• Journal of Pharmaceutical Investigation
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• 제38권2호
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• pp.119-126
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• 2008

Solid dispersions of poorly water-soluble drug, sibutramine, were prepared with hydrophilic polymer, poly-N-vinylpyrrolidone (PVP), hydroxypropylmethylcellulose (HPMC) and organic acid, citric acid, to improve the solubility of drug. Physicochemical variation and shape of microsphere were characterized by scanning electron microscopy (SEM), differential scanning calorimeter (DSC) and Fourier-transform infrared spectroscopy (FT-IR). Microspheres containing additives showed more spherical shape than non additive microspheres. In vitro release behavior of microspheres presented at simulated gastric fluid (pH 1.2) and simulated intestinal fluid (pH 6.8). The solid dispersion form transformed the drug into an amorphous state and dramatically improved its dissolution rate. These data suggest that the solid dispersion technique is an effective approach for developing the appetite depressant drug products and various pharmaceutical excipients are able to control the release behaviors.

• 대한치과재료학회지
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• 제44권1호
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• pp.33-41
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• 2017

In this study, we prepared PLA-tetracycline complexes coated gold nanoparticle-titania nanotubes and estimated their infrared LASER mediated drug release in the abdominal region of ICR mouse. The results of UV-Vis spectrophotometer showed the highest absorbance at the wavelength of 530 nm and 809 nm indicating the existence of gold nanoparticles. EDX analysis showed that the amounts of gold nanoparticle coated on titania nanotubes were approximately 3.62-36.5 wt%. In vivo test resulted that the tetracycline release value of experimental groups (6.5 ng/mL) was higher than that of control group (5.8 ng/mL) on the condition of 30 minutes of LASER irradiation. Therefore, it is expected that PLA-tetracycline complexes coated gold nanoparticle-titania nanotubes have the feasibility in the field of infrared remote controlled drug device and overcome the limitation of location and time of drug release in dental implant.

• 한국임상수의학회지
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• 제22권3호
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• pp.175-180
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• 2005

본 연구는 개에서 키토산 비드를 이용한 cefadroxil 방출에 영향을 주는 인자, 약물을 함유한 최적의 키토산 비드의 제조, 그리고 키토산 비드로부터 약물의 방출을 평가하는 것이다. 키토산 비드는 tripolyphosphate (TPP)와 이온결합으로 생성되며 비드의 크기는 1 mm 미만이었다. 비드로부터 cefadroxil 방출은 여러 인자에 영항을 받는다. TPP의 pH가 감소할수록 cefadroxil의 비드내 함유량은 증가하지만, 비드로부터 방출량은 감소한다. Cefadroxil의 방출속도은 TPP 농도가 증가할수록 감소한다. 결합시간이 길어지면, 방출량이 감소한다. Cefadroxil을 함유한 키토산 비드를 50 mg/kg 용량으로 건강한 개 4두의 피하에 이식한 결과, cefadroxil의 혈청내 농도는 1 ${\mu}g/ml$ 이상으로 7일간 유지되었다. 따라서 cefadroxil을 함유한 키토산 비드는 개의 농피증 치료에 유용한 것으로 사료되며 약물방출을 통제할 수 있는 약물수송체가 이용될 수 있다고 사료된다.

• 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.

• Journal of Pharmaceutical Investigation
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• 제40권spc호
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• pp.45-61
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• 2010

Polymeric based nanomedicines have been developed for diagnosing, treating, and preventing diseases in human body. The nanosized drug delivery systems having various structures such as micelles, nanogels, drug-conjugates, and polyplex were investigated for a great goal in pharmaceutics: increasing therapeutic efficacy for diseases and decreasing drug toxicity for normal tissues. The functional polymers used for constituting these drug delivery systems should have several favorable properties such as stimuli-responsibility and biodegrdability for controlled drug release, and solublization capacity for programmed drug encapsulation. This review discusses recent developments and trends of functional polymers (e.g., pH-sensitive polymers, biodegradable polymers, and cationic polymers) used for nanosized drug carriers.

