scholarly journals Formulation and Evaluation of Fixed-Dose Combination Immediate Release Tablets of Ibuprofen and Famotidine through Quality by Design Approach

2021 ◽  
Vol 24 (2) ◽  
pp. 133-148
Author(s):  
Md Mahbubul Alam ◽  
Md Shahidul Islam ◽  
KM Yasif Kayes Sikdar ◽  
ASM Monjur Al Hossain
Keyword(s):  
Immediate Release ◽  
Pharmaceutical Journal ◽  
In Vitro Dissolution ◽  
Fixed Dose ◽  
Compatibility Study ◽  
Compression Technique ◽  
Disintegration Time ◽  
Independent Variables ◽  
Anti Inflammatory

Nonsteroidal anti-inflammatory drugs (NSAIDs) are frequently prescribed by the physicians for the management of pain due to their anti-inflammatory and analgesic properties. Long term use of NSAIDs causes gastrointestinal (GI) toxicity and the common GI disorders are indigestion, ulcers or bleeding. Therefore, the production of local oral tablets containing NSAIDs and gastro-protectant is inevitable. In this experiment, combination of ibuprofen 600 mg and famotidine 20 mg tablets were prepared by direct compression technique, which is unique in Bangladesh. To pursue the study Design of Experiments (DoE) approach was implemented to create fifteen trial formulations where Polyvinylpyrrolidone (PVPK30) 1%-3%, Microcrystalline Cellulose (Avicel PH-102) 1%-7% and Starch-1500 1%-13% were considered as independent variables and the responses were depicted in friability and disintegration time which were found 0.21–0.45% and 1.8–20.5 minutes respectively. Out of fifteen formulation trials (F-1 to F-15), seven formulations (F-3, F-6, F-8, F-9, F-10, F-13 and F-14) had met the acceptable criteria and one formulation (F-9) with independent variables PVP-K30 2.00%, Avicel PH-102 4.75% and Starch-1500 6.5% was selected because of its better disintegration, dissolution and friability profile. Data obtained from in-vitro dissolution tests were fitted to different kinetic models such as zero order, first order, Higuchi, Hixson-Crowell and Korsmeyer-Peppas models. Also, a compatibility study was conducted using Fourier Transform Infrared Spectroscopy (FTIR), Thermogravimetric Analysis (TGA) and X-Ray Diffraction (XRD). Furthermore, Scanning Electron Microscopy (SEM) was performed to analyze surface morphology. Finally, the selected formulation was compared to FDA regulated QC parameters and proved its superiority over conventional market products. Bangladesh Pharmaceutical Journal 24(2): 133-148, 2021

scholarly journals Fexofenadine HCl Immediate Release Tablets: In vitro Characterization and Evaluation of Excipients

2013 ◽  
Vol 16 (1) ◽  
pp. 1-9
Author(s):  
Shahriar Ahmed ◽  
Mehrina Nazmi ◽  
Ikramul Hasan ◽  
Sabiha Sultana ◽  
Shimul Haldar ◽  
...  
Keyword(s):  
Drug Release ◽  
Immediate Release ◽  
Pharmaceutical Journal ◽  
In Vitro Dissolution ◽  
Disintegration Time ◽  
Sodium Starch Glycolate ◽  
In Vitro Characterization ◽  
Weight Variation ◽  
Fexofenadine Hcl

Fexofenadine HCl immediate release tablets were designed to increase the dissolution rate by using superdisintegrants. Different formulations of Fexofenadine HCl were prepared by direct compression method. These formulations were evaluated for hardness, thickness, friability, weight variation, disintegration time, and in vitro dissolution study. The drug release from the formulations were studied according to USP specification (USP paddle method at 50 rpm for 60 minutes) maintaining the temperature to 37°C. Sodium starch glycolate, cross carmellose sodium, crospovidone (kollidon CL), ludiflash and xanthan gum were used in 3%, 6% and 8% concentrations as superdisintegrants. Thus, the ratio of superdisintegrants was changed whereas all the other excipients as well as the active drug (Fexofenadine HCl) remained same in every formulation. Here, 0.001N HCl was used as dissolution medium according to USP and absorbances were determined by using UV spectrophotometer at 217 nm. The F-3 and F-6 formulation prepared by 8% of Sodium starch glycolate and 8% of Cross carmellose sodium showed 99.99% drug release within 30 minutes and 45 minutes, respectively. The disintegration times of F-3 and F-6 formulation were within 9 seconds. The interactions between drug and excipients were characterized by FTIR spectroscopic study. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14483 Bangladesh Pharmaceutical Journal 16(1): 1-9, 2013

scholarly journals Formulation and evaluation of taste masked oral disintegrating tablets of lornoxicam

