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

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).

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

10.32947/358 ◽  
2018 ◽  
Vol 18 (1) ◽  
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).

Hot melt extrusion of ion-exchange resin for taste masking

2018 ◽  
Vol 547 (1-2) ◽  
pp. 385-394 ◽  
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

Taste masking of Etoricoxib by using ion-exchange resin

2009 ◽  
Vol 15 (5) ◽  
pp. 511-517 ◽  
Author(s):  
Sradhanjali Patra ◽  
Rakesh Samantaray ◽  
Saswat Pattnaik ◽  
B. B. Barik
Keyword(s):  
Ion Exchange ◽  
Exchange Resin ◽  
Ion Exchange Resin ◽  
Taste Masking

scholarly journals Study on the Complexation and Release Mechanism of Methylphenidate Hydrochloride Ion Exchange Resin Complex

Polymers ◽  
2021 ◽  
Vol 13 (24) ◽  
pp. 4394
Author(s):  
Conghui Li ◽  
Xiaolu Han ◽  
Xiaoxuan Hong ◽  
Xianfu Li ◽  
Hui Zhang ◽  
...  
Keyword(s):  
Ion Exchange ◽  
Exchange Resin ◽  
Drug Loading ◽  
Model Fitting ◽  
Ion Exchange Resin ◽  
Dynamics Simulation ◽  
Taste Masking ◽  
Release Mechanism ◽  
Salt Bridges ◽  
Factors Affecting

Since the advent of ion exchange resin, it has been widely used in many fields, including drug delivery systems. The drug binds to the resin through an exchange reaction to form a drug–resin complex, which can gradually release drugs through the exchange of physiological ions in the gastrointestinal tract, to realize functions such as taste masking and regulating release. In this study, the complexes of methylphenidate hydrochloride and Amberlite IRP69 were prepared and evaluated to explore the mechanism of complexation, influencing factors and release mechanism at a molecular level. Firstly, with the properties of the selected complexes, molecular dynamics simulation was innovatively used to find that the intermolecular interaction between drug molecules and ion exchange resin molecules is mainly caused by the stacking effect of π and salt bridges. Secondly, with the drug loading status as an indicator, the factors affecting the compounding process of the drug and resin were explored. Finally, the release mechanism of the drug–resin complex was studied by mathematical model fitting. In summary, a variety of methods were used to study the mechanism of complexation and release between drug and resin, providing a theoretical basis for promoting the marketing of ion−exchange resin−mediated oral preparations.

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

2019 ◽  
pp. 325-332
Author(s):  
NISHANT OZA ◽  
SWATI SAGAR
Keyword(s):  
Ion Exchange ◽  
Drug Release ◽  
Factorial Design ◽  
Exchange Resin ◽  
Ion Exchange Resin ◽  
Cefuroxime Axetil ◽  
Full Factorial Design ◽  
Taste Masking ◽  
Dispersible Tablet ◽  
Full Factorial

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.

Formulation of Dextromethorphan Oral Disintegrating Tablet Using Ion Exchange Resin

2011 ◽  
Vol 201-203 ◽  
pp. 1384-1387
Author(s):  
Wipada Samprasit ◽  
Praneet Opanasopit ◽  
Prasert Akkaramongkolporn ◽  
Tanasait Ngawhirunpat ◽  
Kaewnapa Wongsermsin ◽  
...  
Keyword(s):  
Ion Exchange ◽  
Drug Release ◽  
Bitter Taste ◽  
Exchange Resin ◽  
Drug Loading ◽  
Ion Exchange Resin ◽  
Physical Mixture ◽  
Disintegration Time ◽  
Mouth Feel ◽  
Tablet Hardness

The purpose of this research was to mask the bitter taste of dextromethorphan hydrobromide using a cationic ion exchange resin, Amberlite® IRP-69, to formulate oral disintegrating tablets (ODTs). The drug was loaded (resinate) were prepared in drug to resin ratio of 1:1 and 1:2. The resinate or physically mixed with the resin (physical mixture) was incorporated into ODTs by direct compression. The formula was developed to acquire the optimal formulations of taste masked ODTs, hardness and mouth feel and disintegration time. The ODTs were further evaluated for weight, friability, disintegration time, drug content, degree of bitter taste and drug release, respectively. The weight and friability of the tablet with resinate were not significantly different from those with physical mixture. The tablet with resinate had a lower tablet hardness due to drug loading might be reduced compressibility. The addition of Avicel®PH102 could be increased tablet hardness. Both ODTs with resinate and physical mixture provided a sustained pattern of drug release. However, only ODTs with resinate successfully masked bitter taste of the drug. In conclusion, the loaded drug in ion exchange resin as resinate could increase the palatability and acceptability of ODTs containing bitter drugs.

scholarly journals DESIGN, OPTIMIZATION, AND STATISTICAL EVALUATION OF ORAL RECONSTITUTED SUSPENSION OF CLARITHROMYCIN USING ION-EXCHANGE RESINS

2020 ◽  
pp. 53-60
Author(s):  
KOMAL S ◽  
HARIKRISHNAN N
Keyword(s):  
Complex Formation ◽  
Ion Exchange ◽  
Drug Release ◽  
Bitter Taste ◽  
Drug Loading ◽  
Taste Masking ◽  
Ion Exchange Resins ◽  
Comparison Test ◽  
Multiple Comparison Test ◽  
Exchange Resins

Objectives: The objective of the present study is taste masking of bitter clarithromycin using Indion 204, Indion 234, and Tulsion 335 as ion-exchange resins, which forms insoluble complexes, inhibiting the drug release in saliva as ion-exchange resins are cross-linked polymers, water-insoluble that contains salt-forming groups in repeating positions on the polymer chain. Drugs that are bitter and cationic get adsorbed onto weak cationic exchange resins of carboxylic acid functionality such as Indion 204, Indion 234, and Tulsion 335 to form non-bitter complexes. Methods: The drug-resin complex loading process was optimized for the resin content, activation, swelling time, stirring time, influence of pH, and temperature for maximum drug loading and the formed complex was evaluated by differential scanning calorimetry (DSC) to confirm complex formation. The drug-resin complex was also characterized by their micromeritic and rheological properties. These complexes were used to prepare oral reconstituted suspensions and the taste was evaluated. The formulation was evaluated for various parameters such as sedimentation volume, pH, redispersibility, viscosity, drug content, and in vitro drug release. Results: Acid-activated resins comprising Indion 204, Indion 234, and Tulsion 335 with the drug:resin ratio of 1:2, stirred in a solution of pH 7–8 at 70° for 6 h had a maximum drug loading and masked the bitter taste of clarithromycin. DSC of the drug-resin complex (DRC) revealed that there was interaction leading to complex formation. The drug-resin complex was formulated into suspension formulations (S1-S9) and evaluated. Various parameters were found to be within permissible limits. Formulations S3, S6, and S9 containing 1:2 ratios of the drug-resin complex of Indion 204, Indion 234, and Tulsion 335 revealed maximum taste masking. This was further confirmed by treatment of taste evaluation scores obtained from the volunteers by ANOVA, Dunnett’s multiple comparison test, and Tukey’s multiple comparison test. All the three optimized formulations had a significant difference of p<0.001 when compared to control S10. S6 formulation was widely accepted. Conclusion: Ion-exchange complexation could efficiently mask the bitter taste of clarithromycin and achieve palatable taste suitable for pediatric use.

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