DESIGN, OPTIMIZATION, AND STATISTICAL EVALUATION OF ORAL RECONSTITUTED SUSPENSION OF CLARITHROMYCIN USING ION-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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Taste Masking of Nizatidine Using Ion-Exchange Resins

Processes ◽

10.3390/pr7110779 ◽

2019 ◽

Vol 7 (11) ◽

pp. 779 ◽

Cited By ~ 2

Author(s):

Pattaraporn Panraksa ◽

Kasidech Boonsermsukcharoen ◽

Kyu-Mok Hwang ◽

Eun-Seok Park ◽

Pensak Jantrawut

Keyword(s):

Drug Release ◽

Bitter Taste ◽

Drug Loading ◽

Electronic Tongue ◽

Spherical Shape ◽

Batch Process ◽

Taste Masking ◽

Simulated Gastric Fluid ◽

Exchange Resins

The purpose of this study was to mask the bitter taste of nizatidine (NZD) using cation-exchange resins. Amberlite IRP-69 and Dowex-50 containing cross-linked polystyrene backbones were used. The drug resin complexes were prepared by batch process using drug: resin ratios of 1:1, 1:3, and 1:5. The optimum drug: resin ratio and the time required for maximum percentage drug loading into the complexes were determined. The selected drug-resin complexes were evaluated for morphology, drug release, and taste. The NZD-Dowex complex was obtained at a drug: resin ratio of 1:5 using a stirring time of 1 h in order to get 100% loading of NZD. The NZD-Dowex complex had a spherical shape and smooth texture similar to Dowex resin. The NZD-Dowex complex with a ratio of 1:5 showed that in vitro drug release of 4.27% at 5 min in simulated salivary fluid of pH 6.8 and 99.67% at 1 h in simulated gastric fluid of pH 1.2. NZD’s bitter taste was effectively masked when it formed a complex with Dowex at a ratio of 1:5. This was proved by an electronic tongue and human test panel.

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Ion Exchange Resins as Excipients for Drug Delivery: Issues for Reproducible Drug Loading

The Open Drug Delivery Journal ◽

10.2174/1874126600701010060 ◽

2007 ◽

Vol 1 (1) ◽

pp. 60-67 ◽

Cited By ~ 1

Author(s):

Daniel Zeiss ◽

Annette Bauer-Brandl

Keyword(s):

Drug Delivery ◽

Ion Exchange ◽

Drug Loading ◽

Ion Exchange Resins ◽

Exchange Resins

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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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TASTE MASKING TECHNIQUES: A REVIEW

INDIAN DRUGS ◽

10.53879/id.54.02.10705 ◽

2017 ◽

Vol 54 (02) ◽

pp. 5-19

Author(s):

S Mansi ◽

◽

Menra Muse ◽

J. S. Dua ◽

M. Singh ◽

...

Keyword(s):

Bitter Taste ◽

Molecular Complexes ◽

Taste Masking ◽

Sensory Response ◽

Ion Exchange Resins ◽

Multiple Emulsion ◽

Geriatric Population ◽

Dispersion Systems ◽

Exchange Resins ◽

Effervescent Agents

Taste masking is of critical importance for active ingredients with an undesirable taste, due to the need for increased patient compliance, especially in pediatric and geriatric population. Various techniques for taste masking involve addition of flavours, sweeteners and amino acids, use of effervescent agents, prodrug formation, salt preparation, adsorption, formation of complex with ion- exchange resins, inclusion complexes and molecular complexes, microencapsulation, granulation, viscosity modifiers, multiple emulsion, liposomes and solid dispersion systems. In pharmaceutical industry, taste masking involves the development of a system that prevents the active substance from interacting with taste buds, thereby reducing the negative sensory response. This article reviews the different technologies which are used for masking the bitter taste and methods for evaluation of taste masking efficacy.

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