• Journal of Pharmaceutical Investigation
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• 제37권4호
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• pp.211-216
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• 2007

The bark of Alnus japonica has been used for the treatment of fever, hemorrhage and diarrehea in oriental traditional medicine. Recently, it was revealed that the diarylheptanoids from the bark of Alnus japonica possess anti-inflammatory activity and are expected to be applicable for atopic dermatitis. In this study, oregonin, one of major active components in the bark of Alnus japonica, was developed in the form of semisolid formulations for topical delivery. Oregonin was incorporated into four ointment bases: O/W cream, W/O cream, hydrophilic ointment and lipophilic ointment. Oregonin release from all formulation prepared was evaluated. Franz cell method and immersion method were employed to characterize the release patterns of drug from each formulation based on solvent availability. O/W cream showed a better release profile than the other formulations when evaluated with Franz cell method with an order of O/W cream, hydrophilic ointment, W/O cream and lipophilic ointment. In the immersion method, hydrophilic ointment showed the greatest release rate at times 1 hour exceeding compared to other bases with an order of hydrophilic ointment, O/W cream, W/O cream and lipophilic ointment. Hydrophilicity and solvent availability of formulation seems to significantly influence the release rate of oregonin from ointment bases. In this study, we successfully characterized the oregon in ointment and found that o/w cream is a promising formulation for the topical delivery of oregonin.

• Archives of Pharmacal Research
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• 제8권3호
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• pp.159-168
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• 1985

In attempt to develop a drug delivery system using serum albumin microspheres, bovine serum albumin microspheres containing antitumor agent, cytarabine, were prepared. The shape, surface characteristics, size distribution, behavior of in vitro distribution, drug release behaior, and degradation of albumin microspheres in animal liver tissue homogenate and proteolytic enzyme were investigated. The shape of albumin microspheres was spherical and the surface was smooth and compact. The size distribution of the albumin microspheres was affected by dispersion forces during emulsification and albumin concentration. Distribution of albumin mirospheres after intravenous administration in rabbit was achieved immediately. In vitro, albumin microsphere matrix was so hard that it retained most of cytarabine except initial burst during the first 10 minutes, and the level of drug release during the initial burst was affected by heating temperature, drug/albumin concentration ratio and size distribution. After drug release test, the morphology of albumin micropheres was not changed. Albumin microsphere matrix was degraded by the rabbit liver tissue homogenate and proteolytic enzyme. The degree of degradation was affected by heating temperature.

• Archives of Pharmacal Research
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• 제26권8호
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• pp.644-648
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• 2003

To investigate the feasibility of developing a new ondansetron transdermal system, the effects of vehicles and penetration enhancers on the in vitro permeation of ondansetron hydrochloride (OS) from a pressure-sensitive adhesive (PSA) matrices across dorsal hairless mouse skin were studied. Vehicles employed in this study consisted of various ratios of propylene glycol monocaprylate (PGMC)-diethylene glycol monoethyl ether (DGME) co-solvents and PGMC-propylene glycol (PG) co-solvents with 3% oleic acid. $Duro-Tak^\circledR$ 87-2100 and $Duro-Tak^\circledR$ 87-2196 were used as PSAs. The concentration of DGME in PGMC-DGME co-solvent system affected the release rate; as the concentration of DGME increased, the release rate decreased. The cumulative release amount of OS increased as the ratio of PSA to drug solution decreased. The permeation flux was also primarily affected by the amount of PSAs; as the amount decreased, the permeation flux increased. The overall fluxes from matrix formulations were significantly lower when compared to those obtained from solution formulations. The ratio of PG to PGMC did not affect permeation flux, while the lag time decreased significantly from $5.14\pm3.31 to 0.31\pm0.12$ h as the PG increased from 40% to 60%.

• Macromolecular Research
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• 제10권5호
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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.

• Journal of Pharmaceutical Investigation
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• 제22권2호
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• pp.133-137
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• 1992

A novel oral controlled release tablet which may offer more uniform drug level in the body than simple zero-order was developed. The tablet is composed of three layers; outer film layer, middle part compression-coated hydroxypropylmethylcellulose (HPMC) matrix layer, and inner core layer. Each layer contains nicardipine HCl as a model drug. In vitro dissolution test showed that the tablet released the drug in clear three steps; a rapid initial release, followed by a constant rate of release, and then a second phase of fast release of drug. The dissolution characteristics could be modified easily by changing the grade of HPMC, thickness of matrix layer, content of methylcellulose in matrix layer, content of active ingredient in each layer. The pH of dissolution medium did not affect the release profile. This three-step release system is expected to raise the blood concentration rapidly to effective level and to maintain effective blood level longer than simple slow-release systems.

