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Protein Drug Oral Delivery: The Recent Progress
Lee, Hye-J. The Pharmaceutical Society of Korea 2002 Archives of Pharmacal Research Vol.25 No.5
Rapid development in molecular biology and recent advancement in recombinant technology increase identification and commercialization of potential protein drugs. Traditional forms of administrations for the peptide and protein drugs often rely on their parenteral injection, since the bioavailability of these therapeutic agents is poor when administered nonparenterally. Tremendous efforts by numerous investigators in the world have been put to improve protein formulations and as a result, a few successful formulations have been developed including sustained-release human growth hormone. For a promising protein delivery technology, efficacy and safety are the first requirement to meet. However, these systems still require periodic injection and increase the incidence of patient compliance. The development of an oral dosage form that improves the absorption of peptide and especially protein drugs is the most desirable formulation but one of the greatest challenges in the pharmaceutical field. The major barriers to developing oral formulations for peptides and proteins are metabolic enzymes and impermeable mucosal tissues in the intestine. Furthermore, chemical and conformational instability of protein drugs is not a small issue in protein pharmaceuticals. Conventional pharmaceutical approaches to address these barriers, which have been successful with traditional organic drug molecules, have not been effective for peptide and protein formulations. It is likely that effective oral formulations for peptides and proteins will remain highly compound specific. A number of innovative oral drug delivery approaches have been recently developed, including the drug entrapment within small vesicles or their passage through the intestinal paracellular pathway. This review provides a summary of the novel approaches currently in progress in the protein oral delivery followed by factors affecting protein oral absorption.
Current trends in benzodiazepine research
Klinger, M. The Pharmaceutical Society of Korea 1982 Archives of Pharmacal Research Vol.5 No.1
Thank you for inviting me as a guest speaker to this 30th anniversary of the Pharmaceutical Society of Korea. I take it as a compliment to may firm F. Hoffmann-La Roche and Co., Which, has not only dicovered and introduced the benzodiazepines, but has since then been continually in the fore-front of this research. As may subject is going to be "Current Trends in Benzodiazepine Research" I will try to have a look into pending problems. The history of the benzodiazepines has been told several times (e. g. Sternbach, Haefely).
Ryu, Geon-Seek,Park, Soo-Hee,Kim, Eun-Sook,Choi, Byoung-Wook,Ryu, Shi-Yong,Lee, Bong-Ho The Pharmaceutical Society of Korea 2003 Archives of Pharmacal Research Vol.26 No.10
Two known farnesylacetone derivatives (1 and 2) were isolated from the Korean brown alga Sargassum sagamianum off Jeju Island, Korea. Compounds 1 and 2 were identified as (5E,10Z)-6, 10, 14-trimethylpentadeca-5, 10-dien-2, 12-dione and (5E,9E,13E)-6, 10,4-trimethylpentadeca-5,9,13-trien-2,12-dione, respectively, by comparison with the literature data. Compounds 1 and 2 showed moderate acetylcholinesterase and butyrylcholinesterase inhibitory activities with $IC_{50}$ values of 65.0∼48.0 and 34.0∼23.0 $\muM$, respectively.
Kang, Jong-Seong,Linh, Pham-Tuan,Cai, Xing-Fu,Kim, Hang-Sup,Lee, Jung-Joon,Kim, Young-Ho The Pharmaceutical Society of Korea 2001 Archives of Pharmacal Research Vol.24 No.5
Reversed-phase high performance liquid chromatographic method was applied for the determination of eleutheroside B and E in the various Acanthopanax species collected In Korea. The stationary phase used was Zorbax 300 SB $C_{18}$ and a mobile phase program was used, which started at 6% acetonitrile for 2 min, and then a linear gradient was operated for the next 18 min to 17% acetonitrile at a flow rate of 1.0 ml/min. The column effluent was monitored at UV 210 nm. Identification was carried out by comparing the retention time and the LC/MS spectrum of each peak corresponding to eleutheroside B and E from sample with those of standards. In general, the contents of eleutheroside B and 1 in stems were higher than those In roots. Acanthopanax species could be classified into two groups based upon the contents of eleutheroside B and E: one group contains no or very little eleutheroside B and another contains both eleutheroside B and E.
Effects of Nelumbinis Semen on Contractile Dysfunction in Ischemic and Reperfused Rat Heart
Kim, Jong-Hoon,Kang, Moon-Kyu,Cho, Chong-Woon,Chung, Hwan-Suck,Kang, Chang-Woon,Parvez, Shoukat,Bae, Hyun-Su The Pharmaceutical Society of Korea 2006 Archives of Pharmacal Research Vol.29 No.9
Nelumbinis Semen (NS), or lotus seed, is one of the most well-known traditional herbal medicines and is frequently used to treat cardiovascular symptoms in Korea. The anti-ischemic effects of NS on ischemia-induced isolated rat heart were investigated through analyses of changes in blood pressure, aortic flow, coronary flow, and cardiac output. The subjects in this study were divided into two groups: a control, untreated ischemia-induced group, and an ischemia-induced group treated with NS. There were no significant differences in perfusion pressure, aortic flow, coronary flow and cardiac output between the groups before ischemia was induced. The supply of oxygen and buffer was stopped for ten minutes to induce ischemia in isolated rat hearts, and NS was administered during ischemia induction. NS treatment significantly prevented decreases in perfusion pressure, aortic flow, coronary flow and cardiac output under ischemic conditions (p<0.01). In addition, the mechanism of the anti-ischemic effects of NS was also examined through quantitation of intracellular calcium content in rat neonatal cardiomyocytes. NS significantly prevented intracellular calcium increases induced by isoproterenol (p<0.01). These results suggest that NS has distinct anti-ischemic effects through calcium antagonism.
