Role of Aminated derivatives of Natural Gum in Release Modulating Matrix Systems of Losartan Potassium: Optimization of Formulation using Box-Behnken Design

2021 ◽  
pp. 73-84
Author(s):  
Shankar B. Kalbhare ◽  
Vivek Kumar Redasani ◽  
Mandar J. Bhandwalkar ◽  
Rohit K. Pawar ◽  
Avinash M. Bhagwat
Keyword(s):  
Response Surface Methodology ◽  
Response Surface ◽  
Research Work ◽  
In Vitro Release ◽  
Kinetic Equations ◽  
Matrix Tablets ◽  
Losartan Potassium ◽  
Burst Release ◽  
Fenugreek Gum

The aim of the present research work was to systemically device a model of factors that would yield an optimized release modulating dosage form of an anti-hypertensive agent, losartan potassium, using response surface methodology by employing a 3-factor, 3-level Box-Behnken statistical design. Independent variables studied were the amount of the release retardant polymers – aminated fenugreek gum (X1), aminated tamarind gum (X2) and aminated xanthan gum (X3). The dependent variables were the burst release in 15 min (Y1), cumulative percentage release of drug after 60 min (Y2) and hardness (Y3) of the tablets with constraints on the Y2 = 31–35%. Statistical validity of the polynomials was established. In vitro release and swelling studies were carried out for the optimized formulation and the data were fitted to kinetic equations. The polynomial mathematical relationship obtained Y2=32.91-2.29X1-5.68X2-0.97X3+0.20X1X3-0.005X2X3-0.92X12-1.89X22 explained the main and quadratic effects, and the interactions of factors influencing the drug release from matrix tablets. The adjusted (0.9842) and predicted values (0.9600) of r2 for Y2 were in close agreement. Validation of the optimization study indicated high degree of prognostic ability of response surface methodology. The Box-Behnken experimental design facilitated the formulation and optimization of release modulating matrix systems of losartan potassium.

scholarly journals Optimization and Formulation of Fucoxanthin-Loaded Microsphere (F-LM) Using Response Surface Methodology (RSM) and Analysis of Its Fucoxanthin Release Profile

Molecules ◽  
2019 ◽  
Vol 24 (5) ◽  
pp. 947 ◽  
Author(s):  
Irwandi Jaswir ◽  
Dedi Noviendri ◽  
Muhammad Taher ◽  
Farahidah Mohamed ◽  
Fitri Octavianti ◽  
...  
Keyword(s):  
Response Surface Methodology ◽  
Surface Morphology ◽  
Response Surface ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Double Emulsion ◽  
Release Profile ◽  
Burst Release ◽  
Good Surface

Fucoxanthin has interesting anticancer activity, but is insoluble in water, hindering its use as a drug. Microencapsulation is used as a technique for improving drug delivery. This study aimed to formulate fucoxanthin-loaded microspheres (F-LM) for anticancer treatment of H1299 cancer cell lines and optimize particle size (PS) and encapsulation efficiency (EE). Using response surface methodology (RSM), a face centered central composite design (FCCCD) was designed with three factors: Polyvinylalcohol (PVA), poly(d,l-lactic-co-glycolic acid) (PLGA), and fucoxanthin concentration. F-LM was produced using a modified double-emulsion solvent evaporation method. The F-LM were characterized for release profile, release kinetics, and degradation pattern. Optimal F-LM PS and EE of 9.18 µm and 33.09%, respectively, with good surface morphology, were achieved from a 0.5% (w/v) PVA, 6.0% (w/v) PLGA, 200 µg/mL fucoxanthin formulation at a homogenization speed of 20,500 rpm. PVA concentration was the most significant factor (p < 0.05) affecting PS. Meanwhile, EE was significantly affected by interaction between the three factors: PVA, PLGA, and fucoxanthin. In vitro release curve showed fucoxanthin had a high burst release (38.3%) at the first hour, followed by a sustained release stage reaching (79.1%) within 2 months. Release kinetics followed a diffusion pattern predominantly controlled by the Higuchi model. Biodegradability studies based on surface morphology changes on the surface of the F-LM, show that morphology changed within the first hour, and F-LM completely degraded within 2 months. RSM under FCCCD design improved the difference between the lowest and highest responses, with good correlation between observed and predicted values for PS and EE of F-LM.

scholarly journals Formulation and In Vitro Evaluation of Sustained Release Matrix Tablets of Venlafaxine

