Optimization Of Tablet Formulation Research Articles

Optimization of Tablet Formulations Containing Green Robusta Coffee Beans (Coffea canephora) Extract with Various Concentrations of Sodium Starch Glycolate As a Disintegrant

Chlorogenic acid, found in robusta green coffee beans, is an antidiabetic agent. It is made into robusta green coffee bean extract tablets which are varied with 3 concentrations of sodium starch glycolate (SSG) as a disintegrant. This paper aimed to determine the effect of variations in the concentration of sodium starch glycolate (4%, 6%, 8%) on the physical characteristics of the granules (particle size distribution, flow properties, angle of repose and compressibility) and tablet dosage characteristics, which include, hardness, friability, and disintegration time of robusta green coffee extract tablets. Robusta green coffee bean extract tablets were made with varying concentrations of sodium starch glycolate (4%, 6%, 8%) using the dry granulation method. The granule test parameters: flow properties test, compressibility test and particle size distribution test, were carried along with the tablet test parameters: hardness test, friability test and disintegration time test. Data were analyzed using the one Way-Anova. From the results of the study, it was found that the concentration of SSG did affect granule properties and tablet hardness. There was a significant difference in the friability test and disintegration time test.
 Keywords: sodium starch glycolate, disintegrant, robusta green coffee bean extract, tablet

Modulation of Drug Release from Natural Polymer Matrices by Response Surface Methodology: in vitro and in vivo Evaluation.

PurposeThe present work aimed at challenging the efficacy of natural gums, karaya and locust bean gum, as matrix-forming polymers for the formulation of sustained-release tablets of diltiazem, a model drug.MethodsCentral design composite was adopted for the formulation and optimization of tablet formulations. The two gums have been selected as independent variables. The dependent factors chosen were the amount of drug released in 1st hour (Y1), amount of drug released after 12 h (Y2), diffusion exponent (Y3), and time for half of the total drug released (T50%) (Y4). Wet granulation approach was used for the formulation of tablets. FT-IR, DSC, in vitro dissolution, swelling-erosion investigations, SEM, and stability studies were carried out.Results and DiscussionIt was evident that the release pattern from the prepared formulations was significantly influenced by the quantity of gum(s) in the tablet. FT-IR and DSC results confirm drug–polymer compatibility. Polynomial equations were used for the prediction of quantitative impact of independent factors at different levels on response variables. After ANOVA analysis, the significant factors were considered for constrained optimization to get the optimized formula. The optimized formula generated by the response surface methodology was evaluated both for in vitro and in vivo properties. The optimized formula and a sustained-release marketed product were subjected to in vivo studies in rabbits and the results of the t-test demonstrated insignificant variation in pharmacokinetic parameters among the two formulations, confirming that the prepared tablet showed sustained-release profile.ConclusionThe results indicated that karaya and locust bean gum can be effectively used to formulate sustained-release tablets.

Optimization of tablet formulation containing ginger dry extract

Abstract Introduction. Diabetes mellitus is one of the world’s most common diseases, therefore the development and introduction of new effective drugs for diabetes treatment into clinical practice is an important task for the health systems of many countries of the world. Aim. The aim of our work was to determine and substantiate the quantitative ratio of excipients for the development of the optimal composition of directly compressible ginger dry extract tablets. Materials and methods. To choose the optimal composition of tablets containing ginger dry extract, the effect of various quantitative ratios of the excipients Kollidon K30 and Neusilin UFL 2 on tablet mass pharmaceutical technical parameters, determined by established methods, was studied. For processing the experimental data, mathematical methods were used: design of experiment, regression analysis and a technique based on the theory of vector optimization. Results. The interrelation between factors that were studied and technological parameters of tablet mass and compressed tablets were analyzed using regression equations. Conclusions. The studies conducted allowed to chose the optimal composition of ginger dry extract tablets: ginger dry extract – 60%, Galen IQ 721 – 34.5%, Kollidon K30 – 3.5%, Neusilin UFL 2 – 1%, calcium stearate – 1%. The chosen tablet formulation is characterized by pharmaceutical technical parameters meeting the requirements of the European Pharmacopoeia and the State Pharmacopoeia of Ukraine.