• Journal of Pharmaceutical Investigation
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• 제29권4호
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• pp.343-348
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• 1999

The purpose of this study is to prepare the controlled release adhesive patch containing naproxen. Pressuresensitive adhesive (PSA)-type patch was fabricated by casting of polyisobutylene (PIE.) and mineral oil in toluene. Membrane-controlled release (MCR)-type patch was prepared by the attachment of the controlled release membrane on the PSAtype patch. The membrane was mainly composed of Eudragit, polyethylene glycol(PEG) and glycerin. The drug release profile and skin permeation test with various patches were evaluated in vitro. The release of naproxen from PIE-based PSAtype patch with various loading doses fitted Higuchi's diffusion equation. However, the permeation of naproxen through hairless mouse skin from PSA-type patch followed zero-order kinetics. In MCR-type patch, thickness of controlled release membrane affected on the drug release rate highly. In the composition of membrane, the release rate was decreased as the ratio of Eudragit increased. The drug release from the MCR-type patch followed zero order kinetics. The permeation of naproxen through hairless mouse skin from MCR-type patch showed lag time for the intial release period and didn't fit the zero-order kinetics

• 대한화장품학회지
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• 제33권4호
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• pp.219-225
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• 2007

비스에칠헥실옥시페놀메톡시페닐트리아진(Bis-ethylhexyloxyphenolmeth oxyphenyltrizine; BEMT)은 식품의약품안전청 고시 기능성 원료로 자외선 차단 제품에 널리 사용되는 UVA와 UVB의 화학적 자외선 흡수제이다. 그러나 BEMT는 실제 적용에 있어 여러 가지 결점이 있어 사용이 제한되고 있다. 본 연구의 목적은 BEMT가 적용된 고형지질나노입자(BEMT- SLN)의 자외선차단제품 응용에 있다. 제조된 고형지질나노입자의 입도는 약 330 nm, 봉입율은 93.3 %, 결정화지표는 4.3 %였다. In vitro 방출 및 투과 실험 결과에서, BEMT는 SLN보다 O/W 에멀젼이 대체로 높았다. In vivo 실험에서 SLN의 BEMT 방출비는 80 % 감소하였다. 또한 in vitro UV 방어 효과 실험에서 SLN이 적용된 처방의 자외선방어지수(SPF) 값은 약 2.5배 증가하였다. 결국 SLN은 BEMT를 효과적으로 봉입하고 있었으며, 자외선 차단 상승 효과를 나타낸다.

• 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.

• 폴리머
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• 제24권5호
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• pp.728-735
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• 2000

지속적인 국소 마취의 가능성을 연구하기 위하여 펜타닐이 함유된 생분해성 poly(L-lactide-glycolide) (75 : 25 락타이드와 글리콜라이드의 몰 비, PLGA) 미립구를 제조하였다. 펜타닐 베이스가 함유된 PLGA 미립구는 일반적인 O/W 용매 증발법으로 제조하였으며 미립구의 크기는 10에서 150 $\mu\textrm{m}$의 범위에 있었다. 미립구의 표면과 단면 형태를 전자현미경으로 관찰하였고 생체외 펜타닐 베이스 방출량은 HPLC로 분석하였다. 젤라틴 유화제의 사용으로 가장 낮은 다공성 단면의 형태와 가장 높은 포접율을 가질 수 있었다. 펜타닐의 방출 패턴은 유화제의 종류, PLGA의 분자량 및 농도, 초기 약물 loading양 등과 같은 제조 조건들의 영향이 미치는 것으로 관찰되었다. 생체외에서 펜타닐 베이스의 방출은 제조 조건을 조절함으로써 거의 zero-order 형태로 25일 이상으로 지속적이었다. 또한 XRD와 DSC로 펜타닐이 함유된 PLGA 미립구의 물리화학적인 성질을 조사하였다.

• Journal of Pharmaceutical Investigation
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• 제19권4호
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• pp.185-190
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• 1989

The release of angiotensin and ${\alpha}-amylase$ from monolithic devices of different molecular weight of polyethylene glycol (PEC) grafted polyurethane copolymer was investigated. Water-soluble PEG grafted polymer provided a controlled release of angiotensin and ${\alpha}-amylase$. The release rate of angiotensin and ${\alpha}-amylase$ could be controlled by varying the molecular weight of PEC grafted. The release mechanism may be associated with the creation of pore or domain through the devices following the gel swelling and self-aggregation by PEC grafted polymer. Hydrophobic polyurethane grafted with PEG can provide a biomaterial for prolonged release of angiotensin and ${\alpha}-amylase$ from angiotensin and ${\alpha}-amylase$ blended system.