98.99% (PO4) after 4 min of study. Among all, optimized formulation was PO4, as it showed good wetting time (84 sec), fastest disintegration time (59.2 sec), dispersion time (135 sec) and drug release of 98.99.% within 4 min.Conclusion: Flurbiprofen FDT’s were successfully developed using isolated natural disintegrants. The natural disintegrants isolated showed promising results and can prove as effective alternative for synthetic disintegrants.


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