Hot melt extrusion of ion-exchange resin for taste masking

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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Hot Melt Extrusion and its Application in 3D Printing of Pharmaceuticals

Current Drug Delivery ◽

10.2174/1567201817999201110193655 ◽

2020 ◽

Vol 17 ◽

Author(s):

Sanjeevani Deshkar ◽

Mrunali Rathi ◽

Shital Zambad ◽

Krishnakant Gandhi

Keyword(s):

3D Printing ◽

Dosage Form ◽

Fused Deposition Modeling ◽

Hot Melt Extrusion ◽

Taste Masking ◽

Melt Extrusion ◽

Fused Deposition ◽

Continuous Pharmaceutical Manufacturing ◽

Solubility Improvement ◽

Hot Melt

Abstract:: Hot melt extrusion (HME) is a continuous pharmaceutical manufacturing process that has been extensively inves-tigated for solubility improvement and taste masking of active pharmaceutical ingredients. Recently, it is being explored for its application in 3D printing. 3D printing of pharmaceuticals allows flexibility of dosage form design, customization of dosage form for personalized therapy and the possibility of complex designs with the inclusion of multiple actives in a sin-gle unit dosage form. Fused deposition modeling (FDM) is a 3D printing technique with a variety of applications in pharma-ceutical dosage form development. FDM process requires a polymer filament as the starting material that can be obtained by hot melt extrusion. Recent reports suggest enormous applications of a combination of hot melt extrusion and FDM technol-ogy in 3D printing of pharmaceuticals and need to be investigated further. This review in detail describes the HME process along with its application in 3D printing. The review also summarizes the published reports on the application of HME cou-pled with 3D printing technology in drug delivery.

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

Al Mustansiriyah Journal of Pharmaceutical Sciences ◽

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).

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Hot-melt extrusion microencapsulation of quercetin for taste-masking

Journal of Microencapsulation ◽

10.1080/02652048.2017.1280095 ◽

2017 ◽

Vol 34 (1) ◽

pp. 29-37 ◽

Cited By ~ 21

Author(s):

Chia Miang Khor ◽

Wai Kiong Ng ◽

Parijat Kanaujia ◽

Kok Ping Chan ◽

Yuancai Dong

Keyword(s):

Hot Melt Extrusion ◽

Taste Masking ◽

Melt Extrusion ◽

Hot Melt

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A Review of Hot-Melt Extrusion: Process Technology to Pharmaceutical Products

ISRN Pharmaceutics ◽

10.5402/2012/436763 ◽

2012 ◽

Vol 2012 ◽

pp. 1-9 ◽

Cited By ~ 52

Author(s):

Mohammed Maniruzzaman ◽

Joshua S. Boateng ◽

Martin J. Snowden ◽

Dennis Douroumis

Keyword(s):

Drug Delivery ◽

Oral Drug Delivery ◽

Hot Melt Extrusion ◽

Pharmaceutical Products ◽

Taste Masking ◽

Oral Drug ◽

Melt Extrusion ◽

Process Technology ◽

Processing Technologies ◽

Hot Melt

Over the last three decades industrial adaptability has allowed hot-melt extrusion (HME) to gain wide acceptance and has already established its place in the broad spectrum of manufacturing operations and pharmaceutical research developments. HME has already been demonstrated as a robust, novel technique to make solid dispersions in order to provide time controlled, modified, extended, and targeted drug delivery resulting in improved bioavailability as well as taste masking of bitter active pharmaceutical ingredients (APIs). This paper reviews the innumerable benefits of HME, based on a holistic perspective of the equipment, processing technologies to the materials, novel formulation design and developments, and its varied applications in oral drug delivery systems.

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

Polymers ◽

10.3390/polym13244394 ◽

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.

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