• 환경위생공학
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• 제20권2호
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• pp.33-38
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• 2005

Chitosan is a dietary fiber because of a linear polysaccharide composed of $\beta-(1{\rightarrow}4)$-linked 2-amino-2-deoxy-D-glucopyranose. In this study, control release system of vitamin C has been estimated in chitosan molecular network as a vitamin C carrier of controlled release. The amount of released vitamin C were decreased in higher amount of chitosan concentration. Especially, vitamin C were slowly released from chitosan solution in dialysis membrane when compared with vitamin C solution alone in dialysis membrane. These result assumed that chitosan driving force is dependent on chitosan molecular weight and cationic property of amino group with anionic property of vitamin C.

• 한국염색가공학회지
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• 제9권5호
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• pp.63-74
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• 1997

Polyurethane microcapsules were synthesized by interfacial polymerization in an aqueous poly(ethylene glycol) dispersion with ethylenediamine as chain extender of toluene diisocyanate in perfume oil using poly(vinyl alcohol) as the stabilizing agent. The effect of chemical structure on the average particle size and distributions, morphologies, and thermal properties to design microcapsules for the sustained release system was investigated. It came to be known that polyurethane microcapsules with ethylene diamine as chain extender had a rounder, more permeable and controlled release membranes. And the release test of polyurethane microcapsules with different soft segment content was done to certify the effect of long methylene chain. According to the higher molecular weight of polyether polyol, the release rate of microencapsulated disperse dye molecular was faster.

• Journal of Pharmaceutical Investigation
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• 제18권4호
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• pp.187-195
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• 1988

Poorly permeable $Eudragit^{\circledR}$ RS 100 polymer was used as a wall material for the microencapsulation of zipeprol dihydrochloride by a phase separation method from chloroform-cyclohexane system with 5% polyisobutylene in cyclohexane, and microcapsules obtained were evaluated in vitro by particle size analysis, scanning electron microscopy, drug release test and in vivo bioavailability test in rats. The mechanism of drug release from microcapsules appeared to fit Higuchi matrix model kinetics. The area under the first moment of plasma concentration-time curve of the microcapsules obtained was considerably increased (p<0.05) as compared with that from zipeprol dihydrochloride oral solution. Therefore, it may be suggested that $Eudragit^{\cirledR}$ RS 100 coated zipeprol dihydrochloride microcapsules can be used as a sustained release medication.

• Archives of Pharmacal Research
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• 제16권2호
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• pp.123-128
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• 1993

The surface of cyarabine-entrapped albumin microspheres, the surface modified albumin microspheres hsowed remakably incrased hydrophilicity, good dispersability in aqueous medium and reduced aggregation during storage which met the requirements of injectable drug carriers in acqueous vehicle. In vitro cytarabine release from hydrophilic albumin microspheres (HAM) was a function of the cytarabine to albumin ratio, whereas no significant difference in the releasing capacity was obnserved between surface modified HAM within the small size range$(2\;to\;5\mu{m)}$ studied. HAM containing 15-23% drug were gradually degraded by protease and continuously released up to 60% of the total entrapped cytarabine for 6h. These results thus suggest that HAM is a suitable cytarabine carrier which may be injected intraveneously with the benefits of a reduced risk of blood embolism induced by aggregates and prolonged cytarabine release.

• 약학회지
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• 제42권3호
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• pp.265-274
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• 1998

