• YAKHAK HOEJI
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• v.39 no.4
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• pp.438-443
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• 1995

Four different pseudopolymorphs of amoxicillin-trihydrate, dehydrate, monohydrate and anhydratewere prepared and characterized by UV spectrophotometry, DSC, and TGA. In vitro dissolution studies of four pseudopolymorphs were carried out in pH 6.8 phosphate buffer at $37^{\circ}C$ by means of a rotating disk method. The effect of four pseudopolymorphs on bioavauability of amoxicillin was studied in healthy 6 subjects using urinary excretion method. The dissolution result was shown in the sequence, trihydrate(95.5%)>monohydrate(83.5%)>anhydrate(67.6%)>dihydrate(15.8%). The urinary excretion rate of anhydrate could not be detected and the dissolution results agreed well with in vivo phannacoldnetic study results. The effects of storage conditions, milling and compression on the pseudopolymorpnc transformation were investigated by thermal methods. The results showed that four pseudopolymorphs were not transformed and they were very stable.

• YAKHAK HOEJI
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• v.40 no.3
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• pp.306-310
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• 1996

Five pseudopolymorphic modifications of cefazolin sodium were prepared by recrystallization. They were characterized by DSC and TGA. The solubilities of all modifications were c hecked through the dissolution test.

• Journal of Pharmaceutical Investigation
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• v.34 no.6
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• pp.443-452
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• 2004

Habit is the description of the outer appearance of a crystal. If the environment of a growing crystal affects its external shape without changing its internal structure, a different habit results. Crystal habit and the internal structure of a drug can affect bulk and physicochemical properties, which range from flowability to chemical stability. A polymorph is a solid crystalline phase of a given compound resulting from the possibility of at least two different arrangements of the molecules of that compound in the solid state. Chemical stability and solubility changes due to polymorphism can have an impact on a drug's bioavailability and its development program. During crystallization from a solution, crystals separating may consist of a pure component or be a molecular compound. Solvates are molecular complexes that have incorporated the crystallizing solvent molecule in their lattice. When the solvent incorporated in the solvate is water, it is called a hydrate. To distinguish solvates from polymorphs, which are not molecular compounds, the term pseudopolymorph is used. Identification of possible hydrate compounds is important since their aqueous solubilities can be significantly less than their anhydrous forms. Conversion of an anhydrous compound to a hydrate within the dosage form may reduce the dissolution rate and extent of drug absorption. An amorphous solid may be treated as a supercooled liquid in which the arrangement of molecules is random. Amorphous solids lack the three-dimensional long-range order found in crystalline solids. Since amorphous forms are usually of higher thermodynamic energy than corresponding crystalline forms, solubilities as well as dissolution rates are generally greater. A study on crystal form includes characterization of (l)crystal habit, (2)polymorphism, (3)pseudopolymorphism, (4)amorphous solid.

• YAKHAK HOEJI
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• v.41 no.3
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• pp.321-327
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• 1997

Investigation of polymorphism has become a requirement in the pharmaceutical industry because the physical properties and bioavailabilities of crystalline drugs depend on their polymorphic form. Five polymorphic modifications and one pseudopolymorphic modification of ecphalothin sodium were prepared by recrystallization, and characterized by UV spectrophotometer, DSC, TGA and X-ray crystallography. The solubilities of all modifications were examined by the disslution test. Form 2 and 1 showed higher solubilities than any other crystal forms. The modifications were also investigated for their stability after storage of 2 months at 100%, 76%, 52% and 0% humidity.

• Journal of Pharmaceutical Investigation
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• v.33 no.2
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• pp.99-103
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• 2003

Four different crystal forms of prednisolone, two polymorphic forms and two pseudopolymorphic forms, were obtained by the recrystallization from different organic solvents under varying conditions. The isolated crystal forms were characterized by differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and X-ray powder diffraction (XRD). Form 1 was the most stable form that had the highest melting point and melt at $250.1^{\circ}C$. Form 2 was a monohydrate and Form 3 was a methanol solvate. The endothermic peak of Form 4 was shown at $230.2^{\circ}C$. When stored at different relative humidity over the period of 3 months, all of the modifications did not undergo transformation. The dissolution patterns of these four modifications were also checked in distilled water at $37{\pm}0.5^{\circ}C$, for 120 minutes. The dissolution rate of Form 4 was highest and those of Form 3, Form 2, Form 1 followed. Form 2, Form 3 and Form 4 had higher dissolution rate than Form 1.

• 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.