http://chineseinput.net/에서 pinyin(병음)방식으로 중국어를 변환할 수 있습니다.
변환된 중국어를 복사하여 사용하시면 됩니다.
Lee, Sangkil,Lee, Jaehwi,Choi, Young Wook Pharmaceutical Society of Japan 2008 Biological & pharmaceutical bulletin Vol.31 No.4
<P>Liquid intraurethral prostaglandin E<SUB>1</SUB> (PGE<SUB>1</SUB>) delivery system was developed using self-microemulsifying drug delivery system (SMEDDS). For this, pseudo-ternary phase diagrams were constructed and characterized. The viscosity of optimized formulation was increased gradually upon the addition of water and it was decreased from the water contents over 40%. With excessive mass of water, the present system transformed to a free flowing microemulsion. These results demonstrate that the present liquid PGE<SUB>1</SUB> SMEDDS formulation might stay in the urethra as a viscous sol or gel state with contacting the moisture of urethra and easily eliminated by urination. Draize test and long-term stability study revealed that the present system would be safe and PGE<SUB>1</SUB> would be stable for more than one year at 4 °C, respectively. In the feline animal model, SMEDDS formulation was as effective as PGE<SUB>1</SUB> intracavernosal injections in terms of ICP (intracavernosal pressure), penile length increment, and erection sustaining time was more elongated than PGE<SUB>1</SUB> injections. Therefore, SMEDDS was considered as a promising PGE<SUB>1</SUB> intraurethral liquid formulation for erectile dysfunction treatment.</P>
The distribution and retention of paclitaxel and doxorubicin in multicellular layer cultures
LEE, JOO-HO,NA, KUN,SONG, SOO-CHANG,LEE, JAEHWI,KUH, HYO-JEONG D.A. Spandidos 2012 Oncology reports Vol.27 No.4
<P>Limited distribution of anticancer drugs has been recognized as a significant hurdle to efficacy. We investigated a detailed penetration/distribution profile of paclitaxel-rhodamine (PTX-rd) and doxorubicin (DOX) in multicellular layer (MCL) cultures of human cancer cells as an <I>in vitro</I> model for avascular regions of solid tumors. MCLs were exposed to drugs and fluorescent images of frozen sections were acquired for determination of drug penetration into MCL under various exposure conditions. PTX-rd and DOX showed drastically different profiles of penetration. DOX showed full penetration after 1 h and accumulation over 3 h, whereas PTX-rd showed slow and limited penetration, with accumulation only within the top 20% of layers by 2 h and insignificant penetration even at 72 h. Drug retention in MCL was more dependent on drug concentration, rather than exposure time, i.e., drug distribution increased by 6.3- and 2.5-fold for PTX-rd and DOX, respectively, when exposed to higher concentrations under comparable AUC exposure (1 μM × 24 h vs. 50 μM × 0.5 h). Anti-proliferative activity of PTX and DOX in MCL, as determined by cell cycle analysis, was minimal and may be attributed, at least in part, to their limited distribution in multicellular cultures. Overall, we demonstrated that penetration and retention of PTX and DOX in MCL was not only concentration- and time-dependent, but also schedule-dependent. It is suggested that slow releasing formulations or a slow infusion regimen may not necessarily be desirable, especially for PTX, due to insufficient penetration and accumulation which may result from a low local concentration at the target site.</P>
Ex Vivo Permeability Characteristics of Porcine Buccal Mucosa to Drugs with Various Polarity
Lee, Jaehwi,Lee, Yoonjin,Yoon, MiKyeong,Choi, Young Wook 한국약제학회 2005 Journal of Pharmaceutical Investigation Vol.35 No.2
The aim of this study was to analyze characteristics of the barrier function of excised porcine buccal mucosa to the test compounds, estradiol, propranolol HCI, melatonin, and mannitol with a wide range of partition coefficient values. The permeability of melatonin was measured through frozen, stored, and fresh porcine buccal mucosa to examine the impact of storage conditions on the permeability of porcine buccal mucosa. The results demonstrated that the ex vivo permeability of the porcine buccal mucosa was greater for more lipophilic solutes, which was consistent with a series of molecules trans-ported by passive transepithelial diffusion. The melatonin permeation profiles through frozen, stored. and fresh mucosa illustrated that damage was incurred by the freezing process of the mucosal tissue. leading to loss of the barrier function and thereby an increased permeation coefficient. It can be observed that the influence of compound lipophilicity on the association of the compounds with buccal mucosa was clean. The relationship between permeation coefficient and Log P values for the four compounds investigated demonstrated a proportional relationship, further confirming the importance of the lipophilicity of a compound to permeate the buccal mucosa. These results showed that the ex vivo porcine buccal mucosa model is a suitable tool to screen oral mucosal permeability.
