scholarly journals Compaction, compression and drug release properties of diclofenac sodium and ibuprofen pellets comprising xanthan gum as a sustained release agent

2005 ◽  
Vol 295 (1-2) ◽  
pp. 15-27 ◽  
Author(s):  
Helton Santos ◽  
Francisco Veiga ◽  
M Eugénia Pina ◽  
João J. Sousa
Author(s):  
Heyam Saad Ali ◽  
Rasha Saad ◽  
Babiker M. A. Elhaj ◽  
Jiyauddin Khan ◽  
Mohammed Kaleemullah ◽  
...  

In the present study the influence of designing and development of sustained release (SR) matrix tablets of diclofenac sodium were investigated. The aim was to increase therapeutic efficacy, reduce frequency of administration, and improve patient compliance. Sustained release matrix tablets of diclofenac sodium, were developed by using different drug: gum ratios, using Xanthan gum as matrix former, microcrystalline cellulose as diluent and Polyethylene Glycol (PEG 6000) as release modifier. Formulated tablets were evaluated for friability, hardness, thickness and their relation to the amount of gum: drug ratio and drug release. The drug release was evaluated in different pH, rotation speed and stirrer. All the formulations showed compliance with pharmacopeial standards. Formulation consisting of drug: Gum ratio of 1:0.12 showed sustained release of drug for 12 hours with 89.67% release. The release pattern showed constant kinetics. Thus, (Xanthan Gum) can be used in as effective matrix former.


Author(s):  
S Shanmugam

Objective: The objective of the present study was to develop sustained release matrix tablets of levosulpiride by using natural polymers.Method: The tablets were prepared with different ratios of Chitosan, Xanthan gum and Guar gum by wet granulation technique. The solubility study of the levosulpiride was conducted to select a suitable dissolution media for in vitro drug release studies.Results: Fourier transform infrared (FTIR) study revealed no considerable changes in IR peak of levosulpiride and hence no interaction between drug and the excipients. DSC thermograms showed that no drug interaction occurred during the manufacturing process. In vitro dissolution study was carried out for all the formulation and the results compared with marketed sustained release tablet. The drug release from matrix tablets was found to decrease with increase in polymer ratio of Chitosan, Xanthan gum and Guar gum.Conclusion: Formulation LF3 exhibited almost similar drug release profile in dissolution media as that of marketed tablets. From the results of dissolution data fitted to various drug release kinetic equations, it was observed that highest correlation was found for First order, Higuchi’s and Korsmeyer equation, which indicate that the drug release occurred via diffusion mechanism.  Keywords: Levosulpiride, sustained release tablets, natural polymers, in vitro drug release studies 


2018 ◽  
Vol 10 (1) ◽  
pp. 109
Author(s):  
Musiliu Adedokun ◽  
Clement Nkanta

Objective: The aim of this research work was to comparatively study various proportions of a natural hydrocolloid-Raphia africana, and polyvinylpyrrolidone (PVP) as release sustaining agents in diclofenac sodium tablet formulation.Methods: The purified hydrocolloid (R. africana) was characterized by evaluating its organoleptic, physicochemical and flow properties. Diclofenac-polymer ratios of 1:0, 1:0.2, 1:0.4, 1:0.6, and 1:0.8 were employed to produce different granule batches using wet granulation method (that is, the drug was formulated with 0, 5, 10, 15 and 20 % w/w of either R. africana hydrocolloid or PVP, and coded DWB-00, DRA-05, DRA-10, DRA-15, DRA-20, DPP-05, DPP-10, DPP-15 and DPP-20, respectively). Flow properties of granules were studied by determining bulk density, tapped density, Carr’s index, and Hausner’s ratio for all the formulations. Compressed tablets were evaluated using various parameters as weight variation, friability, hardness, tablet thickness and diameter, content uniformity and in vitro dissolution evaluated in phosphate buffer (pH 7.3).Results: Flowability, mechanical and release parameters determined were within pharmacopoeial limits. Generally, the values of bulk and tapped densities increase as binder concentrations increase for both PVP and R. africana hydrocolloid. The values were significantly different across the batches (p<0.05). Hardness values obtained varied significantly (p<0.05) and were between 5 and 12 KgF which imply that most of the tablet batches are harder than normal depending on the proportion of the polymer used. All the batches exhibited friability within the standard limit without significant difference in values (p>0.05), indicating that tablet formulated with the experimental binders would not undergo surface abrasion. All the formulations exhibited zero order kinetics except batches DPP-10 and DPP-15 which showed Higuchi mechanism. Formulation batches DRA-05 and DRA-10 showed maximum drug release of 98% and 95% respectively after 6 h. A prolonged drug release was observed on increasing polymer ratio. Significantly higher release rates (p<0.05) were observed in the tablets formulated with PVP than those containing R. africana gum. All the batches followed non-fickian diffusion release mechanism.Conclusion: From the study, purified R. africana hydrocolloid generally appeared to perform better than PVP as sustained release agent.


