• 생명과학회지
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• 제24권4호
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• pp.437-446
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• 2014

트립탄 계열의 약물을 경구 복용 시에 트립탄은 소화 시스템에 의하여 생물학적 이용도가 감소되며, 혈중 약물 농도가 시간의 경과에 따라 급격히 감소되고, 위장 장애의 가능성 등이 있다는 문제들을 나타낸다. 일반 겔 패치의 부작용을 개선하기 위하여 패치는 하이드로겔 형태로 제조하였다. 하이드로겔 패치의 주가 되는 메트릭스의 고분자는 PVA를 사용하였고, PEG는 PVA의 분자 간/분자 내 수소결합을 유도하기 위해 첨가물로서 사용되었고 알모트립탄 약물이 부가되었다. 또한 PVA 체인간의 미세 상분리를 가속하기 위해 매우 낮은 온도에서 액체질소가 사용되었다. FT-IR 분석에서 PVA, PEG 그리고 알모트립탄의 흡수 밴드를 확인하였다. PEG 함량이 증가함에 따라 결정화도, 수분흡수력과 인장강도들은 증가하였다. 약물방출 실험에서 약물 방출량은 PEG의 함량이 높은 하이드로겔이 약물 방출 시에 팽윤이 더 잘 이루어져 증가하였다. 본 실험에서 10 wt%의 PEG를 첨가하여 제조된 하이드로겔의 약물 방출량이 가장 좋았다. 또한 10 wt%의 PEG가 함유된 하이드로겔은 2시간째까지 전체 약물의 약 60%가 방출됨을 확인하였고, 24시간째까지도 방출이 계속되었다. 따라서 제조된 하이드로겔은 triptan의 1차 투여 이후 24시간 이내에 재발하는 편두통 환자들을 대상으로 한 트립탄의 2차 투여를 위한 경피흡수형 패치로서 적합하다.

• 한국식품위생안전성학회지
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• 제12권3호
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• pp.228-233
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• 1997

Drug Dclivcry system (DDS) purpose to getting better remedial result by improving medication from ordinary methods. Applied for DDS, to improve selectivity and comtinuity during absorbing and delivery step, polmer drug (prodrug) was prepared by the esterification with dextran in such of biodegradable polymer and phthalylsulfathiazole with is efficient for entilitis. The polymer durg was prepared with dextran and phthalylsulfathiazole by the esterification. The synthetic procedures of polymer drug was performed by acid chloride and DCC methods. Polymer drug was synthesized in high yield by acid chloride method than DCC method. The antibiotic activities of polymer drug exhibited growth-inhibitory activity against Staphylococcus aureus, Staphylococcus epidermidis, E. coli, Salmonella typhimurium, Klebsiella pneumoniae at the concentration of 500 *g/m* in general through in vitro. As a result of test, polymer drug has 1/2 MIC than phthalylsulfathiazole. Also, it has high level MIC as much as phthalylsulfathiazole with Proteus, Pseudomonas. We conducted possibility of DDS as an applied for medicine with synthesized polymer drug by using natrural polymer. We consider that clinical research must be followed to verify safety and efficacy for controlled release, activity and toxicity.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1996년도 춘계학술대회
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• pp.282-282
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• 1996

The purpose of this study was to prepare the nifedipine dry elixir (NDE) and coated nifedipine dry elixir (CNDE) containing nifedipine ethanol solution for improving the dissolution rate and bioavailability of nifedipine. NDE containing nifedipine and ethanol in wall materials of dextrin was prepared using a spray-dryer and then NDE was coated with eudragit acrylic resin to make CNDE. Shape and size of the NDE and CNDE were monitored by scanning electron micrograph and laser particle size analyzer In vitro dissolution tests were performed in simulated gastric and intestinal fluid. Bioavailability of NDE and CNDE were compared with drug powder suspension and commercial soft capsule after oral administration of the preparations to rats. NDE and CNDE are spherical in shape. Cross-sectional view of dry elixirs indicates the large inter cavity containing ethanolic drug solution in shell. Geometric mean diameter of NDE and CNDE is about 6.64 and 8.70 $\mu\textrm{m}$, respectively. Drug dissolution rate within first 5 min from NDE increased dramatically irrespective of dissolution medium. However, CNDE showed a particularly retarded dissolution rate in pH 1.2 simulated gastric fluid compared with NDE. The bioavailability of nifedipine in the NDE was increased dramatically compared with drug powder suspension. CNDE reduced initial burst-out plasma peak compared with NDE. CNDE as a sustained release delivery system could reduce the initial burst-out plasma peak due to controlling the release rate of nifedipine from NDE and maintain the effective plasma level over a longer period within therapeutic window with enhanced bioavailability of nifedipine.

