scholarly journals Formulation and Evaluation of Tablets Containing Fenugreek Extract Using Sodium Starch Glycolate as Super Disintegrant

2021 ◽  
pp. 47-53
Author(s):  
Divya Jyothi
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Antidiabetic Activity ◽  
Wet Granulation ◽  
Onset Of Action ◽  
Plant Materials ◽  
Sodium Starch Glycolate ◽  
Tablet Formulations

The present work is aimed to formulate the tablets containing fenugreek extract as drug by wet granulation method. Further the effect of Sodium Starch Glycolate as super disintegrant on disintegration and drug release was studied. Fenugreek extract contains mucilage which retards the disintegration of tablets and hence shows slower drug release. Hence in order to improve disintegration and thereby in vitro drug release, Sodium Starch Glycolate was used as super disintegrant. Tablet formulations were prepared without the SSG (Conventional-F1) and also with sodium starch glycolate (F2-F4) by wet granulation method. Assessment of flow properties of granules, physicochemical characterization of tablet formulations was carried out. Fenugreek is widely used for its antidiabetic activity which is attributed to mainly to the presence of an alkaloid Trigonelline. Hence in vitro release study of trigonelline was carried out which showed that the percentage release from F1 and F2 was found to be 58.12±4.49 and 99.08±0.01 respectively after 6 hrs. This study concludes that tablet formulation of fenugreek seed extracts with super disintegrants will be more desirable, advantageous and therapeutically more beneficial than incorporating the direct plant materials for the treatment of diabetes for faster onset of action.

Evaluation of Cassia roxburghii Seed Gum as Binder in Tablet Formulations of Selected Drugs

1970 ◽  
Vol 2 (4) ◽  
pp. 726-732
Author(s):  
Arul Kumaran KSG ◽  
Palanisamy S ◽  
Rajasekaran A ◽  
Ahil Hari
Keyword(s):  
Drug Release ◽  
Diclofenac Sodium ◽  
Angle Of Repose ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Dissolution Profile ◽  
Sodium Starch Glycolate ◽  
Tablet Formulations ◽  
Seed Gum

The purpose of the study was to evaluate cassia roxburghii seed gum powder as binder for paracetamol and diclofenac sodium. Granules of both drugs were prepared by wet granulation method. Two different laboratory developed methods were tried for the isolation of seed mucilage from seed powder. The phytochemical, physico-chemical and microbiological properties were performed on the seed gum and the pre-compression parameters like bulk density, tapped density, angle of repose, carr’s index and hausner’s ratio have shown that paracetamol and diclofenac granules prepared using Cassia roxburghii gum were well within the limits and comparable to those prepared using standard starch paste as binder. The in vitro dissolution study was performed for paracetamol formulations with sodium starch glycolate and the dissolution profile shows all the three formulations met with official specifications. The in vitro dissolution profile shows that drug release decreased in the order, tablets prepared by starch>c.roxburghii defatted>c.roxburghii filtered in both paracetamol and diclofenac formulations. The drug release from tablets prepared by C.roxburghii seed gum was more than 85% in 2 hours and filtered C.roxburghii gum has excellent mechanical, binding and release properties in paracetamol tablet formulations with the addition of sodium starch glycolate as an external disintegrant

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.

Formulation and Evaluation of Immediate Release Bilayer Tablets of Telmisartan and Hydrochlorothiazide

2011 ◽  
Vol 4 (3) ◽  
pp. 1477-1483
Author(s):  
Natarajan R ◽  
N Patel ◽  
Rajendran N N ◽  
M Rangapriya
Keyword(s):  
Antihypertensive Drugs ◽  
In Vitro Release ◽  
Immediate Release ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Dissolution Profile ◽  
Formulation Development ◽  
Sodium Starch Glycolate ◽  
Bilayer Tablets

The main goal of this study was to develop a stable formulation of antihypertensive drugs telmisartan and hydrochlorothiazide as an immediate-release bilayer tablet and to evaluate the dissolution profile in comparison with a reference product. The formulation development work was initiated with wet granulation. Telmisartan was converted to its sodium salt by dissolving in aqueous solution of sodium hydroxide to improve solubility and drug release. Lactose monohydrate and microcrystalline cellulose were used as diluents. Starch paste is prepared in purified water and was used as the binder. Sodium starch glycolate is added as a disintegrating agent. Magnesium stearate was used as the lubricant. The prepared granules were compressed into a double-layer compression machine. The tablets thus formulated with higher proportion of sodium starch glycolate showed satisfactory physical parameters, and it was found to be stable and in vitro release studies are showed that formulation (F-T5H5) was 101.11% and 99.89% respectively. The formulation T5H5 is further selected and compared with the release profile of the innovator product, and was found to be similar (f2 factor) to that of the marketed product. The results suggest the feasibility of developing bilayer tablets consisting of telmisartan and hydrochlorothiazide for the convenience of patients with hypertension.  