2018 ◽  
Vol 10 (1) ◽  
pp. 59
Author(s):  
Olvishkumar M. Kothiya ◽  
Bhavana A. Patel ◽  
Kunal N. Patel ◽  
Madhubhai M. Patel

Objective: Ivabradine (IB) is anti-Ischemic drug and used for the symptomatic management of stable angina pectoris. IB acts by reducing the heart rate in a mechanism different from beta blockers and calcium channel blockers, two commonly prescribed anti-anginal drugs. IB has a short biological half-life and the dose of 5/7.5 mg twice a day. In this present study, an attempt has been made to prepare sustained release tablet of IB to achieve the desired drug release.Methods: The sustained release polymers, hydroxypropyl methylcellulose K100M (HPMC K100M), guar gum (GG) and xanthan gum (XG) were taken for the preliminary trail from which guar gum and xanthan gum had shown better drug release. Initially, drug-excipients compatibility studies were carried out by using Fourier transformed infrared spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC) which showed no interaction between drug and excipients. Tablets were prepared by wet granulation technique and evaluated for pre-compression and post-compression parameters.Results: 32 full factorial design was applied to achieve controlled drug release up to 24 h. The concentration of GG (X1) and XG (X2) were selected as independent variables and the % CDR at 2 h. (Y1) and 18 h. (Y2) were taken as dependent variables. In vitro drug release study revealed that as the amount of polymers increased, % CDR decreased.Conclusion: Contour as well as response surface plots were constructed to show the effect of X1 and X2 on % CDR and predicted at the concentration of independent variables X1 (10 mg) and X2 (10 mg) for a maximized response. The optimized batch (O1) was kept for stability study at 40±2 °C/75±5 %RH for a period of 6mo according to ICH guidelines and found to be stable.


Author(s):  
BATUL SAIFEE ◽  
PRAKASH K. SONI ◽  
SURESH K. PASWAN ◽  
T. R. SAINI

Objective: Losartan potassium is one of the widely prescribed antihypertensive drugs administered orally and its extended-release tablet formulations are essentially required for the long-acting effect at reduced dosage frequency. The present research was aimed for the development and optimization of an extended-release tablet of losartan potassium, exploring natural gums, i.e., xanthan gum and guar gum as drug release modifiers. Methods: The tablet formulation was prepared by wet granulation method and the formulation optimization was done by D-optimal mixture design using Design Expert® software. The independent variables studied were xanthan gum (X1), guar gum (X2) and lactose (X3) taking various combinations of the total amount of gum and ratio of xanthan gum to guar gum under the given constraint range. The dependent (response) variables studied were % drug release in 1h (Y1), 4h (Y2), 7h (Y3) and 10h (Y4). The developed tablets were evaluated for physical properties, i.e., hardness, friability, weight variation as well as the in vitro drug release profiles. For optimization studies, the polynomial equations and response surface plots were generated and the optimized formulation was selected on the basis of maximum desirability value. Results: The developed tablet formulation was found to possess all physical properties within the desired range and showed sustained release profile with ~80% drug release in 10 h duration. The model fitting studies demonstrated best fit in the zero-order model and the slope value of Korsmeyer–Peppas plot was ˃0.89, suggesting case II transport as a drug release mechanism. Conclusion: The findings suggested that natural gums-based matrix tablets of losartan could be successfully developed and natural gums can be explored as platform technology as release retardants and in the development of sustained-release matrix tablets of other drugs.


Author(s):  
HARSHAD PADEKAR ◽  
OMKAR LOHOTE

Objective: The objective of the present investigation is to design formulate and characterized the bilayer tablet containing Diclofenac sodium and Aloe Vera gel powder. In which diclofenac sodium is sustained release and Aloe Vera gel powder is immediate release. In order to produce a single dosage form containing two different classes, drug are widely prescribed by the physician to have better patient compliance. Methods: Bilayer tablet was prepared by direct compression, The immediate release layer of Aloe Vera gel powder was prepared by using different excipients such as starch, sodium starch glycolate, lactose, talc etc. sustained release layer of diclofenac sodium was prepared by using HPMC K4M, lactose, Talc Magnesium stearate, talc etc. for preparation of bilayer tablet sodium starch glycolate are use as super disintegrants in immediate release tablet and HPMC K4M are use as controlled release polymer. Various Preformulation parameter i.e. Identification, melting point, compatibility study, solubility are checked. Micromeritics properties of powder blend such as bulk density, tapped density, hausner’s ratio, Carr’s index, angle of repose are performed. Post-compression parameter was done such as hardness, friability, weight variation, drug content uniformity, thickness, in vitro drug release. Results: Result was found within the limit of the standard of optimized formulation. The drug release of the tablet was in the range of 82 to 92%in 8 h. Conclusion: Bilayer tablet was prepared by optimized batches of both layers. The prepared tablets showed satisfactory results for various evaluation parameters. The optimized formulation based on all the parameter A1 (Sodium starch glycolate) is selected for the immediate release layer and D3 (HPMC K4M) was selected for the controlled release layer. The drug release mechanism was found to be zero order release depends upon diffusion.


