Preparation and Dissolution Profiles of the Amorphous, Dihydrated Crystalline, and Anhydrous Crystalline Forms of Paclitaxel

Pyo, Sang‐Hyun; Jinsuk, Cho; Choi, Ho-Joon; Han, Byung-Hee

doi:10.1080/07373930701593180

Cited by 13 publications

(5 citation statements)

References 17 publications

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“…This phenomenon has been reported before. 18 As expected, DSC analysis showed that the anhydrous paclitaxel exhibited a sharp melting point at ca. 225 • C. 19 The water-exposed paclitaxel nonfragmented sample also displayed this melting endotherm, indicating presence of anhydrous paclitaxel.…”

Section: Resultsmentioning

confidence: 83%

“…19 Anhydrous and dihydrate paclitaxel demonstrated different XRD patterns, suggesting that a polymorphic transformation occurred upon hydration of anhydrous paclitaxel. 18,19 . Five new peaks (6.2, 9.8, 11.2, 13.3, and 16.7), which were all absent in the anhydrous paclitaxel, appeared in the water-exposed control, laser-fragmented, and dihydrate samples, thus suggesting partial hydration of paclitaxel.…”

Section: Resultsmentioning

confidence: 99%

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Fabrication of Paclitaxel Nanocrystals by Femtosecond Laser Ablation and Fragmentation

Kenth

Sylvestre

Fuhrmann

et al. 2011

Journal of Pharmaceutical Sciences

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Section: Resultsmentioning

confidence: 83%

Section: Resultsmentioning

confidence: 99%

Fabrication of Paclitaxel Nanocrystals by Femtosecond Laser Ablation and Fragmentation

Kenth

Sylvestre

Fuhrmann

et al. 2011

Journal of Pharmaceutical Sciences

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“…The formation (i.e., amorphous or crystalline) of an API is a very important specification, having a great impact on the solubility, dissolution rate, uniformity of drug dispersion, and bioavailability of the final drug product during the formulation process [11][12][13]. In this respect, the development of a method that easily enables formation control of a purified API can be very useful for the production of the final drug product, especially in the formulation process [14,15]. However, an efficient method of easily and conveniently controlling the formation of paclitaxel as an API has not yet been developed, and related studies have provided insufficient information.…”

Section: Introductionmentioning

confidence: 99%

Establishment of a solvent map for formation of crystalline and amorphous paclitaxel by solvent evaporation process

Yoon

Kim

2011

Korean J. Chem. Eng.

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This study intended to establish a solvent map for formation of crystalline and amorphous paclitaxel by a solvent evaporation process. Crystalline paclitaxel was produced by evaporation with polar solvents (acetone, acetonitrile, ethanol, isobutyl alcohol, methanol, methyl ethyl ketone, and n-butyl alcohol) having a polarity index above 4.00. On the other hand, amorphous paclitaxel was produced by evaporation with non-polar solvents (methylene chloride, n-butyl chloride, and toluene) having a polarity index of about 4.00 or lower. The formation of paclitaxel was very closely associated with the polarity index of the organic solvent used in the solvent evaporation process. In the case of crystalline paclitaxel, the higher the polarity index and the lower the viscosity of the organic solvent (n-butyl alcohol, methyl ethyl ketone, and acetonitrile), the higher the degree of crystallinity. In the case of amorphous paclitaxel, the shape and size of particles varied according to the solvent (methylene chloride, n-butyl chloride, and toluene) used in the solvent evaporation process.

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“…Therefore, modification of API characteristics to achieve the most optimal process for pharmaceutical purposes have been applied. Several strategies such as new polymorph form ( 3 ), salt formation ( 4 ), cocrystalization ( 5 ), an amorphous system ( 6 ), nanoparticles ( 7 ), hydration/solvation ( 8 ), solid dispersion ( 9 ), and inclusion complex ( 10 ) for API modification have been tried to overcome solubility problems ( 11 ).…”

Section: Introductionmentioning

confidence: 99%

Synthesis, characterization, and stability study of desloratadine multicomponent crystal formation

Ainurofiq¹,

Mauludin²,

Mudhakir³

et al. 2018

Res Pharma Sci

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This study describes the formation of multicomponent crystal (MCC) of desloratadine (DES). The objective of this study was to discover the new pharmaceutical MCC of DES using several coformers. The MCC synthesis was performed between DES and 26 coformers using an equimolar ratio with a solvent evaporation technique. The selection of the appropriate solvent was carried out using 12 solvents. The preview of the MCC of DES was performed using polarized light microscopy (PLM). The formation of MCC was confirmed using powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC), fourier transform infrared spectroscopy (FTIR), and scanning electron microscopy (SEM). The accelerated stability of MCC at 40 °C and relative humidity of 75% was investigated using PXRD and FTIR. Depending on the prior evaluation, DES and benzoic acid (BA) formed the MCC. PLM and SEM results showed that crystal habit of combination between DES and BA differed from the constituent components. Moreover, the diffractogram pattern of DES-BA was distinct from the constituent components. The DSC thermogram showed a new peak which was distinct from both constituent components. The FTIR study proved a new spectrum. All characterizations indicated that a new solid crystal was formed, ensuring the MCC formation. In addition, DES-BA MCC had both chemical and physical stabilities for a period of 4 months.

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Preparation and Dissolution Profiles of the Amorphous, Dihydrated Crystalline, and Anhydrous Crystalline Forms of Paclitaxel

Cited by 13 publications

References 17 publications

Fabrication of Paclitaxel Nanocrystals by Femtosecond Laser Ablation and Fragmentation

Fabrication of Paclitaxel Nanocrystals by Femtosecond Laser Ablation and Fragmentation

Establishment of a solvent map for formation of crystalline and amorphous paclitaxel by solvent evaporation process

Synthesis, characterization, and stability study of desloratadine multicomponent crystal formation

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