Development and Optimization of Naproxen Sodium Controlled Release Tablets: QbD Approach

Abstract: Objectives: The aim of present study was to formulate and optimize Multi-unit Naproxen Sodium controlled release tablet by QbD approach. Controlled release dosage form for naproxen sodium was selected to reduce dosing frequency and gastrointestinal side effects of drug. Methods: Naproxen Sodium CR tablets were prepared by using wet granulation method by employing Quality by Design (QbD). This tablet was made by a mixture of a granulate having an immediate release with a granulate having a controlled release, in terms of the active ingredient. Eudragit RSPO and RLPO polymers were used to control the drug release. Optimization of tablet formulation was done using 23 factorial design to study the effect of concentration of Eudragit RSPO, Eudragit RLPO polymers and concentration of disintegrating agent i.e. crospovidone on disintegration time and f2 factor of drug released. Tablets were evaluated for thickness, hardness, friability, assay and drug release. Results: Optimized formulation shows controlled drug release profile upto 14 hrs. with disintegration time of 88 min. Conclusion: It was concluded that tablet formulation of Naproxen Sodium CR tablets employing QbD leads to a single dose per day in the management of rheumatoid arthritis and also concluded that Eudragit RLPO and Eudragit RSPO polymers can be successfully used to controlled drug release profile of tablet. Key words: Multi-unit-controlled release system, Quality by Design, Design of experiment, Eudragit RLPO, Eudragit RSPO.

Dependence of Friability on Tablet Mechanical Properties and a Predictive Approach for Binary Mixtures

To systematically assess the dependence of friability on tablet mechanical properties, compaction pressure, and tablet porosity. Several common excipients and their mixtures exhibiting diverse mechanical properties were analyzed. Tablet elastic modulus, hardness, brittleness, porosity, and tensile strength were determined using standard techniques and then were correlated to tablet friability both individually and as a group to derive a universal model. Viscoelastic starch exhibits the highest friability followed by brittle excipients (mannitol, DCPA, and LM) and then ductile excipients (HPC and MCC). A reasonably accurate model for predicting pharmaceutically relevant range of friability, up to 3%, of binary mixtures is presented based on friability of individual components. In addition, a multivariate model between friability and different mechanical parameters was developed, based on which the weight loss propensity of tablets may be predicted. The experimental findings and predictive model are useful for expedited development and optimization of tablet formulation using a minimum amount of API.

Optimization of poorly compactable drug tablets manufactured by direct compression using the mixture experimental design

The poor flowability and bad compressibility characteristics of paracetamol are well known. As a result, the production of paracetamol tablets is almost exclusively by wet granulation, a disadvantageous method when compared to direct compression. The development of a new tablet formulation is still based on a large number of experiments and often relies merely on the experience of the analyst. The purpose of this study was to apply experimental design methodology (DOE) to the development and optimization of tablet formulations containing high amounts of paracetamol (more than 70%) and manufactured by direct compression. Nineteen formulations, screened by DOE methodology, were produced with different proportions of Microcel ® 102, Kollydon ® VA 64, Flowlac ®, Kollydon ® CL 30, PEG 4000, Aerosil ®, and magnesium stearate. Tablet properties, except friability, were in accordance with the USP 28th ed. requirements. These results were used to generate plots for optimization, mainly for friability. The physical–chemical data found from the optimized formulation were very close to those from the regression analysis, demonstrating that the mixture project is a great tool for the research and development of new formulations.

Optimization of Tablet Formulations Containing

AbstractAn optimized direct compression tablet formulation of a conventional theophylline tablet was developed using the technique of response surface methodology and successive quadratic programming (SQP). The response surfaces were obtained from fitting data generated from a secondorder uniformprecision rotatable hexagonal experimental design. The tablet formulation was optimized for mean in vitro dissolution time using disintegration time, ejection force, friability and hardness, as constraints within the experimental region by the SQP technique. The response surface model was validated by preparing and evaluating the predicted formulation. The characteristics of the tablet formulation were analyzed by principal component analysis. Sensitivity analysis for the optimal solution was performed for each constraint, while all remaining constraints were held constant. The robustness of the response surface model was evaluated by simulation for error in the compression force values.

Optimization of Tablet Formulations Based on Starch/Lactose Granulations for Use in Tropical Countries

AbstractSeveral granulations consisting of α-lactose monohydrate 200 mesh and native starch (corn, potato, rice or tapioca) were prepared. The influence of starch concentration, storage temperature and relative humidity on the physical properties of the tablets prepared from these granulations was estimated. Two granulations, which resulted in tablets with adequate initial values of crushing strength and disintegration time and with an acceptable physical stability were selected as standard granulations. The selected standard granulations were evaluated by incorporating a drug (diazepam, 2 mg or mebendazole, 100 mg). The tablet properties were determined one day after preparation. The crushing strength, the disintegration time and the microbiological quality were also measured after storage under tropical conditions. Both selected formulations proved to be adequate for the preparation of tablets by wet granulation, suitable for use in tropical countries.