DESIGN AND OPTIMIZATION OF PEDIATRIC CEFUROXIME AXETIL DISPERSIBLE TABLET CONTAINING ION-EXCHANGE RESIN

Objective: The aim of present work was to develop of pediatric cefuroxime axetil 125 mg dispersible tablets by using ion exchange resin as a taste masking agent and quality target product profile was defined based on the properties of the cefuroxime axetil. Methods: Initially, cefuroxime axetil and various resin complexes (DRC) were prepared with different conditions and evaluated for taste masking and drug loading. Optimized DRC was used to formulate the dispersible tablet. A 32 full factorial design was employed to study the effect of mannitol (X1) and microcrystalline cellulose PH-101 (X2) on drug release at 10 min and time taken to 80% drug release. In the present study, the following constraints were arbitrarily used for the selection of an optimized batch: Q10>65% and T80%<30 min. Multiple linear regression analysis, ANOVA and graphical representation of the influence factor by 3D plots were performed by using Sigmaplot 11.0. Checkpoint batch was prepared to validate the evolved model. Results: Among the various drug resins complex DRC-9 was found with less bitter taste which was containing kyron T-114 and among the all factorial batch F7 showed highest drug release at 10 min (Q10) and lowest time taken to 80% drug release (T80) hence batch F7 was selected as an optimized batch and it’s found to be stable in the stability evaluation. Conclusion: The results of full factorial design indicate mannitol and MCC PH-101 have a significant effect on drug release.

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Formulation of Extended-Release Beads of Lamotrigine Based on Alginate and Cassia fistula Seed Gum by QbD Approach

Current Drug Delivery ◽

10.2174/1567201817666200317124022 ◽

2020 ◽

Vol 17 (5) ◽

pp. 422-437

Author(s):

Dixita Jain ◽

Akshay Sodani ◽

Swapnanil Ray ◽

Pranab Ghosh ◽

Gouranga Nandi

Keyword(s):

Drug Release ◽

Factorial Design ◽

Extended Release ◽

Polymer Concentration ◽

Green Manufacturing ◽

Full Factorial Design ◽

Cassia Fistula ◽

Negative Environmental Impact ◽

Seed Gum ◽

Full Factorial

Aim: This study was focused on the formulation of the multi-unit extended-release peroral delivery device of lamotrigine for better management of epilepsy. Background: The single-unit extended-release peroral preparations often suffer from all-or-none effect. A significant number of multi-unit delivery systems have been reported as a solution to this problem. But most of them are found to be composed of synthetic, semi-synthetic or their combination having physiological toxicity as well as negative environmental impact. Therefore, fabrication and formulation of multi-unit extended-release peroral preparations with natural, non-toxic, biodegradable polymers employing green manufacturing processes are being appreciated worldwide. Objective: Lamotrigine-loaded extended-release multi-unit beads have been fabricated with the incorporation of a natural polysaccharide Cassia fistula seed gum in calcium-cross-linked alginate matrix employing a simple green process and 23 full factorial design. Methods: The total polymer concentration, polymer ratio and [CaCl2] were considered as independent formulation variables with two different levels of each for the experiment-design. The extended-release beads were then prepared by the ionotropic gelation method using calcium chloride as the crosslinkerions provider. The beads were then evaluated for drug encapsulation efficiency and drug release. ANOVA of all the dependent variables such as DEE, cumulative % drug release at 2h, 5h, 12h, rate constant and dissolution similarity factor (f2) was done by 23 full factorial design using Design-Expert software along with numerical optimization of the independent variables in order to meet USP-reference release profile. Results: The optimized batch showed excellent outcomes with DEE of 84.7 ± 2.7 (%), CPR2h of 8.41± 2.96 (%), CPR5h of 36.8± 4.7 (%), CPR12h of 87.3 ± 3.64 (%) and f2 of 65.9. Conclusion: This approach of the development of multi-unit oral devices utilizing natural polysaccharides might be inspiring towards the world-wide effort for green manufacturing of sustained-release drug products by the QbD route.

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Hot melt extrusion of ion-exchange resin for taste masking

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2018.05.068 ◽

2018 ◽

Vol 547 (1-2) ◽

pp. 385-394 ◽

Cited By ~ 7

Author(s):

David Cheng Thiam Tan ◽

Jeremy Jianming Ong ◽

Rajeev Gokhale ◽

Paul Wan Sia Heng

Keyword(s):

Ion Exchange ◽

Exchange Resin ◽

Hot Melt Extrusion ◽

Ion Exchange Resin ◽

Taste Masking ◽

Melt Extrusion ◽

Hot Melt

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Effect of The Surfactant and Liquid Lipid Type in The Physico-chemical Characteristics of Beeswax-based Nanostructured Lipid Carrier (NLC) of Metformin

