• Title/Summary/Keyword: release property

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

  • Kim, Ah-Mee;Gwak, Hye-Sun;Chun, In-Koo
    • Journal of Pharmaceutical Investigation
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    • v.36 no.6
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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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    • v.10 no.5
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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.

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

  • Song, J.M.;Baek, H.;Lee, S.Y.;Jang, D.H.;Seo, M.Y.;Park, G.J.;Maeng, Eun-Ho
    • Journal of Biomedical Engineering Research
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    • v.34 no.2
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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.

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

  • Park, Jung-Soo;Shin, Joon-Hyun;Lee, Doo-Hee;Rhee, John-M.;Kim, Moon-Suk;Lee, Hai-Bang;Khang, Gil-Son
    • Polymer(Korea)
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    • v.31 no.3
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    • pp.201-205
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    • 2007
  • Biodegradable polymers such as polylactide, polyglycolide and poly (lactide- co-glycolide) (PLGA) have been extensively investigated because of easily controlled drug release rate, completely degradable materials without the toxic by-product, and good biocompatibility. But, according to the bulk erosion property of PLGA in vitro test, it had the disadvantage that first-order release reduced releasing amount slowly after excessive initial burst. In this study we used PLGA powder obtained through recrystallization to revise bulk erosion property of PLGA. The PLGA used in this study was prepared by vacuum drying method and to estimate release profiles of BCNU loaded PLGA wafer. We also evaluated the release profile of drug with the water soluble additive. It was found that the drug loaded PLGA recrystallized by vacuum drying method exhibited the initial burst and the constant rate of drug release compared to that prepared by a conventional method.

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

  • Gwak, Hye-Sun;Kim, Seung-Ung;Chun, In-Koo
    • Journal of Pharmaceutical Investigation
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    • v.32 no.2
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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.

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

  • Kang, Mi-Kyoung;Kim, Jin-Chul
    • Polymer(Korea)
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    • v.34 no.1
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    • pp.79-83
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    • 2010
  • Alginate beads were prepared using poly(N-isopropylacrylamide-co-dimethylamino ethyl methacrylate)(P(NIPAM-co-DMAEMA)). First, P(NIPAM-co-DMAEMA) was immobilized on the surface of alginate beads by taking advantage of electrostatic interaction between alginate and P(NIPAM-co-DMAEMA). Second, P(NIPAM-co-DMAEMA) was contained in the matrix of alginate beads. P(NIPAM-co-DMAEMA) were prepared by a free radical polymerization at $74^{\circ}C$ for 12 h. The weight ratio of NIPAM to DMAEMA monomer was 95/5. The copolymer was identified by $^1H$-NMR. Releases from the alginate beads were observed at 30, 37, and $45^{\circ}C$ using blue dextran or FITC-dextran(fluorescein isothiocyanate-dextran) as a model drug. The effect of temperature on the degree of release from the beads was insignificant. FITC-dextran was released more than blue dextran possibly due to its smaller molecular weight.

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

  • Bandyopadhyay, AK;Perumal, P
    • Advances in Traditional Medicine
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    • v.7 no.1
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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.

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

  • Lee, Do Hun;Lee, Sang-wha;Yoo, In Sang;Park, Kwon-pil;Kang, Ik Joong
    • Applied Chemistry for Engineering
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    • v.16 no.6
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    • pp.790-793
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    • 2005
  • Recently, the interest in the extension of human life and personal health has been increased. Accordingly, many researchers in a pharmacy and a medical world have been making efforts to improve the sustained drug release property and the stability of drug release property in a body. Many biological researches have demonstrated that chitosan derivatives are effective, safe absorption enhancers that can improve the delivery efficiency of drug and vaccine, and they are suitable for controlled drug release because they have good stability, bio-compatibility, and biodegradability. In this study the experiment was performed in vivo by utilizing chitosan nanoparticles as a biopolymer to control drug delivery rate at an optimal temperature, pH, and concentration. It was observed that nanoparticles containing insulin could effectively control the blood glucose at a low level.

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 (Poly(D,L-lactide)를 외부 껍질로 하고 Alginate 또는 Chitosan을 내부 코어로 구성한 이중미립구 담체의 약물방출 특성)

  • Kim, Ja Won;Song, Min Jeong;Lee, Sang Min;Lim, So Ryong;Jung, Su Jin;Kim, Hong Sung
    • Polymer(Korea)
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    • v.36 no.6
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    • pp.699-704
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    • 2012
  • Double-layered polymeric carrier was designed for release control of hydrophilic drug in oral administration. Biopolymeric chitosan and alginate were examined as polar absorbents, poly(D,L-lactide) as a hydrophobic shell, and theophylline and diclofenac sodium as loading drugs. The fabrication of the carriers was prepared in the form of double-layered microsphere for delayed and successively extended release, which consisted of outer shell of poly(D,L-lactide) and inner core of alginate or chitosan with drugs. Morphologies and drug-release behaviors of the carriers were investigated, which were influenced by a combination of polarity between carrier and drug. It was confirmed that the relative polarities of the carriers, the drugs, and the environmental pH affected significantly the drug-release property.