• 한국산학기술학회논문지
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• 제11권7호
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• pp.2451-2458
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• 2010

고혈압 치료제인 카르베딜롤을 모델약물로 하여 새로운 서방성 방출 제어형 매트릭스 정제를 제조하기 위하여 소수성 서방성 부형제인 Compritol 888 ATO와 친수성 고분자인 hydroxypropyl methyl cellulose (HPMC) 또는 polyethylene oxide (PEO)를 이용하여 방출 제어형 매트릭스 정제를 제조하였다. 카르베딜롤 방출 제어형 매트릭스 정제의 제조 시 Compritol 888 ATO의 비율과 친수성 고분자의 종류 및 비율, hot melt coating coagglutination (HMCC) rocess의 적용 유무에 따른 카르베딜롤의 방출 양상을 위하여 용출시험기를 사용하여 pH 1.2의 인공위액과 pH 6.8의 인공장액에서 24시간 동안 $37^{\circ}C$, 50 rpm으로 용출시험을 실시하였다. 그 결과, HMCC process를 적용한 모든 제제가 약물의 방출 제어에 매우 효과적인 것을 확인하였다. 또한 소수성 서방성 부형제인 Compritol 888 ATO의 비율에 따라 약물의 방출 양상 및 시간이 기존 일반정제에 비하여 약 95%의 용출률을 나타내었으며 24시간까지 지연됨을 확인할 수 있었다.

• Journal of Pharmaceutical Investigation
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• 제41권1호
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• pp.51-57
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• 2011

The objective of this study was to enhance the utilitization of Ibuprofen (IBU) by introducing the fast-disintegrating tablet (FDT) form. Presently, IBU is being widely used as a tablet or syrup form. But in contrast to these two formulations, IBU as FDT is not only convenient but also increases the control over the time release of the drug, noted by using Alginate beads. This study was carried out with Sodium Alginate and IBU at the ratios of 1:0, 1:0.5, 1:1, and 1:2 in order to produce a series of beads with different ratios. During the drying process of the beads, talc was added in beads to compare the effects with and without the talc. The final product was scanned with SEM imaging to determine the difference in the surface of the beads. The parameters assessed were the diameter, content assay, dissolution test and effectiveness of time-release. Direct compression method was used to prepare FDT containing IBU bead. The properties of FDT, such as hardness, disintegration time, were investigated. The dissolution profiles of FDT were tested using KP dissolution apparatus 1 (basket method). The results suggest addition of talc and drying the beads made the surface smooth and less vulnerable to clutter into chunks. The size of beads was less than 300 ${\mu}m$ which did not create a sandy feeling in the mouth. Thus, the beads formulation model made the sustained release of the drug possible, the hardness of FDT (1.25~1.50 $Kg/cm^2$) was acceptable and all the values of dissolving period were less than 30 seconds. The dissolution profile of FDT was same as that of IBU bead. The efficient dissolution profile and low price of IBU bead containing Sodium Alginate, the FDT formulation prepared from IBU bead can save the expenses and can improve the convenience of application of this drug.

• Medical Lasers
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• 제9권1호
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• pp.6-11
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• 2020

Hydrogels have been developed and used in tissue engineering and regenerative medicine to deliver therapeutics to injured or diseased tissue because of their versatility and properties that can be tailored to match the natural extracellular matrix. Hydrogels can be made with a variety of physical and chemical properties combined with light responsiveness ideal for applications in different fields of medicine that require the spatiotemporal control of therapeutics. Light, as a stimulus, is relatively inexpensive, contact-free, noninvasive with high spatial resolution and temporal control, convenient and easy to use, and allows deep tissue penetration that is relatively harmless. Photoresponsive hydrogels are ideal candidates for on-demand drug delivery systems that are capable of sustained and controlled drug release, minimizing the side effects, and ensuring the activity and efficient delivery of drugs to the target tissue.

• 공업화학
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• 제8권5호
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• pp.715-721
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• 1997

$W_1/O/W_2$ 다중유화의 내부수상($W_1$)에 전해질인 $MgSO_4$를 모델약물로 주입하여 안정성과 약물방출 거동을 현미경관찰, 점도 및 전도도의 변화를 통해 관찰하였다. 내상에 약물을 도입함으로써 내부와 외부수상간의 삼투압차를 유발하여 다중유화계의 불안정성을 초래하였으며 이를 완화하기 위하여 외부수상($W_2$)에 글루코즈를 첨가하여 효과를 살펴본 결과 글루코즈의 유효삼투압 당량이 내부에 포함된 약물의 삼투압 당량과 유사해짐에 따라 안정성이 향상되었을 뿐아니라 초기 약물방출 속도도 글루코즈 농도에 의해 조절할 수 있음을 발견하였다. 이는 삼투압차에 의한 수분 이동시 친수성 계면활성제를 동반하여 내부수상/오일상 계면을 파괴하는 것을 방지하기 때문으로 보인다. 또한 이와같은 현상은 오일상이 cetostearyl alcohol에 의하여 친수화되었을 때 뚜렷하게 나타났다.

• 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.