CHANGES IN PHYSICOCHEMICAL CHARACTERISTICS AND IMPROVED DISSOLUTION OF POORLY WATER SOLUBLE DRUGS VIA SOLID DISPERSIONS WITH WATER SOLUBLE AND POROUS CARRIER
作成者 Okonogi, Siriporn
キーワード等 DISSOLUTION, OFLOXACIN, SOLID DISPERSION, URSODEOXY CHOLIC ACID
日本十進分類法 (NDC) 499.6
抄録:This study was coped with the behaviors of drug molecules in solid dispersion systems using water soluble and porous carriers. Various techniques such as melting method, solvent method and heat treatment method were used in the preparation of solid dispersions. Physicochemical properties of solid dispersions were characterized using differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD) and infrared (IR) spectroscopy. Dissolution study of the solid dispersion obtained was performed as well. Using urea, mannitol and polyethylene glycol (PEG) 6000 as water soluble carriers, the solid dispersions of poorly water soluble drugs were studied in order to improve their dissolution properties. Solid dispersions of ofloxacin (OFX) using urea and mannitol as a carrier were prepared by solvent method using the 1:1 mixture of ethanol/chloroform as a solvent. The solubility of OFX in water was improved with increased concentration of urea whereas mannitol did not exhibit the solubilization effect. The PXRD measurements revealed that OFX existed in low crystalline state in the solid dispersions with both urea and mannitol and was in amorphous state when the drug to urea ratio was low as 1:19. The DSC study showed that OFX in the solid dispersions melted in the surrounding of melted urea or mannitol at lower temperature than the melting point of intact OFX. The IR study did not suggest any physicochemical interaction between OFX and carriers used. The dissolution study in water demonstrated that the dissolution rate of OFX was markedly enhanced in the solid dispersions with urea and mannitol. The higher dissolution behavior of OFX in the solid dispersions with urea was attributable to the higher solubility of OFX in the presence of urea, the improved wetting caused by higher water soluble urea and the decreased crystallinity of OFX in the solid dispersions.
コンテンツの種類 博士論文 Doctoral Thesis
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