Polymorphism of Pradofloxacin: Crystal Structure Analysis, Stability Study, and Phase Transformation Behavior

Li, Wenlei; Zhou, Lina; Tian, Beiqian; Chen, Kui; Feng, Yaoguang; Wang, Ting; Wang, Na; Huang, Xin; Hao, Hongxun

doi:10.1007/s11095-023-03509-w

Cited by 9 publications

(3 citation statements)

References 36 publications

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“…The crystalline form of the drug varies with hydration, resulting in differences in the dissolution rate and solubility, and affecting bioavailability [ 23 ]. Purification of a stable crystalline form is a steady process with good reproducibility [ 24 ]. Jet milling is a process of reducing the particle size by particle–wall collisions using high-velocity jets [ 25 ].…”

Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Inhalable Amifostine Microparticles Using Wet Ball Milling

et al. 2023

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The conventional dosage form of Ethyol® (amifostine), a sterile lyophilized powder, involves reconstituting it with 9.7 mL of sterile 0.9% sodium chloride in accordance with the United States Pharmacopeia specifications for intravenous infusion. The purpose of this study was to develop inhalable microparticles of amifostine (AMF) and compare the physicochemical properties and inhalation efficiency of AMF microparticles prepared by different methods (jet milling and wet ball milling) and different solvents (methanol, ethanol, chloroform, and toluene). Inhalable microparticles of AMF dry powder were prepared using a wet ball-milling process with polar and non-polar solvents to improve their efficacy when delivered through the pulmonary route. The wet ball-milling process was performed as follows: AMF (10 g), zirconia balls (50 g), and solvent (20 mL) were mixed and placed in a cylindrical stainless-steel jar. Wet ball milling was performed at 400 rpm for 15 min. The physicochemical properties and aerodynamic characteristics of the prepared samples were evaluated. The physicochemical properties of wet-ball-milled microparticles (WBM-M and WBM-E) using polar solvents were confirmed. Aerodynamic characterization was not used to measure the % fine particle fraction (% FPF) value in the raw AMF. The % FPF value of JM was 26.9 ± 5.8%. The % FPF values of the wet-ball-milled microparticles WBM-M and WBM-E prepared using polar solvents were 34.5 ± 0.2% and 27.9 ± 0.7%, respectively; while the % FPF values of the wet-ball-milled microparticles WBM-C and WBM-T prepared using non-polar solvents were 45.5 ± 0.6% and 44.7 ± 0.3%, respectively. Using a non-polar solvent in the wet ball-milling process resulted in a more homogeneous and stable crystal form of the fine AMF powder than using a polar solvent.

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Section: Introductionmentioning

confidence: 99%

Preparation and Evaluation of Inhalable Amifostine Microparticles Using Wet Ball Milling

et al. 2023

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“…To answer these questions, crystals were grown in a variety of apolar, polar aprotic, and polar protic solvents. Solvatomorphism − was observed in compounds 1 and 2 , and polymorphism was revealed in compounds 3 and 4 . The dominant synthon observed in all four molecules is the LLD.…”

Section: Introductionmentioning

confidence: 95%

A Peptoid-like Approach Led to Lactam–Lactam Dimer Formation in 2-Hydroxy-N-alkyl-N-phenyl-nicotinamides and Their Polymorphism and Solvatomorphism

Gao,

Li,

Zhoujin

et al. 2023

ACS Omega

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“…Active pharmaceutical ingredients (APIs) might have a variety of solid forms, including polymorphs, solvates, cocrystals, salts, and amorphous forms . API molecules in different solid forms may adopt different conformations or spatial configurations, resulting in different fundamental physical properties, such as Gibbs free energy, solubility, melting point, density, stability, shape, color, etc. − Differences in these properties for different solid forms may further lead to significant differences in pharmaceutical properties of the same API, such as dissolution, bioavailability, tabletability, and flowability. − Moreover, these different solid forms can also undergo unidirectional or bidirectional transformation under certain conditions (temperature, pressure, humidity, solvent environment, etc. ), which may result in the failure of the drug or even toxic side effects. ,,− Therefore, it is important to study and master the transformation process of solid forms of APIs in detail during drug development, production, and transportation.…”

Section: Introductionmentioning

confidence: 99%

Mechanistic Study on the Effect of Solvents on Polymorphic Transformation of Aripiprazole by Solvent Property Parameters and Molecular Dynamics Simulation

Zheng,

Huang,

Wang

et al. 2024

Crystal Growth & Design

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The choice of solvent is crucial in the drug crystallization process, and the mechanism of solvent effect on the crystallization results can be conducive to the selection of solvents. In this work, the effect of solvents on the suspension crystallization process of Aripiprazole (APZ) was explored by generalized solvent property parameters and molecular dynamics simulation. Eight different crystal products of APZ (Form III, Form IV, Form V, and five solvates) were obtained after suspension crystallization in 15 different solvents, in which APZ semiethylene glycol solvate (S EG ) is one newly discovered product, and its crystal structure was elucidated. Besides, the crystal transformation processes were studied using molecular dynamics simulations. Conformational search was also adopted to investigate the formation mechanisms of different forms. The results indicated that van der Waals interactions between the solute and solvents dominate the conformations of the APZ molecules in the solvents and further influence the crystal form of the products. However, the polymorphism of APZ in solvents with similar van der Waals interactions may also be different, suggesting that other solvent properties also influence the polymorphism results. Thus, the solvent property parameters were analyzed in detail, and the results indicated that in addition to the van der Waals interaction energy between the solvent molecules and the APZ molecules, the hydrogen bond donor propensity, the volume, the sphericity, and the cohesive energy density of the solvent molecules are also decisive for the suspension crystallization results of APZ. Finally, the mechanism of the effects of solvents species on the suspension crystallization results was proposed and discussed.

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Polymorphism of Pradofloxacin: Crystal Structure Analysis, Stability Study, and Phase Transformation Behavior

Cited by 9 publications

References 36 publications

Preparation and Evaluation of Inhalable Amifostine Microparticles Using Wet Ball Milling

Preparation and Evaluation of Inhalable Amifostine Microparticles Using Wet Ball Milling

A Peptoid-like Approach Led to Lactam–Lactam Dimer Formation in 2-Hydroxy-N-alkyl-N-phenyl-nicotinamides and Their Polymorphism and Solvatomorphism

Mechanistic Study on the Effect of Solvents on Polymorphic Transformation of Aripiprazole by Solvent Property Parameters and Molecular Dynamics Simulation

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