2021 ◽  
Vol 11 (5) ◽  
pp. 115-120
Author(s):  
Kritika Rai ◽  
Vivek Jain ◽  
Sunil Kumar Jain ◽  
Pushpendra Kumar Khangar
Keyword(s):  
Cation Exchange Resin ◽  
The Elderly ◽  
In Vitro Dissolution ◽  
Taste Masking ◽  
Direct Compression ◽  
Compression Technique ◽  
Disintegration Time ◽  
Weight Variation ◽  
Croscarmellose Sodium

Orally disintegrating tablets (ODT) disintegrate quickly with saliva when administered into the oral cavity and taken without water or chewed. ODT are easy to take for children and the elderly, who may experience difficultly in taking ordinary oral preparations such as tablets, capsules, and powders.  The ODT threes substantial benefits for the patient (or elder) who cannot swallow (Dysphagia), or who is not permitted water intake due to disease. The reason of the current research was to prepare taste masking oral disintegrating tablets of poorly soluble lornoxicam (LXM) by direct compression technique using Kyron T-114 (cation exchange resin) as a taste masking agent. With in various ratios the Drug-resin of 1:4 was established to present best taste masking. The superdisintegrants used in formulation are croscarmellose sodium and cross povidone. Among these croscarmellose sodium demonstrated superior drug release. The tablets were evaluated for friability, weight variation, wetting time, hardness, disintegration time and uniformity of content. Optimized formulations were evaluated for in vitro dissolution test. Amongst all the formulations F-6 was found to be most successful tablets prepared by this technique had disintegration time of 30sec and % CDR 94.78 within 30min. Hence, this advance can be utilized for taste masking of bitter pharmaceutical ingredients leading to superior patient compliance. Keywords: Oral disintegration tablets, Lornoxicam, Kyron T-114, Superdisintegrants, Direct Compression.

scholarly journals Formulation and in vitro Evaluation of Glimepiride Sustained Release Tablets: Comparison with Immediate Release Tablets

2015 ◽  
Vol 18 (2) ◽  
pp. 157-162
Author(s):  
Samira Karim ◽  
Mohiuddin Ahmed Bhuiyan ◽  
Md Sohel Rana
Keyword(s):  
Sustained Release ◽  
Immediate Release ◽  
Pharmaceutical Journal ◽  
In Vitro Dissolution ◽  
Release Formulation ◽  
Sustained Release Formulation ◽  
Zero Order Kinetics ◽  
Weight Variation ◽  
Sustained Release Tablets

This work aims at the design of a sustained release formulation of glimepiride which is currently available in the treatment of type 2 diabetes mellitus and to investigate the effect of polymers on the release profile of glimepiride. Glimepiride sustained release tablets were prepared by direct compression method using different ratios of various release retarding polymers such as carbopol, ethyl cellulose, methocel K4 MCR, methocel K15 MCR, methocel K100 MCR and xanthum gum. These formulations were also compared with glimepiride immediate release tablets. The prepared tablets were subjected to various physical parameter tests including weight variation, friability, hardness, thickness, diameter, etc. In vitro dissolution studies of the formulations were done at pH 6.8 in phosphate buffer using USP apparatus 2 (paddle method) at 50 rpm. The percent releases of all the formulations (30) were 73.11%- 98.76% after 8 hours. The release pattern followed zero order kinetics and the release of the drug was hindered by the polymers used in the study. On the other hand, 100% drug was released within 1 hour from the immediate release tablet of glimepiride. The study reveals that the polymers used have the capacity to retard the release of the drug from the sustained release tablets and the more is the amount of the polymer in the formulation the less is the release of drug showing more retardation of drug release.Bangladesh Pharmaceutical Journal 18(2): 157-162, 2015

Maraviroc Oral Disintegration Tablet: Analytical Design of Experiments (DoE) for Assessment and Comparison of In-Vitro Dissolution Profiles

