scholarly journals Investigation of Dry Granulation and Wet Granulation Effect on Dissolution Profile of the Developed Film Coated Tablets Containing Eplerenone

2021 ◽  
Vol 7 (2) ◽  
Author(s):  
Deniz Eİ ◽  
Toprak C ◽  
Gun G
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Reference Product ◽  
Wet Granulation ◽  
Dissolution Profile ◽  
Granulation Process ◽  
Similarity Factor ◽  
Bcs Class Ii ◽  
Dry Granulation ◽  
F2 Similarity Factor

The objective is to observe and improve drug release of Eplerenone which is BCS Class II API by applying dry granulation and wet granulation process. Inspra 50 mg film coated tablets, manufactured by Pfizer, were taken as reference product to compare with dissolution profiles of dry granulation applied product and wet granulation applied product. Investigation of the effect of wet granulation process on dissolution profiles of Eplerenone 50 mg film coated tablets has been demonstrated out in the scope the study. While f2 similarity factor is 44.93 for dry granulation applied product, it is 60.62 for wet granulation applied product when compared to reference product. It comply that dissolution rate of wet granulation applied product is more proper to the specification than dry granulation applied product. The study demonstrates the effect of different granulation process on dissolution rate.

Formulation and Characterization of Glimepiride Nanoparticles for Dissolution Enhancement

2020 ◽  
Vol 10 (5) ◽  
pp. 649-663
Author(s):  
Reena Siwach ◽  
Parijat Pandey ◽  
Harish Dureja
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Oral Absorption ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Class Ii ◽  
Dissolution Enhancement ◽  
In Vitro Drug Release ◽  
Bcs Class Ii

Background: The rate-limiting step in the oral absorption of BCS class II drugs is dissolution. Their low solubility is one of the major obstacles in the process of drug development. Dissolution rate can be increased by decreasing the particle size to the nano range, eventually leading to increased bioavailability. Objective: : In the present study, glimepiride loaded nanoparticles were prepared to enhance the dissolution rate. The aim of the work was to examine the effect of polymer-drug ratio, solvent-antisolvent ratio and speed of mixing on in vitro release of glimepiride. Methods: Glimepiride is an antidiabetic drug belonging to the BCS class II drugs. The polymeric nanoparticles were formulated according to Box-Behnken Design (BBD) using nanoprecipitation technique. The prepared nanoparticles were evaluated for in vitro drug release, loading capacity, entrapment efficiency, and percentage yield. Result: It was found that NP-8 has maximum in vitro drug release and was selected as an optimized batch. Analysis of Variance (ANOVA) was applied to the in vitro drug release to study the fitness and significance of the model. The batch NP-8 showed 70.34 ± 1.09% in vitro drug release in 0.1 N methanolic HCl and 92.02 ± 1.87% drug release in phosphate buffer pH 7.8. The release data revealed that the nanoparticles followed zero order kinetics. Conclusion: The study revealed that the incorporation of glimepiride into gelucire 50/13 resulted in enhanced dissolution rate.

scholarly journals Hydroxypropylcellulose controlled release tablet matrix prepared by wet granulation: effect of powder properties and polymer composition

2009 ◽  
Vol 52 (1) ◽  
pp. 157-162 ◽  
Author(s):  
Antonio Zenon Antunes Teixeira
Keyword(s):  
Drug Release ◽  
Release Rate ◽  
Hydrophilic Polymers ◽  
Polymer Composition ◽  
Wet Granulation ◽  
Granulation Process ◽  
Powder Properties ◽  
Low Levels ◽  
Tablet Matrix ◽  
Best Fit