scholarly journals Novel Gliclazide Electrosprayed Nano-Solid Dispersions: Physicochemical Characterization and Dissolution Evaluation

2019 ◽  
Vol 9 (2) ◽  
pp. 231-240
Author(s):  
Khosro Adibkia ◽  
Solmaz Ghajar ◽  
Karim Osouli-Bostanabad ◽  
Niloufar Balaei ◽  
Shahram Emami ◽  
...  
Keyword(s):  
Drug Release ◽  
Solid Dispersions ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Amorphous State ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Peg 6000

Purpose: In the current study, electrospraying was directed as a novel alternative approach to improve the physicochemical attributes of gliclazide (GLC), as a poorly water-soluble drug, by creating nanocrystalline/amorphous solid dispersions (ESSs). Methods: ESSs were formulated using Eudragit® RS100 and polyethylene glycol (PEG) 6000 as polymeric carriers at various drug: polymer ratios (i.e. 1:5 and 1:10) with different total solution concentrations of 10, 15, and 20% w/v. Morphological, physicochemical, and in-vitro release characteristics of the developed formulations were assessed. Furthermore, GLC dissolution behaviors from ESSs were fitted to various models in order to realize the drug release mechanism. Results: Field emission scanning electron microscopy analyses revealed that the size and morphology of the ESSs were affected by the drug: polymer ratios and solution concentrations. The polymer ratio augmentation led to increase in the particle size while the solution concentration enhancement yielded in a fiber establishment. Differential scanning calorimetry and powder X-ray diffraction investigations demonstrated that the ESSs were present in an amorphous state. Furthermore, the in vitro drug release studies depicted that the samples prepared employing PEG 6000 as carrier enhanced the dissolution rate and the model that appropriately fitted the release behavior of ESSs was Weibull model, where demonstrating a Fickian diffusion as the leading release mechanism. Fourier-transform infrared spectroscopy results showed a probability of complexation or hydrogen bonding, development between GLC and the polymers in the solid state. Conclusion: Hence the electrospraying system avails the both nanosizing and amorphization advantages, therefore, it can be efficiently applied to formulating of ESSs of BCS Class II drugs.

scholarly journals FORMULATION, DEVELOPMENT AND IN VITRO EVALUATION OF TRAMADOL EXTENDED RELEASE TABLETS

2019 ◽  
pp. 63-73
Author(s):  
SANJAY KUMAR GUPTA ◽  
AFRAH HUNEZA ◽  
SRADHANJALI PATRA
Keyword(s):  
Drug Release ◽  
Polyethylene Oxide ◽  
Extended Release ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Wet Granulation ◽  
Matrix System ◽  
First Order ◽  
Vitro Release

Objective: The objective of the present study was to develop “once daily” extended release tablets of tramadol (100 mg) by wet granulation using hydrophilic polymer like hydroxy propyl methyl cellulose K100M,K15M and polyethylene oxide (PEO). Methods: The tramadol matrix tablets were prepared by using different polymers like hydroxy propyl methyl cellulose (HPMC K15M and K100M), polyethylene oxide (PEO) as the nontoxic and easily available suitable matrix system. The extended release tablets of tramadol (400 mg) were prepared wet granulation technique. Different pre compression and post compression were performed. In vitro dissolution tests were performed and percentage drug release was calculated. The fourier-transform infrared spectroscopy (FTIR) studies conducted on pure drug tramadol and the optimize formulation (T6). Different release models like zero order, first order, higuchi and Korsemeyer-Peppas were applied to in vitro drug release data in order to evaluate the drug release mechanisms and kinetics. Results: Pre compression and post compression parameters satisfied with pharmacopeia specifications. The In vitro release studies were performed using USP type II apparatus showed that optimized formulation T6 consisting of polyethylene oxide (PEO) with 25 mg of the polymer was found to extended release of tramadol over a period of 24h. The optimized formulation T6 followed the zero order kinetics as correlation coefficient (r2) values are higher than that of first-order release kinetics. In order to understand the complex mechanism of drug release from the optimized formulation T6 matrix system, the in vitro release rate were fitted to Korsemeyer-Peppas model and the release exponent value (n) obtained was 0.82105 exhibited anomalous (non fickian) diffusion mechanism. Conclusion: The present study shows that polyethylene oxide was found to play a great role in controlling release of tramadol from the matrix system. Accordingly it can be concluded that the formulation is robust in the performance is less likely to be affected by the various factors studied.

scholarly journals Enhanced Dissolution of Sildenafil Citrate Using Solid Dispersion with Hydrophilic Polymers: Physicochemical Characterization and In Vivo Sexual Behavior Studies in Male Rats

