• Journal of Pharmaceutical Investigation
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• v.41 no.6
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• pp.371-376
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• 2011

The objective of this work was to investigate the existence of new crystal forms of tulobuterol which is used to prevent morning asthma attacks by ${\beta}_2$ agonist and the transformation of crystal forms. Three crystal forms of tulobuterol have been isolated by recrystallization and Form 2 was transformed to Form 4 at 52% RH and 95% RH and these four crystal forms are characterized by differential scanning calorimetry (DSC), powder X-ray diffractometry (PXRD) and thermogravimetric analysis (TG). The DSC and PXRD patterns of four crystal forms of tulobuterol were different respectively. The dissolution patterns of these three crystal forms of tulobuterol were studied and they showed significant differences in the dissolution rate. After storage of 2 months at 0% RH (silica gel, $20^{\circ}C$), 52% RH (saturated solution of $Na_2Cr_2O_7{\cdot}2H_2O/20^{\circ}C$) and 95% RH (saturated solution of $Na_2HPO_4/20^{\circ}C$), Form 1 and Form 3 were not transformed. But Form 2 was transformed to Form 4 at 52% RH and 95% RH.

• Journal of Pharmaceutical Investigation
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• v.39 no.3
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• pp.173-176
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• 2009

A new crystal form of valsartan dipotassium was isolated by recrystallization using the one-pot method. The new crystal form was identified as a monohydrate form ($C_{24}H_{27}N_5O_3K_2.H_2O$) and characterized by diffential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and X-ray powder diffractometry (PXRD). The new crystal data demonstrated to be clearly different from those known for the tetrahydrate form ($C_{24}H_{27}N_5O_3K_2.4H_2O$). It was observed that the monohydrate of vasartan dipotassium salt was completely dissolved in water within 1 hour and its dissolution rate was much faster than anhydrous free form of valsartan.

• Archives of Pharmacal Research
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• v.25 no.4
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• pp.556-559
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• 2002

The aim of this study was to gain information on the effects of the crystal form of corticosteroids on the topical anti-inflammatory activity. Two different crystal forms, Form A and Form B, of the drugs of prednicarbate, hydrocortisone, betamethasone 17-valerate, prednisolone, and methyl prednisolone were prepared and their topical anti-inflammatory activities were measured using arachidonic acid induced ear edema assay in mice. Two crystal forms of the drugs showed differences in anti-inflammatory activity. Among the drugs examined, Form B of prednicarbate and betamethasone 17-valerate showed significantly more potent anti-inflammatory activities as compared to their Form A.

• YAKHAK HOEJI
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• v.40 no.5
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• pp.513-521
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• 1996

The polymorphism of piroxicam was studied. Form I, II, III and monohydrate designated as Form IX were prepared by recrystallization from different solvents. Depending on the coo ling rate of the piroxicam melt, Form IV, V, VI, VII and VIII were prepared. The crystal forms were characterized by DTA, TGA and UV spectroscopy. Their dissolution patterns were also investigated. During storage at ambient condition. Form VIII was transformed into Form I and it was accelerated by milling. The other crystal forms were also transformed into Form I by milling. Form I and Form IX were very stable.

• Archives of Pharmacal Research
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• v.29 no.2
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• pp.178-182
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• 2006

Four crystal forms of cephradine were isolated by recrystallization and characterized by powder X-ray diffractometry, differential scanning calorimetry, and thermogravimetric analysis. The dissolution patterns of four crystal forms of cephradine were studied in water at $37{\pm}0.5^{\circ}C$, 90 rpm for 120 min. The amount dissolved at 120 min was highest for Form 1 ($100\%$), followed by Form 3 ($98.9\%$), Form 4 ($77.83\%$), and Form 2 ($75.55\%$). After storage for two months at $0\%$ RH (silica gel, $20^{\circ}C$), $52\%$ RH (saturated solution of $Na_{2}Cr_{2}O_{7}{\cdot}2H_{2}O/20^{\circ}C$), and $95\%$ RH (saturated solution of $Na_{2}HPO_{4}/20^{\circ}C$), none of the crystal forms showed transformation.

