• Natural Product Sciences
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• 제15권2호
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• pp.71-75
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• 2009

The great economic and social damage caused by unusual explosion of jellyfish population has attracted the attention of researchers. A chemical study on the bioactive components of the giant jellyfish Nemopilema nomurai led to the isolation of two new (1 and 2) and three known alkoxyglycerols (3 - 5), along with known monoglycerides (6 - 7) and fatty acids. Based on NMR and MS data, the structures of compounds 1 and 2 were elucidated as 1-O-[(Z)-tetradec-3-enyl]-sn-glycerol and 1-O-[(Z)-octadec-10-enyl]-sn-glycerol, respectively. The absolute configurations of compounds 1 - 7 were determined by comparison of specific optical rotation values with those reported. The isolated compounds were evaluated for suppressive effect on the proinflammatory mediators (NO, IL-6, and TNF-${\alpha}$) in murine macrophage cells. However, they were found inactive upto the concentration of 100 ${\mu}M$.

• 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.190.3-190.3
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• 2003

Three new butenolides (1-3), and a new cyclopentenone derivative (4) were isolated from a marine sponge Homaxinella sp. by bioactivity guided fractionation. The gross structures were established on the basis of NMR and MS analyses. The stereochemistry of the butenolides and cyclopentenone derivative was defined on the basis of optical rotation and CD spectroscopy. The compounds were tested against a panel of five human solid tumor cell lines and displayed marginal to significant cytotoxicity.

• Archives of Pharmacal Research
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• 제28권5호
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• pp.619-625
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• 2005

Beads loaded with the water-soluble drug, phenylpropanolamine HCl (PPA), were prepared using an extruder and double arm counter-rotating roller modified from a traditional pill machine. The mean diameter of the cylindrical rod-like extrudate from the ram extruder was 3 mm; that of the uncoated bead after cutting and spheronization by the modified double arm counter-rotating roller was 3.26~3.28 mm. Although the surface of the beads was moderately rough and irregular, some exhibited hump-shaped protrusions, the sphericity was acceptable (roundness 1.15) and adequate for the subsequent coating process. An increase in mean diameter of the coated beads and improvements in friability and sphericity were observed in proportion to the amount of coating material applied (ethylcellulose or Eudragit？？ RS 100). It was also found that the release rate of PPA from the coated beads could be controlled by the amount and type of coating materials applied or with the incorporation of Eudragit ？？ RS 100 into the core matrix. Further modifications to the double arm counter-rotating roller, including adjustment of the rotation speed and distance between the rollers, would yield smaller uncoated beads with improved roundness and surface roughness. In conclusion , the present method could be potentially applied to prepare controlled release drug delivery beads or pellet dosage forms.

• 약학회지
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• 제55권2호
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• pp.131-137
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• 2011

The dissolution test method and an analytical procedure by HPLC were developed and validated for dobesilate calcium tablets and acepifylline tablets. These drugs were not yet characterized by the dissolution specifications in Korean Pharmaceutical Codex. So, with each reference and test drugs, we did the preliminary and standard experiments based on the Korean Pharmacopeia Guideline of dissolution testing for solid oral dosage forms. The dissolution test for dobesilate calcium tablets was carried out under sink conditions as following: dissolution medium water, paddle rotation speed 50 rpm and vessel volume 900 ml. More than 90% of its label amount was released within 30 min in this method. Also the dissolution test for acepifylline tablets was carried out under sink conditions as follows: dissolution medium water, paddle rotation speed 100 rpm and vessel volume 900 ml. More than 90% of its label amount was released within 45 min in this method. The dissolution samples were analyzed with a precise and accurate HPLC method. The developed dissolution test showed specificity, linearity, precision and accuracy within the acceptable range. The dissolution testing method described above was adequate for the purpose and may be proposed as a pharmacopeial standard to assess the performance of dobesilate calcium tablets and acepifylline tablets.