The aim of this study was to attain 100% drug release of caffeine after 24 h from hydroxypropylcellulose (HPC) tablet matrices and to investigate the effect of co-excipient. Physical properties of the powders were evaluated and suggested for a wet granulation process. The tablet containing caffeine was formulated by different weight ratios of hydrophilic polymers. The results of polymer evaluation confirmed that the increase of HPC level with the same drug content significantly decreased the rate of drug release. The presence of co-polymer excipients carboxymethylcellulose (CMC) and polyvinylpyrrolidone (PVP) in the tablet matrix was also investigated. The release rate was also controlled by low levels of CMC (<10%) while PVP did not show any considerably effect. The best fit release rate 100% at 24 h was obtained when 10% of α-lactose monohydrate was added to the formulation.

scholarly journals Enrichment of aqueous solubility and dissolution profile of mesalamine: In vitro evaluation of solid dispersion

2021 ◽  
Vol 9 (2) ◽  
pp. 127-135
Author(s):  
Anil Raosaheb Pawar ◽  
Pralhad Vitthalrao Mundhe ◽  
Vinayak Kashinath Deshmukh ◽  
Ramdas Bhanudas Pandhare ◽  
Tanaji Dilip Nandgude
Keyword(s):  
Ulcerative Colitis ◽  
Drug Release ◽  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Aqueous Solubility ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
Peg 4000

The aim of the present study was to formulate solid dispersion (SD) of Mesalamine to enrich the aqueous solubility and dissolution rate. Mesalamine is used in the management of acute ulcerative colitis and for the prevention of relapse of active ulcerative colitis. In the present study, Solid dispersion of Mesalamine was prepared by Fusion and Solvent evaporation method with different polymers. SD’s were characterized by % practical yield, drug content, Solubility, FT-IR, PXRD (Powder X- ray diffractometry), SEM (Scanning electron microscopy), in vitro dissolution studies and Stability studies. The percent drug release of prepared solid dispersion of Mesalamine by fusion and solid dispersion method (FM47, FM67, SE47 and SE67) in 1:7 ratio was found 81.36±0.41, 86.29±0.64, 82.45±0.57and 87.25±1.14 respectively. The aqueous solubility and percent drug release of solid dispersion of Mesalamine by both methods was significantly increased. The PXRD demonstrated that there was a significant decrease in crystallinity of pure drug present in the solid dispersions, which resulted in an increased aqueous solubility and dissolution rate of Mesalamine.The significant increase in aqueous solubility and dissolution rate of Mesalamine was observed in solid dispersion as the crystallinity of the drug decreased, absence of aggregation and agglomeration, increased wetability and good dispersibility after addition of PEG 4000 and PEG 6000.

Development, Optimization, Characterization and Impact of In vitro Lipolysis on Drug Release of Telmisartan Loaded SMEDDS

2019 ◽  
Vol 9 (4) ◽  
pp. 330-340 ◽  
Author(s):  
Ravinder Verma ◽  
Deepak Kaushik
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Oral Bioavailability ◽  
Research Work ◽  
Mixture Design ◽  
In Vitro Dissolution ◽  
Dissolution Profile ◽  
In Vitro Lipolysis ◽  
Globule Size

Objective: The objective of the current research is systematic optimization and development of microemulsion preconcentrates to get better solubility that results in improvement of oral bioavailability profile of Telmisartan utilizing D-optimal mixture design. Methods: Solubility studies in a variety of lipidic ingredients and optimization of formulations were carried out for the development of liquid SMEDDS. D-optimal mixture design was utilized for assessing the interaction performance of desired responses (such as % cumulative drug release and globule size) and optimized using desirability approach. The optimized batch was evaluated for its % cumulative drug release and globule size performance for determining the dissolution rate and oral bioavailability of drug. Results: The optimized batch (F-8), which contained 10% oil (Capmul MCM EP), 45% surfactant (Labrasol) and 45% co-surfactant (Transcutol HP) resulted in desired qualities of measured responses with 84.6nm globule size and 98.5% drug release within 15 minutes. Optimized SMEDDS showed brilliant goodness of fit between drug release. Stability studies indicated stability of the optimized SMEDDS batch over 3-month storage at 40°C/75% RH and improved dissolution rate in contrast to pure API. The optimized SMEDDS showed no impact of in vitro lipolysis on drug release. Conclusion: Developed and optimized SMEDDS showed improved in vitro dissolution rate and dissolution profile in contrast to pure drug. These investigations further confirm dose reduction in SMEDDS by gaining an equivalent therapeutic profile with non-SMEDDS formulation. This research work successfully shows the potential usage of SMEDDS for delivery of BCS-II class drugs.

