Gummi Formulations Comprising Amenamevir Solid Dispersions with Polyvinyl Alcohol

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...

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Published inChemical & pharmaceutical bulletin Vol. 69; no. 9; pp. 862 - 871
Main Authors Umemoto, Yoshiaki, Tanaka, Shimako, Kambayashi, Atsushi, Sugimoto, Koki, Kashiwagura, Yasuharu, Namiki, Noriyuki, Uchida, Shinya
Format Journal Article
LanguageEnglish
Published Tokyo The Pharmaceutical Society of Japan 01.09.2021
Japan Science and Technology Agency
Subjects
Absorption
amenamevir
Design of experiments
Dispersions
Dissolution
dog
Gelatin
gummi formulation
In vivo methods and tests
Polyvinyl alcohol
solid dispersion
Stability analysis
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Abstract 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.
AbstractList 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.
ArticleNumber c21-00278
Author Umemoto, Yoshiaki
Namiki, Noriyuki
Kambayashi, Atsushi
Uchida, Shinya
Tanaka, Shimako
Sugimoto, Koki
Kashiwagura, Yasuharu
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SubjectTerms Absorption
amenamevir
Design of experiments
Dispersions
Dissolution
dog
Gelatin
gummi formulation
In vivo methods and tests
Polyvinyl alcohol
solid dispersion
Stability analysis
Title Gummi Formulations Comprising Amenamevir Solid Dispersions with Polyvinyl Alcohol
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