Polymers ◽  
2021 ◽  
Vol 13 (20) ◽  
pp. 3512
Author(s):  
Mohammed F. Aldawsari ◽  
Md. Khalid Anwer ◽  
Mohammed Muqtader Ahmed ◽  
Farhat Fatima ◽  
Gamal A. Soliman ◽  
...  
Keyword(s):  
Sexual Behavior ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Hydrophilic Polymers ◽  
Sildenafil Citrate ◽  
Male Rats ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
Onset Of Action

Sildenafil citrate (SLC) is a frequently used medication (Viagra®) for the treatment of erectile dysfunction (ED). Due to its poor solubility, SLC suffers from a delayed onset of action and poor bioavailability. Hence, the aim of the proposed work was to prepare and evaluate solid dispersions (SDs) with hydrophilic polymers (Kolliphor® P188, Kollidon® 30, and Kollidon®-VA64), in order to enhance the dissolution and efficacy of SLC. The SLC-SDs were prepared using a solvent evaporation method (at the ratio drug/polymer, 1:1, w/w) and characterized by Differential Scanning Calorimetry (DSC), Fourier-transform infrared spectroscopy (FTIR), X-ray diffraction (XRD), Scanning electron microscope (SEM), drug content, yield, and in vitro release studies. Based on this evaluation, SDs (SLC-KVA64) were optimized, with a maximum release of drug (99.74%) after 2 h for all the developed formulas. The SDs (SLC-KVA64) were further tested for sexual behavior activity in male rats, and significant enhancements in copulatory efficiency (81.6%) and inter-copulatory efficiency (44.9%) were noted in comparison to the pure SLC drug, when exposed to the optimized SLC-KVA64 formulae. Therefore, SD using Kollidon®-VA64 could be regarded as a potential strategy for improving the solubility, in vitro dissolution, and therapeutic efficacy of SLC.

scholarly journals Formulation and Evaluation of Gabapentin Sustained Release Matrix Tablet Using Hibiscus rosa sinensis Leaves Mucilage as Release Retardant

2021 ◽  
pp. 564-572
Author(s):  
P. Amsa ◽  
G. K. Mathan ◽  
S. Magibalan ◽  
E. K. Velliyangiri ◽  
T. Kalaivani ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Hibiscus Rosa Sinensis

The major goal of this study was to develop and evaluate Sustained release matrix tablets of Gabapentin with Hibiscus rosa - sinensis leaves mucilage prepared by using wet granulation technique with microcrystalline cellulose as a diluents and magnesium stearate as a lubricant. Pre-compression and post-compression evaluation of physicochemical parameters were carried out and to be within acceptable limits. Drug and polymer compatibility were validated by FTIR measurements. Further, tablets were evaluated for in vitro release study. To get the sustained release of Gabapentin, the concentration of Hibiscus rosa- sinensis mucilage was tuned with a gas-generating agent. The % drug release of all formulation from F1 to F5 showed 91.24%, 80.24%, 70.53%, 62.12% and 49.83% respectively. All the dosage form release kinetics was computed using zero order, first order, Higuchi, and Korsmeyer–Peppas methods. From the above results, it is concluded that the n value of formulation F5 showed 0.78 suggesting anomalous (non-fickian) behavior of the drug. Mucilage from the leaves of Hibiscus rosa-sinensis has a great retarding effect in drug release from sustained release tablets.

scholarly journals Development and Evaluation of Alprazolam Controlled Release tablets

2014 ◽  
Vol 1 (1) ◽  
pp. 8-23 ◽  
Author(s):  
Sarmila Shrestha ◽  
Dharma Prasad Khanal ◽  
Panna Thapa
Keyword(s):  
Molecular Weight ◽  
Controlled Release ◽  
Drug Release ◽  
Drug Formulation ◽  
In Vitro Dissolution ◽  
Wet Granulation ◽  
Significant Difference ◽  
Model Independent ◽  
Tablet Formulations

Twenty three different tablet formulations of alprazolam were prepared using Polymer like hydroxypropylmethyl cellulose (HPMC K4M, HPMC K15M and HPMC K100M) in the concentration of 5 – 50 % of total weight of tablets and combination of HPMC K15M and HPMC K100M with ethyl cellulose (EC) was formulated by using wet granulation method. Drug formulation containing 1.0 mg, 1.5 mg, 5 mg, 10 mg and 15 mg alprazolam per tablet maintaining constant HPMC K15M concentration was also developed.The in-vitro dissolution studies of the formulated and marketed product in USP type II apparatus showed that the drug release is dependent upon the drug: polymer ratio; also molecular weight of the polymer and solubility of loaded drug. With increasing concentration and molecular weight of polymer, drug release was found to be decreased. When formulating the tablets the method used whether direct compression or wet granulations also affect the release of the drug from matrix. Wet granulation method by using 40 % HPMC K15M in combination with 5 % EC was found to be most suitable controlled release alprazolam tablet as drug release was found to be appreciable in this formulation. When loading dose of alprazolam was increased, drug release was found to be tremendously decreased because of the poor solubility of alprazolam in water. When one-way ANOVA was applied for various formulated and marketed tablets it was found that there is no significant difference (p > 0.05) in drug release rate among formulation similarly model independent methods was also applied such as similarity and dissimilarity factor and found that there is no significant difference between these formulations.DOI: http://dx.doi.org/10.3126/jmmihs.v1i1.9896 Journal of Manmohan Memorial Institute of Health Sciences Vol.1(1) 2011; 8-23

