In Vitro Dissolution Model Can Predict the in Vivo Taste Masking Performance of Coated Multiparticulates

Keeley, Alexander; Teo, Minyi; Ali, Zarina S.; Frost, John S.; Ghimire, Manish; Rajabi‐Siahboomi, Ali R.; Orlu, Mine; Tuleu, Catherine

doi:10.1021/acs.molpharmaceut.9b00060

Cited by 13 publications

(9 citation statements)

References 31 publications

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“…The bespoke flowthrough oral dissolution apparatus was used in a previous study to evaluate chlorphenamine maleate, a bitter BCS class I drug, incorporated in sugar spheres and coated with different technologies and polymer coatings [ 46 ]. In this study, the system could discriminate the taste masking capabilities of the formulations, using taste thresholds generated with the rat BATA model and confirmed with human taste thresholds.…”

Section: Resultsmentioning

confidence: 99%

“…The in vitro method described by Keeley et al [ 46 ] was used to predict the taste of PZQ released from the milled extrudates and printlets in a simulated buccal environment.…”

Section: Methodsmentioning

confidence: 99%

“…It is known from the drug-polymer composition-temperature previously determined by the authors (data not shown) that, at room temperature, 35 wt% PZQ in KOL corresponds to a supersaturated amorphous binary system. Considering that the highest concentration of PZQ (50 wt%) would be sensitive to recrystallisation, in the present study, M 35 Span and M 35 SLS printlets were chosen to be evaluated for taste masking performance using an in vitro biorelevant buccal dissolution method described previously by Keeley et al [46]. M 35 Span and M 35 SLS milled materials before printing released more than 0.2 mg/mL of PZQ in the artificial saliva in the first minute of the experiment (Figure 10a).…”

Section: Dissolution Profilesmentioning

confidence: 99%

“…As shown in Figure 10b, both printlets (M 35 Span and M 35 SLS) were below the threshold of good tolerability of the PZQ and even further below the PZQ IC50 (0.06 mg/mL), indicating that the formulations provided efficient taste masking without the use of additional taste masking excipients. The bespoke flowthrough oral dissolution apparatus was used in a previous study to evaluate chlorphenamine maleate, a bitter BCS class I drug, incorporated in sugar spheres and coated with different technologies and polymer coatings [46]. In this study, the system could discriminate the taste masking capabilities of the formulations, using taste thresholds generated with the rat BATA model and confirmed with human taste thresholds.…”

Section: Dissolution Profilesmentioning

confidence: 99%

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Direct Powder Extrusion 3D Printing of Praziquantel to Overcome Neglected Disease Formulation Challenges in Paediatric Populations

et al. 2021

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For the last 40 years, praziquantel has been the standard treatment for schistosomiasis, a neglected parasitic disease affecting more than 250 million people worldwide. However, there is no suitable paediatric formulation on the market, leading to off-label use and the splitting of commercial tablets for adults. In this study, we use a recently available technology, direct powder extrusion (DPE) three-dimensional printing (3DP), to prepare paediatric Printlets™ (3D printed tablets) of amorphous solid dispersions of praziquantel with Kollidon® VA 64 and surfactants (Span™ 20 or Kolliphor® SLS). Printlets were successfully printed from both pellets and powders obtained from extrudates by hot melt extrusion (HME). In vitro dissolution studies showed a greater than four-fold increase in praziquantel release, due to the formation of amorphous solid dispersions. In vitro palatability data indicated that the printlets were in the range of praziquantel tolerability, highlighting the taste masking capabilities of this technology without the need for additional taste masking excipients. This work has demonstrated the possibility of 3D printing tablets using pellets or powder forms obtained by HME, avoiding the use of filaments in fused deposition modelling 3DP. Moreover, the main formulation hurdles of praziquantel, such as low drug solubility, inadequate taste, and high and variable dose requirements, can be overcome using this technology.

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Section: Resultsmentioning

confidence: 99%

“…The in vitro method described by Keeley et al [ 46 ] was used to predict the taste of PZQ released from the milled extrudates and printlets in a simulated buccal environment.…”

Section: Methodsmentioning

confidence: 99%

Section: Dissolution Profilesmentioning

confidence: 99%

Section: Dissolution Profilesmentioning

confidence: 99%

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Direct Powder Extrusion 3D Printing of Praziquantel to Overcome Neglected Disease Formulation Challenges in Paediatric Populations

et al. 2021

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“…Since the clinical CPM dose is between 1 mg and 4 mg [57], and the average human secretes 1 mL of saliva per minute [58], this threshold is below the clinical dose and therefore taste-masking of this drug is essential. In the literature the human bitterness threshold of CPM was reported to be 0.506 mg/mL or approximately 1.3 mM [59]. This means that the E-tongue is reporting a slightly lower value, which may indicate higher sensitivity compared to in-vivo findings.…”

Section: Bitterness Thresholdmentioning

confidence: 98%

Utilising Co-Axial Electrospinning as a Taste-Masking Technology for Paediatric Drug Delivery

Abdelhakim¹,

Coupe

Tuleu³

et al. 2021

Pharmaceutics

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The present study describes the use of two taste-masking polymers to fabricate a formulation of chlorpheniramine maleate for paediatric administration. Co-axial electrospinning was utilized to create layered nanofibres; the two polymers, Eudragit® E PO and Kollicoat® Smartseal, were alternated between the core and the shell of the system in order to identify the optimum taste-masked formulation. The drug was loaded in the core on all occasions. It was found that the formulation with Kollicoat® Smartseal in the core with the drug, and Eudragit® E PO in the shell showed the most effective taste-masking compared to the other formulations. These fibres were in the nano-range and had smooth morphology as verified by scanning electron microscopy. Solid-state characterization and thermal analysis confirmed that amorphous solid dispersions were formed upon electrospinning. The Insent E-tongue was used to assess the taste-masking efficiency of the samples, and it was found that this formulation was undetectable by the bitter sensor, indicating successful taste-masking compared to the raw version of the drug. The E-tongue also confirmed the drug’s bitterness threshold as compared to quinine HCl dihydrate, a parameter that is useful for formulation design and taste-masking planning.

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Advanced Taste-Masking Methods of Solid Dosage Forms

Bueva,

Blynskaja,

Alekseev

et al. 2023

Pharm Chem J

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In Vitro Dissolution Model Can Predict the in Vivo Taste Masking Performance of Coated Multiparticulates

Abstract: In vitro dissolution model can predict the in vivo taste masking performance of coated multiparticulates

Cited by 13 publications

References 31 publications

Direct Powder Extrusion 3D Printing of Praziquantel to Overcome Neglected Disease Formulation Challenges in Paediatric Populations

Direct Powder Extrusion 3D Printing of Praziquantel to Overcome Neglected Disease Formulation Challenges in Paediatric Populations

Utilising Co-Axial Electrospinning as a Taste-Masking Technology for Paediatric Drug Delivery

Advanced Taste-Masking Methods of Solid Dosage Forms

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