Interaction of Amine Drugs with a Polycarboxylic Acid Ion-Exchange Resin

Borodkin, Saul; Yunker, Martin H.

doi:10.1002/jps.2600590409

Cited by 54 publications

(27 citation statements)

References 4 publications

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“…DRC equivalent to 500 mg ciprofloxacin was held in the mouth for 15 seconds by each volunteer, and the bitterness level was recorded against pure drug using a numerical scale. 17 …”

Section: Molecular Properties Of Drug Resin Complexmentioning

confidence: 99%

Molecular properties of ciprofloxacin-indion 234 complexes

et al. 2004

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The purpose of this research was to formulate tasteless complexes of ciprofloxacin with Indion 234 and to evaluate molecular properties of drug complexes. The effect of batch and column process, complexation time, temperature, and pH on ciprofloxacin loading on Indion 234 is reported. Drug resin complexes (DRC) were characterized by infrared spectroscopy, thermal analysis, and x-ray diffraction pattern. Ciprofloxacin release from DRC is obtained at salivary and gastric pH and in the presence of electrolytes. The efficient drug loading was evident in batch process using activated Indion 234 with a drug-resin ratio of 1:1.3. Drug complexation enhanced with pH from 1.2 to 6, while temperature did not affect the complexation process. Infrared spectroscopy revealed complexation of -NH (drug) with Indion 234. DRC are amorphous in nature. Drug release from DRC in salivary pH was insufficient to impart bitter taste. Volunteers rated the complex as tasteless and agreeable. Complete drug release was observed at gastric pH in 2 hours. The drug release was accelerated in the presence of electrolytes. Indion 234 is inexpensive, and the simple technique is effective for bitterness masking of ciprofloxacin.

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“…DRC equivalent to 500 mg ciprofloxacin was held in the mouth for 15 seconds by each volunteer, and the bitterness level was recorded against pure drug using a numerical scale. 17 …”

Section: Molecular Properties Of Drug Resin Complexmentioning

confidence: 99%

Molecular properties of ciprofloxacin-indion 234 complexes

et al. 2004

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“…It has been reported that PRM depolarize taste cells by closing K + channels and produce bitterness (2). Palatable formulation development is one of the most difficult tasks, although various taste masking techniques such as the addition of sweeteners and flavors (3), coating with polymers (4), adsorption to ion-exchange resin (5,6), and chemical modifications such as the use of insoluble prodrugs (7,8) have been reported. Each technique has its own disadvantages.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Taste Masked Oral Reconstitutable Suspension of Primaquine Phosphate

Shah

Mashru

2008

AAPS PharmSciTech

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Abstract. The purpose of this research was to mask the intensely bitter taste of primaquine phosphate (PRM) and to formulate suspension powder (cachets) of the taste masked drug. Taste masking was done using beta-cyclodextrin. To characterize and formulate taste masked cachets of PRM, the 1:25 M physical mixture was selected based on bitterness score. Phase solubility studies, fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray powder diffraction (XRPD) were performed to identify the physicochemical interaction between drug and carrier, hence its effect on dissolution. Cachets were evaluated for angle of repose, sedimentation characterization and pH. In vitro drug release studies for physical mixture and kneaded system were performed at pH, 1.2 and 6.8. Bitterness score was evaluated using gustatory sensation test. Phase solubility studies showed weak interaction between PRM and CD. The FTIR, DSC and XRPD studies indicated inclusion complexation in physical mixture and kneaded system. In addition, kneaded system and physical mixture exhibited better drug release at pH 1.2 and negligible effect at pH 6.8. Cachets prepared using physical mixture, (DS24), showed complete bitter taste masking and easy redispersibility. Taste evaluation of cachets in human volunteers rated tasteless with a score of 0 to DS24 and 3 to DS25. Thus, results conclusively demonstrated successful taste masking and formulation of cachets with taste masked drug.

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“…The drug, drug resin complex equivalent to 4 mg risperidone and risperidone ODT with resinate and without resinate and marketed product was held in mouth for 60 s by each volunteer, and the bitterness level was recorded against pure drug using a numerical scale. 21) In case of ODT, disintegration time was also noted. After 60 s, the disintegrated tablet was spitted out and the mouth was rinsed thoroughly with mineral water.…”

mentioning

confidence: 98%

Fabrication and Evaluation of Taste Masked Resinate of Risperidone and Its Orally Disintegrating Tablets

Shukla

Chakraborty

Singh

et al. 2009

CHEMICAL & PHARMACEUTICAL BULLETIN

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The production of a palatable dosage form is very important for patient compliance, which in turn decides the commercial success of the product. The masking of unpleasant taste in orally-disintegrating tablets and chewable tablets is therefore an important consideration in the formulation of many therapeutic agents and is achieved by minimizing direct contact between the active species and the taste receptors in the buccal cavity of the subject. In order to improve the palatability of a pharmaceutical product, many techniques have been developed, which have not only improved the taste, but also the stability of the drug in the formulation and performance of the product. Use of ion exchange is one of the methods for taste masking.Ion Exchange Resins (IERs) for Taste Masking Ion exchange (IE) involves the reversible interchange of ions (of like charge) between a liquid and a solid phase, with no radical change in the structure and properties of the solid. 1) IERs are high molecular weight polymers and most frequently employed polymeric network is a copolymer of styrene and divinylbenzene. They have wide applications in enhancing the stability of sensitive drugs, sustaining the release of drug, 2) as disintegrating agents and for masking the bitter taste of drug.3) Drug binding to the resin can be achieved by two processes. First approach is repeated elution of drug solution through a column of swollen activated resin bead where drug is allowed to interact with binding sites of resin and second is by prolonged contact of resin with the drug solution. 4-7)Drug molecules get adsorbed on the IER, resulting in the formation of an insoluble adsorbate or resinate by forming weak ionic bonds which does not dissociate under the salivary pH conditions, hence, masks the unpleasant taste of drugs.After administration of resinate, the release of drug from the resin depends on the properties of the resin and the ionic environment within the gastrointestinal tract (GIT). Drug molecules get released from resin by exchanging with appropriately charged ions in the GIT and free drug is available for absorption.8) The IER devoid of drug is eliminated or biodegraded from or at the site of delivery. 9)Depending on nature of monomer and their ionic strength, IER can be classified into four major classes: strong acid cation exchange (CE) resin, weak acid CE resin, strong base anion exchange (AE) resin and weak base AE resin. Strong acid CE resins constituted of sulfonated styrene divinylbenzene copolymer are functional throughout the entire pH range and weak acid CE resins function at pH values above 6.0. Both can be used for masking the taste of basic drugs. Similarly, strong base AE resins are functional throughout the entire pH range, while the weak base AE resins function well below pH 7.0. 10) These can be used for masking the taste of acidic drugs.Application of IER for masking the bitter taste of drugs has been explored in many investigations. Oral suspension of quinolones (orbifloxacin) and/or their derivatives are prepared by IE...

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Interaction of Amine Drugs with a Polycarboxylic Acid Ion-Exchange Resin

Cited by 54 publications

References 4 publications

Molecular properties of ciprofloxacin-indion 234 complexes

Molecular properties of ciprofloxacin-indion 234 complexes

Formulation and Evaluation of Taste Masked Oral Reconstitutable Suspension of Primaquine Phosphate

Fabrication and Evaluation of Taste Masked Resinate of Risperidone and Its Orally Disintegrating Tablets

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