• 대한의용생체공학회:의공학회지
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• 제41권1호
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• pp.62-66
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• 2020

Controlled drug release is important for effective treatment of cancer. Poly(DL-lactide-co-glycolide) acid (PLGA) is a Food and Drug Administration (FDA) approved polymer and have been extensively studied as drug delivery carriers with biodegradable and biocompatible properties. However, PLGA drug delivery carriers are limited due to the initial burst release of drug. Certain drugs require an early rapid release, but in many cases the initial rapid release can be inefficient, reducing therapeutic effects and also increasing side effects. Therefore, sustained release is important for effective treatment. Poly Lactic Acid stereo complex (PLA SC) is resistant to hydrolysis and has high stability in aqueous solutions. Therefore, in this work, PLGA based discoidal polymeric particles are modified by Poly Lactic Acid stereocomplex (PLAsc DPPs). PLAsc DPPs are 3 ㎛ in diameter, also showing a relatively sustained release profile. Fluorescein 5(6)-isothiocyanate (FITC) released from PLAsc DPPs was continuously observed until 38 days, which showed the initial release of FITC from PLAsc DPPs was about 3.9-fold reduced as compared to PLGA based DPPs at 1 hour.

• KSBB Journal
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• 제18권2호
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• pp.107-110
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• 2003

스텐트 재질인 stainless steel 표면에 모델 약물인 rose bengal을 포함한 생분해성 고분자 PLGA, PHB, MCL-PHA를 코팅하여 약물방출 특성을 조사하였다. PLGA의 농도가 낮을수록, rose bengal의 농도가 높을수록, dip-coating 시간이 길수록 약물방출이 증가하였으며, PHB > PLGA > MCL-PHA의 순서로 약물이 빨리 방출되었다. 이는 생분해성 고분자의 농도 및 종류, 약물의 농도, dip-coating 시간 등을 변화시켜 약물방출을 조절할 수 있음을 나타낸다.

• Macromolecular Research
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• 제12권1호
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• pp.71-77
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• 2004

We have synthesized various types of poly(ethylene glycol) (PEG)-ibuprofen conjugates by nucleophilic substitution of bromo-terminated PEG with ibuprofen-Cs salt. The conversion of the terminal hydroxyl groups to bromo-termini was quantitative, as was the drug conjugation process, which suggests that the present synthetic method is very useful for the preparation of PEG-based prodrugs from pharmaceuticals having carboxyl functionalities. The drug-release behavior of the prodrugs was examined in both phosphate buffer (PBS, pH 7.4) and rat plasma. From the drug-release behavior in PBS, we determined that each prodrug has high storage stability. The drug-release rate was observed to be much faster in rat plasma than in buffer solution as a result of the acceleration effect provided by enzymes present in the plasma. The drug-release rate in rat plasma depends on the degree of molecular aggregation of the prodrugs, which can be changed effectively by the nature of their spacer groups or by the use of Pluronic as the polymer carrier.

• Journal of Pharmaceutical Investigation
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• 제19권3호
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• pp.145-154
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• 1989

Methyl methacrylate-butyl methacrylate copolymer (MMBM)-povidone (PVP) films were investigated as a potential topical drug delivery system for the controlled release of econazole nitrate as a model drug. The effect of changes in film composition, drug concentration, film thickness, pH and temperature of release medium on the in vitro release of econazole nitrate were studied. The release rate constant was found to be increased with increasing povidone content in dry films. Drug release followed zero-order kinetics in the initial stage and then release rate increased gradually with time, espicially in the films having larger proportions of PVP. The release rate was found to be dependent on drug content, film thickness, the pH and temperature of release medium. Antimicrobial test showed that microbial growth was inhibited markedly with increasing proportions of PVP in films. Also drug content and film thickness affected the antimicrobial activity.

• Journal of Pharmaceutical Investigation
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• 제35권3호
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• pp.157-163
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• 2005

The pellets with multiple drug release system (MDRS) of Diltiazem. HCl which consist of immediate drug release layer, drug reservoir layer and controlled release rate membrane, were prepared by using CF-Coater. As main factors for more effective MDRS of Diltiazem. HCl, ethylcellulose was used for the controlling drug release rate, and diethylphthalate was used for plasticizer, respectively. In vitro evaluation study was performed by comparative dissolution test between our test MDRS and reference Diltiazem. HCl preparation. The physical tests were performed using FT-IR and SEM. In vivo evaluation was also performed by observing the behavior of a plasma drug concentration after oral administration. The bioavailability was determined by analyzing the blood sample after oral administration to healthy, male volunteers once a day. As a result, there were no significant differences in bioequivalence parameters $(AUC_{\infty},\;C_{max},\;t_{1/2})$ between two systems. It might be concluded that our MDRS of Diltiazem. HCl could be an alternative delivery system to reference drug preparation.

• Archives of Pharmacal Research
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• 제17권4호
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• pp.240-243
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• 1994

Release rates of flurbiprofen from transdermal gels made of poloxamer 407 were evaluated using a membraneless diffusion cell in order to study the effects of formulation variables on flurbiprofen release such as poloxamer 407 (17.5-25%) drug (0.1-1.0%), ethanol (10-20%), PG or PEF 300 (5-15%) concentrations and gel pH(3-7). Isopropyl myristate was employed as a receptor medium for the drug released from the gel. The diffusion coefficient of flurbiprofen decreased linearly as the amount of poloxamer 407 and the drug in the gel increased. The release rate of flurbiprofen was gel increased. The The addition of more ethanol in the gel increased the drug release, resulting from the increase of the thermodynamic activity of the drug in the aqueous phase of the gel. However, the concentration effects of PG and PEG 300 on the release rate of flurbiprofen were negligible over the concentration range used.