2017 ◽  
Vol II (I) ◽  
pp. 10-24
Author(s):  
Zubair Anwar ◽  
Tanveer Ahmed Khan ◽  
Muhammad Farhan Sohail ◽  
Maryam Anwar
Keyword(s):  
Sustained Release ◽  
Hydroxypropyl Methylcellulose ◽  
In Vitro Release ◽  
Matrix Tablets ◽  
Wet Granulation ◽  
Burst Release ◽  
Sustained Effect ◽  
Release Data ◽  
Drug Studies

Sustained release matrix tablets of venlafaxine were formulated using synthetic polymers (ethylcellulose & hydroxypropyl methylcellulose). Six (06) different batches of matrix tablets of venlafaxine (dose 75 mg) were prepared by the wet granulation method. Polymers were used alone or in combination. The physical properties of compressed tablets were evaluated. In vitro release drug studies were performed in phosphate buffer at pH 6.8 over 24 hours. The drug release data fitted well to the First-order (R2 = 0.9725 � 0.9900). The n value obtained for most batches ranged from 0.523 to 0.946 indicates that the drug is released through an anomalous or non�Fickian transport. Results revealed that the combination of ethyl cellulose (EC) and hydroxypropyl methylcellulose produced a sustained effect compared to hydroxypropyl methylcellulose alone. Formulation F6 containing single polymer (EC) showed the highest control over initial burst release, and extended-release of the drug continued up to 16 hours.

scholarly journals Studies on Bio-adhesion of Matrix Tablets: I. Release Profile of Theophylline Anhydrous

1970 ◽  
Vol 5 (1) ◽  
pp. 33-37
Author(s):  
Md. Shamsuddin ◽  
Parvin Akter ◽  
Md. Ziaur Rahman Khan ◽  
Jakir Ahmed Chowdhury ◽  
Md. Selim Reza
Keyword(s):  
Controlled Release ◽  
Mucous Membrane ◽  
Xanthan Gum ◽  
In Vitro Release ◽  
Gastric Fluid ◽  
Release Profile ◽  
Matrix Tablets ◽  
Drug Dissolution ◽  
Burst Release

Controlled release matrix tablets of theophylline anhydrous were designed with different types of bioadhesive polymers. HPMC 15 cps and 50 cps, Na-CMC, Gelatin, Xanthun gum and PVP K-30 were selected to formulate matrix tablets. Tablets of theophylline were prepared by direct compression method and were subjected to in vitro drug dissolution for 8 hrs in a gastric fluid media by using thermal shaker with a shaking speed of 50 rpm at a temperature of 37 ± 0.5°C. The in vitro release study as well as retention time of bioadhesive tablets on mucous membrane were investigated to develop a bioadhesive polymer based controlled release delivery system and to evaluate the performance of such delivery device. Na-CMC, HPMC and Xanthan gum based tablets showed greater bio-adhesive strength where as gelatin and PVP K-30 based tablets showed poor bioadhesive strength. Na-CMC and Xanthun gum loaded tablets were not discharged from the mucous membrane and these tablets were fully dissolved in the gastric fluid. Xanthan gum, Na-CMC and HPMC based formulation showed nearly zero-order release. On the contrary, gelatin and PVP K-30 based formulation showed a burst release within one hour of dissolution. Key words: Bio-adhesion, Release profile, theophylline anhydrous. Dhaka Univ. J. Pharm. Sci. Vol.5(1-2) 2006 The full text is of this article is available at the Dhaka Univ. J. Pharm. Sci. website

scholarly journals Preparation and in vitro release kinetics of ivermectin sustained-release bolus optimized by response surface methodology

PeerJ ◽  
2018 ◽  
Vol 6 ◽  
pp. e5418 ◽  
Author(s):  
Xiangchun Ruan ◽  
Xiuge Gao ◽  
Ying Gao ◽  
Lin Peng ◽  
Hui Ji ◽  
...  
Keyword(s):  
Response Surface Methodology ◽  
Sustained Release ◽  
Response Surface ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Information Criterion ◽  
Quadratic Model ◽  
Dissolution Time ◽  
Release Mechanism