• 공업화학
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• 제35권3호
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• pp.192-199
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• 2024

본 연구에서 carbamazepine (CBZ) 각인 도토리 전분(acorn starch, AS)/PVA 기반 바이오소재를 casting method와 UV 조사를 이용하여 제조하고 물리·화학적 특성, CBZ 흡착 및 방출 특성을 조사하였다. 제조한 바이오소재의 표면 특성은 FE-SEM을 통해 확인하였고, UV 조사에 따른 CBZ의 안정성과 바이오소재 작용기는 FT-IR 분석을 이용하였다. CBZ에 대한 바이오소재의 흡착 특성은 binding isotherm 및 Scatchard plot으로 평가하였고 이를 통해 CBZ 각인 바이오소재에 CBZ 결합 부위가 존재하는 것을 확인하였다. 경피 약물 전달 시스템의 응용 가능성을 평가하기 위하여 36.5 ℃에서 다양한 pH의 완충용액과 인공피부를 이용해 제조한 바이오소재의 CBZ 방출 특성을 조사하였다. 이 결과, CBZ는 pH 가 증가할수록 빠른 방출 속도를 보였으며, 인공피부 테스트에서 12 h 동안 지속적으로 방출되었다. 또한, 수학적 모델을 적용시킨 결과, 완충용액에서 CBZ 방출 메커니즘은 pseudo-Fickian diffusion 메커니즘을 따랐고 인공피부에서 non-Fickian diffusion 메커니즘을 따르는 것으로 평가되었다.

• Journal of Pharmaceutical Investigation
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• 제35권1호
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• pp.25-31
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• 2005

Depot system for local drug delivery using chitosan hydrogel has been developed to enhance the therapeutic efficacy and to prevent the severe side effect in whole body. Thus, we have prepared an injectable chitosan hydrogel containing liposomes to treat cancers clinically. Anionic liposomes incorporated to improve sustained release efficiency within chitosan hydrogel. The chitosan solution containing liposomes was designed to form a hydrogel complex at body temperature. The released behavior of doxorubicin from liposomes in chitosan hydrogel showed sustained-release caused by diffusion of doxorubicin from temperature responsive liposome into chitosan hydrogel. The chitosan hydorgel containing liposomes enhanced the therapeutic potency for the solid tumor in vivo system. Our results indicate that the liposomes in chitosan hydrogel represent a depot system for local drug delivery.

• Archives of Pharmacal Research
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• 제22권5호
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• pp.474-478
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• 1999

Modulation of unscheduled DNA synthesis by dehydroepiandrosterone (DHEA) after exposure to various chemical carcinogens was investigated in the primary rat hepatocytes. Unscheduled DNA synthesis was induced by treatment of such direct acting carcinogens as methly methanesulfonate (MMS) and ethyl methanesulfonate (EMS) or procarcinogens including benzo(a)pyrene (BaP) and 7, 12-dimethylbenz(a)anthracene (DMBA). Unscheduled DNA synthesis was determined by measuring [methyl-3H]thymidine radioactivity incorporated into nuclear DNA of hepatocytes treated with carcinogens in the presence or absence of DHEA. Hydroxyurea $(5{\times}10^{-3} M)$was added to growth medium to selectively suppress normal replication. DHEA at concentrations ranging from $(1{\times}10^{-6} M)$ to$(5{\times}10^{-4} M)$ did not significantly inhibit unscheduled DNA synthesis induced by either MMS $(1{\times}10^{-4} M)$ or EMS $(1{\times}10^{-2} M)$. In contrast, DHEA-significantly inhibited unscheduled DNA synthesis induced by BaP $(6.5{\times}10^{-5} M)$ and DMBA.$(2{\times}10^{-5} M)$. DHEA-induced hepatotoxicity in rats was examined using lactate dehydrogenase (LDH) release as an indicator of cytotoxicity. DHEA exhibit no significant increase in LDH release compared with the control at 18 h. These data suggest that nontoxic concentration of DHEA does not affect the DNA excision repair process, but it probably influence the enzymatic system responsible for the metabolic activation of procarcinogens and thereby decreases the amount of the effective DNA adducts formed by the ultimate reactive carcinogenic species.

