• Archives of Pharmacal Research
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• 제25권6호
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• pp.964-968
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• 2002

Colon drug delivery is advantageous in the treatment of colonic disease and oral delivery of drugs unstable or suceptible to enzymatic degradation in upper GI tract. In this study, multilayer coated system that is resistant to gastric and small intestinal conditions but can be easily degraded by colonic bacterial enzymes was designed to achieve effective colon delivery of prednisolone. Variously coated tablets containing prednisolone were fabricated using chitosan and cellulose acetate phthalate (CAP) as coating materials. Release aspects of prednisolone in simulated gastrointestinal fluid and rat colonic extracts (CERM) were investigated. Also, colonic bacterial degradation study of chitosan was performed in CERM. From these results, a three layer (CAP/Chitosan/CAP) coated system exhibited gastric and small intestinal resistance to the release of prednisolone in vitro most effectively. The rapid increase of prednisolone in CERM was revealed as due to the degradation of the chitosan membrane by bacterial enzymes. The designed system could be used potentially used as a carrier for colon delivery of prednisolone by regulating drug release in stomach and the small intestine.

• KSBB Journal
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• 제18권2호
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• pp.161-164
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• 2003

경구 투여가 비교적 어려운 단백질 약물을 생체적합성이 우수하고 생분해성을 가진 펙틴을 이용하여 목적하는 colon에 전달하고자 하였다. 이온결합을 통해 펙틴, 펙틴-알긴산비드를 제조할 수 있었고, 단백질 약물인 BSA를 포함하여 방출을 행한 결과, 비드의 건조온도가 높을수록 방출률이 높은 경향을 보인 반면, 동결건조된 비드가 가장 높은 방출을 나타냈다. 또한, 가교제의 농도를 높게 처리한 비드일수록 방출률이 낮았다. 경구 투여 후 colon에 도달할 것으로 예상되는 5시간 후에 펙틴 분해효소를 처리한 결과, 효소 처리하지 않은 비드에 비해 급격한 방출이 일어났다. 이러한 결과로 colon내에 존재하는 미생물이 분비하는 효소에 의해 펙턴 비드에 포함된 약물이 방출될 것으로 판단된다. 따라서, 경구로 투여된 펙틴 비드 안의 약물이 소화기관에서 안정하게 통과하고 colon에서 방출되어 효과를 나타낼 것으로 판단된다.

• Journal of Pharmaceutical Investigation
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• 제22권4호
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• pp.251-266
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• 1992

A major problem with the peptide-based drugs is that these drugs must generally be administered by injection. Therefore, there is considerable research interest in alternative routes of delivery, such as buccal, nasal, gastrointestinal route and etc. Site-specific drug delivery to the colon, as an alternative to parenteral drug delivery, is of interest for the delivery of peptide-based drugs as well as the delivery of low molecular weight drugs for the treatment of colonic disease, This review describes some considerations of colon-specific drug delivery using hydrogels.

• Archives of Pharmacal Research
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• 제29권8호
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• pp.712-719
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• 2006

In this study, we prepared core-shell type nanoparticles of a poly(DL-lactide-co-glycolide) (PLGA) grafted-dextran (DexLG) copolymer with varying graft ratio of PLGA. The synthesis of the DexLG copolymer was confirmed by $^1H$ nuclear magnetic resonance (NMR) spectroscopy. The DexLG copolymer was able to form nanoparticles in water by self-aggregating process, and their particle size was around $50\;nm{\sim}300\;nm$ according to the graft ratio of PLGA. Morphological observations using a transmission electron microscope (TEM) showed that the nanoparticles of the DexLG copolymer have uniformly spherical shapes. From fluorescence probe study using pyrene as a hydrophobic probe, critical association concentration (CAC) values determined from the fluorescence excitation spectra were increased as increase of DS of PLGA. $^1H-NMR$ spectroscopy using $D_2O$ and DMSO approved that DexLG nanoparticles have core-shell structure, i.e. hydrophobic block PLGA consisted inner-core as a drug-incorporating domain and dextran consisted as a hydrated outershell. Drug release rate from DexLG nano-particles became faster in the presence of dextranase in spite of the release rate not being significantly changed at high graft ratio of PLGA. Core-shell type nanoparticles of DexLG copolymer can be used as a colonic drug carrier. In conclusion, size, morphology, and molecular structure of DexLG nanoparticles are available to consider as an oral drug targeting nanoparticles.