Evaluation of the compaction of sulfathiazole polymorphs

Picker‐Freyer, Katharina M.; Liao, Xiangmin; Zhang, Guifang; Wiedmann, Timothy S.

doi:10.1002/jps.21042

Cited by 39 publications

(27 citation statements)

References 24 publications

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“…19 However, the results from this previous study agree with our hypothesis on particle hardness. Based on the discussion above, it is expected that the sulfathiazole form III would have good tablet strength based on its medium particle hardness value of 2.1 GPa.…”

Section: Discussionsupporting

confidence: 89%

“…[10][11][12][13][14] With the rapid development of atomic force microscopy (AFM), AFM nanoindentation has quickly become a very promising technique to assess particle mechanical properties of pharmaceutical materials. [15][16][17][18][19][20] With little material, AFM nanoindentation provides rich information on high-resolution imaging with nanometer spatial resolution and local mechanical studies with nanoNewton forces. 21,22 Previous studies have been conducted in hopes to predict powder compaction performance using microor nanoindentation.…”

Section: Introductionmentioning

confidence: 99%

“…24 Additionally, a recent study on tableting performance of sulfathiazole polymorphs found little correspondence between the microscopic and macroscopic measurements. 19 It has been shown that correlating particle mechanical properties with powder compaction performance is a very complicated issue. Moreover, the lack of data on particle mechanical properties hinders establishment of such correlation.…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Correlating Particle Hardness with Powder Compaction Performance

Cao

Morganti

Hancock

et al. 2010

Journal of Pharmaceutical Sciences

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Section: Discussionsupporting

confidence: 89%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Correlating Particle Hardness with Powder Compaction Performance

Cao

Morganti

Hancock

et al. 2010

Journal of Pharmaceutical Sciences

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“…17,18) Takeuchi et al reported that Lac particles had a strong tendency to fragment. 4) Eriksson and Alderborn observed that particles of the fragmenting materials would break down during compression and size reduction would occur.…”

Section: Resultsmentioning

confidence: 99%

Differences in Powder Properties of Two 1,4-Dihydropyridine-Type Compounds Evaluated through Thermal Analysis

Hosaka¹,

Tokunaga²

2017

CHEMICAL & PHARMACEUTICAL BULLETIN

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The powder properties of two 1,4-dihydropyridine type compounds, manidipine dihydrochloride (Man) and benidipine hydrochloride (Ben), which possess similar physicochemical properties, were compared through thermal and mechanical analyses. Man and Ben were compressed with lactose monohydrate (Lac) and magnesium stearate (Mgst) at different compression forces. As an index, we focused on the onset temperatures of Lac dehydration during thermal analysis and plotted them against compression forces to evaluate the differences in powder properties between Man and Ben. To discuss in detail, the Lac ratio was selected as a formulation factor and compression speed as a process factor, which would be influenced to the onset temperature or its profile. It could be represented that Man was more adherent than Ben through thermal analysis by changing these critical factors, which were consistent with the results obtained through mechanical analysis.Key words compression; powder property; crystal water; thermal analysis; fragmentation 1,4-Dihydropyridine-type compounds such as nifedipine and nicardipine hydrochloride are frequently prescribed calcium channel antagonists with antihypertensive activity. Manidipine dihydrochloride (Man) and benidipine hydrochloride (Ben) have been shown to be more potent and longeracting than previous generations of 1,4-dihydropyridines. 1,2)In a generic company, a series of medicinal compounds with a similar structure are developed as generic products. Accordingly, an approach with which to compare powder properties with the information about the crystallinity is desirable for formulation and process studies. In some papers, compression properties have been discussed by analyzing compaction parameters.3-8) The information obtained from these studies is useful for formulation development with appropriate tablet hardness and forecasting tableting trouble (capping or sticking tendency) at a commercial scale. However, information about the crystallinity of the compressed materials has not been considered. A comparison of powder properties considering the crystallinity of the compressed materials through thermal analysis has not yet been conducted in the pharmaceutical field.In a series of our research, 9-13) it could be speculated that Man was more adherent than Ben through thermal analysis considering the crystallinity of compressed lactose (Lac) with different levels of particle size. The goals of this study are as follows: 1) To find critical factors other than Lac particle size for discussing the differences in powder properties between Man and Ben through thermal analysis. 2) To confirm the differences in powder properties between Man and Ben through mechanical analysis as we have speculated before. ExperimentalMaterials Man (Sanyo Chemical Laboratories Co., Ltd., Japan); Ben (Daito Pharmaceutical Co., Ltd., Japan); two types of Lac, Pharmatose ® 200M (DMV, the Netherlands), and Dilactose ® R (Freund Sangyo, Japan); and magnesium stearate (Mgst, Taihei Kagaku, Japan) were used for the preparatio...

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“…Other drawbacks of these bulk methods include the influence of porosity, particle size and shape, and potential changes in mechanical properties due to the compaction process, resulting in large variations in reported data. Recently, AFM nanoindentation studies have been employed to study pharmaceutical materials such as lactose [47], sucrose [48], sodium stearate [49], acetaminophen [50] and sulfathiazole [51]. These studies reported the particle hardness data and showed the potential applications of AFM nanoindentation to pharmaceutical research.…”

Section: Pharmaceutical Investigationmentioning

confidence: 99%

Study of Atomic Force Microscopy in Pharmaceutical and Biopharmaceutical Interactions - A Mini Review

Veerapandian¹,

Yun

2009

CPA

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The atomic force microscope (AFM) is the subject of numerous papers and reports and is full of promises for nanoscience and nanotechnological applications. Pharmaceutical and biopharmaceutical studies using AFM have been functionalized during last two decades. Since, its invention in 1986, the number of published articles has considerably increased. Owing to its unique ability to not only image but also probe mechanical and chemical properties with sub nanometer resolution under physiological condition made it an attractive tool. It can be relatively easily operated in fluids, and thus experiments can be conducted under nearly physiological conditions, which pace its numerous applications in biological problems. In the field of pharmaceutical sciences, AFM presents a unique opportunity to study a variety of phenomena at the cellular and sub cellular level, down to individual (macro) molecular complexes. These advantages of AFM allowed the advent invention of fabrication variables, dynamic processes, drug structure-function relationships, in real time. This article reviews the study of AFM to investigate the crystal growth, polymorphism, particles, granules and coating morphology of solid dosage form for optimization of pharmaceutical behaviors. It also highlights the in situ biopharmaceutical investigation of cell-macromolecular surface, drug-drug, drug-cell, drug-DNA, DNA-protein, drugenzyme and antigen-antibody interactions, and disease mechanisms to understand the better physiological mechanisms associated with disease to rationalize the drug design and development.

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Evaluation of the compaction of sulfathiazole polymorphs

Cited by 39 publications

References 24 publications

Correlating Particle Hardness with Powder Compaction Performance

Correlating Particle Hardness with Powder Compaction Performance

Differences in Powder Properties of Two 1,4-Dihydropyridine-Type Compounds Evaluated through Thermal Analysis

Study of Atomic Force Microscopy in Pharmaceutical and Biopharmaceutical Interactions - A Mini Review

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