2021 ◽  
Vol 17 ◽  
Author(s):  
Akula Ramesh ◽  
Jagadish P C ◽  
Vinay Jhawar ◽  
Proneel Das ◽  
Prajakta Patil ◽  
...  
Keyword(s):  
Drug Product ◽  
Hplc Method ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Compression Technique ◽  
Disintegration Time ◽  
Reference Drug ◽  
Orally Disintegrating Tablet ◽  
Rp Hplc

Background: The bioavailability of a drug in a solid oral dose depends on its release from the drug product and its balance in dissolution. Compared with a reference drug, the newly developed formulation needs to establish bioequivalence by comparing the dissolution profile. Objective: To compare dissolution profiles of a newly developed maraviroc oral disintegration tablet and the reference Axentri® tablet. The current research was designed to establish and validate an integral analytical consistency by Quality by Design (QbD) approach to quantify maraviroc from dissolution samples using the RP-HPLC method. Methods: Maraviroc was formulated into an orally disintegrating tablet using a direct compression technique at different concentrations of sodium starch glycolate as super disintegrants and talc and magnesium stearate as glidants. The dissolution test in 0.1N HCl was performed according to standard procedures to predict bioequivalence. The results of dissolution tests were analyzed using the QbD Box Behnken Design multivariate RP-HPLC method. Results: The optimized formulation (F2) was selected as it showed 90% drug release in 5 min and a disintegration time of 22 sec with dissolution profiles to the marketed reference to meet the FDA requirements of f2 similarity factor statistics. The integrated analytical QbD method was statistically analyzed by ANOVA, counter-plot, and 3D response surface plots, which demonstrated that the model is statistically significant. The developed method was validated as per ICH guidelines Q2 (R1). Conclusion : In conclusion, maraviroc oral disintegrating tablets have been well prepared, and superior statement consistency is established by the implementation of the QbD analytical method for orally disintegrating tablet excellence and adoption.

scholarly journals Designing fabrication and evaluation of Oral fast Disintegrating tablet of Ranitidine HCL

2019 ◽  
Vol 9 (1) ◽  
pp. 95-102
Author(s):  
Afroza Akbar Patel ◽  
Siraj N Shaikh ◽  
Huzaifa Patel ◽  
Afzal Band ◽  
Ahmed Shaoor
Keyword(s):  
Drug Release ◽  
Optimization Technique ◽  
Research Work ◽  
Stability Study ◽  
In Vitro Dissolution ◽  
Compression Technique ◽  
Disintegration Time ◽  
Fenugreek Gum ◽  
Fast Disintegrating Tablets

The aim of this research work was to design develop & evaluate oral fast disintegrating tablets of Ranitidine HCL. The Orodispersible tablets of Ranitidine HCl were prepared by using direct Compression technique with a Synthetic Superdisintegrant such as Crosspovidone and a natural Superdisintegrant Fenugreek gum in different concentration. 32 factorial designs was applied to study the effect of independent variables,  concentration of Crosspovidone & Fenugreek gum on dependent variables like Cumulative % Drug release and Disintegration time by using design expert software. Prepared oral fast disintegrating tablets evaluated for Pre and Post-compression parameters. The prepared tablets exhibited satisfactory physico-chemical characterise especially fast disintegration & dissolution property. Full factorial design and optimization technique successfully used in the development oral fast disintegrating tablets. Comparing the all the formulations, formulation F9 was considered as optimized formulation which shows excellent fast disintegration, in vitro dissolution, and faster drug release within 6 min in comparison to other batches also stable in stability study. Keywords:  Fast disintegrating, Ranitidine, Crosspovidone, Gum, Optimizations, Water absorption ratio

scholarly journals Formulation and Evaluation of Novel Formulation for Diabetes Induced Hypertension using Modified Innate Superdisintegrant

2020 ◽  
Vol 10 (5) ◽  
pp. 240-250
Author(s):  
Vinay Pandit ◽  
Dipanker Kashive ◽  
Tarun Kumar Sharma
Keyword(s):  
The Body ◽  
Drug Dissolution ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Compression Technique ◽  
Disintegration Time ◽  
Opuntia Ficus Indica ◽  
Cardiovascular Morbidity And Mortality ◽  
Induced Hypertension