Synthesis of Praziquantel Derivatives and Their In Vitro Activity Against Adult Clonorchis sinensis
Kim, Choong-Sup,Min, Duk-Young The Pharmaceutical Society of Korea 1998 Archives of Pharmacal Research Vol.21 No.6
Several praziquantel derivatives have been prepared by the acylation of compound 5, and examined on their biological activity in vitro agninst adult clonorchis sinensis collected from rabbits infected with metacercariae which was isolated from Pseudorasbora parva, a second intermediate host, captured in Nakdong river in Korea.
Extraction and Determination of Phytosterols from Corn Oil Foots
Kim, Sang-Ho,Park, Sang-Hoo,Ahn, Byung-Goo,Yi, Jeong-Sang,Park, Moo-Sin,Lee, Byeong-Ryong,Kim, Kweon The Pharmaceutical Society of Korea 1990 Archives of Pharmacal Research Vol.13 No.3
By saponification and extraction of corn oil foots abandoned as waste during oil refining, a mixture of phytosterols was obtained, and its major components were determined as .betha.-sitosterol, campesterol and stigmasterol by gas chromatographic analysis. The mixture is very cheap and regarded as an excellent substrate for direct fermentation of C-17 keto steroid intermediate for various steroid pharmaceuticals.
Kim, Hee-Sun,Choi, Eung-Chil,Kim, Byong-Kak,Park, Young-In The Pharmaceutical Society of Korea 1992 Archives of Pharmacal Research Vol.15 No.1
Bacillus anthracis 590 having an inducibla resistance determinant to MLS antibiotics was isolated from a soli sample in Korea. The resistance gene (ernJ) was cloned by Southern blotting of chromosomal DNA fragment digested by various restriction enzymes and coloy hybridization method and the cloned plasmid was named as pBA423. The size of inserted DNA fragment of pBS42 vector was about 2.9 kb and the DNA sequence of the subcloned fragment (Hinc II-Hinc II, 1.4kb) WAS determined. The DNA sequence of ernJ was composed of 357 bp for leader region and 861 bp for the structural gene. Because the leader sequence of ernJ was homologous to that of ermK, the expression of ernJ is also thought to be controlled by a transcriptionl attenuation mechanism.
Demographic Characteristics of Zipeprol-associated Deaths in Korea
Chung, Hee-Sun,Choi, Hwa-Kyung,Kim, Eun-Mi,Park, Mee-Jung,Chung, Kyu-Hyuck,Yoo, Young-Chan The Pharmaceutical Society of Korea 1998 Archives of Pharmacal Research Vol.21 No.3
The abuse of zipeprol, an antitussive agent, was found to be most prevalent among young people in Korea. Because abusers take large doses of this drug for its hallucinogenic effects, fatalities from zipeprol overdose abuse have been on the rise since 1991. Since 1991, a total of 69 zipeprol-related deaths have occurred throughout the nation. A demographic study shows that in ninety six percent of cases involving zipeprol alone, the victims were in their teens and twenties. The mate/female ratio in zipeprol related death was 3.5:1. Most of these zipeprol-associated deaths occurred in the larger cities of Seoul and Inchon. The blood concentration of zipeprol ranged from 0.8 to $38.3{\mu}g/mL $in single drug involved deaths, while zipeprol varied from to 35.3 $0.1{\mu}g/mL $in zipeprol and dextromethorphan victims.
Seong, Chi-Nam,Shim, Eun-Sook,Kim, Shin-Moo,Yoo, Jin-Cheol The Pharmaceutical Society of Korea 2004 Archives of Pharmacal Research Vol.27 No.2
The prevalence, genotype for antibiotic resistance and antibiotic susceptibility of vancomycin resistant enterococci (VRE) were determined. And molecular typings of the Enterococcus faecium isolates were analyzed. Prevalence of VRE in chickens, healthy children and intensive care unit (ICU) patients was 41.6%,7.9%, and 20.4%, respectively. Forty out of 54 isolates from chicken intestines, and 9 out of 11 from ICU patients were identified as Enterococcus faecium. Eleven out of 13 isolates from non-hospitalized young children were E. gallinarium. Twelve strains of E. faecalis were isolated from chicken intestines. The gene for the antibiotic resistance in E. faecium, and E. faecalis was vanA, while that in E. gallinarium was vanC1. E. faecium isolates were resistant to most of antibiotics except ampicillin and gentamicin. Molecular typing of the E. faecium strains obtained by pulse field gel electrophoresis and repetitive sequence-based PCR suggest that VRE transmit horizontally from poultry to humans, especially young children, via the food chains in Korea.