scholarly journals Understanding the formulation variables of orodispersible tablets containing simvastatin solid dispersion using Box-Behnken design

2012 ◽  
Vol 2 (1) ◽  
pp. 7
Author(s):  
Ahmed Abd Elbary ◽  
Howida K. Ibrahim ◽  
Balquees S. Hazaa
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Magnesium Stearate ◽  
Stability Study ◽  
Disintegration Time ◽  
Box Behnken Design ◽  
Orodispersible Tablets ◽  
Formulation Variables

Simvastatin is a well established oral antihypercholesterolemic agent. This study aimed to formulate simvastatin as orodispersible tablets. The drug was incorporated as a solid dispersion using Pluronic® F68 as carrier. Croscarmellose Na was used as superdisintegrant, microcrystalline cellulose as filler, PVP K-30 as binder and 1:1 magnesium stearate/talc mixture as lubricant. Box- Behnken design was adapted to explore the main and interaction effects of three independent formulation variables on the prepared tablets, namely superdisintegrant concentration (X1), lubricant mixture concentration (X2), and binder concentration (X3). A total of 13 tablet formulations were fabricated in addition, to two replicates of the center point to assess variability and experimental error. The selected dependant variables were the<em> in vitro</em> and <em>in vivo</em> disintegration times, dissolution rate at 4 min, and dissolution efficiency after 30 min. Wetting time, drug content, hardness and friability were also evaluated. Tablet formula, composing of 12% superdisintegrant, 2% lubricant mixture and 3% binder, showed the highest dissolution rate with an acceptable disintegration time (43 sec), hardness, and friability and was chosen as the best formula. An accelerated stability study was conducted for 6 months at 40°C/75% RH. Results showed no significant changes in any of the tested parameters.

Optimization and Evaluation of Orodispersible Solid Dispersion Tablet of Ketotifen Fumarate

2021 ◽  
pp. 3610-3616
Author(s):  
Zeina D Salman
Keyword(s):  
Dissolution Rate ◽  
Solid Dispersion ◽  
Solid Dispersions ◽  
Fusion Method ◽  
Disintegration Time ◽  
Solubility Study ◽  
Ketotifen Fumarate ◽  
Orodispersible Tablets

The present study was aimed to integrate the developed and optimized ketotifen fumarate dispersion into Orodispersible tablets formulations, to enhance the dissolution rate and bioavailability aspects of the drug. Ketotifen fumarate solid dispersion was prepared using different concentrations of poloxamer 407via solvent evaporation and fusion method. Solubility study, x-ray diffraction (XRD), scanning electron microscopy (SEM), Fourier transform infrared spectroscopy (FTIR) and other investigations were done. Ten formulations of the optimum dispersed ketotifen fumarate Orodispersible tablets were prepared with various superdisintegrants, the results of in vitro - in vivo tests revealed that, the dispersion of the drug in the polymer considerably enhanced the solubility, the batch (Fsd 3) prepared by fusion method showed increased the solubility as ~2-fold compared with a pure drug. FTIR spectra, SEM and XRD data, showed amorphrization of ketotifen fumarate, which explains the better dissolution rate of the drug from its solid dispersions. Formulation F1 containing 15%w/w of crospovidone was showed in vitro- in vivo disintegration time (17 sec., 15 sec. respectively) and percent of drug dissolved in 2 min. was 90.04%, proved to be the optimum formulation, which is required for obtaining rapidly disintegrating tablets. The solubility of the drug had increased, and the resultant orodispersible tablets can be considered as a promising dosage form to achieve better patient compliance.