scholarly journals Formulation Development and Evaluation of New Albendazole Tablets with Integrated Quality by Design (QbD) Approach

2021 ◽  
Vol 11 (2) ◽  
pp. 123-134
Author(s):  
Dnyaneshwar G Sitre ◽  
Ravindra K. Kamble
Keyword(s):  
Risk Assessment ◽  
Drug Release ◽  
Quality By Design ◽  
Reference Product ◽  
Contour Plot ◽  
Dissolution Profile ◽  
Formulation Development ◽  
Pareto Chart ◽  
Full Factorial ◽  
Formulation Variables

Hydatid disease occurs in most areas of the world and currently affects about one million people. Albendazole is an orally administered broad spectrum anthelmintic drug approved by US FDA in 1996. Literature review suggests Albendazole is low solubility compound and most of the studies were performed to improve the solubility with traditional approach of product development. The present study was aimed to apply Design of Experiments (DoE) in the development and optimization of drug release from new Albendazole tablets using three factor two level (23) full factorial designs with integrated Quality be Design (QbD) approach. New Albendazole tablets were formulated using micronized grade of the Albendazole active and excipients were selected inline with market reference product. Quality target product profile (QTPP) and Critical quality attributes (CQAs) were designed. Risk assessment was used to identify the Formulation variables impacting CQA dissolution. The amount of Formulation variables were optimized on the basis of drug release profiles at 15 minutes and 30 minutes of different formulation batches manufactured based on 23 full factorial design. Tablets were prepared by wet granulation technique and evaluated for various physicochemical parameters and in vitro drug release. Formulation trials dissolution results at 15 minutes and 30 minutes were evaluated to derive the concentration of Formulation variables which will achieve the release of more than 80%. Analysis of variance (ANOVA) analysis, Pareto chart and Contour plot were used to predict the values of formulation variables and their effect on dissolution.  Updated risk assessment of the Formulation Variables was performed and justification was provided for reduction of risk from medium to low level. Optimized formulation from DOE had comparable dissolution profile with market reference tablet. Stability studies of new Albendazole tablets 200 mg were conducted at ICH accelerated conditions and found to be stable. Thus studies revealed that full factorial experimental design could efficiently be applied for optimization of formulation variables affecting drug release. New Albendazole tablets 200 mg successfully formulated with application of the integrated quality by design (QbD) and design of experiment (DOE) approach and thereby achieved comparable release profile with market reference product.  

scholarly journals The Effects of Lubricants on the Disintegration and Dissolution Profile of Metronidazole Tablets Formulated Using Sida acuta Gum as a Binder

2021 ◽  
pp. 350-362
Author(s):  
Sinodukoo Eziuzo Okafo ◽  
Avbunudiogba John Afokoghene ◽  
Christian Areruruoghene Alalor ◽  
Deborah Ufuoma Igbinake
Keyword(s):  
Drug Release ◽  
Magnesium Stearate ◽  
Sodium Lauryl Sulphate ◽  
Wet Granulation ◽  
Dissolution Profile ◽  
Disintegration Time ◽  
In Vitro Drug Release ◽  
Sida Acuta ◽  
Drug Content

