Examining mechanical properties of various pharmaceutical excipients with the gravitation-based high-velocity compaction analysis method

Co-amorphous mixtures have rarely been formulated as oral dosage forms, even though they have been shown to stabilize amorphous drugs in the solid state and enhance the dissolution properties of poorly soluble drugs.In the present study we formulated tablets consisting of either spray dried co-amorphous ibuprofenarginine or indomethacin-arginine, mannitol or xylitol and polyvinylpyrrolidone K30 (PVP).Experimental design was used for the selection of tablet compositions, and the effect of tablet composition on tablet characteristics was modelled. Multimodal non-linear imaging, including coherent anti-Stokes Raman scattering (CARS) and sum frequency/second harmonic generation (SFG/SHG) microscopies, as well as scanning electron microscopy, X-ray diffractometry and Fourier-transform infrared spectroscopy were utilized to characterize the tablets.The tablets possessed sufficient strength, but modelling produced no clear evidence about the compaction characteristics of co-amorphous salts. However, co-amorphous drug-arginine mixtures resulted in enhanced dissolution behaviour, and the PVP in the tableting mixture stabilized the supersaturation. The co-amorphous mixtures were physically stable during compaction, but the excipient selection affected the long term stability of the ibuprofen-arginine mixture. CARS and SFG/SHG proved feasible techniques in imaging the component distribution on the tablet surfaces, but possibly due to the limited imaging area, recrystallization detected with x-ray diffraction was not detected.

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“…According to Tanner et al [52], elastic recovery values between inelastic (e.g. glucose or calcium hydrogen phosphate) and highly elastic (e.g.…”

Section: Mechanical Propertiesmentioning

confidence: 99%

Preparation and characterization of multi-component tablets containing co-amorphous salts: Combining multimodal non-linear optical imaging with established analytical methods

Ojarinta

Saarinen

Strachan

et al. 2018

European Journal of Pharmaceutics and Biopharmaceutics

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“…Lactose is a crystalline solid behaving within defined physical properties during tablet manufacture. It can be compressed close to its true density and due to the hard nature of lactose it can be consolidated well [15] . Therefore, it is necessary to convert MS closer to the better defined properties of crystalline lactose for it to perform well as a substitute for lactose.…”

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confidence: 99%

Dextrinized Maize Starch-Maize Starch Combination as Exclusive Fillers in Tablet Manufacture

Sabalingam¹,

Dharmawansha²,

Wijayabandara³

et al. 2019

ijps

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Sabalingam et al.: Dextrinized Starch-starch as Exclusive Tablet Fillers Traditional tablet filler combinations, lactose-maize starch were replaced with a new dextrinized maize starch-maize starch filler combination. Dextrinization process under controlled conditions was targeted for this purpose and specifications were determined for the dextrinized product. Granules were prepared by wet granulation method using the new filler combination. Placebo tablets T1 were first prepared with lactose-maize starch filler combination as a model. Based on the properties of resulting tablets, lactose was replaced with dextrinized maize starch, introduced a different binder and the active ingredient furosemide anticipating a tablet of acceptable quality. The flow properties of dextrinized maize starch had improved over maize starch with an angle of repose of 40°. Hausner ratio and Carr's index of dextrinized maize starch and lactose were found to be 1.34, 1.54, and 25.45, 35.24 %, respectively favourable to the former. The placebo tablets (T2) prepared with the new filler combination using 12.0 % w/w maize starch binder resulted in unacceptable hardness and friability. However, furosemide tablets (T3) prepared with the new filler combination and the binder solution of low substituted hydroxypropyl cellulose 3.2 % w/w showed excellent physical properties. The study shows that dextrinized maize starch and maize starch filler combination without lactose could be employed successfully in tablet manufacture.

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Predicting tablet tensile strength with a model derived from the gravitation-based high-velocity compaction analysis data

Tanner

Antikainen

Pollet

et al. 2019

International Journal of Pharmaceutics

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Examining mechanical properties of various pharmaceutical excipients with the gravitation-based high-velocity compaction analysis method

Cited by 10 publications

References 32 publications

Preparation and characterization of multi-component tablets containing co-amorphous salts: Combining multimodal non-linear optical imaging with established analytical methods

Preparation and characterization of multi-component tablets containing co-amorphous salts: Combining multimodal non-linear optical imaging with established analytical methods

Dextrinized Maize Starch-Maize Starch Combination as Exclusive Fillers in Tablet Manufacture

Predicting tablet tensile strength with a model derived from the gravitation-based high-velocity compaction analysis data

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