Formulation and Evaluation of Orodispersible Tablets Containing Taste Masked Mirabegron Resinate

2021 ◽  
pp. 4736-4742
Author(s):  
Sarika S. Malode ◽  
Milind P. Wagh
Keyword(s):  
Overactive Bladder ◽  
Bitter Taste ◽  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Dissolution Time ◽  
Disintegration Time ◽  
Orodispersible Tablets ◽  
Weight Variation

The objective of present work was to develop taste masked orodispersible tablets of mirabegron. Mirabegron is beta 3 adrenoceptor agonist used to treat overactive bladder. Overactive bladder (OAB) is defined as a symptom syndrome showing feeling of urgency to urinate, typically accompanied by frequent daytime and nocturnal urination, in the absence of proven infection or other obvious pathology. Over active bladders are generally common in geriatrics. Moreover, this drug has a very strong bitter taste. Frequent dosing requires frequent water intake, which further aggregates the condition of over active bladder and bitter taste of drug affects patient compliance. Hence a need arises to mask the bitter taste for development of an ODT which does not require consuming water with every dosage. In this work, the bitter taste of mirabegron was masked by forming a complex with an ion exchange resin tulsion 344. The drug resin complexation process was optimized for resin activation, drug: resin ratio, soaking time and stirring time. In –vitro release studies revealed complete drug elution from the complex within 10 minutes in pH 1.2 buffer. The taste-masked complex was then formulated into palatable orodispersible tablets using a direct compression approach by use of superdisintegrants to achieve a rapid disintegration. The tablets were evaluated for weight variation, hardness, friability, drug content, wetting time, In- vivo disintegration time and in-vitro dissolution time.

TASTE MASKING OF OXYBUTYNIN CHLORIDE USING LIPID EXCIPIENTS AND FORMULATION AS ORODISPERSIBLE TABLETS FOR GERIATRIC POPULATION

INDIAN DRUGS ◽  
2013 ◽  
Vol 50 (10) ◽  
pp. 39-46
Author(s):  
V Prakash ◽  
◽  
L. Keshri ◽  
V. Sharma ◽  
K. Pathak
Keyword(s):  
In Vitro Release ◽  
In Vitro Dissolution ◽  
Taste Masking ◽  
Dissolution Time ◽  
Disintegration Time ◽  
Geriatric Population ◽  
Orodispersible Tablets ◽  
Lipid Excipients

The aim of the present study was to mask the bitter taste of oxybutynin chloride by lipid excipients and to develop its fast disintegrating tablet. For this purpose, a blend of two lipids, glyceryl behenate and glyceryl palmitostearate was utilized for taste masking by solvent evaporation method. The evaporation of solvent was accomplished by freeze drying and taste masked granules were characterized for their micromeritic and rheological properties. The state of dispersion was analyzed by SEM and DSC. Orodispersible tablets were then formulated (F1- F6) using Polyplasdone XL as extragranular superdisintegrant and evaluated for hardness, disintegration time, in vitro dissolution time and in vivo disintegration time. Results indicated that the formulation F6 exhibited minimum in vivo disintegration time of 8 sec with effective taste masking. In vitro release analysis indicated %DE10 and %DE25 of 51.48 and 76.53 respectively. Conclusively, taste masked orodispersible formulation of oxybutynin chloride was developed that could be beneficial for geriatric population.

scholarly journals Enhanced Oral Bioavailability of Celecoxib Nanocrystalline Solid Dispersion based on Wet Media Milling Technique: Formulation, Optimization and In Vitro/In Vivo Evaluation

Pharmaceutics ◽  
2019 ◽  
Vol 11 (7) ◽  
pp. 328 ◽  
Author(s):  
Zhuang Ding ◽  
Lili Wang ◽  
Yangyang Xing ◽  
Yanna Zhao ◽  
Zhengping Wang ◽  
...  
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Solid Dispersion ◽  
Oral Bioavailability ◽  
Stability Study ◽  
Sprague Dawley ◽  
Scanning Calorimetry ◽  
In Vivo Evaluation

