Preparation and Evaluation of Solid Dispersion Tablets by a Simple and Manufacturable Wet Granulation Method Using Porous Calcium Silicate

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

doi:10.1248/cpb.c15-00838

Cited by 10 publications

(9 citation statements)

References 27 publications

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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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Section: Introductionmentioning

confidence: 99%

Solubility Enhancement of Ibuprofen by Adsorption onto Spherical Porous Calcium Silicate

2021

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“…Porous Calcium Silicate (PCS) and magnesium aluminosilicate (Neusilin ® ) have huge surface areas and are used as solid dispersion carriers to improve the dissolution of poorly water-soluble drugs [10][11][12]. We reported the development of solid dispersion tablets via a simple and easily manufactured wet granulation method using PCS [13,14]. These materials contain silanol groups and metal ions.…”

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Controlled-Release Solid Dispersion Granules Containing a Poorly Water-Soluble Drug, Hydrated Silicon Dioxide, and Polyvinylpyrrolidone

2019

J Pharm Pharmacol

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The study aim was to develop controlled-release, solid dispersion granules containing a poorly water-soluble drug, Hydrated Silicon Dioxide (HSD), and Polyvinylpyrrolidone (PVP), and to elucidate the mechanism underlyingsustained release from the soliddispersion granules. To achieve this purpose, we used the wet granulation method to prepare the first-release granules containing a poorly water-soluble drug and HSD. Then, the effect of PVP on the dissolution of the poorly water-soluble drug was estimated. Initially, the selection of a binder and contentsof drug and binder were investigated to determine the optimum formulation fora rapidly dissolving granule with HSD. Firstrelease granules containing Nifedipine (NIF) as a poorly water-soluble drug, erythritol as a binder, and HSD were developed. Differential scanning calorimetry confirmed reduced NIF crystallinity in the granules. To investigate the first-release granules' applicabilityto other drugs, six poorly water-soluble drugs (griseofulvin, indomethacin, ibuprofen, carbamazepine, progesterone, and phenytoin) were prepared. Rapid dissolutionof all tested drugs from the granule with the same NIF formulation was observed. These findings suggest that HSD is useful for improving dissolution ratesof poorly water-soluble drugs insoliddispersion granules. Next, we investigated PVP's effect on the dissolution of drug from the first-release granules. The effects of PVP on sustained release from the granules containing the seven drugs weredivided into three types: Type 1 was no effect (rapid dissolution), type 2 was a middle effect, and type 3 was a strong effect (sustained release). To elucidate the mechanism underlying sustained release from the solid dispersion granules, the intermolecular interactions between the drugs and HSD or PVP were investigated by Fourier transform infrared spectroscopy. The results suggested that the balance between the interaction of a drug and HSD and the interaction of a drug and PVP is important for sustained release of the drug.

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“…PCS is also used as a carrier of solid dispersion for improving the dissolution of poorly water-soluble drugs [38][39][40][41]. We previously reported the development of solid dispersion tablets by the simple and manufacturable wet granulation method using PCS [42,43].…”

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluationof Ibuprofen Solid Dispersion Tablets with Improved Dissolution and Less Sticking Using Porous Calcium Silicate

2018

J Pharm Pharmacol

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The aim of this study was to prepare and evaluate Ibuprofen (IBU) solid dispersion tablets with improved dissolution and less sticking using Porous Calcium Silicate (PCS). Solid dispersion granules were prepared using water-based solid dispersion and water-retained PCS with the wet granulation method and a high-speed agitation granulator. We attempted to use four binders [Hydroxypropylcellulose (HPC), dextrin, maltitol, and xylitol] to prepare the granules; however, HPC could not be used. After 1h of continuous tableting using a rotary machine, sticking was estimated by a visual inspection of all tablets and photographs of the upper punches with a digital camera. All prepared tablets demonstrated quick disintegration and dissolution. From the results of DSC and PXRD studies, IBU may exist in an amorphous form in the adsorption solid dispersion and the granules. From FT-IR studies, IBU appears to interact with PCS through a salt formation between the COO-groups of IBU and the Ca2+ ions of PCS. To investigate differences in binders on the sticking problem, DSC, NIR spectra, and bulk density were measured. From these results, we speculated that the primary localization of the specific binder in the PCS pores may differ among binders, with this localization affecting the sticking property.

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Preparation and Evaluation of Solid Dispersion Tablets by a Simple and Manufacturable Wet Granulation Method Using Porous Calcium Silicate

Cited by 10 publications

References 27 publications

Solubility Enhancement of Ibuprofen by Adsorption onto Spherical Porous Calcium Silicate

Solubility Enhancement of Ibuprofen by Adsorption onto Spherical Porous Calcium Silicate

Preparation and Evaluation of Controlled-Release Solid Dispersion Granules Containing a Poorly Water-Soluble Drug, Hydrated Silicon Dioxide, and Polyvinylpyrrolidone

Preparation and Evaluationof Ibuprofen Solid Dispersion Tablets with Improved Dissolution and Less Sticking Using Porous Calcium Silicate

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