Quantification of Swelling and Erosion in the Controlled Release of a Poorly Water-Soluble Drug Using Synchrotron X-ray Computed Microtomography

Yin, Xianzhen; Li, Haiyan; Guo, Zhen; Wu, Li; Chen, Fangwei; Matas, Marcel de; Shao, Qun; Xiao, Tiqiao; York, Peter; He, Yeping; Zhang, Jiwen

doi:10.1208/s12248-013-9498-y

Cited by 61 publications

(34 citation statements)

References 27 publications

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“…X-ray microtomography have been explored to study a wide range properties related to pharmaceutical tablets. These include, but not limited to, qualitative and quantitative measurements of tablet density and thickness, determination of tablet shape and size, studying the microstructure of fast-dissolving tablets, monitoring tablet coating process, detecting internal and/or external tablet defects, and uniformity of API distribution in the tablets (Cao et al, 2003;Fu et al, 2006;Hancock and Mullarney, 2005;Liu et al, 2013;Miguélez-Morán et al, 2009;Sinka et al, 2004;Yin et al, 2013). Additionally, this technique has been used to detect counterfeit tablets, and the presence of foreign materials added intentionally or unintentionally during tablet manufacturing (Hancock and Mullarney, 2005).…”

Section: X-ray Microtomographymentioning

confidence: 99%

Emerging technologies for the non-invasive characterization of physical-mechanical properties of tablets

Dave

Shahin

Youngren-Ortiz³

et al. 2017

International Journal of Pharmaceutics

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The density, porosity, breaking force, viscoelastic properties, and the presence or absence of any structural defects or irregularities are important physical-mechanical quality attributes of popular solid dosage forms like tablets. The irregularities associated with these attributes may influence the drug product functionality. Thus, an accurate and efficient characterization of these properties is critical for successful development and manufacturing of a robust tablets. These properties are mainly analyzed and monitored with traditional pharmacopeial and non-pharmacopeial methods. Such methods are associated with several challenges such as lack of spatial resolution, efficiency, or sample-sparing attributes. Recent advances in technology, design, instrumentation, and software have led to the emergence of newer techniques for non-invasive characterization of physical-mechanical properties of tablets. These techniques include near infrared spectroscopy, Raman spectroscopy, X-ray microtomography, nuclear magnetic resonance (NMR) imaging, terahertz pulsed imaging, laser-induced breakdown spectroscopy, and various acoustic- and thermal-based techniques. Such state-of-the-art techniques are currently applied at various stages of development and manufacturing of tablets at industrial scale. Each technique has specific advantages or challenges with respect to operational efficiency and cost, compared to traditional analytical methods. Currently, most of these techniques are used as secondary analytical tools to support the traditional methods in characterizing or monitoring tablet quality attributes. Therefore, further development in the instrumentation and software, and studies on the applications are necessary for their adoption in routine analysis and monitoring of tablet physical-mechanical properties.

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Section: X-ray Microtomographymentioning

confidence: 99%

Emerging technologies for the non-invasive characterization of physical-mechanical properties of tablets

Dave

Shahin

Youngren-Ortiz³

et al. 2017

International Journal of Pharmaceutics

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“…An example of an application can be seen from a study on felodipine sustained release tablets observed at various time points during dissolution [26,28]. In another study, tablet swelling behaviour of various in-house polymeric preparations was investigated over time using SR-CT.…”

Section: Synchrotron Radiation X-ray Com-puted Microtomography (Sr-ct)mentioning

confidence: 99%

Recent Advances in Solid-State Analysis of Pharmaceuticals

Bukhari¹,

Hwei²,

Jantan³

2015

PHARMSCI

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Current analytical techniques for characterizing solid-state pharmaceuticals include powder x-ray diffraction, differential scanning calorimetry, thermogravimetric analysis, infrared spectroscopy, Raman spectroscopy, electron microscopy and nuclear magnetic resonance. Powder x-ray diffraction and differential scanning calorimetry are mainstream techniques but they lack spatial resolution. Scanning electron microscopy and micro-Raman spectroscopy provide good chemical and optical characterization but they are not capable of analysing very small nanoparticles. Transmission electron microscopy and nano-thermal analysis can provide explicit characterization of nanoparticles but they are invasive. Nuclear magnetic resonance offers good spatial resolution but its use is mainly limited by poor sensitivity and high costs. In view of the many challenges posed by existing methods, new and novel techniques are being continually researched and developed to cater to the growing number of solid formulations in the pipeline and in the market. Some of the recent advances attained in the solid-state analysis of pharmaceutical are summarized in this review article.

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“…The rate and mechanism of drug release from solid dosage forms depends strongly on their shape and microstructure (11)(12)(13)(14)(15). Lorck et al found that rough pellets had a higher release rate than smooth pellets after approximately 2 h of release where spherical pellets were classified as smooth, and all other shapes were denoted as rough (11).…”

Section: Introductionmentioning

confidence: 99%

“…The internal micro-structure of pharmaceutical tablets can not only influence mechanical strength but also impact the rate at which APIs are released from some types of dosage forms (12). Our previous studies have shown that the interior porous channels and surface structure were simplified when the fractal dimension correlated well with the drug release kinetics of felodipine osmotic pump tablets (13). For microcrystalline cellulose (MCC)-carbopol pellets with a high proportion of carbopol, the size, shape, mechanical properties and release behaviour can be tuned by modulating the CaCl 2 /carbopol ratio and the drying conditions due to the influence of these variables on the pellet microstructure (14).…”

Section: Introductionmentioning

confidence: 99%

Release Behaviour of Single Pellets and Internal Fine 3D Structural Features Co-define the In Vitro Drug Release Profile

Yang

Yin

Wang

et al. 2014

AAPS J

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Multi-pellet formulations are advantageous for the controlled release of drugs over single-unit dosage forms. To understand the diffusion controlled drug release mechanism, the pellet structure and drug release from a single pellet (not at dose level) were studied using synchrotron radiation X-ray computed microtomography (SR-μCT) and a sensitive LC/MS/MS method. The purpose of this article is to introduce a powerful, non-invasive and quantitative technique for studying individual pellet microstructures and to investigate the relationship between the microstructure and drug release from single pellets. The data from the single pellet dissolution measurements demonstrated that the release profile of capsules containing approximately 1,000 pellets per unit dose was the summation of the release profiles of the individual pellets. The release profiles of single tamsulosin hydrochloride (TSH) pellets formed three groups when a cluster analysis was performed, and the dissolution rate of the individual pellets correlated well with the combined effects of the drug loading, volume and surface area of the pellets (R(2) = 0.9429). In addition, the void microstructures within the pellet were critical during drug release. Therefore, SR-μCT is a powerful tool for quantitatively elucidating the three-dimensional microstructure of the individual pellets; because the microstructure controls drug release, it is an important parameter in the quality control of multi-pellet formulations.

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Quantification of Swelling and Erosion in the Controlled Release of a Poorly Water-Soluble Drug Using Synchrotron X-ray Computed Microtomography

Cited by 61 publications

References 27 publications

Emerging technologies for the non-invasive characterization of physical-mechanical properties of tablets

Emerging technologies for the non-invasive characterization of physical-mechanical properties of tablets

Recent Advances in Solid-State Analysis of Pharmaceuticals

Release Behaviour of Single Pellets and Internal Fine 3D Structural Features Co-define the In Vitro Drug Release Profile

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