• 한국의료질향상학회지
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• 제1권2호
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• pp.60-72
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• 1994

Background: The number of outpatients visiting large university teaching hospitals has increased drastically with the introduction of a nationwide health care insurance in 1989 and the improvement of the socio-economic status of the population. This resulted in long waiting times for services, particularly prescribed drugs, which have been patients' chief complaints. Hospitals have tried to solve the problem with limited success because their approach lacked comprehensive research. The objective of this study is to investigate associations between waiting times and variables defining a total work system. Methods: Data for the outpatient pharmacy department in a tertiary care university teaching hospital located in Seoul was analyzed to achieve the study objective. Associations of pharmacy system variables -- work load, work force, pharmacist work schedule, machine problems, and inventory control -- with mean and 99th percentile of waiting times were examined by the hierarchical stepwise regression method. Day was a unit of the analyses. Results: The regression models explained 65.8% of variance in the mean waiting time and 61.34% in the 99th percentile of waiting times. The break-down of the printer for drug envelops, Automatic Tablet Counters (ATCs), and main computer system lasted longer than 30 minutes increased the mean for 7.7 minutes, 4.5 minutes, and 7.0 minutes, respectively, and the 99th percentile for 14.8 minutes, 9.0 minutes, and 15.7 minutes, respectively. Concerning the work force, study results showed that there were significant differences in the productivity of pharmacists with work experience more than three years, one to three years, and less than one year, and showed that peak time aid work by pharmacists at job assignments other than the outpatient pharmacy, part-time pharmacists, and the installation of ATCs were effective in reducing waiting times, Finally, study findings indicated that the operational policy of work assignment and rotation schedule, supply and inventory of drugs at work tables, and readiness for undisrupted work during the work hours could have a significant effect on waiting times. Conclusion: The study results indicated that efforts to reduce waiting times for prescribed drugs should be geared toward every components of the pharmacy work system ranging from work schedule of pharmacists and supply of dugs at work tables. These findings should provide hospital managers with right directions in battling the problem.

• 약학회지
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• 제40권6호
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• pp.632-639
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• 1996

Most stable conformers of some antiinflammatory fenamates were obtained by conformational free energy change calculations. Conformational energies for the molecules as unhydrate d state were estimated first, and those as hydrated state were calculated then to simulate the molecules in aqueous solution using a hydration shell model. The initial geometries of the molecules were obtained either from X-ray crystallographic data or from homologous molecular fragments. The bond lengths and angles were not varied, but all the torsion angles were varied step by step during the conformational free energy surface searching. The results show that there are several feasible conformations for a compound. And the molecules are somewhat stabilized by hydration (-${\delta}G_{hyd}{\cong}$13 to 16kcal/mole), but the conformations were not changed significantly by the hydration itself. There seems to be a strong tendency of intramolecular hydrogen bonding between imino hydrogen and carboxyl oxygen of the compounds. As a result, the carboxyl group cannot be rotated freely, and the rotation of the second aromatic ring is the main reason for the conformational variations of the compounds. The ECEPP force fields via the program CONBIO were used throughout this study.

• Archives of Pharmacal Research
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• 제16권3호
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• pp.219-226
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• 1993

For the analysis of structure relationship of ar-turmerone analogues, the compounds containing the various substituents on the phenyl ring and 1(or 2)-naphthyl group in the place of phenyl of ar-turmerone were prepared and tested their cytotoxicity against HL-60, K-562, and L1210 leukemia cells in vitro. The substituents at para position are methoxy, phenoxy, methyl, trifluoromethyl, fluoro, and chloro. At meta position methoxy, methyl, trifluoromethyl, or chloro groups at ortho position mathoxy or chloro group were introduced. Against HL-60 and K-562 cells, $ED_{50}$ values of the analogues are ranged from 0.8 to $30.0\;\mu{g/ml}$. Againste L1210 cell, these are located more than $20.0\;\mu{g/ml}$. However, 5-carbone-thoxy-2-methyl-6(1-naphthyl)-2-octen-4-one (5n)possesses $ED_{50}$ valuses 0.8, 2.1, $6.5\;\mu{g/ml}$ against HL-60, L1210 cells, respectively. The electronic nature of the substituents on phenyl ring of ar-tumerone dose not affect the biological activity. Therefore the flat structure of aromatic potion of ar-tumerone analogues is the more important factor for their activity rather than its electronic nature. The potentiation of the cytotoxicity with the enlargement of aromatic ring region also supports the importance of the plane structure of this area. The restriction of the single bond rotation between C-6 and aromatic ring through the introduction of substituents at the ortho position of phenyl ring and the increment of size of alkyl group at C-6 position enhances the activity. Therefore the effective conformation should by the one having the orthogonal arrangement between the aromatic ring and the side chain.

