Polymorphism of thiamine hydrochloride. II. Crystal structure of thiamine hydrochloride hemihydrate and its stability.

Watanabe, Atsushi; Tasaki, Saburo; Wada, Yutaka; Nakamachi, Hideo

doi:10.1248/cpb.27.2751

Cited by 28 publications

(28 citation statements)

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“…Due to the complexity of solid-state reaction, the stability-indicating kinetic interpretation has been fully discussed in only a few reports (1,7,8). differential scanning calorimetry (4,5), and X-ray powder diffractometry (7,8). differential scanning calorimetry (4,5), and X-ray powder diffractometry (7,8).…”

mentioning

confidence: 99%

Kinetic Study of the Polymorphic Transformations of Phenylbutazone

Matsuda

Tatsumi

Chiba

et al. 1984

Journal of Pharmaceutical Sciences

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mentioning

confidence: 99%

Kinetic Study of the Polymorphic Transformations of Phenylbutazone

Matsuda

Tatsumi

Chiba

et al. 1984

Journal of Pharmaceutical Sciences

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“…2) Since it was assumed that the crystalline transformation from form I to form II under various temperature and humidity conditions in the present experiments also followed the Prout-Tompkins equation, curve fitting of the Prout-Tompkins equation was performed as reported by Watanabe et al, 2) and the kinetic constant of the crystalline transformation was calculated (Table 2).…”

Section: Resultsmentioning

confidence: 99%

“…Pseudo-Crystalline Transformation Behavior from Form I to Form II At the beginning of this experiment, the crystal forms of those materials were checked by XRPD for according to the XRPD patterns of form I and form II on the previous reports, [2][3][4] and solid state NMR for the purity of crystal forms. In this result, those materials were confirmed form I and form II, and had good crystal purity.…”

Section: Resultsmentioning

confidence: 99%

“…6,7) It was reported that the pseudo-crystalline transformation from form I to form II occurs when form I is stored for a long time under usual laboratory conditions, in a wet granulation process, in a slurry wash with water, or under specific conditions of 40°C and 75% relative humidity (RH). 2,8) However, the elucidation of the rate of the pseudo-crystalline transformation depending on storage conditions was lacking. The present study was therefore undertaken to examine the pseudo-crystalline transformation behavior from form I to form II in detail, including kinetic analysis by varying the storage conditions of temperature and humidity.…”

mentioning

confidence: 99%

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Study of the Pseudo-Crystalline Transformation from Form I to Form II of Thiamine Hydrochloride (Vitamin B1)

Masuda¹,

Ishige²,

Yamada³

et al. 2011

CHEMICAL & PHARMACEUTICAL BULLETIN

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There are three types of pseudo-polycrystalline forms of thiamine hydrochloride (vitamin B 1 ): form I (monohydrate); form II (hemihydrate); and form III (anhydrate). These crystal structures were elucidated using single-crystal X-ray structural analysis, form I by Kraut and Reed in 1962, 1) form II by Watanabe et al. in 1979, 2) and form III by Te et al. in 2003. 3) Since then, there have been various reports on the physiochemical properties of these pseudo-polycrystalline forms. 4,5) The relationship between form I (monohydrate) and form III (anhydrate) is that of the enantiotropic transformation accompanying changes in the hydration state. The pseudo-crystalline transformation from form I to form III is achieved by drying, and form III returns to form I by rehydration. The reversibility of form I and form III as well as the dehydration behavior of form II were reported in detail based on each crystal structure. 6,7) It was reported that the pseudo-crystalline transformation from form I to form II occurs when form I is stored for a long time under usual laboratory conditions, in a wet granulation process, in a slurry wash with water, or under specific conditions of 40°C and 75% relative humidity (RH). 2,8) However, the elucidation of the rate of the pseudo-crystalline transformation depending on storage conditions was lacking. The present study was therefore undertaken to examine the pseudo-crystalline transformation behavior from form I to form II in detail, including kinetic analysis by varying the storage conditions of temperature and humidity. In addition, we aimed to determine whether the rate was affected by formulation with establishing the most appropriate method to detect small amounts of the crystalline polymorph in tablets.As part of the evaluation of the quality of tablets, which are the final product, the evaluation of crystalline forms of drug substances is important in the quality control of pharmaceutical products. Even if the crystalline form of drug substances in a tablet changes, it is not easy to confirm small amounts of crystalline change in drug substances when combined with various excipients. In this study, we observed changes in the crystalline forms of thiamine hydrochloride in tablets using the synchrotron X-ray powder diffraction (XRPD) method which allows sensitive measurement with parallel bright X-ray beams. We have optimized the methodology of synchrotron XRPD to detect small amount of the drug substance. The detection rate using this methodology is equivalent to about 0.02% of the amount of drug substances in a common size tablet. The details of this methodology will be published separately in the near future. In addition to the high sensitivity, it should be emphasized that the XRPD method is a non-destructive inspection, and the whole tablets can be used as specimen without grinding preparation by utilizing the advantage of highly brilliant and parallel synchrotron radiation. ExperimentalMaterials Form I thiamine hydrochloride crystals were purchased from Sigma Chemical (...

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“…[63] Diese Stoffeigenschaft wurde schon in frühen Studien erkannt. [63] Diese Stoffeigenschaft wurde schon in frühen Studien erkannt.…”

Section: Herausforderungenunclassified

Einhundert Jahre Vitamine – eine naturwissenschaftliche Erfolgsgeschichte

et al. 2012

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Die Entdeckung der Vitamine als lebenswichtige Verbindungen in der Nahrung vor 100 Jahren stellte einen wissenschaftlichen Durchbruch dar, der die Welt veränderte. Die Erkenntnis, dass sich früher weit verbreitete Krankheiten wie Skorbut, Pellagra, Rachitis und Beriberi durch eine ausgewogene Ernährung vermeiden oder heilen lassen, hatte einschneidende Auswirkungen auf Gesellschaft und wirtschaftliche Entwicklung. Dieser Aufsatz fasst Schlüsselerfolge in Entwicklung und industrieller Herstellung von acht der insgesamt dreizehn Vitamine zusammen.

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Polymorphism of thiamine hydrochloride. II. Crystal structure of thiamine hydrochloride hemihydrate and its stability.

Cited by 28 publications

References 0 publications

Kinetic Study of the Polymorphic Transformations of Phenylbutazone

Kinetic Study of the Polymorphic Transformations of Phenylbutazone

Study of the Pseudo-Crystalline Transformation from Form I to Form II of Thiamine Hydrochloride (Vitamin B1)

Einhundert Jahre Vitamine – eine naturwissenschaftliche Erfolgsgeschichte

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