Sustained-release formulations of ivermectin (IVM) are useful for controlling parasitic diseases in animals. In this work, an IVM bolus made from microcrystalline cellulose (MCC), starch and low-substituted hydroxypropyl cellulose (LS-HPC) was optimized by response surface methodology. The bolus was dissolved in a cup containing 900 mL of dissolution medium at 39.5 °C, under with stirring at 100 rpm. A quadratic model was formulated using analysis of variance according to the dissolution time. The optimized formulation of the bolus contained 8% MCC, 0.5% starch, and 0.25% LS-HPC. The length, width, and height of the prepared IVM bolus were 28.12 ± 0.14, 16.1 ± 0.13, and 13.03 ± 0.05 mm, respectively. The bolus weighed 11.4842 ± 0.1675 g (with a density of 1.95 g/cm3) and contained 458.26 ± 6.68 mg of IVM. It exhibited in vitro sustained-release for over 60 days, with a cumulative amount and percentage of released IVM of 423.72 ± 5.48 mg and 92.52 ± 1.20%, respectively. The Korsmeyer–Peppas model provided the best fit to the dissolution release kinetics, exhibiting anR2value close to 1 and the lowest Akaike Information Criterion among different models. The parametern(0.5180) of the Korsmeyer–Peppas model was between 0.45 and 0.89. It was demonstrated that the release mechanism of the IVM bolus followed a diffusive erosion style.

scholarly journals Formulation and in vitro evaluation of mucoadhesive controlled release matrix tablets of flurbiprofen using response surface methodology

2014 ◽  
Vol 50 (3) ◽  
pp. 493-504 ◽  
Author(s):  
Ikrima Khalid ◽  
Mahmood Ahmad ◽  
Muhammad Usman Minhas ◽  
Muhammad Sohail
Keyword(s):  
Response Surface Methodology ◽  
Controlled Release ◽  
Drug Release ◽  
Response Surface ◽  
Release Profile ◽  
Matrix Tablets ◽  
In Vitro Dissolution ◽  
Direct Compression ◽  
Response Variables

The objective of the current study was to formulate mucoadhesive controlled release matrix tablets of flurbiprofen and to optimize its drug release profile and bioadhesion using response surface methodology. Tablets were prepared via a direct compression technique and evaluated for in vitro dissolution parameters and bioadhesive strength. A central composite design for two factors at five levels each was employed for the study. Carbopol 934 and sodium carboxymethylcellulose were taken as independent variables. Fourier transform infrared (FTIR) spectroscopy studies were performed to observe the stability of the drug during direct compression and to check for a drug-polymer interaction. Various kinetic models were applied to evaluate drug release from the polymers. Contour and response surface plots were also drawn to portray the relationship between the independent and response variables. Mucoadhesive tablets of flurbiprofen exhibited non-Fickian drug release kinetics extending towards zero-order, with some formulations (F3, F8, and F9) reaching super case II transport, as the value of the release rate exponent (n) varied between 0.584 and 1.104. Polynomial mathematical models, generated for various response variables, were found to be statistically significant (P<0.05). The study also helped to find the drug's optimum formulation with excellent bioadhesive strength. Suitable combinations of two polymers provided adequate release profile, while carbopol 934 produced more bioadhesion.

scholarly journals Development of biodegradable scaffolds loaded with vancomycin micropartricles for the treatment of osteomyelitis

2019 ◽  
Vol 10 (4) ◽  
pp. 2612-2621 ◽  
Author(s):  
Souvik chakraborty ◽  
Gowda D V ◽  
Vishal Gupta N
Keyword(s):  
Evaluation Studies ◽  
Research Work ◽  
In Vitro Release ◽  
Double Emulsion ◽  
Initial Time ◽  
Burst Release ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Biodegradable Scaffolds

In this present research work, the development of biodegradable scaffolds loaded with Vancomycin micropartricles was carried out for the treatment of Osteomyelitis. Characterization Vancomycin Loaded microparticles and evaluation of the microparticles loaded scaffolds and also to carry out In-vitro release studies. Vancomycin hydrochloride microparticles were prepared with the help of double emulsion method. HPMC and Polaxomer 407 has been taken as the main polymers for the preparation of the microparticles. Chitosan was taken as the major polymer for the preparation of scaffolds for its greater biocompatibility and biodegradability. The preparation was done with the help of the solvent casting method. The formulation was taken for further characterization and evaluation studies. Fourier-Transform Infrared Spectroscopy and Differential scanning calorimetry were carried out for the pure vancomycin drug, and the chitosan polymer X-ray diffraction was carried out to check the crystallinity of the prepared scaffolds. The particle size, zeta potential and polydispersity index for vancomycin loaded microparticles were found to be 577.0±102.5 nm, 1624 mv and 0.254. The maximum and sustained release rate of the drug was found to be 95.6±0.478, at 16th Hr. By taking all the reports, a conclusion can be drawn that, the formulated VLM biodegradable scaffolds will show burst release at the initial time of administration, which is essential for the wound healing activity and will be sustained throughout the process of treatment of osteomyelitis.