In order to attain a sustained release at targeted organs in a prolonged time which can reduce the side effects and maximize the therapeutic effect, aclarubicin (ACL) was entrap ped into liposomes of different lipid compositions using Microfluidizer, and dry liposomes were prepared by lyophilization. The dry aclarubicin-entrapped liposomes were evaluated in terms of mean particle size and size distribution, entrapment efficiency and in vitro drug release profile. The Entrapment efficiency of liposome, when the concentration of aclarubicin and lipid were 0.5 to 1.0mg/ml and $200{\mu}mol$/ml, respectively, was over 80% using Microfluidizer, in contrast to 70% of entrapment efficiency using hand-shaking method. Mean particle size and size distribution of aclarubicin-entrapped liposomes of various lipid compositions did not change considerably by the freeze drying. The range of particle size was between 80 and 200nm. Among aclarubicin-entrapped liposomes, ACL-liposome of PC/DPPC/CH0L/TA displayed the most significant sustained release. The addition of DPPC appeared to be favorable for the control of release. In general, aclarubicin entrapped in liposomes was less stable than free aclarubicin either in pH 7.4 phosphate buffer or in human plasma. Formulation I($t_{1/2}$, 20.3 hr) devoid of lipid additive was the most unstable in the phosphate-buffer solution while formulation II($t_{1/2}$, 40.7 hr) with cardiolipin was the most stable. Half lives of aclarubicin-entrapped liposomes in human plasma were 43.2, 50.7, 35.9 and 35.3 hr for formulation I. II, III and IV, respectively, in contrast to 57.8 hr for free aclarubicin.

• 대한소아치과학회지
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• 제25권4호
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• pp.797-810
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• 1998

The purpose of this study was to develop a new way of delivery system of chlorhexidine using self-curing acrylic resin. Different preparations of chlorhexidine, such as chlorhexidine varnish($Chlorzoin^{(R)}$) and chlorhexidine diacetate crystalline, were mixed into self-curing acrylic resin with different methods. Every resin plate was made and was immersed in 100ml of distilled water individually, and kept in an incubator at $37^{\circ}C$. Solution(0.8ml) was collected from the each container at every 24 hours, and the amount of released chlorhexidine in the solution was measured in an ultraviolet spectrophotometer at 255nm. Flexural strength of all of the resin plates in the Experiment 2-A and 2-B were measured using Instron at the end of the experimental periods. The results were as follows: 1. It was found that chlorhexidine was released from the experimental groups in the Experiment 1, 2-A, and 2-B. And the release of chlorhexidine from all of the experimental groups showed a pattern of sustained-release preparation. 2. It seemed likely that a condition of "dryness" reduced a release of chlorhexidine from the chlorhexidine varnish. 3. It may be stated that a method of "chlorhexidine diacetate mix" with the polymer be more efficient than a method of "Chlorzoin mix" with the monomer. 4. Although it was evident that a flexural strength of the acrylic resin plates be reduced by a mix of either Chlorzoin or chlorhexidine diacetate crystalline, it seemed likely that the resin plates except Group 4 and 5 in the Experiment 2-B may be usable in the clinical situation.

• Journal of Pharmaceutical Investigation
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• 제40권4호
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• pp.231-236
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• 2010

This study was to fabricate the porous poly(lactide-co-glycolide) (PLGA) microparticles with anthocyanin (as a model antioxidant) for pulmonary drug delivery. The highly porous PLGA microparticles were prepared by the waterin-oil-in-water ($W_1/O/W_2$) multi-emulsion method, followed by the decomposition of ammonium bicarbonate (AB) in $W_1$ phase to the base of ammonia, carbon dioxide and water vapor at $50^{\circ}C$, making a porous structure in PLGA microparticles. Herein, hyaluronate (HA), a viscous polysaccharide, was incorporated in the porous microparticles for sustained anthocyanin release. In in vitro release studies, the anthocyanin release from the porous microparticles with HA continued up to 24 hours, while the porous microparticles without HA released 80 wt.% of encapsulated anthocyanin within 2 hours. In addition, these microparticle are expected to be effectively deposited at a lung epithelium due to its high porosity (low density) and avoid alveolar macrophage's uptake in the lung due to its large particle size. We believe that this system has a great pharmaceutical potential as a long acting antioxidant for relieving the oxidative stress in chronic obstructive pulmonary disease (COPD).

