• Journal of the Korean Chemical Society
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• v.67 no.2
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• pp.129-136
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• 2023

Osteoarthritis is to the abnormality of the inflammatory response of joint tissue caused by various causes such as aging, and muscle loss. In this study, the activity in joint inflammation was verified using SKBE, a plant extract, and the expression levels of arthritis-inducing proteins including MMP-1, MMP-3, MMP-13, and collagen type II in vitro were compared and analyzed. Furthermore, we synthesized α-spinasterol, an active ingredient of SKBE, by the previously reported synthesis method and these findings could provide a new starting point for the development of treatments for osteoarthritis.

• YAKHAK HOEJI
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• v.31 no.5
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• pp.343-346
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• 1987

The effect of mixing ratios of active ingredient on the content uniformity of tablets was studied using caffeine as active ingredient and hydroxypropyl starch as diluent. In the case that caffeine content was not more than 1%, the standard deviation of individual tablet assays was inversely proportional to caffeine content. In the case of more than 1%, the standard deviation was constant independently of caffeine content. In the case that the designed tablet weight was not more than 200mg, the standard deviation of individual tablet assays was inversley proportional to tablet weight designed. In the case of more than 200mg, it was constant and the results for weight variation against the designed weight showed same tendency.

• Journal of Pharmaceutical Investigation
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• v.41 no.1
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• pp.45-50
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• 2011

Nonclassical pathway of crystallization has been utilized to modify the properties and morphologies of inorganic and organic/inorganic materials. In here, the polymer-directed crystallization method has been applied to the pharmaceutical active ingredient to assess the applicability for as a particle engineering tool. The polymer-directed crystallization was successful to modifying the crystal size, habit and morphology, but it was not effective to discover the novel polymorphs of Sibutramine (SB). SB was selected as a model drug and polyacrylic acid (PAA), polyethylene imine (PEI) and chitosan (CHI) were added as a crystallization pathway modifier. SB was crystallized via drowning crystallization using methanol or ethanol as a solvent and water as a non-solvent. The significant interactions between polymer and the drug were confirmed by measuring the solubility of the drug in presence of polymer during the crystallization. The crystal forms of SB are characterized by X-ray diffraction (XRD), scanning electron microscope (SEM) and optical microscope (OM). The polymer-directed crystallization seems to be able to modify the crystal properties of pharmaceutical active ingredient, which is critical in determining the bioavailability, processability, and stability.

• Archives of Pharmacal Research
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• v.5 no.2
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• pp.53-60
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• 1982

The mixing of salicylic acid and wheat starch powders was studied using a V-type mixer. After the optimum operating conditions of the mixer were examined, the mixing characteristics relating to dilution ratio, particle size of active ingradient and addition ratio of lubricants were investigated. The coefficient of variation was expressed by a power law relating to the dilution ratio and the particle size of active ingredient. Furthermore, the comparison of results with the theoretically estimated value of mixing index suggested that the mixing of cohesive pharmacceutical powders is a complex stochastic process and cannot be explained fully by a simple theory based on a complete random mixing.

• Journal of Ginseng Research
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• v.48 no.1
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• pp.59-67
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• 2024

Background: Alzheimer's disease (AD) has memory impairment associated with aggregation of amyloid plaques and neurofibrillary tangles in the brain. Although anti-amyloid β (Aβ) protein antibody and chemical drugs can be prescribed in the clinic, they show adverse effects or low effectiveness. Therefore, the development of a new drug is necessarily needed. We focused on the cognitive function of Panax ginseng and tried to find active ingredient(s). We isolated panaxcerol D, a kind of glycosyl glyceride, from the non-saponin fraction of P. ginseng extract. Methods: We explored effects of acute or sub-chronic administration of panaxcerol D on cognitive function in scopolamine- or Aβ_25-35 peptide-treated mice measured by several behavioral tests. After behavioral tests, we tried to unveil the underlying mechanism of panaxcerol D on its cognitive function by Western blotting. Results: We found that pananxcerol D reversed short-term, long-term and object recognition memory impairments. The decreased extracellular signal-regulated kinases (ERK) or Ca²⁺/calmodulin-dependent protein kinase II (CaMKII) in scopolamine-treated mice was normalized by acute administration of panaxcerol D. Glial fibrillary acidic protein (GFAP), caspase 3, NF-kB p65, synaptophysin and brainderived neurotrophic factor (BDNF) expression levels in Aβ_25-35 peptide-treated mice were modulated by sub-chronic administration of panaxcerol D. Conclusion: Pananxcerol D could improve memory impairments caused by cholinergic blockade or Aβ accumulation through increased phosphorylation level of ERK or its anti-inflammatory effect. Thus, panaxcerol D as one of non-saponin compounds could be used as an active ingredient of P. ginseng for improving cognitive function.

• Journal of Dairy Science and Biotechnology
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• v.23 no.1
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• pp.9-17
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• 2005

Nanotechnology has penetrated into the various branches of research and development and it is particularly of benefit to the particle size engineering. It has been widely known that the particle size of an active pharmaceutical ingredient (API) is critical in determining the bioavailability and processability of pharmaceutical formulation. However, the window of appropriate particle size has been limited mainly due to related processing difficulties. The windows have been widened by the recent development of nanotechnologies, resulting in diversified drug delivery systems. The impact of this development is far more fundamental than what can be expected from conventional particle size engineering. It is the case that the preparation and use of nanoparticles will soon be a common task in the particle engineering step of pharmaceutical unit operations. In this chapter, the basic principles of variouspreparation techniques will be discussed in detail. Regardless of processing details, the preparation methods of pharmaceutical nanoparticles mainly concern how to deal with the extra energy related with particle size. Depending on the ways of treating the e103 energy, preparation methods can be classified into two major classes, i.e.. thermodynamic and kinetic approaches. The recent progresses have shown the possibilities of much more complex combinations of different approaches and the use of new types of energy and nanostructures.