scholarly journals Release Profile of Losartan Potassium from Formulated Sustained Release Matrix Tablet

2015 ◽  
Vol 16 (2) ◽  
pp. 177-183
Author(s):  
Md Ziaur Rahman ◽  
Sayed Koushik Ahamed ◽  
Sujan Banik ◽  
Mohammad Salim Hossain
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
In Vitro Release ◽  
Methyl Cellulose ◽  
Matrix Tablets ◽  
Losartan Potassium ◽  
Matrix Tablet ◽  
Vitro Release

The present study was undertaken to develop sustained release (SR) matrix tablets of Losartan potassium, an angiotensin-II antagonist for the treatment of hypertension. The tablets were prepared by direct compression method along with Kollidon SR and Methyl Cellulose as release retardant polymers. The evaluation involves two stages- the physical properties studies of tablets and in vitro release kinetics assessment. The USP paddle method was selected to perform the dissolution test and 900 ml phosphate buffer of pH 6.8 was used as dissolution medium at 50 rpm at 370C. The release kinetics were analyzed. All the formulations followed Higuchi release kinetics. When the release data was plotted into Korsmeyer-Peppas equation, then it was confirmed that F-1, F-2, F-3, F-4 and F-5 exhibited non-fickian type drug release whereas F-6 exhibited fickian type drug release from the tablet matrix. The in-vitro release studies revealed that the formulation F-2 can be taken as an ideal or optimized formulation of sustained release tablets for 24 hours release as it fulfills all the requirements for sustained release tablet. Furthermore, when the tablets were preheated at different temperature (300C, 450C, 600C) before dissolution they showed decrease in drug release compared with ambient temperature DOI: http://dx.doi.org/10.3329/bpj.v16i2.22301 Bangladesh Pharmaceutical Journal 16(2): 177-183, 2013

scholarly journals APPLICATION OF RESPONSE SURFACE METHODOLOGY IN OPTIMIZATION OF PACLITAXEL LIPOSOMES PREPARED BY THIN FILM HYDRATION TECHNIQUE

2018 ◽  
Vol 10 (2) ◽  
pp. 62
Author(s):  
Amol A. Tatode ◽  
Arun T. Patil ◽  
Milind J. Umekar
Keyword(s):  
Thin Film ◽  
Response Surface Methodology ◽  
Response Surface ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Regression Equations ◽  
Independent Variables ◽  
32 Factorial Design ◽  
Two Parameters

Objective: The present investigation was aimed to optimize the formula of paclitaxel-loaded liposomes (PTL) by using the application of response surface methodology (RSM).Methods: Paclitaxel-loaded liposome (PTL) was optimized by response surface methodology based on two parameters, namely, percent entrapment efficiency (% EE) and percent in vitro drug release at 12 h (% DR). The liposome formula was prepared using 32 factorial design, and the selected independent variables were, phospholipid (phospholipon 90G) and cholesterol (CH) concentrations. Nine formulas of paclitaxel-loaded liposome were prepared by thin film hydration technique (THF). The entrapment efficiency, in vitro release studies and drug content, were evaluated using on UV-visible spectrophotometer at λmax-230 nm. The developed PTL formulation vesicle morphology, particle size, polydispersity index (PDI) and zeta potential (ζ) were evaluated by Motic digital microscope and Malvern zetasizer respectively.Results: Using response surface methodology the estimated coefficient values obtained for independent variables in the regression equations, exhibited that the phospholipid (PL90G) and cholesterol (CH) molar concentration was observed to be highly influencing variables in optimizing % EE (86.67±0.67) and % DR (63.49±1.21). In the prediction of % EE and % DR values, the percent relative errors (PRE) was found to be low (–0.290%) and (0.058%) respectively. This suggests that design-developed model was found to be suitable for PTL formulations and thus, validate the model.Conclusion: Experimental results show that the observed responses were in close agreement with the predicted values and this demonstrates the reliability of the RSM in an optimization of % EE and % DR in paclitaxel liposomal (PTL) formulations.

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