Aims: This research was done to study the effects of types and concentrations of lubricants on the dissolution and disintegration profile of metronidazole tablets formulated using Sida acuta gum as a binder. Methodology: Sida acuta gum (SAG) was extracted from powdered dried leaves of Sida acuta. Metronidazole granules were produced by wet granulation technique using different concentrations (1 and 2%) of SAG as a binder and mixed with different concentrations (0.5, 1.0, and 1.5%) of magnesium stearate (MS) or sodium lauryl sulphate (SLS) as a lubricant. The granules/lubricant -mix was compressed into tablets and evaluated for hardness, weight uniformity, drug content, disintegration time, friability and in vitro drug release. Results: The hardness for the tablets was from 4.08 to 7.97 Kgf. The friability was from 0.02±0.45 to 3.40±0.43%. Tablets from formulations A1-A3, B2, and B3 failed the friability test. Formulations prepared with 1% SAG were more friable than those formulated with 2% SAG. Disintegration time for formulations A1-A3 (1% SAG + MS) ranged from 19.07 to 63.5 min, while that of A4-A6 (2% SAG + MS) was from 39.06 to 81.48 min. Formulations B1-B3 (1% SAG + SLS) had disintegration time that ranged from 4.22 to 6.8 min while that of B4-B6 (2% SAG + SLS) was from 9.35 to 15.90 min. The % drug release at 60 min for formulations that contained SAG and MS was 76.60-104.28% and SAG and SLS was 99.89-101.35% Conclusion: Metronidazole tablets formulated using SLS as lubricant disintegrated faster than those formulated using magnesium stearate as lubricant. Percentage drug release from tablets containing SLS was slightly higher than those that contained magnesium stearate. Higher concentrations of the lubricants produced softer tablets.

scholarly journals Prediction of quality attributes (mechanical strength, disintegration behavior and drug release) of tablets on the basis of characteristics of granules prepared by high shear wet granulation

PLoS ONE ◽  
2021 ◽  
Vol 16 (12) ◽  
pp. e0261051
Author(s):  
Amjad Khan
Keyword(s):  
Expert System ◽  
Drug Release ◽  
Mechanical Strength ◽  
Wet Granulation ◽  
High Shear ◽  
Process Variables ◽  
Crushing Strength ◽  
Granulation Process ◽  
Binder Concentration ◽  
High Shear Wet Granulation

High shear wet granulation is commonly applied technique for commercial manufacturing of tablets. Granulation process for tablets manufacturing is generally optimized by hit and trial which involves preparation of granules under different processing parameters, compression of granules and evaluation of the resultant tablets; and adjustment is made in granulation process on the basis of characteristics of tablets. Objective of the study was to optimize the process of high shear wet granulation and prediction of characteristics of tablets on the basis of properties of granules. Atenolol granules were prepared by high shear wet granulation method, using aqueous solution of polyvinyl pyrrolidone (PVP k-30) as binder. Concentration of binder solution and granulation time were taken as process variables, both studied at three levels. Different combinations of process variables were determined by Design Expert software. Granules were evaluated for different parameters on the basis of SeDeM-ODT (Sediment Delivery Model-Oro Dispersible Tablets) expert system. Granules from all the trials were compressed using round (10.5 mm) flat faced punches at compression weight of 250 mg/tablet. Tablets were evaluated of different quality control parameters as per USP. Results showed that both the process variables had positive effect on mechanical strength of tablets and negative effect on disintegration and dissolution rate. Granule prepared with highest level of binder concentration (15%) and highest granulation time (60 sec) resulted in tablets with highest crushing strength (11.8 kg), specific crushing strength (0.328 kg/mm2), tensile strength (0.208 kg/mm2), lowest value of friability (0.19%) and highest disintegration time (10.9 min), as predicted from granules characteristics on the basis of SeDeM-ODT expert system. Drug release from Trial-13 (processed under highest level of both process parameters) was also lower than rest of the trials. It is concluded from the study that quality characteristics of tablets can be predicted from granules characteristics using SeDeM-ODT expert system. Furthermore, SeDeM-ODT expert system can also be used for optimization of the process of high shear wet granulation.

scholarly journals Assessment of physicochemical properties and comparison of the dissolution profile of amoxicillin caplets