• Journal of Pharmaceutical Investigation
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• 제40권5호
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• pp.263-267
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• 2010

Nanoemulsions have been widely investigated for many years because of their attractive and unique characteristics. Nanoemulsions are composed of oil, surfactant, co-surfactant and water. Especially, cosurfactant plays a critical role in formation of nanoemulsions. In pharmaceutical area, a pre-concentrate form of nanoemulsions which is known as self-nanoemulsifying drug delivery systems (SNEDDS) was available for some water-insoluble drugs. In this study, we investigated the functional behaviors of cosurfactant in design of SNEDDS and nanoemulsions. Cremophor RH 40$^{(R)}$, Propylene carbonate and medium chain triglyceride were selected for surfactant, cosurfactant and oil, respectively. Cyclosporine was employed as a drug. Phase diagrams showed the area of isotropic o/w region which forms o/w nanoemulsions was not significantly affected by the compositional ratio of cosurfactant. But, drug solubilization capacity, droplet size of nanoemulsions and drug release rate were greatly affected by the cosurfactant.

• Biotechnology and Bioprocess Engineering:BBE
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• 제11권6호
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• pp.526-529
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• 2006

The aim of this study was to prepare cyclosporin A-loaded liposome (CyA-Lip) as an oral delivery carrier, with their encapsulation into microspheres based on alginate or extracellular polysaccharide (EPS) p-m10356. The main advantage of liposomes in the microspheres (LIMs) is to improve the restricted drug release property from liposomes and their stability in the stomach environment. Alginate microspheres containing CyA-Lip were prepared with a spray nozzle; CyA-Liploaded EPS microspheres were also prepared using a w/o emulsion method. The shape of the LIMs was spherical and uniform, and the particle size of the alginate-LIMs ranged from 5 to $10\;{\mu}m$, and that of the EPS-LIMs was about $100\;{\mu}m$. In a release test, release rate of CyA in simulated intestinal fluid (SIF) from the LIMs was significantly enhanced compared to that in simulated gastric fluid (SGF). In addition, the CyA release rates were slower from formulations containing the liposomes compared to the microspheres without the liposome. Therefore, alginate-and EPS-LIMs have the potential for the controlled release of CyA and as an oral delivery system.

• Journal of Korean Neurosurgical Society
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• 제63권1호
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• pp.45-55
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• 2020

Objective : Fibrin sealants have been used for hemostasis, sealant for cerebrospinal fluid leakage, and adhesive barrier in neurosurgery. Further, as its clinical use and role of an effective drug delivery vehicle have been proposed. This study was performed to measure antibacterial activity and continuous local antibiotic release from different concentrations of vancomycin-impregnated fibrin sealant in vitro. Methods : Antibacterial activity was investigated by disk diffusion test by measuring the diameter of the growth inhibition zone of bacteria (methicillin-resistant Staphylococcus aureus, ATCC29213) from vancomycin-embedded fibrin sealant disc diluted at five different concentrations (C1-C5; 8.33, 4.167, 0.83, 0.083, and 0.0083 mg/disc, respectively). Continuous and conditioned release of vancomycin concentration (for 2 weeks and for 5 days, respectively) were also measured using high-performance liquid chromatography (HPLC) method. To mimic the physiologic wound conditions with in vitro, conditioned vancomycin release in phosphate buffer solution (PBS) was measured and replaced PBS for five consecutive days, half a day or completely daily. Results : In the disk diffusion test, the mean diameters of bacterial inhibition zone were 2.54±0.07 cm, 2.61±0.12 cm, and 2.13±0.15 cm (C1, C2, and C3 respectively) but 1.67±0.06 cm and 1.23±0.15 cm in C4 and C5, respectively. Continuous elution test elicited the peak release of vancomycin from the fibrin sealant at 48 hours, with continued release until 2 weeks. However, conditioned vancomycin release decreased to half or more on day 2, however, the sustainable release was measured over the therapeutic dose (10-20 ㎍/mL) for 5 days and 4 days in assays of half and total exchange of PBS. Conclusion : This study suggests that fibrin sealant can provide an efficient vehicle for antibiotic drug release in a wide range of neurosurgical procedures and the safe and effective therapeutic dose will be at the concentration embedded of 4.167 mg/disc or more of vancomycin.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.230.1-230.1
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• 2003

In case of oral application of quinupramine, antidepressants, it may cause adverse effects such as diarrhea, nausea due to transient high blood concentration. Ethylene vinyl acetate (EVA) which is heat-processible, flexible, inexpensive material was used for transdermal drug delivery. The purpose of this study was to develop the new transdermal delivery system of quinupramine using EVA polymer matrix that can provide sustained release and avoid the side effects. The EVA matrix containing quinupramine was prepared by solvent-evaporation method. (omitted)