Discrimination of ranitidine hydrochloride crystals using X-ray micro-computed tomography for the evaluation of three-dimensional spatial distribution in solid dosage forms

Yamamoto, Eiichi; Takeda, Yoshihiro; Ando, Daisuke; Koide, Tatsuo; Amano, Yuta; Miyazaki, Shingo; Miyazaki, Tamaki; Izutsu, Ken‐ichi; Kanazawa, Hideko; Goda, Yukihiro

doi:10.1016/j.ijpharm.2021.120834

Cited by 14 publications

(10 citation statements)

References 31 publications

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“…31) The obtained crystal was analyzed using pXRD to confirm the polymorphic form. 11,12,14,32,33) The HPLC purity of each crystal form exceeded 99.6% at a UV wavelength of 235 nm.…”

Section: Preparation Of Ranitidine Polymorphsmentioning

confidence: 99%

“…9) Crystal forms of ranitidine hydrochloride have been identified using discriminatory methods, such as diffuse reflectance IR Fourier transform spectroscopy (DRIFTS), Raman spectroscopy, optical microscopy, differential scanning calorimetry (DSC), scanning electron microscopy (SEM), scXRD, and pXRD. 2,[10][11][12] Analyses of ranitidine hydrochloride and its crystal forms using SSNMR methods, including 13 C and 14 N onedimensional (1D) and 1 H-15 N 2D analyses, have also been reported. 13,14) However, the intermolecular correlations in the crystalline state have not been examined.…”

Section: Chemical and Pharmaceutical Bulletin Advance Publicationmentioning

confidence: 99%

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Advanced Solid-State NMR Analysis of Two Crystal Forms of Ranitidine Hydrochloride: Detection of 1H–14N Intra-/Intermolecular Correlations

Yokoo

Tanaka²,

Yamamoto³

et al. 2023

CHEMICAL & PHARMACEUTICAL BULLETIN

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Understanding the characteristics of crystal polymorphism of active pharmaceutical ingredients and analyzing them with high sensitivity is important for quality of drug products, appropriate characterization strategies, and appropriate screening and selection processes. However, there are few methods to measure intra-and intermolecular correlations in crystals other than X-ray crystallography, for which it is sometimes difficult to obtain suitable single crystals. Recently, solid-state NMR has been recognized as a straightforward method for measuring molecular correlations. In this study, we selected ranitidine hydrochloride, which is known to exist in two forms, 1 and 2, as the model drug and investigated each form using solid-state NMR. In conducting the analysis, rotating the sample tube, which had a 1-mm inner diameter, increased the solid-state NMR resolution at 70 kHz. The 1 H-14 N dipolar heteronuclear multiple-quantum coherence (D-HMQC) analysis revealed the intermolecular correlation of Form 1 between the N atom of the nitro group and a proton of the furan moiety, which were closer than those of the intramolecular correlation reported using single X-ray crystal analysis.Thus, 1 H-14 N D-HMQC analysis could be useful for characterizing intermolecular interaction in ranitidine hydrochloride crystals. In addition, we reassigned the 13 C solidstate NMR signals of ranitidine hydrochloride according to the liquid-state and multiple solid-state NMR experiments.

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“…31) The obtained crystal was analyzed using pXRD to confirm the polymorphic form. 11,12,14,32,33) The HPLC purity of each crystal form exceeded 99.6% at a UV wavelength of 235 nm.…”

Section: Preparation Of Ranitidine Polymorphsmentioning

confidence: 99%

Section: Chemical and Pharmaceutical Bulletin Advance Publicationmentioning

confidence: 99%

Advanced Solid-State NMR Analysis of Two Crystal Forms of Ranitidine Hydrochloride: Detection of 1H–14N Intra-/Intermolecular Correlations

Yokoo

Tanaka²,

Yamamoto³

et al. 2023

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…The identification of crystal forms of ranitidine and visualization of their 3D spatial distribution in tablets was realized using X-μCT and Raman spectroscopy. 6 In general, the intensity of X-ray attenuates after penetrating through a material, and the extent of attenuation is proportional to the electron density of specific materials. Typically, the gray-scale value of the image obtained through X-μCT indicates the attenuation extent.…”

Section: Study Of Pellets and Microsphere Preparationmentioning

confidence: 99%

“…Aside from investigating the deformation procedure of crystal particles, the discrimination of drug polymorphs could also be achieved utilizing X-μCT. The identification of crystal forms of ranitidine and visualization of their 3D spatial distribution in tablets was realized using X-μCT and Raman spectroscopy . In general, the intensity of X-ray attenuates after penetrating through a material, and the extent of attenuation is proportional to the electron density of specific materials.…”

Section: Discovery Of 3d Structures In Ddssmentioning

confidence: 99%

“…Fortunately, many advanced tools and techniques have been developed in the last few decades that have been incorporated into DDSs’ 3D structure research, such as computed tomography (CT), − magnetic resonance imaging (MRI), , terahertz (THz) imaging, − etc. Compared to traditional characterization techniques and methods that characterize DDSs perfectly from one-dimensional (1D) or two-dimensional (2D), the 3D structure information enables researchers to observe and comprehend the underlying laws determining the ultimate performance of DDSs more completely and accurately.…”

Section: Introductionmentioning

confidence: 99%

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Advances in Structure Pharmaceutics from Discovery to Evaluation and Design

Xue

et al. 2023

Mol. Pharmaceutics

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Drug delivery systems (DDSs) play an important role in delivering active pharmaceutical ingredients (APIs) to targeted sites with a predesigned release pattern. The chemical and biological properties of APIs and excipients have been extensively studied for their contribution to DDS quality and effectiveness; however, the structural characteristics of DDSs have not been adequately explored. Structure pharmaceutics involves the study of the structure of DDSs, especially the three-dimensional (3D) structures, and its interaction with the physiological and pathological structure of organisms, possibly influencing their release kinetics and targeting abilities. A systematic overview of the structures of a variety of dosage forms, such as tablets, granules, pellets, microspheres, powders, and nanoparticles, is presented. Moreover, the influence of structures on the release and targeting capability of DDSs has also been discussed, especially the in vitro and in vivo release correlation and the structure-based organ- and tumor-targeting capabilities of particles with different structures. Additionally, an in-depth discussion is provided regarding the application of structural strategies in the DDSs design and evaluation. Furthermore, some of the most frequently used characterization techniques in structure pharmaceutics are briefly described along with their potential future applications.

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High-resolution X-ray computed tomography for identifying herbal medicines was as effective as microscopic examination

Tokumoto,

Uchiyama,

Ito

2024

J Nat Med

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Discrimination of ranitidine hydrochloride crystals using X-ray micro-computed tomography for the evaluation of three-dimensional spatial distribution in solid dosage forms

Cited by 14 publications

References 31 publications

Advanced Solid-State NMR Analysis of Two Crystal Forms of Ranitidine Hydrochloride: Detection of <sup>1</sup>H–<sup>14</sup>N Intra-/Intermolecular Correlations

Advanced Solid-State NMR Analysis of Two Crystal Forms of Ranitidine Hydrochloride: Detection of <sup>1</sup>H–<sup>14</sup>N Intra-/Intermolecular Correlations

Advances in Structure Pharmaceutics from Discovery to Evaluation and Design

High-resolution X-ray computed tomography for identifying herbal medicines was as effective as microscopic examination

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