• 제목/요약/키워드: Biodegradable polyphosphazene

검색결과 4건 처리시간 0.023초

전기분무에 의한 생분해성 폴리포스파젠 마이크로입자의 제조 (Fabrication of Biodegradable Polyphosphazene Microparticles by Electrohydrodynamic Atomization)

  • ;;유승곤
    • 폴리머
    • /
    • 제35권5호
    • /
    • pp.424-430
    • /
    • 2011
  • Biodegradable poly[(glycine ethyl ester)-(phenylalanine ethyl ester) phosphazene](PGPP) microparticles were fabricated by electrohydrodynamic atomization to apply drug release test. Atomization parameters such as applied voltage, polymer concentration, and molecular weight were investigated to inspect their effects on the size and morphology of microparticles. The average diameter of PGPP microparticles decreased as increasing applied voltage and solution flow rate. Dichloromethane/dioxane mixture shows better results for the preparation of microparticles than single solvent owing to the different PGPP solubility in solvent. Blending PGPP polymers with proper molecular weights not only favored the production of spherical PGPP microparticles via electrohydrodynamic atomization, but also provided a way to adjust drug (rifampicin) release behavior. Drug-loaded biodegradable polyphosphazene microspheres can be fabricated via electrohydrodynamic atomization, which has potential use in biomedical applications.

마약길항제의 방출 제어형 제제 (제1보) : 생체분해성 polyphosphazenes의 합성과 나록손 이식제제의 제조 및 용출특성 (Controlled Release Dosage Form of Narcotic Antagonist(I): Synthesis of Biodegradable Polyphosphazenes and Preparation and Release Characteristics of Naloxone Implant)

  • 박주애;이승진;김형국;김길수
    • Journal of Pharmaceutical Investigation
    • /
    • 제25권2호
    • /
    • pp.109-116
    • /
    • 1995
  • For the administration of narcotic antagonist with short half-life and low patient compliance, the sustained release system using biodegradable matrix is effective. Polyphosphazenes are of considerable interest as biodegradable matrix systems for controlled release of drugs. In this study, biodegradable polyphosphazenes available for the sustained release implantable device were synthesized, and their application was examined. Poly[dichlorophosphazene] was synthesized by solution polymerization method and confirmed with IR spectrum. Poly[bis(ethyl glycinate) phosphazene] and poly[ (diethyl glutamate)-co-(ethyl glycinate)phosphazene] were then produced by substitution of amino acid alkyl esters for chloride side groups. Using these polymers, the implantable devices of 1 mm thickness and $10{\times}10\;mm$ size containing naloxone hydrochloride were prepared and their release and degradation profiles were measured. In the case of poly[bis(ethyl glycinate)phosphazene] with swelling characteristics, degradation rate was slower than the release rate, showing that the release rate is partly dependent on the swelling rate. In contrast, the degradation rate of polyl[(diethyl glutamate)-co-(ethyl glycinate)phosphazene] matrix was identical with release rate of naloxone hydrochloride. On the basis of these results, it is expected that these polymers can be applied to sustained release implantable systems delivering narcotic antagonist.

  • PDF

마약길항제의 방출 제어형 제제 (제2보): 나록손 이식제제의 생체적합성 및 약물속도론적 평가 (Controlled Release Dosage Form of Narcotic Antagonist(II) : Biocompatibility and Pharmacokinetics of Naloxone Implant)

  • 문미란;박주애;이승진;김형국;김길수
    • Journal of Pharmaceutical Investigation
    • /
    • 제25권2호
    • /
    • pp.117-123
    • /
    • 1995
  • For the effective administration of narcotic antagonist, the application of sustained release implantable systems with biodegradable polyphosphazene was examined. Using poly[(diethyl glutamate)-co-(ethyl glycinate) phosphazene], the implantable devices containing naloxone hydrochloride were prepared and in vivo implantation studies were carried out subcutaneously in rat and rabbit with this preparation for the biocompatibility and pharmacokinetics. The histological finding in rats at initial time period was the inflammation that occurred focally around the implants, but they were showed subsequent mild and limited chronic inflammations and the irreversible changes such as necrosis and degeneration of the muscle or connective tissues were not observed. Therefore the placebo and naloxone implants are considered to be biocompatible formulations histologically. In pharmacokinetic studies, the release of naloxone from the naloxone implants into blood plasma was maintained in 192 hours, but the initial burst effect was observed. If this problem was solved, the application for the narcotic antagonist sustained release systems can be expected.

  • PDF

Naloxone의 Polyphosphazene 이식제제에 관한 연구 (Release and Bioavailability of Naloxone Sustained-Release Implants)

  • 서성연;박주애;김길수
    • Journal of Pharmaceutical Investigation
    • /
    • 제27권3호
    • /
    • pp.225-231
    • /
    • 1997
  • For the effective administration of naloxone, we attempted to investigate the naloxone sustained-release implants. Using the biodegradable polymer, poly[(diethyl glutamate)-co-(ethyl glycinate)phosphazenes](PGGP), the implantable devices containing naloxone hydrochloride(NLX HCl) and naloxone base(NLX) were prepared. The release rates of NLX and NLX HCl were compared. Influences of NLX contents on release rates were examined. For pharmacokinetic studies, NLX and NLX HCl loaded devices were implanted subcutaneously in rabbits and then the plasma concentrations of NLX were determined by HPLC(ECD). NLX-containing devices were implanted with various doses and pharmacokinetic parameters according to dose were calculated. The relative bioavailabilities were evaluated and compared. Incorporation of NLX in the polymer leaded to a slow release. There were no differences of release rates based on drug contents. In pharmacokinetic parameters determined in 216 hours, NLX loaded devices resulted in enhanced bioavailability with the higher AUC (p<0.01) than NLX HCl loaded devices and MRT was significantly (p<0.05) increased. This result demonstrates that NLX is more suitable for sustained release devices than NLX HCl. Therefore it is anticipated that the effective concentrations of naloxone could be maintained for longer periods and bioavailabilities could be improved by naloxone sustained-release implants, with varying drug base/hydrochloride.

  • PDF