Objectives: Diabetes is a chronic disease and is a group of metabolic disorders characterized by high levels of sugar in blood (hyperglycemia). Hypertension is a major modifiable risk factor for cardiovascular morbidity and mortality in patients with diabetes. The objective of this research is to formulate Fast dissolving tablets of Pioglitazone and Cilnidipine for the effective treatment of diabetes induced hypertension. Methods: Six formulations were prepared by direct compression technique by using Opuntia ficus-indica as an innate superdisintegrant. Result and Discussion: All the formulations were subjected for precomprression, post compression parameters and shows all the data within the specific limits. F5 formulation with the mixture of polymers viz. Opuntia ficus indica, SSG, croscarmellose sodium, magnesium stearate, DiCOM showed comparatively fast disintegration and best release of drug than that of all other formulation. The tablets of F5 formulation disintegrated within 18.53 seconds can provide fast relief in the body. The in-vitro dissolution results revealed that the drug release of F5 formulation tablets was more than 90% for Pioglitazone and near to 70% for Cilnidipine within 30 minutes. Stability studies were performed on F5 formulation tablets showed no significant changes in color, disintegration time and in-vitro dissolution which showed that appearance of tablets was having no effect. Conclusion: Fast dissolving tablets of Pioglitazone and Cilnidipine can be successfully prepared using direct compression technique and it will enhance the drug dissolution, which will further increase absorption and bioavailability of both drugs. Keywords: Pioglitazone, Cilnidipine, diabetes induced hypertension, fast dissolving tablets, direct compression.

scholarly journals Formulation and Dissolution Study of Valsartan Immediate Release Tablets

2013 ◽  
Vol 1 (02) ◽  
pp. 01-08
Author(s):  
B. Brahmaiah ◽  
K. Sasikanth ◽  
Sreekanth Nama ◽  
P. Suresh ◽  
Patan Adam Khan
Keyword(s):  
Potato Starch ◽  
Immediate Release ◽  
Magnesium Stearate ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Dissolution Profile ◽  
Compression Technique ◽  
Dissolution Studies ◽  
Main Motive

In the present study, design of oral immediate release tablets of Valsartan by direct compression technique was carried out. The main aim and objective of the work is to formulate immediate release tablets using different direct compression vehicles (DCV’S) in different ratios. The main motive is to compare the dissolution profile of these formulations and conclude the best formulation which release drug at a faster rate. To determine the best fit dissolution profile for the dosage forms. Valsartan tablets were formulated by using microcrystalline cellulose (diluents), potato starch, acacia (binder) and magnesium stearate (lubricant). The granules were compressed into tablets and were subjected to dissolution studies. The dissolution profile of the formulation F2 was found to have better dissolution rate compared to others. The In-vitro dissolution studies of all the formulations were conducted and the results were obtained, it was concluded that formulation F2 was the best with fast release of drug compared to others.

scholarly journals Bioavailability of the Common Cold Medicines in Jellies for Oral Administration

Pharmaceutics ◽  
2020 ◽  
Vol 12 (11) ◽  
pp. 1073
Author(s):  
Ki Hyun Kim ◽  
Minju Jun ◽  
Mi-Kyung Lee
Keyword(s):  
Oral Administration ◽  
Geometric Mean ◽  
Immediate Release ◽  
In Vitro Dissolution ◽  
Fixed Dose ◽  
Chlorpheniramine Maleate ◽  
Patient Centered ◽  
Dose Combination

Jellies for oral administration have been suggested as alternative dosage forms to conventional tablets for improved palatability and compliances for pediatric and geriatric patients. To evaluate the effect of jelly formulation on the bioavailability of cold medicines, two types of jellies were prepared for a fixed-dose combination of acetaminophen (AAP), chlorpheniramine maleate (CPM), dextromethorphan hydrobromide (DMH), and dl-methylephedrine hydrochloride (MEH). Jelly-S and Jelly-H were fabricated using carrageenan and locust bean gum in the absence and presence of xanthan gum, respectively. In vitro dissolution and in vivo absorption of the four drugs in the jellies were compared with other conventional formulations, a syrup and two types of immediate-release (IR) tablets with different hardness, Tablet-S (15 kPa) and Tablet-H (20 kPa). All the formulations exhibited more than 80% dissolution rate within 2 h even though the syrup, Jelly-S, and Tablet-S showed higher 30-min dissolution compared to Jelly-H and Tablet-H. The dissolution rates from the jellies decreased with increasing pH, which resulted in the slowest dissolution in pH 6.8 compared to the syrup and IR tablets. When administered orally to beagle dogs, all five formulations were determined not to be bioequivalent. However, Jelly-S and Jelly-H showed 0.82–1.05 of the geometric mean ratios (GMRs) of AUC0-t for all four drugs compared to the syrup suggesting comparable absorption. In two IR tablets, GMRs of AUC0-t were in a range of 0.55–0.95 indicating a tendency of lower absorption than the syrup and jellies. In conclusion, jelly can be a patient-centered formulation with comparable bioavailability to syrup.