• Proceedings of the PSK Conference
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• 2003.10b
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• pp.214.2-214.2
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• 2003

Eupatilin (5,7-dihydroxy-3",4",6-trimethoxyflavone) is an active ingredient of an ethanol extract of Artemisia asiatica (DA-9601) that is used in the treatment of gastritis. In vitro and in vivo metabolism of eupatilin in the rats has been studied by LC- electrospray mass spectrometry. Rat liver microsomal incubation of eupatilin in the presence of NADPH and UDPGA resulted in the formation of four metabolites (M1-M4). M1, M2, M3 and M4 were tentatively identified as 3"- or- 4"-O-demethyl-eupatilin glucuronide, eupatilin glucuronide, 6-O-demethyleupatilin and 3"-or 4"-O-demethyl- eupatilin glucuronide, eupatilin glucuronide, 6-O-demethyleupatilin and 3"-or 4"-O- demethyl-eupatilin glucuronide, eupatilin glucuronide, 6-O demethyleupatilin and 3"-or 4"-O-demethyl-eupatilin glucuronide, respectively. (omitted)

• Biomolecules & Therapeutics
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• v.26 no.2
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• pp.201-209
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• 2018

G protein-coupled receptor 119 (GPR119) is expressed in the pancreas and gastrointestinal tract, and its activation promotes insulin secretion in the beta cells of the pancreatic islets as well as the secretion of glucagon-like peptide-1 (GLP-1) in intestinal L cells, consequently improving glucose-stimulated insulin secretion. Due to this dual mechanism of action, the development of small-molecule GPR119 agonists has received significant interest for the treatment of type 2 diabetes. We newly synthesized 1,2,4-triazolone derivatives of GPR119 agonists, which demonstrated excellent outcomes in a cyclic adenosine monophosphate (cAMP) assay. Among the synthesized derivatives, YH18968 showed cAMP=2.8 nM; in GLUTag cell, GLP-1secretion=2.3 fold; in the HIT-T15 cell, and insulin secretion=1.9 fold. Single oral administration of YH18968 improved glucose tolerance and combined treatment with a dipeptidyl peptidase 4 (DPP-4) inhibitor augmented the glucose lowering effect as well as the plasma level of active GLP-1 in normal mice. Single oral administration of YH18968 improved glucose tolerance in a diet induced obese mice model. This effect was maintained after repeated dosing for 4 weeks. The results indicate that YH18968 combined with a DPP-4 inhibitor may be an effective therapeutic candidate for the treatment of type 2 diabetes.

• Journal of Biosystems Engineering
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• v.40 no.4
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• pp.394-408
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• 2015

Spectroscopy is an emerging technology for the quality assessment of pharmaceutical samples, from tablet manufacturing to final quality assurance. The traditional methods for the quality management of pharmaceutical tablets are time consuming and destructive, while spectroscopic techniques allow rapid analysis in a non-destructive manner. The advantage of spectroscopy is that it collects both spatial and spectral information (called hyperspectral imaging), which is useful for the chemical imaging of pharmaceutical samples. These chemical images provide both qualitative and quantitative information on tablet samples. In the pharmaceutics, spectroscopic techniques are used for a variety of applications, such as analysis of the homogeneity of powder samples as well as determination of particle size, product composition, and the concentration, uniformity, and distribution of the active pharmaceutical ingredient in solid tablets. This review paper presents an introduction to the applications of various spectroscopic techniques such as hyperspectroscopy and vibrational spectroscopies (Raman spectroscopy, FT-NIR, and IR spectroscopy) for the quality and safety assessment of pharmaceutical solid dosage forms. In addition, various chemometric techniques that are highly essential for analyzing the spectroscopic data of pharmaceutical samples are also reviewed.

• YAKHAK HOEJI
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• v.58 no.4
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• pp.262-267
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• 2014

Unused medication disposal is a burden due to the cost of disposing as well as the cost of the drugs. Investigating medication returns is expected to suggest areas of intervention to reduce unused medications. Purpose: The aim of this study was to examine types, quantity, costs, active pharmaceutical ingredients, and therapeutic category of the medications returned to community pharmacies. Method: From January 15, 2014 to February 28, 2014, the medications returned to the 17 community pharmacies in Gimhae, Jinju, and Incheon, Korea were examined. The pharmacists and student volunteers worked cooperatively to identify the medications and analyze drug cost of prescription pill medications returned to the pharmacies. Results: A total of 2,720 pills of prescription medication were analyzed and 91 active pharmaceutical ingredients were identified. According to the Anatomical Therapeutic Chemical (ATC) classification, the most predominant group was A (alimentary tract and metabolism) with 33.3%, followed by N (nervous system) with 15.0%. With regard to the drug cost of groups, group A was the highest with 26.6%, followed by J01 (antibacterials for systemic use) with 20.2% and N (nervous system) with 18.3%. The total cost of the oral pill prescription medications was 468,477 won. Conclusion: The result from this study implies that unused drugs impose a significant cost to the health care system in Korea. In this study, medicines used to treat gastrointestinal conditions were returned most frequently with the highest drug cost. Further research in nationwide level is necessary to establish strategies to reduce the wastage of unused medicines.