Pharmaceutical Nanotechnology ◽

10.2174/2211738509666210222143716 ◽

2021 ◽

Vol 09 ◽

Author(s):

Mona Qushawy

Keyword(s):

Drug Release ◽

Factorial Design ◽

Biological Membrane ◽

Entrapment Efficiency ◽

Tween 80 ◽

Full Factorial Design ◽

Nanostructured Lipid Carrier ◽

Class Iii ◽

Scanning Calorimetry ◽

Full Factorial

Background: Metformin (MF) is an antidiabetic drug that belongs to class III of the biopharmaceutical classification system (BCS) which is characterized by high solubility and low permeability. Objective: The study aimed to prepare metformin as nanostructured lipid carriers (MF-NLCs) to control the drug release and enhance its permeability through the biological membrane. Method: 22 full factorial design was used to make the design of MF-NLCs formulations. MF-NLCs were prepared by hot-melt homogenization-ultra sonication technique using beeswax as solid lipid in presence of liquid lipid (either capryol 90 or oleic acid) and surfactant (either poloxamer 188 or tween 80). Results: The entrapment efficiency (EE%) of MF-NLCs was ranged from 85.2±2.5 to 96.5±1.8%. The particle size was in the nanoscale (134.6±4.1 to 264.1±4.6 nm). The value of zeta potential has a negative value ranged from -25.6±1.1 to -39.4±0.9 mV. The PDI value was in the range of (0.253±0.01 to 0.496±0.02). The cumulative drug release was calculated for MF-NLCs and it was found that Q12h ranged from 90.5±1.7 % for MF-NLC1 to 99.3±2.8 for MF-NLC4. Infra-red (IR) spectroscopy and differential scanning calorimetry (DSC) studies revealed the compatibility of the drug with other ingredients. MF-NLC4 was found to the optimized formulation with the best responses. Conclusion: 22 full factorial design succeed to obtain an optimized formulation which controls the drug release and increases the drug penetration.

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Drug Release Properties of Polymer Coated Ion-Exchange Resin Complexes: Experimental and Theoretical Evaluation

Journal of Pharmaceutical Sciences ◽

10.1002/jps.20677 ◽

2007 ◽

Vol 96 (3) ◽

pp. 618-632 ◽

Cited By ~ 16

Author(s):

Seong Hoon Jeong ◽

Nahor Haddish Berhane ◽

Kamyar Haghighi ◽

Kinam Park

Keyword(s):

Ion Exchange ◽

Drug Release ◽

Exchange Resin ◽

Ion Exchange Resin ◽

Theoretical Evaluation

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Taste masking of Etoricoxib by using ion-exchange resin

Pharmaceutical Development and Technology ◽

10.3109/10837450903322787 ◽

2009 ◽

Vol 15 (5) ◽

pp. 511-517 ◽

Cited By ~ 11

Author(s):

Sradhanjali Patra ◽

Rakesh Samantaray ◽

Saswat Pattnaik ◽

B. B. Barik

Keyword(s):

Ion Exchange ◽

Exchange Resin ◽

Ion Exchange Resin ◽

Taste Masking

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Effect of Curing and Compression Process on the Drug Release of Coated Ion-Exchange Resin Complexes

Journal of Pharmaceutical Investigation ◽

10.4333/kps.2011.41.2.067 ◽

2011 ◽

Vol 41 (2) ◽

pp. 67-73

Author(s):

Seong-Hoon Jeong ◽

Hun-Sik Wang ◽

Ja-Seong Koo ◽

Eun-Joo Choi ◽

Ki-Nam Park

Keyword(s):

Ion Exchange ◽

Drug Release ◽

Exchange Resin ◽

Ion Exchange Resin ◽

Compression Process

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FORMULATION, OPTIMIZATIONANDEVALUATION OF SUBLINGUAL FILM OF ENALAPRILMALEATE USING 32 FULL FACTORIAL DESIGN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i1.39446 ◽

2021 ◽

pp. 178-186

Author(s):

SATYAJIT SAHOO ◽

KIRTI MALVIYA ◽

AMI MAKWANA ◽

PRASANTA KUMAR MOHAPATRA ◽

ASITRANJAN SAHU

Keyword(s):

