Importance of free water in controlling granule and tablet properties in a novel granulation method, green fluidized bed granulation (GFBG)

Takasaki, Hiroshi; Sakurai, Atsushi; Katayama, Tadao C.; Matsuura, Yuji; Ohyagi, Naoko; Mizoguchi, Masashi; Takano, Jyunichi; Wada, Koichi; Matsui, Koh; Nagato, Takuya; Ishikawa, Agata; Yonemochi, Etsuo

doi:10.1016/j.ijpharm.2019.118647

Cited by 7 publications

(16 citation statements)

References 28 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…This gelatinization activated the binding properties of starch, leading to an increase in the granule size [ 36 ]. Takasaki et al reported that the main mechanism for granulation using MADG is binding between particles in the presence of mechanical shear [ 37 ].…”

Section: Resultsmentioning

confidence: 99%

Design, Optimization, and Correlation of In Vitro/In Vivo Disintegration of Novel Fast Orally Disintegrating Tablet of High Dose Metformin Hydrochloride Using Moisture Activated Dry Granulation Process and Quality by Design Approach

et al. 2020

View full text Add to dashboard Cite

Compression of cohesive, poorly compactable, and high-dose metformin hydrochloride into the orally disintegrating tablet (ODT) is challenging. The objective of this study was to develop metformin ODT using the moisture activated dry granulation (MADG) process. There are no reports in the literature regarding the development of ODT based on MADG technology. The feasibility of developing metformin ODT was assessed utilizing a 32 full factorial design to elucidate the influence of water amount (X1) and the amount of pregelatinized starch (PGS; X2) as independent variables on key granules and tablets’ characteristics. The prepared granules and tablets were characterized for granule size, bulk density, flow properties, tablets’ weight variation, breaking force, friability, capping tendency, in vitro and in vivo disintegration, and drug release. Regression analysis showed that X1 and X2 had a significant (p ≤ 0.05) impact on key granules and tablets’ properties with a predominant effect of the water amount. Otherwise, the amount of PGS had a pronounced effect on tablet disintegration. Optimized ODT was found to show better mechanical strength, low friability, and short disintegration time in the oral cavity. Finally, this technique is expected to provide better ODT for many kinds of high-dose drugs that can improve the quality of life of patients.

show abstract

Section: Resultsmentioning

confidence: 99%

Design, Optimization, and Correlation of In Vitro/In Vivo Disintegration of Novel Fast Orally Disintegrating Tablet of High Dose Metformin Hydrochloride Using Moisture Activated Dry Granulation Process and Quality by Design Approach

et al. 2020

View full text Add to dashboard Cite

show abstract

“…The batch size was 700 g. The details of the manufacturing conditions of GFBG have been described in our previous study. 21) Briefly, APAP, lactose monohydrate, and polypividone were placed into a fluidized bed granulator and blended for 1 min. Pre-blended mixtures were granulated with sprayed water.…”

Section: Methodsmentioning

confidence: 99%

“…Moreover, tablets prepared with GFBG granules showed the fastest disintegration compared to those with MADG, FBG, and HSG. 21) In terms of tensile strength and disintegration time, GFBG showed a wider acceptable range in the amount of added water than that of MADG. 22) These results indicate that GFBG is a simple and eco-friendly manufacturing process compared to the classical wet granulation process, achieving good granule and tablet properties and reducing the undesirable characteristics of APIs such as high cohesivity and low compaction properties.…”

Section: Introductionmentioning

confidence: 93%

“…8,[13][14][15][16][17][18][19][20] We have reported a new granulation technology, green fluidized bed granulation (GFBG), which applies the concept of MADG to a conventional fluidized bed granulator. 21) The disadvantage of the conventional fluidized bed granulation (FBG) process is that it requires a longer granulation time. According to a previous study, 21) GFBG took 15 min to prepare the final mixture, whereas conventional FBG took 107 min, because GFBG uses a lower amount of granulation water without a heating process.…”

Section: Introductionmentioning

confidence: 99%

“…21) The disadvantage of the conventional fluidized bed granulation (FBG) process is that it requires a longer granulation time. According to a previous study, 21) GFBG took 15 min to prepare the final mixture, whereas conventional FBG took 107 min, because GFBG uses a lower amount of granulation water without a heating process. Hence, GFBG could be considered an ecofriendly wet granulation technology.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Manufacturability and Properties of Granules and Tablets Using the Eco-Friendly Granulation Method Green Fluidized Bed Granulation Compared to Direct Compression

et al. 2021

Self Cite

View full text Add to dashboard Cite

This study aimed to compare the manufacturability and granule and tablet properties of green fluidized bed granulation (GFBG) and of direct compression (DC). Acetaminophen was used as a low compactability model drug. The process time of GFBG to produce final mixtures was comparable to that of DC, and thus GFBG could be considered a simple process. DC could not produce 30% drug load tablets owing to poor granule flowability, whereas no problems were observed in the GFBG tableting process up to 80% of drug load. Tablets prepared with GFBG showed higher tensile strength than those prepared using DC. Compactability evaluation results show that the yield pressure of the granules prepared with GFBG was significantly lower than that of DC, suggesting that the granules prepared with GFBG were easily plastically deformed. Moreover, tablets prepared with GFBG showed fast disintegration, which was faster than that of DC. We conclude that GFBG produces granules with higher drug content and desired physicochemical properties at low cost.

show abstract

Time-domain NMR analysis for the determination of water content in pharmaceutical ingredients and wet granules

Ohgi

Hayashi

Tsuji

et al. 2021

International Journal of Pharmaceutics

View full text Add to dashboard Cite

Importance of free water in controlling granule and tablet properties in a novel granulation method, green fluidized bed granulation (GFBG)

Cited by 7 publications

References 28 publications

Design, Optimization, and Correlation of In Vitro/In Vivo Disintegration of Novel Fast Orally Disintegrating Tablet of High Dose Metformin Hydrochloride Using Moisture Activated Dry Granulation Process and Quality by Design Approach

Design, Optimization, and Correlation of In Vitro/In Vivo Disintegration of Novel Fast Orally Disintegrating Tablet of High Dose Metformin Hydrochloride Using Moisture Activated Dry Granulation Process and Quality by Design Approach

Manufacturability and Properties of Granules and Tablets Using the Eco-Friendly Granulation Method Green Fluidized Bed Granulation Compared to Direct Compression

Time-domain NMR analysis for the determination of water content in pharmaceutical ingredients and wet granules

Contact Info

Product

Resources

About