Celecoxib (CLX), a selective COX-2 inhibitor, is a biopharmaceutics classification system (BCS) class II drug with its bioavailability being limited by thepoor aqueoussolubility. The purpose of this study was to develop and optimize CLX nanocrystalline(CLX-NC) solid dispersion prepared by the wet medium millingtechnique combined with lyophilizationto enhance oral bioavailability. In formulation screening, the resulting CLX-NC usingpolyvinylpyrrolidone (PVP) VA64 and sodiumdodecyl sulfate (SDS) as combined stabilizers showed the minimum particle size and a satisfactory stability. The formulation and preparation processwere further optimized by central composite experimentaldesign with PVP VA64 concentration (X1), SDS concentration (X2) and milling times (X3) as independent factors and particle size (Y1), polydispersity index (PDI, Y2) and zeta potential (Y3) as response variables. The optimal condition was determined as a combination of 0.75% PVP VA64, 0.11% SDS with milling for 90 min.The particle size, PDI and zeta potential of optimized CLX-NC were found to be 152.4 ± 1.4 nm, 0.191 ± 0.012 and −34.4 ± 0.6 mV, respectively. The optimized formulation showed homogeneous rod-like morphology as observed by scanning electron microscopy and was in a crystalline state as determined by differential scanning calorimetry and powder X-ray diffraction. In a storage stability study, optimized CLX-NC exhibited an excellent physical stability during six months’ storage at both the refrigeration and room conditions. In vivo pharmacokinetic research in Sprague-Dawley ratsdisplayed that Cmax and AUC0–∞ of CLX-NC were increased by 2.9 and 3.1 fold, compared with physical mixture. In this study, the screening and optimizing strategy of CLX-NC formulation represents a commercially viable approach forenhancing the oral bioavailability of CLX.

Optimization of Aceclofenac Solid Dispersion Using Box-Behnken Design: in-vitro and in-vivo Evaluation

2014 ◽  
Vol 11 (3) ◽  
pp. 380-391 ◽  
Author(s):  
Furqan Maulvi ◽  
Vaishali Thakkar ◽  
Tejal Soni ◽  
Tejal Gandhi
Keyword(s):  
Solid Dispersion ◽  
In Vivo Evaluation ◽  
Box Behnken Design

scholarly journals Formulation and Optimization of Orodispersible Tablet of Loratadine Using Box Behnken Design

2019 ◽  
Vol 9 (4-A) ◽  
pp. 86-94
Author(s):  
Aliasgar Kundawala ◽  
Pratik Patel ◽  
Khushbu Chauhan ◽  
Anjali Desai ◽  
Dhwani Kapadia
Keyword(s):  
Drug Release ◽  
Solid Dispersion ◽  
Angle Of Repose ◽  
Drug Dissolution ◽  
Taste Masking ◽  
Disintegration Time ◽  
Box Behnken Design ◽  
Orodispersible Tablets ◽  
Orodispersible Tablet ◽  
Wetting Time

In present study Orodispersible tablets (ORDT) of Loratadine were prepared and optimized. Solid dispersion of Loratadine- β cyclodextrin complex were prepared and used in preparation of Orodispersible tablets. Various super-disintegrating agent like Cross carmellose sodium, Cross povidone and Kyron T-314 were employed for faster disintegrating effect. The 24 factorial and Box-Behnken design were utilized to optimize the tablet formulation. The Orodispersible tablet of Loratadine was optimized by Box Behnken Design, where concentrations Kyron T-314, CRP and Pearlitol SD200 were employed and its effect on Disintegration time (DT), Wetting time (WT) and % drug release at 20 min (Q20) was evaluated. Precompression parameters like angle of repose, bulk density, % compressibility, Hausner’s ratio was studies. The different batches of Orodispersable tablets were prepared and evaluated for disintegration time, friability, wetting time and drug release studies. Different batches prepared showed disintegration time in the range of 23 ± 2.52 to 59 ± 2.64, wetting time in between 27± 0.57 to 66.3 ± 3.4, drug release (Q 20) in between 86.1 ± 0.6 to 96.7 ± 0.4 in 20 min., friability less than 1 % and hardness 3.4 to 4.2 Kg/cm2. The optimized formula when compared with marketed product it showed faster disintegration time and rapid drug dissolution in phosphate buffer 6.8. The solid dispersion of Loratadine not only helped improve in solubility but may also help in taste masking. Keywords: Orodispersible tablets, Loratadine, β cyclodextrin Solid dispersion

scholarly journals Use of Box–Behnken design for optimization of compounded medication: acyclovir capsules report

