Domperidone resinate complex as new formulation for gastroretentive drug delivery

Daihom, Baher; Bendas, Ehab R.; Mohamed, M. I.; Badawi, Alia

doi:10.1016/j.jddst.2020.101868

Cited by 8 publications

(7 citation statements)

References 27 publications

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“…Moreover, the CERs (AmberLite TM IRP69, DIAION TM UBK530, and AmberLite TM IRP69F) in this study possess the structural sulfonate functional group, which is almost completely ionized regardless of solution pH. The pKa of piperadine in PPD was 8.3 and it was ionizable in 0.1 N HCl solution (pH 1.2) used for PCC formation [ 26 , 33 , 34 ].…”

Section: Resultsmentioning

confidence: 99%

“…This reduces mass transfer and makes most of the inner resin bead less accessible for binding. This results in a lower binding efficiency compared to smaller CER particles with larger specific surface areas [ 26 ]. Among the CERs used, C1 and C2 had the most desirable properties for the binding efficiency of PPD.…”

Section: Resultsmentioning

confidence: 99%

“…The PPD binding efficiency (%) in PCC was calculated by analyzing the concentration of unbound drug in the filtrate (total of 30 mL). The binding efficiency (%) of PPD–CER in PCC was calculated via the following equations [ 26 ].

…”

Section: Methodsmentioning

confidence: 99%

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Paliperidone–Cation Exchange Resin Complexes of Different Particle Sizes for Controlled Release

et al. 2023

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This study aimed to develop electrolyte complexes of paliperidone (PPD) with various particle sizes using cation-exchange resins (CERs) to enable controlled release (both immediate and sustained release). CERs of specific particle size ranges were obtained by sieving commercial products. PPD–CER complexes (PCCs) were prepared in an acidic solution of pH 1.2 and demonstrated a high binding efficiency (>99.0%). PCCs were prepared with CERs of various particle sizes (on average, 100, 150, and 400 μm) at the weight ratio of PPD to CER (1:2 and 1:4). Physicochemical characterization studies such as Fourier-transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy between PCCs (1:4) and physical mixtures confirmed PCC formation. In the drug release test, PPD alone experienced a complete drug release from PCC of >85% within 60 min and 120 min in pH 1.2 and pH 6.8 buffer solutions, respectively. Alternatively, PCC (1:4) prepared with CER (150 μm) formed spherical particles and showed an almost negligible release of PPD in pH 1.2 buffer (<10%, 2 h) while controlling the release in pH 6.8 buffer (>75%, 24 h). The release rate of PPD from PCCs was reduced with the increase in CER particle size and CER ratio. The PCCs explored in this study could be a promising technology for controlling the release of PPD in a variety of methods.

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Section: Resultsmentioning

confidence: 99%

Section: Resultsmentioning

confidence: 99%

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Paliperidone–Cation Exchange Resin Complexes of Different Particle Sizes for Controlled Release

et al. 2023

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“…Initially, the drug is released into the oral cavity and gradually acts on the whole body from the local area, which improves the oral bioavailability and therapeutic effect of the drug. Daihom et al [ 24 ] prepared a complex of domperidone and resinate, which has good fluidity and thermochemical stability for the delivery of gastric retention drugs. The release profile of domperidone shows the characteristics of slow and controlled release.…”

Section: Introductionmentioning

confidence: 99%

Investigation on the Potential Application of Na-Attapulgite as an Excipient in Domperidone Sustained-Release Tablets

Xiao

Zheng

et al. 2022

Molecules

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In this study, Na-attapulgite was explored as an excipient to prepare domperidone sustained-release tablets and test them in accordance with United States Pharmacopoeia requirements. Fourier transform infrared spectroscopy (FTIR), X-ray powder diffraction (XRD) and differential scanning calorimetry (DSC) were employed to explore the compatibility between Na-attapulgite and domperidone. The XRD and DSC show no interaction between the drug and Na-attapulgite. The FTIR spectrum indicates a shift in the absorption of N-H in the drug molecule, which can be explained by the hydrogen bonding interaction between the N-H in the DOM molecule and the -OH on the surface of Na-ATP. The diameter, hardness, friability and drug content of the tablets were measured, and they all met the relevant requirements of the United States Pharmacopoeia. In addition, the tablets with Na-attapulgite as excipient exhibit a better release performance within the release time of 12 h. These results demonstrate that the domperidone sustained-release tablets have been successfully prepared by using Na-attapulgite as an excipient. The doping of Na-ATP in domperidone sustained-release tablets improves the cytocompatibility. Moreover, with the increase of Na-ATP content, cells proliferate remarkably and cell activity is significantly enhanced.

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“…This is because the research on the mechanism of complexation between the drug and IER is still not comprehensive. The relevant literature in the past five years have introduced the preparation and characterization methods of the drug−ion exchange resin complex, and proved the control release of drug-resin complex by in vitro methods, and evaluated the taste−masking efficiency by integrated score evaluation method (ISEM) [12][13][14][15][16][17]. Most research on IER is still at the macro level and the stage of experience accumulation.…”

Section: Introductionmentioning

confidence: 99%

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

Li¹,

Han²,

Hong³

et al. 2021

Polymers

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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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Domperidone resinate complex as new formulation for gastroretentive drug delivery

Cited by 8 publications

References 27 publications

Paliperidone–Cation Exchange Resin Complexes of Different Particle Sizes for Controlled Release

Paliperidone–Cation Exchange Resin Complexes of Different Particle Sizes for Controlled Release

Investigation on the Potential Application of Na-Attapulgite as an Excipient in Domperidone Sustained-Release Tablets

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

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