Importance of excipient wettability on tablet characteristics prepared by moisture activated dry granulation (MADG)

Takasaki, Hiroshi; Yonemochi, Etsuo; Messerschmid, Roman; Ito, Masanori; Wada, Koichi; Terada, Katsuhide

doi:10.1016/j.ijpharm.2013.08.027

Cited by 27 publications

(18 citation statements)

References 11 publications

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“…Furthermore, water-soluble PVP K25 also had a substantial reduction in friability compared with the insoluble microcrystalline cellulose (Takasaki et al, 2013).…”

Section: Resultsmentioning

confidence: 99%

Improving the granule strength of roller-compacted ibuprofen sodium for hot-melt coating processing

Lopes

Garsuch

Becker

et al. 2016

International Journal of Pharmaceutics

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“…Furthermore, water-soluble PVP K25 also had a substantial reduction in friability compared with the insoluble microcrystalline cellulose (Takasaki et al, 2013).…”

Section: Resultsmentioning

confidence: 99%

Improving the granule strength of roller-compacted ibuprofen sodium for hot-melt coating processing

Lopes

Garsuch

Becker

et al. 2016

International Journal of Pharmaceutics

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“…Ullah et al described the manufacturability of a high-dose drug formulation (62.5%) using MADG [30] . Tablets produced with the MADG process showed higher tensile strength and faster disintegration compared to tablets produced with high shear granulation [26] .…”

Section: Introductionmentioning

confidence: 90%

The importance of binder moisture content in Metformin HCL high-dose formulations prepared by moist aqueous granulation (MAG)

Takasaki

Yonemochi

Ito

et al. 2015

Results in Pharma Sciences

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The aim of this study was to evaluate binders to improve the flowability of granulates and compactibility of Metformin HCL (Met) using the moist aqueous granulation (MAG) process. The effect of the binder moisture content on granulate and tablet quality was also evaluated. Vinylpyrrolidone–vinyl acetate copolymer (Kollidon VA64 fine: VA64), polyvidone (Povidone K12: PVP), hydroxypropyl cellulose (HPC SSL SF: HPC) and hydroxypropyl methylcellulose (Methocel E5 LV: HPMC) were evaluated as binders. These granulates, except for HPMC, had a lower yield pressure than Met active pharmaceutical ingredient (API). HPMC Met was not sufficiently granulated with low water volume. No problems were observed with the VA64 Met granulates during the tableting process. However, HPC Met granulates had a bowl-forming tendency, and PVP Met granulates had the tendency to stick during the tableting process. These bowl-forming and sticking tendencies may have been due to the low moisture absorbency of HPC and the high volume of bound water of PVP, respectively. VA64 Met granulates had the highest ambient moisture content (bulk water, bound water) and moisture absorbency. It was concluded that the type of binder used for the Met MAG process has an impact on granulate flow and compactibility, as well as moisture absorbency and maintenance of moisture balance.

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“…Thus, it is a suitable binder/disintegrant for moisture sensitive drugs in granulation applications. Regarding colloidal silicon dioxide, most studies claim that it is a highly suitable absorbent for MADG as it has a very low water content [ 18 ]. Finally, sodium stearyl fumarate was preferable as a lubricant in the preparation of ODT because it has a great lubrication effect without obviously reducing other critical tablet attributes, including tablet mechanical strength, disintegration time, and drug release [ 30 ].…”

Section: Methodsmentioning

confidence: 99%

“…This may lead to formation of solid bridges ”necks” among metformin particles that impart mechanical strength, lack powder flow, and sticking issues through the tableting process owing to consequent moisture migration or desorption during the wet granulation process [ 16 , 17 ]. In addition, from an industrial perspective, the wet granulation method is inferior to a direct compression and dry granulation methods because an additional drying step in a separate equipment like fluidized-bed dryer and tray dryer is necessary after the agglomeration phase [ 18 , 19 ]. Furthermore, adhesion of produced granules on granulator walls as well as granule collapse by mechanical stress demonstrate process challenges during the drying stage [ 19 ].…”

Section: Introductionmentioning

confidence: 99%

“…Compared with popular wet granulation methods like high shear granulation (HSG) and fluidized bed granulation (FBG), MADG is considered a promising alternative technique to combine the benefits of HSG, while avoiding the issues associated with the drying step described above [ 18 , 22 ]. Besides, HSG and FBG require the discharge and filling of intermediate granules for cascading the manufacturing process.…”

Section: Introductionmentioning

confidence: 99%

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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

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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.

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Importance of excipient wettability on tablet characteristics prepared by moisture activated dry granulation (MADG)

Cited by 27 publications

References 11 publications

Improving the granule strength of roller-compacted ibuprofen sodium for hot-melt coating processing

Improving the granule strength of roller-compacted ibuprofen sodium for hot-melt coating processing

The importance of binder moisture content in Metformin HCL high-dose formulations prepared by moist aqueous granulation (MAG)

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

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