2021 ◽  
Vol 5 (1) ◽  
pp. 59-67
Author(s):  
Suelen Da Silva Reis ◽  
Valdemir Da Silva Quintanilha Junior ◽  
Gabriella Da Silva Boto ◽  
Thalita Martins Da Silva ◽  
Elizabeth Valverde Macedo ◽  
...  
Keyword(s):  
Numerical Optimization ◽  
Magnesium Stearate ◽  
In Vitro Dissolution ◽  
Average Weight ◽  
Box Behnken Design ◽  
Drug Content ◽  
Weight Test ◽  
Pharmacopoeial Specifications ◽  
Formulation Variables

Campus compounding pharmacies play an important role in public health. Herpes simplex is one of the most common viral diseases in humans, which generates a great demand for acyclovir capsules in compounding pharmacy. It is well known that the formulation's components influence the effectiveness of the drug. The objective of this study is to show the applicability of Box-Behnken design in optimization of a compounded formulation and to evaluate the effect of excipients on dissolution and drug content in acyclovir 200 mg capsules produced at UFF´s University Pharmacy (FAU). The formulations were prepared and evaluated for average weight test, uniformity of dosage units and in vitro dissolution, while meeting pharmacopoeial specifications. A statistical analysis showed that sodium starch glycolate, Aerosil®, influences drug content and dissolution results. Magnesium stearate shows no influence on the dissolution at different concentrations but influences the assay results. A numerical optimization was applied to adjust the formulation variables based on the foresaid responses, accomplishing the best formulation that will be prepared and dispensed at FAU upon medical prescription.

FORMULATION AND EVALUATION OF THYROID HORMONE(T3) IMMEDIATE RELEASE TABLETS

2021 ◽  
Vol 1 (10) ◽  
pp. 383-388
Author(s):  
Farghana Begam ◽  
Rajalakshmi A. N ◽  
Padmapriya S
Keyword(s):  
Thyroid Hormone ◽  
Chemical Characterization ◽  
Immediate Release ◽  
Magnesium Stearate ◽  
Stability Study ◽  
Direct Compression ◽  
Maize Starch ◽  
Disintegration Time ◽  
Study Results

The study was aimed to formulate and evaluate Thyroid hormone (T3) immediate release tablets of a model Reference Listed Drug (RLD). The objective was to develop a cost effective immediate release tablet formulation and to optimize the formula in product development same that of the reference product. The ingredients used were API (thyroid hormone), lactose monohydrate (diluent), acacia (binder), maize starch (disintegrant), sodium chloride (alkalinizing agent) and magnesium stearate (lubricant). The concentration of maize starch and magnesium stearate were altered to reach the objective. Totally five formulations (F1 - F5) were prepared by direct compression method. The plan of work involved involved in the study was1 Selection of drug and excipients, 2Physico–chemical characterization and drug identification, 3Preformulation parameters of the drug, 4Pre–compression parameters for the tablet blend, 5Formulation and development of the tablet dosage form, 6Post compression parameters of the tablet and 7Stability study. The stability studies were performed as per ICH guidelines. Among all the formulations F5 was found to be the best as it showed better results than the other formulations. In vitro disintegration time and percentage drug release results shown satisfactory results. Stability study results showed no significant changes in the formulation. Keywords: Thyroid hormone (T3), Immediate release tablets, Direct compression, Dissolution.

scholarly journals DEVELOPMENT AND CHARACTERIZATION OF ORODISPERSIBLE TABLETS OF PROPRANOLOL HYDROCHLORIDE USING CALCIUM CROSS-LINKED CASSIA FISTULA GUM AND CROSS CARMELLOSE SODIUM

2020 ◽  
pp. 160-169
Author(s):  
KULJIT SINGH ◽  
SHAILESH SHARMA
Keyword(s):  
Propranolol Hydrochloride ◽  
Cassia Fistula ◽  
Disintegration Time ◽  
Dry Granulation ◽  
Orodispersible Tablets ◽  
Absorption Studies ◽  
Cotton Candy ◽  
Drug Polymer Interaction

