Taste masking and rheology improvement of drug complexed with beta-cyclodextrin and hydroxypropyl-β-cyclodextrin by hot-melt extrusion

Malaquias, Lorena F.B.; Barreto, Lívia Cristina Lira de Sá; Freire, Daniel; Silva, Izabel Cristina Rodrigues da; Karan, Kapish; Dürig, Thomas; Lima, Eliana Martins; Marreto, Ricardo Neves; Gelfuso, Guilherme M.; Cunha-Filho, Marcílio

doi:10.1016/j.carbpol.2018.01.011

Cited by 55 publications

(23 citation statements)

References 33 publications

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“…According to table 2 that the spray drying method had undergone an inclusion complex in which inclusion complex results were ranging from tasteless to sweet which successfully masked its original bitter taste. This agrees with several studies that reported that CD inclusion complexes possessed taste-masking properties [24,25]. Taste masking was the result of entrapment of drug molecule into CD cavity and the presence of sugar molecule in CD, hindered the unpleasant taste [26].…”

Section: Examination Of Organolepticsupporting

confidence: 91%

EVALUATION OF ORALLY DISINTEGRATING TABLET OF IBUPROFEN-β-CYCLODEXTRIN INCLUSION COMPLEX

Purnamasari

Saputra

2020

Int J App Pharm

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Objective: This study aims to determine the effect of the inclusion complex formation of ibuprofen (IB) with β-cyclodextrin (β-CD) in improving water solubility and taste masking as well as to study the effect of the combined use of super disintegrants in IB-β-CD ODT (Orally disintegrating tablet). Methods: IB-β-CD inclusion complex was prepared by spray drying technique with a 1:1 molar ratio. ODTs were prepared by the direct compression method using various ratios of Ac-Di-Sol® and Kollidon® CL as super disintegrant. The inclusion complex was characterized using spectroscopy FT-IR (Fourier-transform infrared) and DSC (Differential Scanning Calorimetry). The physical properties and dissolution rate of ODTs were evaluated. Dissolved drug concentration at 60 min (Q60) and Dissolution Efficiency (DE60) was calculated using the dissolution test result. Results: The unpleasant taste of IB had been successfully masked by IB-β-CD. Formula 1 was observed having 14.5 sec of disintegration, fastest compared to the other formulas. Moreover DE60 value of formula I was higher than the other formulas (113.45). Conclusion: IB-β-CD Inclusion complex prepared by spray drying method (1: 1) increased the water solubility and masked the unpleasant taste compared to IB moreover combination of Ac-Di-Sol® and Kollidon® CL increased ODT dissolution rate.

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Section: Examination Of Organolepticsupporting

confidence: 91%

EVALUATION OF ORALLY DISINTEGRATING TABLET OF IBUPROFEN-β-CYCLODEXTRIN INCLUSION COMPLEX

Purnamasari

Saputra

2020

Int J App Pharm

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“…It was established that a relationship constructed between K a , K d , and K a:b has the potential to project the magnitude of taste masking (Guo et al, ). Recently, the potential of hot melt extrusion technique has been demonstrated to mask the bitter taste of drugs using β‐CD and HP‐β‐CD (Malaquias et al, ). In addition, the CDs are also combined with other approaches such as ion exchange resin to reduce the bitter taste as well as to improve solubility of poorly soluble drugs (Samprasit et al, ).…”

Section: Significance Of CD Complexationmentioning

confidence: 99%

“…Recently, the potential of hot melt extrusion technique has been demonstrated to mask the bitter taste of drugs using β-CD and HP-β-CD (Malaquias et al, 2018). In addition, the CDs are also combined with other approaches such as ion exchange resin to reduce the bitter taste as well as to improve solubility of poorly soluble drugs (Samprasit et al, 2015).…”

