• 제목/요약/키워드: release property

검색결과 187건 처리시간 0.022초

수분 감응성 아시클로버 패취제의 설계 및 평가 (Formulation and Evaluation of Moisture-activated Acyclovir Patches)

  • 김아미;곽혜선;전인구
    • Journal of Pharmaceutical Investigation
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    • 제36권6호
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    • pp.393-399
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    • 2006
  • This study was aimed to design, formulate and characterize the moisture-activated patches containing acyclovir for antiviral action. Gel intermediates for film-type patches were prepared with mucoadhesive polymer, viscosity builders, enhancers and acyclovir. Patches containing acyclovir were characterized by in vitro measurement of drug release rates through a cellulose barrier membrane, and of drug flux through the hairless mouse skin. Film-type patches obtained were uniform in the thickness and showed a mucoadhesive property when contacted with moisture. The formulation was optimized, which consisted of $Cantrez^{\circledR}$ AN-169(2%), $Kollidon^{\circledR}$ VA 64(1%), $Natrosol^{\circledR}$(1%), hydroxypropyl-$\beta$-cyclodextrin(1%) and dimethylsulfoxide(0.5%). Release rates of acyclovir patches increased dose-dependently. The addition of terpenes such as d-limonene or cineole increased release rates of acyclovir, but decreased permeation rates. The permeation rates were enhanced by 2 and 2.5 times by the addition of glycyrrhizic acid ammonium salt and sodium glycocholate, respectively, compared with that of no enhancer. These results suggest that it may be feasible to deliver acyclovir through the skin or gingival mucosa from the moisture-activated patches.

Evaluation of In Vitro Release Profiles of Fentanyl-Loaded PLGA Oligomer Microspheres

  • Gilson Khang;Seo, Sun-Ah;Park, Hak-Soo;John M. Rhee;Lee, Hai-Bang
    • Macromolecular Research
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    • 제10권5호
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    • pp.246-252
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    • 2002
  • In order to the development of the delivery device of long-acting local anesthetics for postoperative analgesia and control of chronic pain of cancer patient, fentnyl-loaded poly (L-lactide-co-glycolido) (PLGA, molecular weight, 5,000 g/mole; 50 : 50 mole ratio by lactide to glycolide) microspheres (FMS) were studied. FMS were prepared by an emulsion solvent-evaporation method. The influence of several preparation parameters such as initial drug loading, PLGA concentration, emulsifier concentration, oil phase volume, and fabrication temperature has been investigated on the fentanyl release profiles. Generally, the drug showed the biphasic release patterns, with an initial diffusion followed by a lag period before the onset of the degradation phase, but there was no lag time in our system. Fentanyl was slowly released from FMS over 10 days in vitro with a quasi-zero order property. The release rate increased with increasing drug loading as well as decreasing polymer concentration with relatively small initial burst effect. From the results, FMS may be a good formulation to deliver the anesthetic for the treatment of chronic pain.

약물방출스텐트의 약물 방출 특성 평가 방법 개발 (Development of Evaluation Method for Drug Release Propreties in Drug Eluting Stent)

  • 송정민;백홍;이승영;장동혁;서무엽;박길종;맹은호
    • 대한의용생체공학회:의공학회지
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    • 제34권2호
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    • pp.69-72
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    • 2013
  • The goal of this study is to develop test method for evaluating the drug eluting properties of drug eluting stents (DES). PBS and the detergent solutions, presented by each DES manufacturer, were used for drug release of DES coated with paclitaxel, zotarolimus and everolimus. The drugs which are coating DES were not released by PBS but released by the detergent solutions, finally paclitaxel 83.38%, zotarolimus 103.85% and everolimus 115.78%. It seems that the use of the detergents is necessary in order to release the drugs because those drugs are extremely hydrophobic. In conclusion, using of detergent solutions presented by each manufacturer were suitable for evaluating the drug eluting property of drug eluting stent.