2020 ◽  
Vol 16 (2) ◽  
pp. 118-129
Author(s):  
Een Widiyasari ◽  
Teuku Nanda Saifullah Sulaiman
Keyword(s):  
Physicochemical Properties ◽  
Product Quality ◽  
Dosage Form ◽  
Reference Product ◽  
Immediate Release ◽  
Dissolution Profile ◽  
Type Ii ◽  
Dissolution Test ◽  
Disintegration Time ◽  
Similarity Factor

Background: Marketed drugs must meet the required standards to guarantee product quality. Amoxicillin is a generic compound marketed under various trademarks as copy drugs. Amoxicillin caplets are an immediate release dosage form of BCS class I. An essential aspect of evaluating copy drugs is to assess the equivalence for their treatment to the innovator drugs to ensure the safety and effectiveness of the circulating copy drugs. Objective: The study aims to evaluate the physicochemical properties and compare the dissolution profile of amoxicillin caplets available in the market. Methods: Five amoxicillin caplet products, four test products, and one reference product were tested for their physicochemical properties and dissolution. The dissolution test was carried out with a type II device at a speed of 75 rpm in 900 mL of media buffered at pH 1.2, 4.5, and 6.8 and at a temperature of 37 +/- 0.5degrees celcius. The dissolution profile was analyzed by comparing it with the similarity factor (f2) parameters. Results: Two of the four amoxicillin caplet products had a similar dissolution profile to the reference products, namely products A and B. Products C and D were dissimilar because f2 was lower than 50 at pH 4.5. The caplets tested had almost the same dimensions, and all caplets met the requirements for uniformity of content, hardness, disintegration time, and dissolution. Conclusion: Not all of the amoxicillin caplets in the market have a similar dissolution profile to the reference products. Keywords: caplets, amoxicillin, dissolution, similarity factor

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

scholarly journals Effect of solubility enhancers on the release of Carbamazepine from Hydrophilic Polymer based matrix tablet

2015 ◽  
Vol 13 (2) ◽  
pp. 167-173 ◽  
Author(s):  
Sharifa Sultana ◽  
Shimul Halder ◽  
AK Lutful Kabir ◽  
Abu Shara Shamsur Rouf
Keyword(s):  
Drug Release ◽  
Dissolution Rate ◽  
Release Rate ◽  
Release Profile ◽  
Matrix Tablets ◽  
Release Mechanism ◽  
Wet Granulation ◽  
Matrix Tablet ◽  
Solubility Enhancers ◽  
The Impact

In the present study, an attempt has been taken to evaluate the effect of sodium lauryl sulphate (SLS) and glyceryl mono stearate (GMS) as solubility enhancers on the release profile of a poorly soluble drug, carbamazepine. Matrix tablets of carbamazepine were prepared by wet granulation technique using hydrophilic polymers (10% of Methocel K15 MCR and 10% of Methocel K100LV CR) as release controlling agents. Varying amounts of SLS and GMS were used in six different formulations to observe the impact on the release rate and mechanism of drug release. The dissolution study of carbamazepine from these extended release matrix tablets was conducted for 24 hours using basket method in 900 ml distilled water as dissolution medium. The data obtained from the dissolution studies were explored and explained with the help of zero order, Higuchi, first order, Korsmeyer- Peppas and Hixson-Crowell equations. It was found that the dissolution rate of carbamazepine with the formulation containing SLS was higher than GMS containing formulation and increased concentration of SLS increasing the release rate. Where there was no SLS or smaller amount of SLS or GMS release rate was decreased. Formulation having equal ratio of SLS and GMS did not show the desire release profile. The drug release mechanism followed mainly super case II transport. These results clearly demonstrated that the dissolution rate, extent and mechanism of carbamazepine release could be changed by optimizing the amount of SLS and GMS in the tablet formulation. DOI: http://dx.doi.org/10.3329/dujps.v13i2.21894 Dhaka Univ. J. Pharm. Sci. 13(2): 167-173, 2014 (December)

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