• 폴리머
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• 제32권2호
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• pp.103-108
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• 2008

삼투정 펠렛은 경구를 통한 약물전달 시스템에 폭넓게 사용되고 있으며, 이러한 삼투정 펠렛은 수팽윤성 시드층과 모델약물인 니페디핀을 포함하는 약물층 그리고 약물의 방출을 조절하는 반투막 층으로 구성되어 있다. 이번 연구에서는 모델약물인 니페디핀을 포함한 삼투정 펠렛을 제조하고, 반투막층으로 사용되는 초산셀룰로오스(CA)와 Eudragit RS의 코팅두께에 따른 약물방출 거동과 알긴산 나트륨과 알긴산 나트륨의 가교가 삼투정 펠렛의 약물방출에 미치는 영향에 대하여 확인하고자 하였다. 모델약물인 니페디핀을 포함한 삼투정 펠렛의 제조는 유동층코팅기를 이용하여 제조하였으며, 비교적 높은 코팅 수율로 $1500{\sim}1700{\mu}m$ 내외의 펠렛이 제조됨을 SEM을 통하여 확인하였다. 이렇게 얻어진 펠렛의 반투막 층의 코팅두께에 따른 약물방출 거동을 보면 반투막의 코팅 두께가 증가할수록 약물의 방출이 지연됨을 확인하였다. 알긴산 나트륨을 반투막층 위에 코팅하였을 경우 인공위액(pH 1.2)에서는 약물방출이 거의 일어나지 않았으며, 인공장액(pH 6.8)으로 교체한 후 약물방출이 서서히 증가함을 알 수 있었다. 또한 알긴산 나트륨을 염화칼슘을 이용하여 가교시켰을 경우 약물의 방출이 급격히 감소함을 알 수 있었다. 이번 실험을 통하여 삼투정 펠렛의 약물방출은 반투막충의 코팅두께에 영향을 받으며, 알긴산 나트륨이 삼투정 펠렛의 약물방출에 영향을 끼침을 확인하였다.

• 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.

• 생체재료학회지
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• 제22권4호
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• pp.290-302
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• 2018

Background: The main purpose of drug delivery systems is to deliver the drugs at the appropriate concentration to the precise target site. Recently, the application of a thin film in the field of drug delivery has gained increasing interest because of its ability to safely load drugs and to release the drug in a controlled manner, which improves drug efficacy. Drug loading by the thin film can be done in various ways, depending on type of the drug, the area of exposure, and the purpose of drug delivery. Main text: This review summarizes the various methods used for preparing thin films with drugs via Layer-by-layer (LbL) assembly. Furthermore, additional functionalities of thin films using surface modification in drug delivery are briefly discussed. There are three types of methods for preparing a drug-carrying multilayered film using LbL assembly. First methods include approaches for direct loading of the drug into the pre-fabricated multilayer film. Second methods are preparing thin films using drugs as building blocks. Thirdly, the drugs are incorporated in the cargo so that the cargo itself can be used as the materials of the film. Conclusion: The appropriate designs of the drug-loaded film were produced in consideration of the release amounts and site of the desired drug. Furthermore, additional surface modification using the LbL technique enabled the preparation of effective drug delivery carriers with improved targeting effect. Therefore, the multilayer thin films fabricated by the LbL technique are a promising candidate for an ideal drug delivery system and the development possibilities of this technology are infinite.

• 대한비뇨기종양학회지
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• 제15권3호
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• pp.178-186
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• 2017

Purpose: Poloxamer 407 (P407) thermo-sensitive hydrogel formulations were developed to enhance the retention time in the urinary bladder after intravesical instillation. Materials and Methods: P407 hydrogels (P407Gels) containing 0.2 w/w% fluorescein isothiocyanate dextran (FD, MW 4 kDa) as a fluorescent probe were prepared by the cold method with different concentrations of the polymer (20, 25, and 30 w/w%). The gel-forming capacities were characterized in terms of gelation temperature (G-Temp), gelation time (G-Time), and gel duration (G-Dur). Homogenous dispersion of the probe throughout the hydrogel was observed by using fluorescence microscopy. The in vitro bladder simulation model was established to evaluate the retention and drug release properties. P407Gels in the solution state were administered to nude mice via urinary instillation, and the in vivo retention behavior of P407Gels was visualized by using an in vivo imaging system (IVIS). Results: P407Gels showed a thermo-reversible phase transition at $4^{\circ}C$ (refrigerated; sol) and $37^{\circ}C$ (body temperature; gel). The G-Temp, G-Time, and G-Dur of FD-free P407Gels were approximately $10^{\circ}C-20^{\circ}C$, 12-30 seconds, and 12-35 hours, respectively, and were not altered by the addition of FD. Fluorescence imaging showed that FD was spread homogenously in the gelled P407 solution. In a bladder simulation model, even after repeated periodic filling-emptying cycles, the hydrogel formulation displayed excellent retention with continuous release of the probe over 8 hours. The FD release from P407Gels and the erosion of the gel, both of which followed zero-order kinetics, had a linear relationship ($r^2=0.988$). IVIS demonstrated that the intravesical retention time of P407Gels was over 4 hours, which was longer than that of the FD solution (<1 hour), even though periodic urination occurred in the mice. Conclusions: FD release from P407Gels was erosion-controlled. P407Gels represent a promising system to enhance intravesical retention with extended drug delivery.