진공 건조법에 의해 제조된 BCNU/PLGA웨이퍼의 BCNU 방출거동 (BCNU Release Behaviour from BCNU/PLGA Wafer Prepared by Vacuum Drying Method)

  • 박정수;신준현;이두희;이종문;김문석;이해방;강길선
    • 폴리머
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    • 제31권3호
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    • pp.201-205
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    • 2007
  • 폴리락타이드, 폴리글리콜라이드, 및 글리콜라이드-락타이드 공중합체(PLGA)와 같은 생분해성 고분자들은 쉬운 약물방출량 조절과 부산물독성이 없이 지지체의 완벽한 분해과 좋은 생체적합성을 갖고 있다. 그러나 PLGA는 in vitro 실험에서의 괴상침식, 과도한 초기방출 후의 방출량이 감소하는 단점을 갖고 있다. 본 연구에서 PLGA 재결정 분말은 진공건조법을 이용하여 제조하였으며 1,3-bis(2-chloroethyl)-1-nitro-sourea(BCNU, carmustine)가 함유된 PLGA 웨이퍼의 방출거동을 알아보았으며 동시에 수용성 첨가제를 넣어 약물의 방출거동을 알아보고자 하였다. 진공건조법으로 재결정한 PLGA 웨이퍼가 일반방법으로 제조한 PLGA 웨이퍼보다 수분흡수율 감소와 웨이퍼 자체 초기의 분해 속도 감소로 인하여 초기 방출량이 감소하고 지속적 방출거동을 가지는 것을 확인하였다.

멜라토닌 플라스터의 제제설계 및 평가 (Formulation and Evaluation of Melatonin Plasters)

  • 곽혜선;김승웅;전인구
    • Journal of Pharmaceutical Investigation
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    • 제32권2호
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    • pp.107-112
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    • 2002
  • To investigate the feasibility of developing a novel melatonin plaster, the effects of vehicles and drug loading dose on the in vitro permeation of melatonin across dorsal hairless mouse skin from pressure-sensitive adhesive (PSA) matrices were examined. Vehicles employed were propylene glycol laurate (PGL), propylene glycol monocaprylate (PGMC) and diethylene glycol monoethyl ether (DGME). Among PSAs used, only $Duro-Tak^{\circledR}$ 87-2196 showed a good peeling property. The release from $Duro-Tak^{circledR}$ 87-2196 was proportional to the square root of time, and dose-dependent. The fluxes increased as the loading dose increased over the doses under solubility. The relatively high permeation flux $(3.03{\pm}1.37\;{\mu}g/cm^2/hr)$ was obtained when using PGMC at the melatonin loading dose of $45\;mg/140\;cm^2$. Lag time was not affected by the vehicles used but by the thickness spread. The melatonin plasters prepared using PGMC showed a good adhesive property onto skin, and showed no crystal formation.

Poly(N-isopropylacrylamide-co-dimethylamino ethyl methacrylate)가 고정화된 알지네이트 비드 제조 및 방출 특성 (Preparation and Release Property of Alginate Beads Immobilizing Poly(N-isopropylacrylamide-co-dimethylamino ethyl methacrylate))

  • 강미경;김진철
    • 폴리머
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    • 제34권1호
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    • pp.79-83
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    • 2010
  • Poly(N-isopropylacrylamide-co-dimethylamino ethyl methacrylate)(P(NIPAM-co-DMAEMA))가 고정화된 알지네이트 비드를 제조하였다. 알지네이트와 P(NIPAM-co-DMAEMA)의 정전기적 인력을 이용하여 P(NIPAM-co-DMAEMA)로 코팅된 알지네이트 비드와 P(NIPAM-co-DMAEMA)을 함유한 알지네이트 비드를 제조하였다. P(NIPAM-co-DMAEMA)은 자유 라디칼 반응으로 제조하였고 핵자기 공명분광기를 통해 확인하였다. 비드의 온도 민감성 방출 거동을 관찰하였으며, 모델시약으로 blue dextran과 fluorescein isothiocyanate-dextran을 사용하였다. P(NIPAM-co-DMAEMA)가 고정화된 알지네이트 비드로부터의 방출 정도는 온도 의존성이 낮았고, 방출모델시약의 분자량이 작을수록 더 높았다.

