A novel in vivo predictive dissolution testing coupled with a modeling and simulation for hydrogel matrix monolithic extended release oral dosage forms

Kambayashi, Atsushi; Dressman, Jennifer B.

doi:10.1016/j.ejps.2019.105044

Cited by 7 publications

(7 citation statements)

References 30 publications

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“…As an alternative method, the in vitro determination of the particle size of the dissolved SDs that correlates with in vivo absorption may be useful because the presence of large amorphous particles in dissolved SDs in an aqueous solution has been reported. 25) Furthermore, methods for the investigation of hydrogel formulations and amorphous solid dispersions-in which in vitro biorelevant dissolution testing is coupled with in silico modeling and simulation to predict oral absorption-may be relevant to the current gummi with SD formulations. 26,27) The findings of the current study suggest that PVA 66, PVA 66/88, and PVA 80 are suitable in terms of dissolution, stabil- Each geometric mean ratio between two phases is given with the corresponding 90% confidence interval.…”

Section: Discussionmentioning

confidence: 99%

Gummi Formulations Comprising Amenamevir Solid Dispersions with Polyvinyl Alcohol

Umemoto

Tanaka

Kambayashi

et al. 2021

CHEMICAL & PHARMACEUTICAL BULLETIN

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The aim of the present study was to determine whether solid dispersions (SDs) are applicable to gummi formulations. Amenamevir was selected as a model of a poorly water-soluble drug, and polyvinyl alcohols (PVAs) with various degrees of hydrolysis (PVA 66, PVA 80, PVA 88, and PVA 66/88) were used as SD carriers. Design of experiments (DOE) was used to develop a gummi formulation that was suitable for an amenamevir SD using SD with PVA 66. Dissolution studies and clinical sensory tests on 11 formulations calculated by DOE revealed that a gummi formulation comprising 10.5% gelatin and 22.8% water was suitable for SD of the drug. Gummi formulations comprising amenamevir SDs with various PVAs were prepared using the determined gummi formulation, and their ability to dissolve amenamevir, their stability, and their oral absorption in dogs were evaluated. The results suggested that PVA 66, PVA 66/88, and PVA 80 were appropriate in terms of dissolution, stability, and in vivo absorption, respectively. Considering these results comprehensively, it was concluded that PVA 80, which enabled the highest degree of absorption, was the most suitable SD carrier for gummi formulations. Thus, it was possible to apply a PVA SD of amenamevir to gummi formulations.

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Section: Discussionmentioning

confidence: 99%

Gummi Formulations Comprising Amenamevir Solid Dispersions with Polyvinyl Alcohol

Umemoto

Tanaka

Kambayashi

et al. 2021

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…The good in vitro dissolution apparatus along with modeling has been a good predictive method of the bioperformance for BCS class II drugs to assess its oral absorption because of their high permeability characteristics. 30,46,47 BCS class IIa drugs (pKa~4e5) like ibuprofen of immediate release (IR) dosage forms dissolve well at the pH environment in the small intestine and behave like BCS class I drugs due to the much faster dissolution entering the small intestine. With that reason, BCS class IIa drugs often become biowaiver candidates.…”

Section: Discussionmentioning

confidence: 99%

The Introduction of a New Flexible In Vivo Predictive Dissolution Apparatus, GIS-Alpha (GIS-α), to Study Dissolution Profiles of BCS Class IIb Drugs, Dipyridamole and Ketoconazole

Tsume

Patel

Wang

et al. 2020

Journal of Pharmaceutical Sciences

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“…SR tablets with faster dissolution would be more sensitive to in vitro conditions; accordingly, an original in vitro method with very limited volume of fluid� relevant to the small intestinal lumen�was appropriate for the SR tablet used. 37 Many examples of in vivo performance prediction for lipophilic matrix SR tablets reported to date have used an in vitro USP Apparatus III coupled with an in silico modeling and simulation, 31,34,38 although the C max of a lipophilic matrix SR tablet of diclofenac was significantly overestimated using the approach. 34 This might be because the drugs used in this DDS formulation in these previous studies had pH-dependent solubility, possibly for the same reason as in the hydrophilic matrix SR tablets.…”

Section: Controlled Release Formulations 221 Sustained Release Formul...mentioning

confidence: 99%

In Silico Modeling Approaches Coupled with In Vitro Characterization in Predicting In Vivo Performance of Drug Delivery System Formulations

Kambayashi

2023

Mol. Pharmaceutics

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Optimization of the in vivo performance of dosage forms in humans is essential in developing not only conventional formulations but also drug delivery system (DDS) formulations. Although animal experiments are still useful for these formulations, in silico approaches have become increasingly important for DDS formulations with regard to species-specific differences in physiology that can affect the in vivo performance of dosage forms between animals and humans. Furthermore, it is also important to couple in vitro characterizations with in silico models to predict in vivo performance in humans precisely. In this review article, I summarized in vitro−in silico approaches to predicting the in vivo performance of oral DDS formulations (amorphous solid dispersions, lipid-based formulations, nanosized formulations, cyclodextrins-based formulations, sustained release products, enteric coat products, and orally disintegrating tablets) and parenteral DDS formulations (cyclodextrins-based formulations, liposomes, and inhaled formulations).

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A novel in vivo predictive dissolution testing coupled with a modeling and simulation for hydrogel matrix monolithic extended release oral dosage forms

Cited by 7 publications

References 30 publications

Gummi Formulations Comprising Amenamevir Solid Dispersions with Polyvinyl Alcohol

Gummi Formulations Comprising Amenamevir Solid Dispersions with Polyvinyl Alcohol

The Introduction of a New Flexible In Vivo Predictive Dissolution Apparatus, GIS-Alpha (GIS-α), to Study Dissolution Profiles of BCS Class IIb Drugs, Dipyridamole and Ketoconazole

In Silico Modeling Approaches Coupled with In Vitro Characterization in Predicting In Vivo Performance of Drug Delivery System Formulations

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