Biopharmaceutical Evaluation of a Solid Dispersion System Containing Sibutramine Freebase
Lee, Min-Suk,Chang, Hee-Chul,Kim, Taewan,Park, Jung-Hwa,Lee, Bong-Sang,Kim, Sung-Hee,Kim, Do-Hwan,Kim, Bo-Gyun,Oh, Seong-Tae,Kang, Myung-Joo,Park, Jong-Hyeok,Lee, Jaehwi,Choi, Young-Wook Korean Chemical Society 2008 Bulletin of the Korean Chemical Society Vol.29 No.4
To increase the solubility of sibutramine freebase, the solid dispersion was prepared using a fluid-bed granulator. The solid dispersion containing sibutramine freebase was characterized by differential scanning calorimetry (DSC) and powder X-ray diffraction (XRD). After filling the sibutramine solid dispersion in the gelatin hard capsule, we performed in vitro dissolution test, the stability test under accelerated conditions and pharmacokinetic study in beagle dogs. The DSC and XRD data showed that sibutramine solid dispersion would be amorphous state. The dissolution rate of sibutramine solid dispersion was significantly increased about 70% than sibutramine freebase. The stability of sibutramine solid dispersion capsules was equivalent or above to commercial product of sibutramine. In beagle dogs, the sibutramine solid dispersion showed equivalent pharmacokinetic behavior with commercial product of sibutramine hydrochloride. In conclusion, the solid dispersion system provided a possible way to overcome the low solubility of sibutramine freebase, and the sibutramine solid dispersion can be a bioequivalent with the commercial product in humans.
수성미세채널을 형성하는 서방성 매트릭스 장용정을 이용한 탐스로신의 방출제어
이기봉,최성업,전홍렬,이봉상,김현일,이재휘,최영욱 한국약제학회 2004 Journal of Pharmaceutical Investigation Vol.34 No.6
Tamsulosin has been frequently used for the treatment of benign prostatic hyperplasia. To avoid dose-dependent side effects of tamsulosin upon oral administration, the development of sustained-release delivery system is required, that can maintain therapeutic drug levels for a longer period of time. The aim of this study was therefore to formulate sustained-release tamsulosin matrix tablets and assess their formulation variables. We designed enteric coated sustained-release tamsulosin matrices to fulfill above statement. Aqueous microchannels in the enteric film need to be formed in order to obtain tamsulosin release even in an acidic environment such as gastric region. In the sustained-release tamsulosin matrix, low viscosity hydroxypropylmethylcellulose was used as a rate controller. Povidone K30 was also added to the matrices to facilitate water uptake so that a decrease in the release rate of tamsulosin as time elapses was prevented, possibly leading to pseudo zero-order release of the drug. The matrices were enteric-coated with hydroxypropylmethylcellulose phthalate (HPMCP), along with povidone K30 as an aqueous microchannel former. With the aqueous microchannels formed within the enteric film, tamsulosin could be released in an acidic condition. The release of tamsulosin decreased with increasing thickness of HPMCP membrane while the release rates of tamsulosin from those having different HPMCP thickness in pH 7.2 aqueous media were not considerably different, indicating that the enteric film was promptly dissolved at pH 7.2. These results clearly suggest that the sustained-release oral delivery system for tamsulosin could be designed with satisfying drug release profile approved by the KFDA.
Lee, Kyung-Min,Oh, Taek-Joo,Kim, So-Hyun,Kim, Hye-Youn,Chung, Hyunmi,Min, Daniel Seungwook,Auh, Joong-Hyuck,Lee, Hong Jin,Lee, Jaehwi,Choi, Hyung-Kyoon Korean Society of Food Science and Technology 2016 Food Science and Biotechnology Vol.25 No.4
In this study, comprehensive metabolic profiles of mulberry fruits (Morus alba Linnaeus) at various maturation stages were determined using GC-MS and HPLC. In total, 48 compounds, including 3 alcohols, 16 amino acids, 7 organic acids, 2 sugars, 4 phenolics, 2 terpenes, 3 vitamins, 9 fatty acids, and 2 cyanidins were identified in the mulberry samples. Levels of chlorogenic acid, cryptochlorogenic acid, neochlorogenic acid, ascorbic acid, and ${\delta}-tocopherol$, and total fatty acid content were significantly higher in the semi-matured mulberry fruits. Furthermore, levels of glycerol, citrate, fructose, glucose, 3-O-glucoside, and cyanidin-3-O-rutinoside were significantly higher at the fully matured stage than at the other stages. Twelve biosynthetic pathways were suggested as major pathways involved in mulberry fruit maturation. The information obtained in this study will provide a basis for future investigations toward quality control or metabolic engineering for development of mulberry fruits possessing commercially valuable characteristics.