• Macromolecular Research
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• 제14권1호
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• pp.87-93
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• 2006

Copolymers composed of hyaluronic acid (HA) and poly(N-isopropylacrylamide) (PNIPAAm) were prepared to create temperature-sensitive injectable gels for use in controlled drug delivery applications. Semi-telechelic PNIPAAm, with amino groups at the end of each main chain, was synthesized by radical polymerization using 2-aminoethanethiol hydrochloride (AESH) as the chain transfer agent, and was then grafted onto the carboxyl groups of HA using carbodiimide chemistry. The result of the thermo-optical analysis revealed that the phase transition of the PNIPAAm-grafted HA solution occurred at around 30$\∼$33$^{circ}C$. As the graft yield of PNIPAAm onto the HA backbone increased, the HA-g-PNIPAAm copolymer solution exhibited sharper phase transition. The short chain PNIPAAm-grafted HA ($M_{w}$=6,100) showed a narrower temperature range for optical turbidity changes than the long chain PNIPAAm-grafted HA ($M_{w}$=13,100). PNIPAAm-grafted HA exhibited an increase in viscosity above 35$^{circ}C$, thus allowing the gels to maintain their shape for 24 h after in vivo administration. From the in vitro riboflavin release study, the HA-g-PNIPAAm gel showed a more sustained release behavior when the grafting yield of PNIPAAm onto the HA backbone was increased. In addition, BSA released from the PNIPAAm-g-HA gels showed a maximum concentration in the blood 12 h after being injected into the dorsal surface of a rabbit, followed by a sustained release profile after 60 h.

• Archives of Pharmacal Research
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• 제24권6호
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• pp.568-571
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• 2001

The purpose of this work was to study the effect of storage time and temperature on the in vitro release kinetics of a commercial sustained-release dosage form of theophylline, at different pHs of the dissolution medium. The formulation was stored at $35^{\circ}C$ for 16 months and at $45^{\circ}C$ for 8 months, with a relative humidity of 60%. The in vitro release tests were performed at pHs 2, 4, 6 and 7.4. The mean values of the transport coefficient n, were close to 0.5 in all the conditions tested, which indicates that the transport system is not modified after storage of the formulation at $35^{\circ}C$ and $45^{\circ}C$. The mean values of the dissolution rate constant ranged from 0.036 to 0.043 $min^{-n}$, under all the conditions tested. Significant differences (${\alpha}=0.05$) were found between pHs 2, 4 and 6, 7.4 for all the model-independent parameters studied. When the formulation was kept at $35^{\circ}C$ for 16 months, the mean percentage of drug dissolved at 8 hours was 25.61% (pHs 2, 4) and, 36.12% (pHs 6, 7.4), representing a 26% and 24% reduction, respectively. Simitar results were obtained after storing the formulation at $45^{\circ}C$ for 8 months, corresponding to 33.3% (pHs 2, 4) and, 22.5% (pHs 6, 7.4) diminution, respectively. The values of the similarity factory $f_2$, obtained were lower than 50, which indicates the lack of similarity among the dissolution profiles, after storing the formulation under the experimental Conditions tested.

• Journal of Pharmaceutical Investigation
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• 제31권2호
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• pp.101-106
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• 2001

Alginate-chitosan (anion-cationic polymeric complex) was prepared to control the release rate of silver sulfadiazine (AgSD). Na-alginate (2%) solution containing AgSD was gelled in $CaCl_2$ solution. The gel beads formed were immediately encapsulated with chitosan (CS). The gel matrix and membrane were then reinforced with chondroitin-6-sulfate (Ch6S). Release rate of AgSD from the gel matrix was investigated by placing alginate beads in the sac of cellulose membrane simmered in HEPES-buffer solution. The concentration of AgSD released was analyzed by UV at 264 nm. Incorporation capacity of AgSD in Ca-alginate gel was more than 90%. Alginate-Ch6S-CS could control the release rate of AgSD. The amount of AgSD release was dependent on the AgSD loading dose. Incorporation of tripolyphosphate (polyanionic crosslinker) onto the alginate-Ch6S-CS bead increased the release rate of AgSD. Collagen-coating had no influence on the AgSD release rate. Alginate-Ch6S-CS beads with a sufficiently high AgSD encapsulation were capable of controlling the release of the drug over 10 days. In summary, alginate-Ch6S-CS beads could be used as a sustained delivery for AgSD and provide local targeting with low silver toxicity and patient discomfort.