Effect of synthetic super disintegrants and natural polymers in the preparation of donepezil hydrochloride fast disintegration films

2014 ◽  
Vol 3 (3) ◽  
pp. 243-246 ◽  
Author(s):  
P.K. Lakshmi ◽  
D. Lavanya ◽  
M.M. Husnien Ali
Keyword(s):  
Sodium Alginate ◽  
Guar Gum ◽  
Pharmaceutical Journal ◽  
In Vitro Dissolution ◽  
Poly Vinyl Alcohol ◽  
Natural Polymers ◽  
Disintegration Time ◽  
Sodium Starch Glycolate ◽  
Donepezil Hydrochloride

The main aim of the present research was to develop a fast dissolving oral polymeric film with good mechanical properties, faster disintegration and dissolution when placed on tongue. Donepezil hydrochloride (DPH) is prescribed in the treatment of mild to moderate Alzheimer’s disease (AD). The polymers selected for preparing films were sodium alginate (SA), poly vinyl alcohol (PVA) and guar gum (GG). Three batches of films were prepared by solvent casting method with sodium alginate, sodium alginate & PVA and with the combination of sodium alginate & guar gum. From these three batches, three optimized film formulations S3, SP7 and SG8 were selected based on disintegration time. To these three selected film formulations, superdisintegrants sodium starch glycolate (SSG), cross carmellose sodium (CCS) and cross povidone (CP) were added at a concentration of 4% w/w of polymer to improve the disintegration time. The films prepared with or without superdisintegrants were compared for fast releasing properties. Based on DT and in vitro dissolution data, S3CP was selected as the best formulation among the all formulations.DOI: http://dx.doi.org/10.3329/icpj.v3i3.17892 International Current Pharmaceutical Journal, February 2014, 3(3): 243-246

scholarly journals PART I: OPTIMIZATION OF HYDRALAZINE HYDROCHLORIDE IMMEDIATE RELEASE LAYER IN ANTIHYPERTENSIVE BILAYER TABLET

2020 ◽  
pp. 227-223
Author(s):  
HARSH TRIVEDI ◽  
KUNAL PATEL ◽  
NISHANT A. OZA ◽  
SWATI SAGAR
Keyword(s):  
Drug Release ◽  
Graphical Representation ◽  
Linear Regression Analysis ◽  
Immediate Release ◽  
Compatibility Study ◽  
Disintegration Time ◽  
Dependent Variables ◽  
Ft Ir ◽  
Hydralazine Hydrochloride

Objective: Aim of the present study was the optimization of the immediate release (IR) layer containing hydralazine hydrochloride (HHC) 25 mg and compressed with a sustained-release (SR) layer of isosorbide dinitrate (ISDN) 40 mg to decrease the dosing frequency. Methods: In this study, Drug-excipients compatibility study was carried out by FT-IR and a preliminary trial was conducted for screening of super disintegrating agents. The amount of sodium starch glycolate (SSG) (X1) and the amount of ac-di-sol® (X2) was chosen as independent variables in 32 full factorial design while wetting time (WT) (Y1), disintegration time (DT) (Y2) and In vitro drug release at 15 min (Q15) (Y3) were taken as dependent variables. Multiple linear regression analysis, ANOVA, and graphical representation of the influence of factor by 3D plots were performed by using sigma plot 13.0. In the present study, the following constraints were used for the selection of an optimized batch: WT<16 s, DT<25 s, and Q15>90%. To validate the evolved mathematical models, a checkpoint batch was selected from its desirability value. Results: FT-IR spectra show that the drug and excipients were compatible with each other. The calculated F values found for WT, DT, and Q15 were 045.559, 077.100 and 278.760, respectively. All Calculated F values are greater than tabulated values for all dependent variables. Prepared checkpoint was selected from its desirability value 0.935 and it gives a 100% drug release within 30 min. Conclusion: These results confirm that the prepared HHC 25 mg IR layer is used for rapid control of hypertension.

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