Objective: The present investigation was aimed towards developing calcium crosslinked derivative of carboxymethylated cassia fistula gum and crosscarmellose sodium based orodispersible tablets (ODTs) of propranolol hydrochloride for enhancing the bioavailability and efficacy. Methods: Orodispersible tablets (ODTs) of propranolol hydrochloride was formulated using natural (a carboxymethylated derivative of cassia fistula gum) and synthetic polymer (crosscarmellose sodium) by wet and dry granulation, lyophilization and cotton candy methods and then finally compressed by direct compression. The prepared ODTs were evaluated for several parameters such as hardness, friability, in vitro disintegration time, in vitro drug release. In vivo and stability studies were carried out on optimized formulation coding PC1. Results: Drug polymer interaction were judged by FT-IR, DSC and XRD. The optimized formulation coding PC1 prepared by cotton candy process containing 2.5% w/w of crosslinked cassia fistula gum has the least disintegration time (18.9±0.4s), weeting time (12.5±0.8s) and relased the drug of 88.2% within 10 min in contrast to croscarmellose sodium. In vivo absorption studies revealed that same formulation has Cmax (µg/ml) 2.13±0.73, tmax (h) 0.21±0.17 and (µg ml-1 h-1) 14.33±1.59. Conclusion: This research manuscript clearly shows the successful development of the ODTs loaded with an antihypertensive drug, namely propranolol hydrochloride. The formulation developed by cotton candy process utilizing crosslinked cassia fistula gum as a natural superdisintegrant in contrast to other existing techniques can be a best option over synthetic superdisintegrant i.e. crosscarmellose sodium. The prepared ODTs was enhanced the absorption rate by lowering tmax, which inturn enhance the bioavailability and the efficacy of drug.

scholarly journals Developing and evaluation of orodispersible tablets containing caffeine

2021 ◽  
Vol 14 (1) ◽  
pp. 34-40
Author(s):  
Robert-Alexandru Vlad ◽  
◽  
Elena-Beatrice Trifan ◽  
Paula Antonoaea ◽  
Emőke-Margit Rédai ◽  
...  
Keyword(s):  
Point Of View ◽  
Direct Compression ◽  
Active Pharmaceutical Ingredients ◽  
European Pharmacopoeia ◽  
Disintegration Time ◽  
Pharmaceutical Ingredients ◽  
Sodium Starch Glycolate ◽  
Orodispersible Tablets ◽  
Formulation Variables

Starting from the premise that a reduced number of active pharmaceutical ingredients (APIs) are used to treat hypotension, the aim of this study consisted of developing new formulations of caffeine-orodispersible tablets (CAFODTs). The formulation variables were the type of disintegrant and its concentration. The CAF-ODTs were prepared by direct compression, (CAF1, CAF2 and, CAF3) each of them containing 100 mg of CAF / tablet. The proposed formulations were analyzed from a pharmacotechnical point of view. For the formulations developed the tablets’ physical appearance, resistance to crushing, friability, disintegration behaviour, and the in vitro caffeine release were evaluated. White tablets, with a resistance to crushing decreasing in the following order CAF1 > CAF2 > CAF3 were obtained. The friability test showed that all the formulations are respecting the in-force European Pharmacopoeia (Ph. Eur. 10) requirements with values less than 1 %. The disintegration time for all three formulations was less than 180 seconds, the smallest time being registered in the case of CAF2 formulation, where Sodium Starch Glycolate (SSG) was used as a disintegrant (24-30 s, as a result of the different methods used. Through the in vitro releasing study, it was observed that over 99.9 % caffeine was released from all three analyzed formulations. By investigating the amount of caffeine released after 1 minute, it can be noticed that the largest amount released was recorded in CAF2 formulations, where SSG was used as a disintegrant. Compared to CAF2, the amount of CAF released was reduced to half, after the first five minutes for CAF1 formulation, where sodium croscarmellose was used, and ten times lower in the case of CAF3 where no disintegrant was used. Based on the results obtained we can conclude that all three formulations are respecting the pharmacotechnical in-force officinal requirements. The presence of SSG in the CAF2 formulation led to obtaining tablets with a reduced disintegration time in comparison to the other two formulations proposed in this study.

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