scholarly journals Physicochemical Characterization and Evaluation of the Binding Effect of Acacia etbaica Schweinf Gum in Granule and Tablet Formulations

2021 ◽  
Vol 2021 ◽  
pp. 1-13
Author(s):  
Kidan Haily Desta ◽  
Ebisa Tadese ◽  
Fantahun Molla
Keyword(s):  
Water Solubility ◽  
In Vitro Release ◽  
Physicochemical Characterization ◽  
Hot Water ◽  
Angle Of Repose ◽  
Wet Granulation ◽  
Flow Properties ◽  
Disintegration Time ◽  
Binding Effect ◽  
Tablet Formulations

This study is aimed at evaluating the binding effect of Acacia etbaica gum in granule and tablet formulations using paracetamol as a model drug. Some physicochemical properties of the purified gum such as pH, the presence of tannin and dextrin, solubility, viscosity, loss on drying, total ash value, water solubility index, swelling power, moisture sorption, and powder flow properties were investigated. Paracetamol granules were prepared using wet granulation method at 2%, 4%, 6%, and 8% w / w of the Acacia etbaica gum and compared with granules prepared with reference binders (PVP K-30 and Acacia BP) in similar concentrations. The granules were characterized for bulk and tapped densities, compressibility index and Hausner ratio, angle of repose, flow rate, and friability. Finally, the prepared granules were compressed into tablets and evaluated for different tablet characteristics: weight uniformity, thickness, diameter, crushing strength, tensile strength, friability, disintegration time, and in vitro release profile. The physicochemical characterization revealed that tannins and dextrin are absent in the gum, and the gum has acidic pH. Both the moisture content and total ash values were within the official limits. Furthermore, the gum was found to be soluble in cold and hot water but insoluble in organic solvent and exhibited a shear thickening viscosity profile and excellent flow properties with excellent compressibility. The granules prepared with the gum of Acacia etbaica and reference binders showed good particle size distribution and excellent flow and compressibility properties. All the prepared tablets passed pharmacopeial specifications with respect to their uniformity of weight, thickness, and disintegration time. Tablets formulated with Acacia etbaica gum and acacia BP meet the compendial specification for friability at binder concentrations more than 2%. Drug release properties of all the batches formulated with Acacia etbaica, PVP, and acacia BP complied with the pharmacopeial specification. It can be concluded that the gum of Acacia etbaica could be explored as an alternative excipient for its binder effect in granule and tablet formulations.

scholarly journals Formulation and evaluation of matrix tablets of Eperisone hydrochloride

2020 ◽  
Vol 1 (4) ◽  
pp. 131-136
Author(s):  
Peruboina Neelima ◽  
Maddula Venkata Ramana
Keyword(s):  
Drug Release ◽  
In Vitro Release ◽  
Hepatic Metabolism ◽  
Magnesium Stearate ◽  
Matrix Tablets ◽  
Spinal Reflexes ◽  
Wet Granulation ◽  
Physical Parameters ◽  
Weight Variation

The aim of the present research is to develop and optimize Eperisone Hydrochloride extended release matrix tablets. Eperisone Hydrochloride is an antispasmodic drug mainly used to relieve pains it acts by relaxing the skeletal and smooth vascular muscles by blocking spinal reflexes drug which has oral bioavailability of 70% due to hepatic metabolism. Sustained release matrix tablets of Eperisone Hydrochloride were prepared through wet granulation technique by using HPMC K4M and EC as polymers, PVPK30 as binder, Magnesium stearate as lubricant and Talc as glidant. The granules of different formulations were determined for pre compression parameters. The prepared granules along with the excipients were then compressed. The formulated tablets were evaluated for physical characteristics viz. Hardness, Thickness, % Weight variation, Friability and the drug content. Furthermore the tablets evaluated for the in vitro release studies. Out of all the 8 formulations F7 showed desired characteristics in the physical parameters and in vitro drug release of 85.48% in 12hrs.The F7 dissolution data was best fitted to the Zero order model. The prepared Eperisone Hydrochloride matrix tablets found to be having a potential extended drug release.

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