Tensile Strength ◽

Drug Release ◽

Factorial Design ◽

Full Factorial Design ◽

Disintegration Time ◽

Surface Ph ◽

Independent Variables ◽

Folding Endurance ◽

Full Factorial ◽

32 Full Factorial Design

Objective: The purpose of this investigation was to formulate, optimize and evaluate sublingual film of Enalapril maleate for rapid management of Hypertension. Methods: Sublingual films were prepared by solvent casting method. Present investigation were formulated by using HPMC E 15 (X1) as polymer and Polyethylene glycol (X2) as plasticizer were chosen as independent variables in 32 full factorial design while Tensile strength (TS), Disintegration time (DT) and % Cumulative drug release at 10 min. (% CDR) were taken as dependent variables. The various physical parameters were evaluated for sublingual films such as thickness, tensile strength, folding endurance, disintegration time, surface pH and % CDR. Results: From the experimental study, it was concluded that the optimized batch F8 showed 98.6 %, the highest release of the drug. Stability study was performed by taking an optimized formulation and it was observed stable. The sublingual films showed acceptable results in all studies such as thickness, tensile strength, folding endurance, disintegration time, surface pH and % CDR at 10 min. R2 values for Tensile Strength (Y1), Disintegration time (Y2) and % cumulative drug release at 10 min. of Enalaprilmaleate(Y3) found to be 0.9852, 0.9829 and 0.9641 respectively. Thus, a good correlation between dependent and independent variables was developed. Conclusion: 32 full factorial design was successfully applied during preparation, optimization and evaluation of sublingual films of Enalapril maleate. The present investigation showed quick disintegration and fast release of the drug for rapid management of Hypertension.

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Preparation and characterization of taste masked valsartan by ion-exchange resin approach

Al Mustansiriyah Journal of Pharmaceutical Sciences ◽

10.32947/ajps.18.01.0358 ◽

2018 ◽

pp. 11-25

Keyword(s):

Complex Formation ◽

Ion Exchange ◽

Bitter Taste ◽

Exchange Resin ◽

Mixing Time ◽

Spectroscopic Method ◽

Ion Exchange Resin ◽

Drug Formulation ◽

Taste Masking ◽

Scanning Calorimetry

The bitter taste is one of the most important drug formulation problems. The unpleasant taste leads to noncompliance, which consequently decreases the therapeutic efficacy of the drug. Therefore, masking of bitter taste is very important in drug formulation. In this study an antihypertensive drug, valsartan, which is a weak acid with bitter taste, was used as a model drug to mask its taste with dowex2 (weak base anion exchange resin). The taste masking of a drug using ion exchange resin basically depends on the complex formation between the drug and a specific type of resin. Complex formation under various preparation conditions including; the ratio of drug to resin, mixing time, the pH of the processing medium and the concentration of valsartan was investigated in this study. Optimum conditions for complex formation and maximum drug load were obtained at a drug-resin ratio 1:8, mixing time 4 hours, pH 6.8, temperature 50º C and drug concentration 0.02% w/v. The drug resin ate complex was evaluated for the drug content, taste, drug release and molecular properties. The resinate formation was confirmed using different analytical techniques like thermal analysis using differential scanning calorimetry (DSC), spectroscopic method like Fourier transform infrared spectroscopy (FTIR) and by X-ray powder diffraction analysis (XRPD).

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IMPLEMENTATION OF QUALITY BY DESIGN (QBD) APPROACH IN FORMULATION AND DEVELOPMENT OF RITONAVIR PELLETS USING EXTRUSION SPHERONIZATION METHOD

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2020v12i1.35453 ◽

2019 ◽

pp. 139-146

Author(s):

SATISH K. MANDLIK ◽

PAYAL P. AGARWAL ◽

HARSHAL P. DANDGAVHAL

Keyword(s):

Drug Release ◽

Sustained Release ◽

Factorial Design ◽

Quality By Design ◽

Research Work ◽

Full Factorial Design ◽

Extrusion Speed ◽

Full Factorial ◽

Extrusion Spheronization

Objective: Ritonavir is an antiretroviral drug used for HIV-AIDS treatment. The purpose of this research work was to implement the quality by design (QbD) approach in formulation of ritonavir sustained-release pellets by industrially applied extrusion spheronization technique. Methods: Pellets were prepared by extrusion spheronization method and evaluated for their physicochemical properties. Initially, on the basis of prior knowledge Quality Target Product Profile (QTTP) element was identified and further Critical Quality Attributes (CQA) elements were defined. Risk assessment (RA) was done by two tools as failure mode and effect analysis (FMEA) and fishbone diagram (Ishikawa plot). Placket Burman design was implemented as a screening design using seven high-risk factors (spheronization speed, spheronization time, extrusion speed, drying method, PVP K 30, cross povidone, and solvent). Optimization study was done by 23 full factorial design with three critical factors as (spheronization speed, extrusion speed and PVP K 30). The in vitro drug release was studied in both gastric and intestinal fluids for 12 h using USP Ι apparatus. Control space was established for the sustained release pellets. Results: Among all batches obtained in 23 full factorial design, batch R7 was found to be effective with carr’s index value of 5.281, percentage yield of 69.6%, time required to release 50% drug was 8 h and percent drug release after 12 h was found 83.132 %, R7 batch was selected as optimized batch. Statistical analysis showed model terms were significant. Conclusion: We can conclude that; sustained-release pellets of ritonavir were successfully designed using QbD approach.

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