Author(s):  
Padmaja Bookya ◽  
Ramakrishna Raparla ◽  
Ramakrishna Raparla ◽  
Harikishan Prasad Sriramula ◽  
Ramakrishna Raparla ◽  
...  

 Objective: The aim of this investigation was to develop and optimize metformin hydrochloride matrix tablets for sustained release application. The sustained release matrix tablet of metformin hydrochloride was prepared by wet granulation technique using chitosan, xanthan gum, and hydroxypropyl methylcellulose at varying concentrations.Material and Methods: Extended release of metformin hydrochloride matrix tablets was prepared by wet granulation method. The influence of varying the polymer ratios was evaluated. The excipients used in this study did not alter physicochemical properties of the drug.Results: All the batches were evaluated for thickness, weight variation, hardness, and drug content uniformity. The in vitro drug dissolution study was carried out using USP apparatus Type II, paddle method, and the release mechanisms were explored. Mean dissolution time is used to characterize drug release rate from a dosage form and indicates the drug release is retarding efficiency of the polymer. This study revealed that as the concentration of matrix material increased, drug release from matrices decreased. This may be due to slower penetration of the dissolution medium into the matrices.Conclusion: Formulation with chitosan MS1 drug release was 86%, xanthan gum MS489%, and finally MS7 with hydroxypropyl methyl cellulose which exhibited the highest drug release retardation also had the lowest matrix concentration. Hence, lower concentration of polymers is suitable to prepare metformin hydrochloride tablets compared to higher concentrations.


Author(s):  
Silvia Surini ◽  
Nurul Nizma ◽  
Azizahwati Azizahwati

Objectives: This study aims to determine the amount of excipient that is degraded by alpha-amylase and the influence of alpha-amylase to thedissolution profile of sustained-release tablets that use matrix CL-Co-A-XG.Methods: Excipient is cross-linked with two concentrations of sodium trimetaphospate, which are 6% (CL6-Co-A-XG) and 12% (CL12-Co-A-XG).Each excipient is made with the ratios 1:1, 1:2, and 2:1 amylose-xanthan gum. Enzymatic degradation tests are performed on excipient powders for60 minutes. Sustained-release tablet with CL-Co-A-XG excipient as a matrix is formulated through direct compression method. Then, drug dissolutiontests are performed in a phosphate buffer with a pH of 7.4 both using and without using alpha-amylase as a medium for 8 hrs.Results: The results of this study show that CL6-Co-A-XG and CL12-Co-A-XG degraded 20% at 10 and 30 minutes, respectively. In addition, the releaseprofile of F1-F6 tablets show the sustained-release profile that follows zero-order and Korsmeyer–Peppas kinetics and is unaffected by the presenceof alpha-amylase.Conclusions: From this study, it can be concluded that the CL-Ko-A-XG excipients are more resistant to enzymatic degradation than amylose. Therefore,this excipient shows potential as a single matrix sustained-release tablet.


Author(s):  
SAHIDUL ALAM ◽  
AMLAN BISHAL ◽  
BRATATI BANDYOPADHYAY

Objective: Now a days as very few antidiabetic drugs are coming out of research and development and some existing drugs are showing several side effects when administered orally, multiple times in a day, hence change in the operation is a suitable and optimized way to make some drug more effective by slight alteration in the drug delivery. Matrix type drug delivery systems of an antidiabetic drug like Metformin Hydrochloride, is an interesting and promising option when developing an oral sustained release system Methods: An appropriately designed controlled release drug delivery system can be a major advance towards solving problems concerning the targeting of a drug to a specific organ or tissue and controlling the rate of drug delivery to the target sites. This research work is made in designing of sustained release dosage form of Metformin Hydrochloride by wet granulation method employing both Xanthan Gum and Hydroxy Propyl Methyl Cellulose (HPMC K4M) as a rate controlling polymer. Results: The development of oral sustained 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. From all the formulation trial batches, formulation F7 shows the best results. It has been observed that HPMC K4M alone cannot give satisfactory drug release profile but the blend of HPMC K4M and Xanthan gum together give the best drug release kinetics. Conclusion: The drug release mechanism from the matrix tablets follows Fickian diffusion with first order kinetics. Thus, sustained release matrix tablets of metformin hydrochloride can be expected to reduce the frequency of administration and decrease the dose dependent side effects


Sign in / Sign up

Export Citation Format

Share Document