• 약학회지
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• 제55권4호
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• pp.324-331
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• 2011

Although the dissolution test can serve as an effective tool for quality control and predictor of in vivo performance, there are a number of drugs with no established dissolution specifications in Korean Pharmaceutical Codex (KPC). Among those commercially available, Piracetam Tablets and Fenoterol hydrobromide Tablets were selected to develop the dissolution testing method. The dissolution condition was determined based on the "Guidelines on Specifications of Dissolution tests for Oral dosage forms" of Korea Food & Drug Administration (KFDA). The dissolution test for Piracetam Tablets was carried out under sink condition with distilled water as dissolution medium, paddle rotation speed at 50 rpm and medium volume of 900 ml. More than 80% of its label claim was released within 30 min. In case of Fenoterol hydrobromide Tablets, distilled water was also found to be suitable to ensure sink condition. The rotation speed of 50 rpm and 900 ml of dissolution medium were used to evaluate the dissolution profile. The dissolution rate of fenoterol hydrobromide was over 90% in 15 min. The HPLC analysis methods were validated in terms of accuracy, precision, specificity, linearity, quantitation limit and range. The results suggested that the analytical methods used are simple and suitable to measure the dissolution rate of piracetam and fenoterol hydrobromide. Therefore, the analysis methods could be utilized in setting dissolution specifications of Piracetam Tablets and Fenoterol hydrobromide Tablets in the revised version of KPC.

• Bulletin of the Korean Chemical Society
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• 제7권5호
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• pp.367-371
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• 1986

Dynamic and equilibrium properties of n-alkane chains immersed in solvent molecules have been investigated by a molecular dynamics method. The n-alkane chain is assumed to be a chain of elements (CH$_2$) interconnected by bonds having a fixed bond length and bond angle, but each bond of the chain is allowed to execute hindered internal rotation. We studied the effect of the number of the chain elements (N$_c$ = 10, 15 and 20) on the equilibrium properties of the system, e.g., the pair correlation functions between a chain element and solvent molecules, g$_{cs}$(r), and between the chain elements, g$_{cc}$(r), and the configurational properties such as the mean-square end-to-end distance < R$^2$ >, the mean-square radius of gyration < S$^2$ >, and the eigenvalues of the moment-of-inertia tensor < S$_i^2$ > / < S$^2$ > (i = 1, 2 and 3). We also studied the dynamic properties of the system, e.g., the autocorrelation function C(A;t) where A = R$^2$(t), = S$^2$(t), or = ${\vec{V}}(t)({\vec{V}}$ = velocity of the center of mass), and the diffusion coefficient D. The g$_{cs}$(r)'s are almost equal irrespective of the change of Nc while g$_{cc}$(r) becomes larger as N$_c$ increases; The MD computed configurational properties < R$^2$2 > and < S$^2$ > were found to be a little different from the values calculated from the statistical equations of < R$^2$ > and < S$^2$ >, it may be due to the fact that our model for the MD simulations includes a long-range volume effect. From the < S$_i^2$ > / < S$^2$ >, it is found that the chain molecule has a nearly spherical shape irrespective of the variation of N$_c$. For the dynamic properties we found that the C(R$^2$;t) and C(S$^2$;t) of lower N$_c$ decay faster than those of higher N$_c$, while the C($\vec V$;t) of the center of mass in the chain is weakly dependent on the N$_c$. The center of mass diffusion coefficient D$_c$ decreases as N$_c$ increases while the end point diffusion coefficient D$_e$ is nearly equal irrespective of the change of N$_c$.

• 생명과학회지
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• 제20권12호
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• pp.1792-1800
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• 2010

바실러스 폴리퍼멘티쿠스 케이제이에스-2의 발효액에서 5 종류의 마크로락틴을 분리하였다. 각각의 구조를 분석한 결과로 마크로락틴 에이, 말로닐 마크로락틴 에이, 숙시닐 마크로락틴 에이, 마크로락틴 이, 마크로락틴 에프 등으로 규명되었다. 특히 3종의 항생제인 마크로락틴 에이, 말로닐 마크로락틴 에이, 숙시닐 마크로락틴 에이는 반코마이신 내성 장구균과 메치실린 내성 황생포도상구균에 효과적으로 성장억제를 나타내었다. 이것은 반코마이신이나 테이코플라닌보다 우수한 항생효과를 보였다.