• Journal of the Korean Chemical Society
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• v.63 no.1
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• pp.7-11
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• 2019

Olmutinib, N-[3-({2-[4-(4-methylpiperazine-1-yl)aniline]thieno[3,2-d]Pyrimidin-4-yl}oxy)phenyl]prop-2-enamide dihydrochloride monohydrate, $Olita^{TM}$ is an oral, third-generation epidermal growth factor receptor tyrosine kinase inhibitor (EGFR TKI) that was developed by Boehringer Ingelheim and Hanmi Pharmaceutical Co. Ltd for the treatment of non-small cell lung cancer (NSCLC). The aim of this work was to investigate the existence of polymorphs and pseudopolymorphs of olmutinib. Three crystal forms of olmutinib have been isolated by recrystallization and characterized by differential scanning calorimetry (DSC), thermogravimetric (TG) analysis and powder X-ray diffractometry (PXRD). From the DSC and TG data it was confirmed that Form 1 is monohydrate, Form 2 is dihydrate, Form 3 is 1.5 hydrate. The PXRD patterns of three crystal forms were different respectively. After storage of 1 month at $2^{\circ}C$, 24% RH (Relative Humidity), Form 1, Form 2, and Form 3 were not transformed.

• Journal of the Korean Ceramic Society
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• v.50 no.2
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• pp.116-121
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• 2013

Zinc crystal glaze has its limits in practical use of commercial glaze due to the controlling crystal. In order to overcome this limit, and to heighten the practical usage, this study is aimed to develop artificially controlling willemite ($Zn_2SiO_4$) zinc crystalline glaze. For this purpose, it has experimented with the effect of anatase form and rutile form using $TiO_2$ known as nucleating agent. In zinc glaze, adding $TiO_2$ resulted with anatase form becoming more effective at nucleating formation and growth of willemite than the rutile form. Furthermore, it turned out that using the $TiO_2$ - anatase form, with synthetic seeds (zinc silicate), the numbers and positions of crystals can be controlled artificially.

• Journal of the Korean Chemical Society
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• v.62 no.5
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• pp.352-357
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• 2018

Celecoxib (4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide) is a cyclooxygenase-2 inhibitor used in the treatment of arthritis, acute pain, and dysmenorrhoea. Celecoxib is a Biopharmaceutics Classification System (BCS) class II compound whose oral bioavailability is highly limited owing to its poor aqueous solubility. Several polymorphs of celecoxib have been identified as Form I, Form II, and Form III with melting points of about $162.8^{\circ}C$, $161.5^{\circ}C$, and $160.8^{\circ}C$, respectively. Form IV was generated from the precipitated suspension in the presence of HPMC (Hydroxypropyl methylcellulose) and Polysorbate 80. A rapid rate of dissolution is useful because the rate of dissolution of a drug typically increases its bioavailability. The aim of this study was to investigate the possibility of production of new crystal form of celecoxib that has higher solubility than Form III. New crystal form of celecoxib (Form A) has been isolated by recrystallization and characterized by differential scanning calorimetry (DSC), thermogravimetric (TG) analysis and powder X-ray diffractometry (PXRD). Form A was dissolved faster than Form III. At 30 minutes, the dissolution of Form A was 97.3%, whereas the dissolution of Form III was 82.2% (p < 0.1). After storage of three months at $20^{\circ}C$, in 24% RH (Relative Humidity), the crystal form was not transformed.

• Journal of Pharmaceutical Investigation
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• v.28 no.2
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• pp.81-85
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• 1998

Three polymorphic modifications and two pseudopolymorphic modifications of cefotaxime sodium were obtained by crystallization from different organic solvents. The isolated crystal forms were characterized by UV spectrophotometry, DSC, TGA and X-ray crystallography. Crystal forms of cefotaxime sodium were also compared by dissolution rate. The dissolution rate of form 1 was the highest, followed by form 2, form 4, form 6, form 5 and form 3. Among these polymorphic modifications the dissolution rate of form 3 and form 5 was much slower than that of cefotaxime sodium on the market. All forms showed no change after 2-month storage test in the silica gel desiccator. But after the storage of 2-month at 95% relative humidity condition, all forms were deliquesced by hygroscopic property except form 1 that showed the highest dissolution rate. At 52% relative humidity condition, form 1, form 2 and form 6 had no evidence of phase transformation, but form 3, form 4 and form 5 were also deliquesced.

• Journal of Pharmaceutical Investigation
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• v.39 no.2
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• pp.117-120
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• 2009

Two crystal forms of ziprasidone have been isolated by recrystallization from different organic solvents and characterized by differential scanning calorimetry, powder X-ray diffractometry and thermogravimetric analysis. It was confirmed that Form 2 has the same crystal structure as Form 1.