Novel tablet formulation of amorphous indomethacin using wet granulation with a high-speed mixer granulator combined with porous calcium silicate

Fujimoto, Yumi; Hirai, Nobuaki; Takatani‐Nakase, Tomoka; Takahashi, Kyoko

doi:10.1016/j.jddst.2016.03.001

Cited by 17 publications

(16 citation statements)

References 28 publications

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“…For instance, mechanical strength during roller compaction or moisture content during wet granulation has a huge impact on the stability and on the release of the amorphous API; therefore investigating the trace crystallinity is very important in these cases. Successful roller compaction of evacetrapib-loaded ASDs and wet granulation of indomethacine-loaded ASDs proves the feasibility of the granulation processes in this field [85,86]. However, it is important to note that a feeding step is also needed before continuous granulation thus this kind of flowability enhancement is usually used before the tableting and not before the blending [87].…”

Section: Feeding As the Key Step During The Continuous Formulation Ofmentioning

confidence: 99%

Continuous Formulation Approaches of Amorphous Solid Dispersions: Significance of Powder Flow Properties and Feeding Performance

et al. 2019

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Preparation and formulation of amorphous solid dispersions (ASDs) are becoming more and more popular in the pharmaceutical field because the dissolution of poorly water-soluble drugs can be effectively improved this way, which can lead to increased bioavailability in many cases. During downstream processing of ASDs, technologists need to keep in mind both traditional challenges and the newest trends. In the last decade, the pharmaceutical industry began to display considerable interest in continuous processing, which can be explained with their potential advantages such as smaller footprint, easier scale-up, and more consistent product, better quality and quality assurance. Continuous downstream processing of drug-loaded ASDs opens new ways for automatic operation. Therefore, the formulation of poorly water-soluble drugs may be more effective and safe. However, developments can be challenging due to the poor flowability and feeding properties of ASDs. Consequently, this review pays special attention to these characteristics since the feeding of the components greatly influences the content uniformity in the final dosage form. The main purpose of this paper is to summarize the most important steps of the possible ASD-based continuous downstream processes in order to give a clear overview of current course lines and future perspectives.

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Section: Feeding As the Key Step During The Continuous Formulation Ofmentioning

confidence: 99%

Continuous Formulation Approaches of Amorphous Solid Dispersions: Significance of Powder Flow Properties and Feeding Performance

et al. 2019

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“…8,74 The result of increased drug dissolution caused by PCS was also found in other studies. 75 Furthermore, FLR could even improve the solubility of drugs. Kinoshita et al 72 studied the dissolution characteristics of 3-bis(4-methoxyphenyl) methylene-2-indolinone (TAS-301) aer it was melt-adsorbed on FLR.…”

Section: Porous Calcium Silicate (Pcs)mentioning

confidence: 99%

“…Additionally, low-density PCS may blend nonuniformly with other materials due to marked differences in density. 75 So, novel techniques should be adopted to improve the bulk density of PCS.…”

Section: Porous Calcium Silicate (Pcs)mentioning

confidence: 99%

Design and pharmaceutical applications of porous particles

et al. 2017

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“…Problems can occur if used for oral dosage tablets because FLR is difficult to handle due to its low flowability and high dustiness. Some recent studies have reported that granules including FLR, and poorly water-soluble drugs can be prepared by the wet granulation method to improve the low flowability [ 39 , 40 , 41 ]. Florite ® PS300 (PS300) was developed in response to these problems, and its shape is spherical.…”

Section: Introductionmentioning

confidence: 99%

Solubility Enhancement of Ibuprofen by Adsorption onto Spherical Porous Calcium Silicate

2021

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The solubility of a drug is higher when it is in an amorphous form than when it is in a crystalline form. To enhance the solubility of ibuprofen (IBU), a poorly water-soluble drug, we attempted to adsorb IBU onto spherical porous calcium silicate (Florite® PS300, PS300) in two ways: the evaporation (EV) and sealed heating (SH) methods. The crystallinity of the samples was evaluated using powder X-ray diffraction analysis (PXRD) and differential scanning calorimetry (DSC). The molecular interaction between IBU and PS300 was evaluated with FTIR. In addition, the dissolution behavior of IBU in the samples was assessed by the dissolution test. Based on the results of the PXRD and DSC measurements, both methods allowed adsorption of IBU onto PS300, and IBU was amorphized. Based on the FTIR observations, in the SH or EV mixtures containing 10% and 30% IBU, respectively, it seemed that the IBU molecules intermolecularly interacted with calcium molecules as the main component of PS300. Improvement in the solubility of IBU was observed with both methods; however, the dissolution rate of IBU from samples prepared via SH was higher than that from EV, or of IBU crystals. Collectively, our findings indicate that the petal-like structure of PS300, which has a spherical shape and good flowability, is an effective tool for adsorbing IBU onto PS300 via SH.

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Novel tablet formulation of amorphous indomethacin using wet granulation with a high-speed mixer granulator combined with porous calcium silicate

Cited by 17 publications

References 28 publications

Continuous Formulation Approaches of Amorphous Solid Dispersions: Significance of Powder Flow Properties and Feeding Performance

Continuous Formulation Approaches of Amorphous Solid Dispersions: Significance of Powder Flow Properties and Feeding Performance

Design and pharmaceutical applications of porous particles

Solubility Enhancement of Ibuprofen by Adsorption onto Spherical Porous Calcium Silicate

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