• KSBB Journal
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• 제10권4호
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• pp.461-467
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• 1995

본 연구에서는 약물 전달체(키토산, 키토산.엽, 술폰화키토산)에 prednisolone을 분산시켜 제조한 고분자 매트릭스를 poly (DL-lactide)로 피막을 형성시킨 후 pH 1.2와 pH 7.4 인산염 완충용액에서 약물 방출실험을 하였다. 약물 방출시간은 pH 1.2에서 보다 pH 7.4에서 더 지연되였으며 약물 전달체의 함유량이 증가함에 따라 약물의 방출시간도 지연되었다. 피막된 고분자 매트릭스의 종류에 따라 지연된 약물의 방출시간은 키토산의 경우가 가장 길었으 며, 술폰화키토산, 키토산.염의 순셔였다. Monolith IC 고분자 매트릭스에 비해 2배 정도의 약물의 방출 지연성을 보인 피막된 monolithic 고분자 매트럭스 가 방출조절형 제제로서 더 바람직한 것으로 관찰되었다. 이러한 제형들은 초기 급격한 약물 방출속도의 변화를 억 제 하는 sustained release pattern 제 제 임을 확인할 수 있었다.

• Archives of Pharmacal Research
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• 제12권2호
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• pp.88-93
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• 1989

In order to obtain some informations about the effect of molecular weight on the release rate of drug from drug carrier, two types of poly-L-glutamic acid (PLGA)-cytarabine (ara-C) conjugates, PLGA-ara-C:I and PLGA-ara-C:II, were synthesized using two types of PLGA having different average molecular weight, 43,000 and 77,800, respectively. The PLGA-ara-C conjugates were synthesized by mixed anhydride method and found to be covalently linked. Both types of conjugates charged negatively at biological pH. The pH-dependent release rate of ara-C was observed in both cases, and the release rate was accelerated in basic, acidic conditions (the k values were 0.015 $day^{-1}$ at pH 7.0, 0.024 $day^{-1}$ at pH 5.0, and 0.059 $day^{-1}$ at pH 9.0 in the case of PLGA-ara-C:I) and in the presence of pretense. The time required for the release of 16.5% of ara-C from PLGA-ara-C:I were 8 hr and 144 hr in the presence and absence of protease, respectively. Although both types of conjugates showed similar drug substitution ratio, they showed different release rates. Between the two types of conjugates, PLGA-ara-C:II showed the faster release rate (0.030 vs 0.042 $day^{-1}$ in pH 7.4 phosphate buffer solution at $37^{\circ}C$) and the smaller activation energy for the release of drug (12.5 vs 7.7 Kcal/mol) than PLGA-ara-C:I. The characteristic effect of molecular weight on the release rates of PLGA-ara-C conjugates suggests that the drug release rate might be effectively controlled over a prolonged period of time by the combined use of the different types of PLGA-ara-C conjugates having different molecular weights.

• KSBB Journal
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• 제14권3호
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• pp.297-302
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• 1999

Poly(DL-lactide)로 피막된 고분자 매트릭스를 약물전달시스템에 이용하기 위해 키토산, 키토산 염산염 및 술폰화 키토산으로 제조되었다. 모델 약물로 프레드니솔론을 사용하는 본 약물방출에 관한 연구는 pH 1.2 염산 용액에서 실험을 하였다. 약물 방출 속도는 고분자 매트릭스의 함유량이 증가할 수록 감소하였다. 피막된 고분자 매트릭스의 종류에 따라 지연된 약물의 방출시간은 키토산의 경우가 가장 길었으며, 술폰화 키토산, 키토산 염산염의 순서였다. DL-PLA로 피막된 고분자 매트릭스가 피막되지 않는 고분자 매트릭스 보다 약물 방출시간이 2배 정도의 지연되었을 뿐만 아니라 초기에 약물 과잉방출 현상도 작아 피막된 경우가 방출 조절형 제재로서 더 바람직한 결과를 보였다. 따라서 DL-PLA로 피막된 고분자 매트릭스는 장시간의 약물 방출을 위한 약물전달체로써의 응용이 기대된다.

• Journal of Pharmaceutical Investigation
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• 제19권2호
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• pp.99-107
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• 1989

In order to develop a pediatric liquid preparation with sustained release properties, dextromethorphan hydrobromide (DEXT) was complexed with strong cation exchange resin (CG 120) and the-complex was coated with Eudragit RS using a phase separation method by non-solvent addition. The effect of pH, ionic strength of the release medium and drug/resin ratio on the release rate of DEXT was studied. The release rate of free drug from the uncoated complex, and coated complexes with 9.5 and 18.5% Eudragit RS in artificial gastric juice were measured. The release rate from the uncoated complex was faster with higher pH, higher ionic strength of the release medium and higher drug/resin ratio. The release rate from the coated complex could be controlled by the amount of coating material, and the surface after release did not rupture into.