In vitro and in vivo studies on theophylline mucoadhesive drug delivery system

  • Bandyopadhyay, AK;Perumal, P
    • Advances in Traditional Medicine
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    • 제7권1호
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    • pp.51-64
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    • 2007
  • Mucus is an aqueous gel complex with a constitution of about 95% water, high molecular weight glycoprotein (mucin), lipid, salts etc. Mucus appears to represent a significant barrier to the absorption of some compounds. Natural mucoadhesive agent was isolated and purified from the aqueous extract of the seeds of prosopis pallida (PP). Formulated tablet with the isolated material by wet granulation method. Some natural edible substances are in consideration for candidates as mucoadhesive agents to claim more effective controlled drug delivery as an alternative to the currently used synthetic mucoadhesive polymers. Subjected the materials obtained from natural source i.e. PP and standard synthetic substance, sodium carboxymethyl cellulose for evaluation of mucoadhesive property by various in vitro and in vivo methods. Through standard dissolution test and a model developed with rabbit, evaluated in vitro controlled release and bioadhesive property of theophylline formulation. Mucoadhesive agent obtained from PP showed good mucoadhesive potential in the demonstrated in vitro and in viνo models. The results suggest that the mucoadhesive agent showed controlled release properties by their application, substantially. In order to assess the gastrointestinal transit time in vivo, a radio opaque X-ray study performed in healthy rabbit testing the same controlled release formulation with and without bioadhesive polymer. Plasma levels of theophylline determined by the HPLC method and those allowed correlations to the in vitro mucoadhesive study results. Better correlation found between the results in different models. PP may acts as a better natural mucoadhesive agent in the extended drug delivery system.

생명고분자 키토산의 나노입자를 이용한 약물전달 효과 (Drug Delivery Effect Using Biopolymer Chitosan Nanoparticles)

  • 이도헌;이상화;유인상;박권필;강익중
    • 공업화학
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    • 제16권6호
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    • pp.790-793
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    • 2005
  • 최근 인간의 생명 연장과 건강 등에 관심이 많아지면서 약학 및 의학계는 생체 내에서 보다 안정적이며 효과를 나타낼 수 있는 약물 전달 시스템의 개발에 많은 힘을 기울이고 있는 실정이다. 수많은 생화학 연구자들은 키토산이 인체에 거부반응이 없으며 약물과 백신의 전달을 효율적이고 안전하게 흡착능력을 향상시킨다는 것을 밝혀 왔다. 또한 그것은 생분해성, 생체 친화적이라는 장점 때문에 약물 방출 조절에 적당하다고 알려져 있다. 본 연구에서는 생명고분자인 키토산의 나노입자를 제조하여 농도, pH, 최적 온도에서 약물 전달 조절을 in vivo 조건에서 수행하였다. 인슐린을 담지한 키토산 나노입자는 당뇨성 쥐의 혈당을 효과적으로 낮춰 줄 수 있음을 알 수 있었다.

Poly(D,L-lactide)를 외부 껍질로 하고 Alginate 또는 Chitosan을 내부 코어로 구성한 이중미립구 담체의 약물방출 특성 (Drug-release Properties of Double-layered Microspherical Carriers which Consist of Outer Shell of Poly(D,L-lactide) and Inner Core of Alginate or Chitosan)

  • 김자원;송민정;이상민;임소령;정수진;김홍성
    • 폴리머
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    • 제36권6호
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    • pp.699-704
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    • 2012
  • 경구투여를 통한 친수성 약물의 방출조절을 위하여 이중층으로 된 고분자 담체를 설계하였다. 생체고분자인 alginate와 chitosan은 각각 극성 흡수성분으로, poly(D,L-lactide)는 소수성 피막으로, 그리고 theophylline과 diclofenac sodium은 모델 약물로 사용하였다. 담체는 지연방출과 이어지는 지속방출을 위하여 외부 껍질은 poly(D,L-lactide)로, 내부중심은 약물과 함께 알지네이트 또는 키토산으로 구성되어진 이중층의 미립구 담체로 성형하였다. 담체와 약물간의 극성 조합으로 인한 담체의 모폴로지와 약물방출 거동을 조사하였다. 담체와 약물 그리고 pH 환경의 상대적 극성이 약물방출 특성에 상당한 영향이 있음을 확인하였다.