Four new polymorphic forms of suplatast tosilate

Nagai, Keiko; Ushio, Takanori; Miura, Hidenori; Nakamura, Takashi; Moribe, Kunikazu; Yamamoto, Keiji

doi:10.1016/j.ijpharm.2013.10.049

Cited by 10 publications

(5 citation statements)

References 32 publications

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“…Different hydrogen bonding modes may affect the crystals in many compounds, such as barbiturate derivatives, sulfonamides, and oxalic acid [252627]; thus, the occurrence of hydrogen bonds in the two valnemulin hydrogen tartrate polymorphs was assessed by comparing the IR spectra of Form I and Form II. As discussed in the theoretical study of geometries of valnemulin salts included in our previous work [14], there is hydrogen bonding between the valnemulin molecule and the tartaric acid molecule as –C=O (tartaric acid) … H–N (valnemulin).…”

Section: Discussionmentioning

confidence: 99%

“…Due to different crystallization conditions: such as solvents, temperature, pressure, and pseudoseeding with a crystal, different polymorphs may be obtained and which can have different arrangements of the molecule in the crystal [2628]. Moreover, polymorphic solids can have different chemical and physical properties and pharmaceutical effects.…”

Section: Discussionmentioning

confidence: 99%

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Preparation, characterization, and in vivo evaluation of a polymorphic form of valnemulin hydrogen tartrate

Zhu

et al. 2019

J Vet Sci

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We prepared a polymorphic form of valnemulin hydrogen tartrate (Form I) to overcome the instability and irritating odor of valnemulin hydrochloride that affect its use in the production and application of veterinary drugs. The physicochemical properties of Form I were characterized by scanning electron microscopy, X-ray powder diffraction, infrared spectroscopy, differential scanning calorimetry, and thermogravimetric analysis. The results showed the crystal structure and thermal properties of Form I were very different from those of a commercially available form of valnemulin hydrogen tartrate (Form II). Form I and Form II were more stable than valnemulin hydrochloride after storage under irradiation and high humidity conditions, respectively. The solubility of Form I was 2.6 times that of Form II, and Form I was selected for use in pharmaceutical kinetics experiments in vivo . Compared to valnemulin hydrochloride, after oral administration at a dose of 10 mg/kg in pigs, Form I had similar pharmaceutical kinetic behavior but a slightly higher area under the concentration–time curve from time zero to the last measurable concentration. Consequently, Form I should be suitable for the development of simple formulations and be effective in the clinical application of veterinary drugs.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Preparation, characterization, and in vivo evaluation of a polymorphic form of valnemulin hydrogen tartrate

Zhu

et al. 2019

J Vet Sci

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“…The difference in crystal structure is due to the variation of intermolecular interactions between the molecules, resulting in alternative packing arrangements and leading to the occurrence of a new polymorph. [6] To tackle the challenge of polymorphism, a number of variables need to be considered, which represents an opportunity to produce new forms with improved physicochemical properties. The ultimate aim of crystallization is to produce a certain texture of the crystal to make the product acceptable.…”

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

A New Polymorphic Form of Maltol: Crystallization and Structure Refinement

Srinivasan,

Karuppannan

2024

Cryst. Res. Technol.

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A new polymorph of maltol, a food and intermediate pharmaceutical material, is discovered through solution crystallization process using a mixed solvent of water and ethanol with l‐menthol as an additive. It belongs to monoclinic crystal system with lattice parameters: a = 7.136(8) Å, b = 24.23(3) Å, c = 7.020(8) Å, and β = 106.22(3)°, volume = 1165 (2) Å3 and the refinement factor is R = 6.64%. With single crystal X‐ray diffraction (SCXRD) data as input, the intermolecular interactions between the new polymorph of maltol is investigated through Hirshfeld surface analysis, the higher percentage of overall interaction between the polymorph (H…H) interaction, and the (O…H) interaction contributes more to the generation of new polymorph. The 2D finger print plot depicts the interactions are mainly due to the hydrogen bonds.

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“…Polymorphism of a drug compound usually results from the possibility of at least two different spatial arrangements of the molecules in the crystal lattice, or in some cases, from variations in molecular conformation, including crystalline and amorphous forms as well as solvate and hydrate forms [1][2][3][4].…”

Section: Introductionmentioning

confidence: 99%

A New Hemihydrate of Valacyclovir Hydrochloride

et al. 2017

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Several crystal forms of valacyclovir hydrochloride, including two anhydrous and three hydrates, were investigated in this study. At the same time, a new hemihydrate of valacyclovir hydrochloride was first discovered and its properties were characterized by PXRD, TGA, DSC, and Raman in this study. The hemihydrate shows a distinctive PXRD pattern and a melting point of 209 • C with a water weight loss of 2.42% from the thermal analysis. The Raman spectra show a few distinctive peaks in the region of 1250-1400 cm −1 due to different crystal forms. The thermostability testing suggests it is a stable crystal form and remain the same for several months under high temperature and humidity. All these crystal forms show good dissolubility in the water at room temperature with excess 100 mg/mL.

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Four new polymorphic forms of suplatast tosilate

Cited by 10 publications

References 32 publications

Preparation, characterization, and in vivo evaluation of a polymorphic form of valnemulin hydrogen tartrate

Preparation, characterization, and in vivo evaluation of a polymorphic form of valnemulin hydrogen tartrate

A New Polymorphic Form of Maltol: Crystallization and Structure Refinement

A New Hemihydrate of Valacyclovir Hydrochloride

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