Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine

Ali, Joseph; Zgair, Atheer; Hameed, Ghaidaa S.; Garnett, Martin C.; Roberts, Clive J.; Gershkovich, Pavel

doi:10.1016/j.ijpharm.2018.11.051

Cited by 16 publications

(5 citation statements)

References 43 publications

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“…Therefore, different methods to be applied for the invitro bioavailability testing for samples in the oral cavity. 33 As a result, dissolution was performed in FaSSGF and FaSSIF solutions only.…”

Section: Assaymentioning

confidence: 99%

Comparative Study of Dissolution for Cannabidiol in EU and US Hemp Oil Products by HPLC

Analakkattillam

Langsi²,

Hanrahan³

et al. 2021

Journal of Pharmaceutical Sciences

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Section: Assaymentioning

confidence: 99%

Comparative Study of Dissolution for Cannabidiol in EU and US Hemp Oil Products by HPLC

Analakkattillam

Langsi²,

Hanrahan³

et al. 2021

Journal of Pharmaceutical Sciences

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“…Using data from the BT0 sensor, the bitterness threshold of CPM was calculated to be 1.2 mM or 0.47 mg/mL, meaning any concentration above this point is expected to exert a bitterness response by the person tasting it, and therefore requires taste-masking. 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].…”

Section: Bitterness Thresholdmentioning

confidence: 99%

“…Pharmaceutics 2021, 13, x FOR PEER REVIEW 19 of 23 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.…”

Section: Formulations Taste-assessmentmentioning

confidence: 99%

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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“…RUP loading was in the range from 0.4 to 0.5 mg-the lowest values were marked for F8, F12, F16 and they did not meet pharmacopoeial requirements (<85%) [25]. Disintegration time tests, conducted under conditions imitating those prevailing in the oral cavity (2-7 mL) are recommended [50][51][52][53], therefore tests in vivo with healthy volunteers, on petri dishes and using a texture analyzer were utilized. Regardless of the method, disintegration time of all ODMT formulations was below 30 s, and most formulations disintegrated even below 15 s. The longest disintegration time was recorded for F13, F14, F15, F16-19-24 s. In all tablets, wetting time below 30 s was noted.…”

Section: Pharmaceutical Evaluation Of Odmtmentioning

confidence: 99%

Utilization of Ethylcellulose Microparticles with Rupatadine Fumarate in Designing Orodispersible Minitablets with Taste Masking Effect

et al. 2020

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Minitablets in orodispersible form constitute a flexible drug delivery tool for paediatric and geriatric population as they eliminate the risk of chocking and do not require drinking water in the application. Due to their direct contact with taste buds, taste sensation is an important factor. Preparing microparticles with taste masking polymers utilizing spray drying is an efficient technique for reducing the bitterness of drugs. Ethylcellulose is a hydrophobic polymer widely used as a taste masking material. Rupatadine fumarate, one of the newest antihistamines, features an intensive bitter taste, hence in designing orodispersible formulations, achieving an acceptable taste is a crucial issue. The main objective of this work was to formulate orodispersible minitablets containing taste masked ethylcellulose-based microparticles with rupatadine fumarate and evaluation of their quality, especially in terms of taste masking efficacy. The accessed data indicated that all obtained minitablets were characterized by beneficial pharmaceutical properties. Three independent methods: in vivo with healthy volunteers, in vitro drug dissolution, and “electronic tongue” confirmed that all designed formulations provided satisfactory taste masking rate and that formulation F15 (prepared with Pearlitol® Flash and Surelease® microparticles with rupatadine fumarate) was characterized by the lowest bitterness score.

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Application of biorelevant saliva-based dissolution for optimisation of orally disintegrating formulations of felodipine

Cited by 16 publications

References 43 publications

Comparative Study of Dissolution for Cannabidiol in EU and US Hemp Oil Products by HPLC

Comparative Study of Dissolution for Cannabidiol in EU and US Hemp Oil Products by HPLC

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

Utilization of Ethylcellulose Microparticles with Rupatadine Fumarate in Designing Orodispersible Minitablets with Taste Masking Effect

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