• 한국생물공학회:학술대회논문집
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• 한국생물공학회 2003년도 생물공학의 동향(XII)
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• pp.739-742
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• 2003

생분해성인 Curdlan을 이용하여 pH 의존성 약물 전달계 개발을 위한 실험을 수행한 결과, pH 1,4에서 약물 방출 보다 pH 7.4에서 약물 방출이 10배 이상 증가하였다. 이러한 결과로 curdlan acetate microsphere는 pH 의존성 약물 전달계로 유용하다고 판단된다.

• 대한의용생체공학회:학술대회논문집
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• 대한의용생체공학회 1996년도 추계학술대회
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• pp.281-285
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• 1996

Pulsatile swelling behaviors and their application to drug delivery system were studied by using interpenetrating polymer networks(IPN) hydrogels constructed with poly(vinyl alcohol) and poly(acrylic acid). The PVA/PAAc IPNs hydrogels were symthesized by UV irradiation tallowed by repetitive freezing and thawing method. These hydrogels showed pH and temperature sensitive swelling behaviors. From the release experiment, the release amount of model drug incorporated into these hydrogels showed pulsatile patterns. Permeability coefficients obtained by various solutes differed in response to changes of permeation conditions.

• Archives of Pharmacal Research
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• 제12권3호
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• pp.191-195
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• 1989

The release of progesterone from monolithic devices composed of different ratios of polyethylene oxide (PEO; mw 20, 000) and hydrophobic polydimethylsiloxane was investigated. Water soluble PEO soaked into the polymer provided controlled release of progesterone. The release rate of progesterone could be controlled by varying the contents of PEO and progesterone in soaking solution. The progesterone release rate from silicone devices increased as the content of PEO in devices increased, while it decreased as the content of PEO in soaking solution increased. The release rate may be made by simple alterations of geometry of devices controlled swelling and the change in the physical structure of polymer network. Hydrophobic polydimethylsiloxane containing PEO and progesterone can provide a contraceptive material for prolonged release of progesterone.

• 한국임상약학회지
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• 제21권4호
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• pp.347-352
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• 2011

Health insurance review & Assessment service (HIRA) has enforced cutting the drug costs when physicians prescribe split extended release drugs, starting from December, 2010. The objective of this study is to analyze extended release and enteric coated drugs on pharmaceutical reimbursement list in Korea, and to investigate the impact and barriers of the health insurance review on splitting extended-release formulation drugs. By using the ingredient code, extended release and enteric coated formulations make up 7.8% of all drugs in April, 2011. The most frequently used drugs are agent affecting circulatory and digestive system. From the extended release and enteric coated formulations (n=112), 34.8% (n=39) were not available in other dosage forms. According to questionnaire survey for 169 pharmacists (response rate: 73.8%), the rate of splitting and crushing of extended release and enteric coated drugs decreased. When pharmacists correct physician's prescription errors, the biggest problem was lack of other dosage forms. So it is necessary to develop variety of other dosage forms, and computerized checking system for splitting extended-release drugs. It is also important to inform physicians and patients in regard to the problems of split prescription of extended release and enteric coated drugs.

• 대한화학회지
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• 제42권1호
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• pp.92-98
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• 1998

DL-lactide와 glycolide로부터 공중합체 Poly(DL-lactide-co-glycolide)(80:20)를 합성하였다. 합성된 공중합체에 소수성 약물인 clonazepam을 함유하는 미소구체를 제조하여 약물전달시스템 제제로서 응용 가능성을 고찰하였다. 미소구체로부터 약물방출실험은 pH 7.4 phosphate buffer solution $37.0{\pm}0.05^{\circ}C$에서 시행하였다. 미소구체로부터 약물이 선형적으로 방출된 시간범위는 고분자와 약물의 무게비가 20:40(mg)인 경우는 51일 이었고, 20:20과 40:20 (mg)의 비율의 경우는 각각 41일, 29일로 미소구체 제조시 약물의 비율이 증가함에 따라 방출시간 또 한 길어짐을 알 수 있다. 결론적으로 본 실험의 diafiltration법에 의해 균일한 크기의 미소구체를 제조할 수 있었으며, 약물은 조절 방출형 pattern을 보여 약물전달시스템 제제로의 응용 가능성을 알 수 있었다.

• Journal of Pharmaceutical Investigation
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• 제36권6호
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• pp.355-361
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• 2006

Intraarticular corticosteroid injections for therapy of rheumatic arthritis are administered with the aim of optimal local anti-inflammatory effect at the injection site. Since the side effects of corticosteroidal drug, dexamethasone(DEX), administered at hish dose limited the therapeutic efficacy, there was a need to design a new drug delivery system for controlled release of dexamethasone. As a prodrug for continuous therapeutic efficacy, dexamethasone-21-palmitate(DEX-PAL) was prepared via esterification of palmitoyl chloride and dexamethasone. DEX-PAL was identified by NMR and MASS analysis. DEX-PAL or DEX was entrapped in lipid nanosphere which could be prepared by using a self emulsification-solvent evaporation method. Physicochemical characteristics such as mean particle diameter, zeta potential and drug loading efficiency of the lipid nanospheres were investigated with variation of either the kind of lipid or the lipid composition. The lipid nanospheres had a mean diameter $83{\sim}95$ nm and DEX-PAL loading efficiency of up to 95%. The drug loading efficiency increased with the increase of aliphatic chain length attached to the phospholipid. The incorporation of cationic lipid was very efficient for both reducing particle size of lipid nanospheres and enhancing drug loading efficiency. The lipid nanospheres containing DEX-PAL may be a promising novel drug carrier for the controlled release of the poorly water-soluble drugs.