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아시클로비어와 수용성 고분자를 이용한 고체분산체 제조 및 생체외 방출
안용산,이하영,홍금덕,정성범,조선행,이종문,이해방,강길선 한국약제학회 2004 Journal of Pharmaceutical Investigation Vol.34 No.3
Acyclovir(ACV) is an important antiviral drug used extensively against infections caused by herpes viruses, especially herpes simplex and varicella zoster. Because of high crystallinity and large particle size, solubility of intact ACV is very low in water(1.3 ㎎/㎖). The goal of this work is to enhance the solubility of ACV. To make solid dispersion, Polyethyleneglycol. Hydroxyprophylmethyleelluose and Polyvinylpyrrolidone were used as polymer carriers in this work. Polymer carriers and drug were dissolved in acetic acid. And then spray drying method and freeze drying method were used as solvent extraction. Morphology, crystallization and functional group were characterized using SEM. XRD and ET-IR. The result of in vitro test showed the sample using PVP as polymer carrier had higher dissolution rate(up to 466%) than intact ACV.
아시클로비어 고체분산체의 용해도에 대한 수용성 고분자의 종류 및 배합 비율에 따른 효과
안용산,이하영,홍금덕,정성범,조선행,이종문,이해방,강길선 한국약제학회 2004 Journal of Pharmaceutical Investigation Vol.34 No.4
Acyclovir (ACV) is one of the most effective and selective agents against viruses of the herpes group. Because of low solubility, bioavailability of ACV has shown below 30% with oral dosage form. In our previous study, we reported that the fabrication of solid dispersion of ACV was possible and the solid dispersion of ACV and PVP was the most useful in all samples. In this study, we examined the effect of mixture ratio of polymers (PEG and PVP) to ACV. Solubility of ACV was dramatically increased up to 25 mg/ml in 80°C distilled water. So water was used as a solvent to eliminate problem of residual solvent. Spray drying method was used for the solid dispersion of ACV as solvent extraction. Different scanning calorimeter was used to check degradation of drug. Polymer carriers were PEG 6,000 and PVP. In summary, ACV-PVP (1:3) showed the best solubility in distilled water.
자가미세유화를 이용한 이부프로펜 액상제제의 제조와 특성
안용산,송지희,강복기,김문석,조선행,이종문,이해방,강길선 한국약제학회 2004 Journal of Pharmaceutical Investigation Vol.34 No.1
Ibuprofen (IBU), is a non-steroidal anti-inflammatory drug, used to treat rheumatoid arthritis, removal of fever and mild to moderate pain. Because of small dosage and very low accumulation in the body, IBU has been used to heal children's fever. However, IBU was very low solubility in a low pH and water (in water 0.03∼2.5 ㎎/ml). A nanoemulsion containing IBU by means of self-micromulsion drug delivery system (SMEDDS) was prepared in order to enhance the solubility of IBU. The SMEDDS was composed of cosurfactant, oil and surfactant. The solubility of IBU in various components such as cosurfactant, oil and surfactant was examined. Carbitol^(??) (389.99±20.5 ㎎/ml) as a cosurfctant, Labrafil^(??) M1944CS (90.16±1.60 ㎎/ml) as an oil and Cremopher^(??) RH-40(239.01±2.8 ㎎/ml) as a surfactant were used in this study for preparing SMEDDS. Optimized formulation of SMEDDS was obtained by phase diagram which express the section of nanoemulsion formation. The SMEDDS containing IBU had higher dissolution rate than conventional IBU sirups. Thus the SMEDDS was a potential candidate of stable conventional and effective oral dosage form for IBU.