Section: Taste Maskingmentioning

confidence: 99%

Cyclodextrin complexes: Perspective from drug delivery and formulation

Jacob

Nair

2018

Drug Development Research

174

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Cyclodextrins (CDs) have been widely investigated as a unique pharmaceutical excipient for past few decades and is still explored for new applications. They are highly versatile oligosaccharides which possess multifunctional characteristics, and are mainly used to improve the physicochemical stability, solubility, dissolution rate, and bioavailability of drugs. Stability constant, factors affecting complexation, techniques to enhance complexation efficiency, the preparation methods for molecular inclusion complexes and release of guest molecules are discussed in brief. In addition, different CD derivatives and their pharmacokinetics are elaborated. Further, the significance of CD complex in aqueous solubility, dissolution and bioavailability, stability, and taste masking is explained. The recent advancement of CDs in developing various drug delivery systems is enlightened. Indeed, the potential of CDs by means of inclusion complex formation have widen the applicability of these materials in various drug delivery systems including ocular, osmotic, mucoadhesive, transdermal, nasal, and targeted delivery systems. Feasibility studies have been performed on the benefit of these cyclic oligomers as nanocarriers, a strategy that can modify the drugs with improved physicochemical properties. Studies also demonstrated the feasibility of CDs to self-assemble in the form of stable nanoaggregates, which may extend the scope of CDs in drug delivery to the continually expanding list of new drug entities.

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“…However, the addition of sweeteners and flavors is not effective enough to mask the extremely disgusting taste of the atomoxetine HCl after swallowing. Cyclodextrins have also been widely used in the pharmaceutical industry due to their cavities, which can form inclusion complexes to mask the bitterness of drugs [18] , [19] , [20] . Especially, HP-β-CyD ( Fig.…”

Section: Introductionmentioning

confidence: 99%

Quantitative prediction of the bitterness of atomoxetine hydrochloride and taste-masked using hydroxypropyl-β-cyclodextrin: A biosensor evaluation and interaction study

Zhang²,

Khan

et al. 2020

Asian Journal of Pharmaceutical Sciences

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The bitterness of a drug is a major challenge for patient acceptability and compliance, especially for children. Due to the toxicity of medication, a human taste panel test has certain limitations. Atomoxetine hydrochloride (HCl), which is used for the treatment of attention deficit/hyperactivity disorder (ADHD), has an extremely bitter taste. The aim of this work is to quantitatively predict the bitterness of atomoxetine HCl by a biosensor system. Based on the mechanism of detection of the electronic tongue (E-tongue), the bitterness of atomoxetine HCl was evaluated, and it was found that its bitterness was similar to that of quinine HCl. The bitterness threshold of atomoxetine HCl was 8.61 µg/ml based on the Change of membrane Potential caused by Adsorption (CPA) value of the BT0 sensor. In this study, the taste-masking efficiency of 2-hydroxypropyl-β-cyclodextrin (HP-β-CyD) was assessed by Euclidean distances on a principle component analysis (PCA) map with the SA402B Taste Sensing System, and the host–guest interactions were investigated by differential scanning calorimetry (DSC), powder X-ray diffraction (XRD), nuclear magnetic resonance (NMR) spectroscopy and scanning electron microscopy (SEM). Biosensor evaluation and characterization of the inclusion complex indicated that atomoxetine HCl could actively react with 2-hydroxypropyl-β-cyclodextrin.

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Taste masking and rheology improvement of drug complexed with beta-cyclodextrin and hydroxypropyl-β-cyclodextrin by hot-melt extrusion

Cited by 55 publications

References 33 publications

EVALUATION OF ORALLY DISINTEGRATING TABLET OF IBUPROFEN-β-CYCLODEXTRIN INCLUSION COMPLEX

EVALUATION OF ORALLY DISINTEGRATING TABLET OF IBUPROFEN-β-CYCLODEXTRIN INCLUSION COMPLEX

Cyclodextrin complexes: Perspective from drug delivery and formulation

Quantitative prediction of the bitterness of atomoxetine hydrochloride and taste-masked using hydroxypropyl-β-cyclodextrin: A biosensor evaluation and interaction study

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